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Anti-Human Immunodeficiency Virus and Anti-Hepatitis-B Virus Activities and Toxicities of the Enantiomers of 2'-Deoxy-3'-oxa-4'-thiocytidine and Their 5-Fluoro Analogs in Vitro Tarek S. Mansour, Haolun Jin, Wei Wang, Elizabeth U. Hooker, Clare Ashman, Nick Cammack, Horacio Salomon, Antonietta R. Belmonte, and Mark A. Wainberg pp 1 - 4; DOI: 10.1021/jm00001a001 |
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Preparation of 18F-Labeled Muscarinic Agonist with M2 Selectivity Dale O. Kiesewetter, JaeTae Lee, Lixin Lang, Seok Gun Park, Chang H. Paik, and William C. Eckelman pp 5 - 8; DOI: 10.1021/jm00001a002 |
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Potent non-peptide fibrinogen receptor antagonists which present an alternative pharmacophore Thomas W. Ku, William H. Miller, William E. Bondinell, Karl F. Erhard, Richard M. Keenan, Andrew J. Nichols, Catherine E. Peishoff, James M. Samanen, Angela S. Wong, and William F. Huffman pp 9 - 12; DOI: 10.1021/jm00001a003 |
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Benzophenone- and Indolecarboxylic Acids: Potent Type-2 Specific Inhibitors of Human Steroid 5.alpha.-Reductase Dennis A. Holt, Dennis S. Yamashita, Arda L. Konialian-Beck, Juan I. Luengo, Andrew D. Abell, Derk J. Bergsma, Martin Brandt, and Mark A. Levy pp 13 - 15; DOI: 10.1021/jm00001a004 |
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Potential Anxiolytic Agents. Pyrido[1,2-a]benzimidazoles: A New Structural Class of Ligands for the Benzodiazepine Binding Site on GABA-A Receptors Bruce E. Maryanoff, Winston Ho, David F. McComsey, Allen B. Reitz, Philip P. Grous, Samuel O. Nortey, Richard P. Shank, Barry Dubinsky, Russell J. Jr. Taylor, and Joseph F. Gardocki pp 16 - 20; DOI: 10.1021/jm00001a005 |
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Discovery of 6,11-Ethano-12,12-diaryl-6,11-dihydrobenzo[b]quinolizinium Cations, a Novel Class of N-Methyl-D-aspartate Antagonists Chakrapani Subramanyam, John P. Mallamo, John A. Dority, William G. Earley, Virendra Kumar, Lisa D. Aimone, Brian Ault, Matthew S. Miller, Daniel A. Luttinger, and Diane L. DeHaven-Hudkins pp 21 - 27; DOI: 10.1021/jm00001a006 |
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(+)-cis-4,5,7a,8,9,10,11,11a-Octahydro-7H-10-methylindolo[1,7-bc][2,6]- naphthyridine: A 5-HT2C/2B Receptor Antagonist with Low 5-HT2A Receptor Affinity Joachim Nozulak, Hans O. Kalkman, Philipp Floerscheim, Daniel Hoyer, Philipp Schoeffter, and Hans R. Buerki pp 28 - 33; DOI: 10.1021/jm00001a007 |
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Novel Thiazole-Based Heterocycles as Selective Inhibitors of Fibrinogen-Mediated Platelet Aggregation Pauline J. Sanfilippo, Patricia Andrade-Gordon, Maud J. Urbanski, Kimberly N. Beers, Annette Eckardt, Robert Falotico, Mark H. Ginsberg, Steve Offord, Jeffrey B. Press, and et al. pp 34 - 41; DOI: 10.1021/jm00001a008 |
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Relative Binding Free Energies of Peptide Inhibitors of HIV-1 Protease: The Influence of the Active Site Protonation State Xiannong Chen and Alexander Tropsha pp 42 - 48; DOI: 10.1021/jm00001a009 |
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Synthesis, Properties, and Pharmacokinetic Studies of N2-Phenylguanine Derivatives as Inhibitors of Herpes Simplex Virus Thymidine Kinases Hongyan Xu, Giovanni Maga, Federico Focher, Emil R. Smith, Silvio Spadari, Joseph Gambino, and George E. Wright pp 49 - 57; DOI: 10.1021/jm00001a010 |
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Tyrosine Kinase Inhibitors. 4. Structure-Activity Relationships among N- and 3-Substituted 2,2'-Dithiobis(1H-indoles) for in vitro Inhibition of Receptor and Nonreceptor Protein Tyrosine Kinases Brian D. Palmer, Gordon W. Rewcastle, Andrew M. Thompson, Maruta Boyd, H. D. Hollis Showalter, Anthony D. Sercel, David W. Fry, Alan J. Kraker, and William A. Denny pp 58 - 67; DOI: 10.1021/jm00001a011 |
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Derivatives of 2-[[N-(Aminocarbonyl)-N-hydroxyamino]methyl]-1,4-benzodioxan as Orally Active 5-Lipoxygenase Inhibitors Yoshitaka Satoh, Colleen Powers, Leticia M. Toledo, Timothy J. Kowalski, Paul A. Peters, and Earl F. Kimble pp 68 - 75; DOI: 10.1021/jm00001a012 |
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Peptidyl .alpha.-ketoheterocyclic inhibitors of human neutrophil elastase. 2. Effect of varying the heterocyclic ring on in vitro potency Philip D. Edwards, Donald J. Wolanin, Donald W. Andisik, and Matthew W. Davis pp 76 - 85; DOI: 10.1021/jm00001a013 |
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Non-peptidic inhibitors of human leukocyte elastase. 4. Design, synthesis, and in vitro and in vivo activity of a series of .beta.-carbolinone-containing trifluoromethyl ketones Chris A. Veale, James R. Jr. Damewood, Gary B. Steelman, Craig Bryant, Bruce Gomes, and Joseph Williams pp 86 - 97; DOI: 10.1021/jm00001a014 |
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Nonpeptidic inhibitors of human leukocyte elastase. 5. Design, synthesis, and x-ray crystallography of a series of orally active 5-aminopyrimidin-6-one-containing trifluoromethyl ketones Chris A. Veale, Peter R. Bernstein, Craig Bryant, Christopher Ceccarelli, James R. Jr. Damewood, Roger Earley, Scott W. Feeney, Bruce Gomes, Ben J. Kosmider, and et al. pp 98 - 108; DOI: 10.1021/jm00001a015 |
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Pyrrolo[1,2-a]benzimidazole-Based Quinones and Iminoquinones. The Role of the 3-Substituent on Cytotoxicity William G. Schulz, Imadul Islam, and Edward B. Skibo pp 109 - 118; DOI: 10.1021/jm00001a016 |
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Calcium Entry Blockers and Activators: Conformational and Structural Determinants of Dihydropyrimidine Calcium Channel Modulators George C. Rovnyak, S. David Kimball, Barbara Beyer, Gabriella Cucinotta, John D. DiMarco, Jack Gougoutas, Anders Hedberg, Mary Malley, James P. McCarthy, and et al. pp 119 - 129; DOI: 10.1021/jm00001a017 |
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New Antianginal Nitro Esters with Reduced Hypotensive Activity. Synthesis and Pharmacological Evaluation of 3-[(Nitrooxy)alkyl]-2H-1,3-benzoxazin-4(3H)-ones Francesca Benedini, Giorgio Bertolini, Roberta Cereda, Giancarlo Dona, Gianni Gromo, Silvio Levi, Jacques Mizrahi, and Alberto Sala pp 130 - 136; DOI: 10.1021/jm00001a018 |
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Ac-[3- and 4-Alkylthioproline31]-CCK4 Analogs: Synthesis and Implications for the CCK-B Receptor-Bound Conformation Stephen A. Kolodziej, Gregory V. Nikiforovich, Richard Skeean, Marie-Francoise Lignon, Jean Martinez, and Garland R. Marshall pp 137 - 149; DOI: 10.1021/jm00001a019 |
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Derivatives of cis-2-Amino-8-hydroxy-1-methyltetralin: Mixed 5-HT1A-Receptor Agonists and Dopamine D2-Receptor Antagonists Ye Liu, Hong Yu, Nina Mohell, Gunnar Nordvall, Tommy Lewander, and Uli Hacksell pp 150 - 160; DOI: 10.1021/jm00001a020 |
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Glycosylated Peptide Hormones: Pharmacological Properties and Conformational Studies of Analogs of [1-Desamino,8-D-arginine]vasopressin Jan Kihlberg, Jens Aahman, Bjoern Walse, Torbjoern Drakenberg, Anders Nilsson, Christina Soederberg-Ahlm, Bengt Bengtsson, and Haakan Olsson pp 161 - 169; DOI: 10.1021/jm00001a021 |
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X-ray Crystal Structure, Partitioning Behavior, and Molecular Modeling Study of Piracetam-Type Nootropics: Insights into the Pharmacophore Cosimo Altomare, Saverio Cellamare, Angelo Carotti, Giovanni Casini, Marcello Ferappi, Enrico Gavuzzo, Fernando Mazza, Pierre-Alain Carrupt, Patrick Gaillard, and Bernard Testa pp 170 - 179; DOI: 10.1021/jm00001a022 |
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Design and Synthesis of Piperidine-3-carboxamides as Human Platelet Aggregation Inhibitors Xiaozhang Zheng, Somna R. Salgia, Walter B. Thompson, Elwood O. Dillingham, Stephen.E. Bond, Zixia Feng, K. Ram Prasad, and Ram Gollamudi pp 180 - 188; DOI: 10.1021/jm00001a023 |
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Synthetic Routes to 4-Amino-3-carboxy-.beta.-carboline Derivatives: Incidental Formation of Novel Furo[3,4-c]-.beta.-carbolin-2-ones Displaying High Affinities for the Benzodiazepine Receptor Gilbert Dorey, Laurent Dubois, Lia Prdo Prado de Carvalho, Pierre Potier, and Robert H. Dodd pp 189 - 198; DOI: 10.1021/jm00001a024 |
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Synthesis and cytotoxic activity of 6-vinyl- and 6-ethynyluridine and 8-vinyl- and 8-ethynyladenosine Stefano Manfredini, Pier G. Baraldi, Rita Bazzanini, Mirella Marangoni, Daniele Simoni, Jan Balzarini, and Erik De Clercq pp 199 - 203; DOI: 10.1021/jm00001a025 |
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Synthesis and Activity of Some Antimalarial Bisquinolines Kaylene Raynes, Denise Galatis, Alan F. Cowman, Leann Tilley, and Leslie W. Deady pp 204 - 206; DOI: 10.1021/jm00001a026 |
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CCK-A Receptor Selective Antagonists Derived from the CCK-A Receptor Selective Tetrapeptide Agonist Boc-Trp-Lys(Tac)-Asp-MePhe-NH2 (A-71623) Elizabeth E. Sugg, Millard J. Kimery, Jian Mei Ding, Deborah C. Kenakin, Laurence J. Miller, Kennedy L. Queen, and Thomas J. Rimele pp 207 - 211; DOI: 10.1021/jm00001a027 |
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Nonpeptidic Inhibitors of Human Leukocyte Elastase. 6. Design of a Potent, Intratracheally Active, Pyridone-Based Trifluoromethyl Ketone Peter R. Bernstein, Bruce C. Gomes, Benedict J. Kosmider, Edward P. Vacek, and Joseph C. Williams pp 212 - 215; DOI: 10.1021/jm00001a028 |
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Book Reviews pp 216 - 216; DOI: 10.1021/jm00001a600 |
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Validation of Screening Immobilized Peptide Libraries for Discovery of Protease Substrates Jasbir Singh, Martin P. Allen, Mark A. Ator, James A. Gainor, David A. Whipple, James E. Solowiej, Adi M. Treasurywala, and Donald A. Upson pp 217 - 219; DOI: 10.1021/jm00002a001 |
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Aspartyl .alpha.-((Diphenylphosphinyl)oxy)methyl Ketones as Novel Inhibitors of Interleukin-1.beta. Converting Enzyme. Utility of the Diphenylphosphinic Acid Leaving Group for the Inhibition of Cysteine Proteases Roland E. Dolle, Jasbir Singh, David Whipple, I. Kelly Osifo, Gary Speier, Todd L. Graybill, Jill S. Gregory, Alex L. Harris, Carla T. Helaszek, and et al. pp 220 - 222; DOI: 10.1021/jm00002a002 |
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Inhibition of Human Neutrophil Elastase. 3. An Orally Active Enol Acetate Prodrug Joseph P. Burkhart, Jack R. Koehl, Shujaath Mehdi, Sherrie L. Durham, Michael J. Janusz, Edward W. Huber, Michael R. Angelastro, Shyam Sunder, William A. Metz, and et al. pp 223 - 233; DOI: 10.1021/jm00002a003 |
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Antitumor Activity of 5-Aryl-2,3-dihydroimidazo[2,1-a]isoquinolines William J. Houlihan, Paul G. Munder, Dean A. Handley, Seung H. Cheon, and Vincent A. Parrino pp 234 - 240; DOI: 10.1021/jm00002a004 |
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Rationally Designed Analogs of Tamoxifen with Improved Calmodulin Antagonism Ian R. Hardcastle, Martin G. Rowlands, John Houghton, Iris B. Parr, Gerard A. Potter, Michael Jarman, Karen J. Edwards, Charles A. Laughton, John O. Trent, and Stephen Neidle pp 241 - 248; DOI: 10.1021/jm00002a005 |
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Design and Structure-Activity Relationships of C-Terminal Cyclic Neurotensin Fragment Analogs Andrea M. Sefler, John X. He, Tomi K. Sawyer, Katherine E. Holub, Diana O. Omecinsky, Michael D. Reily, Venkataraman Thanabal, Hyacinth C. Akunne, and Wayne L. Cody pp 249 - 257; DOI: 10.1021/jm00002a006 |
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5-(Diethoxyphosphoryl)-5-methyl-1-pyrroline N-oxide: A New Efficient Phosphorylated Nitrone for the in Vitro and in Vivo Spin Trapping of Oxygen-Centered Radicals Claudine Frejaville, Hakim Karoui, Beatrice Tuccio, Francois Le Moigne, Marcel Culcasi, Sylvia Pietri, Robert Lauricella, and Paul Tordo pp 258 - 265; DOI: 10.1021/jm00002a007 |
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Homologs of Histamine as Histamine H3 Receptor Antagonists: A New Potent and Selective H3 Antagonist, 4(5)-(5-Aminopentyl)-1H-imidazole Roeland C. Vollinga, Wiro M. P. B. Menge, Rob Leurs, and Hendrik Timmerman pp 266 - 271; DOI: 10.1021/jm00002a008 |
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Structure-Activity Relationships of Analogs of Thapsigargin Modified at O-11 and O-12 Simon Feldbk Nielsen, Ole Thastrup, Rudi Pedersen, Carl Erik Olsen, and Soren Brogger Christensen pp 272 - 276; DOI: 10.1021/jm00002a009 |
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Synthesis and Biological Evaluation of a New Series of Sterols as Potential Hypocholesterolemic Agents Ho-Shen Lin, Ashraff A. Rampersaud, Robert A. Archer, Joseph M. Pawlak, Lisa S. Beavers, Robert J. Schmidt, Raymond F. Kauffman, William R. Bensch, Thomas F. Bumol, and et al. pp 277 - 288; DOI: 10.1021/jm00002a010 |
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Derivatives of 17-Phenyl-18,19,20-trinorprostaglandin F2.alpha. Isopropyl Ester: Potential Antiglaucoma Agents Charlotta Liljebris, Goeran Selen, Bahram Resul, Johan Stjernschantz, and Uli Hacksell pp 289 - 304; DOI: 10.1021/jm00002a011 |
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A priori prediction of activity for HIV-1 protease inhibitors employing energy minimization in the active site M. Katharine Holloway, Jenny M. Wai, Thomas A. Halgren, Paula M. D. Fitzgerald, Joseph P. Vacca, Bruce D. Dorsey, Rhonda B. Levin, Wayne J. Thompson, L. Jenny Chen, and et al. pp 305 - 317; DOI: 10.1021/jm00002a012 |
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Evaluation of cis- and trans-9- and 11-Hydroxy-5,6,6a,7,8,12b-hexahydrobenzo[a]phenanthridines as Structurally Rigid, Selective D1 Dopamine Receptor Ligands William K. Brewster, David E. Nichols, Val J. Watts, Robert M. Riggs, Dave Mottola, and Richard B. Mailman pp 318 - 327; DOI: 10.1021/jm00002a013 |
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Fluorine-18-labeled progestin 16.alpha.,17.alpha.-dioxolanes: development of high-affinity ligands for the progesterone receptor with high in vivo target site selectivity Brad O. Buckman, Thomas A. Bonasera, Karen S. Kirschbaum, Michael J. Welch, and John A. Katzenellenbogen pp 328 - 337; DOI: 10.1021/jm00002a014 |
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Halicylindramides A-C, antifungal and cytotoxic depsipeptides from the marine sponge Halichondria cylindrata Hong-yu Li, Shigeki Matsunaga, and Nobuhiro Fusetani pp 338 - 343; DOI: 10.1021/jm00002a015 |
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Deconvolution of Combinatorial Libraries for Drug Discovery: A Model System Susan M. Freier, Danielle A. M. Konings, Jacqueline R. Wyatt, and David J. Ecker pp 344 - 352; DOI: 10.1021/jm00002a016 |
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Novel Thiazole Derivatives as Inhibitors of Superoxide Production by Human Neutrophils: Synthesis and Structure-Activity Relationships Masatoshi Chihiro, Hisashi Nagamoto, Isao Takemura, Kazuyoshi Kitano, Hajime Komatsu, Kazuo Sekiguchi, Fujio Tabusa, Toyoki Mori, Michiaki Tominaga, and Youichi Yabuuchi pp 353 - 358; DOI: 10.1021/jm00002a017 |
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8-Substituted O6-Benzylguanine, Substituted 6(4)-(Benzyloxy)pyrimidine, and Related Derivatives as Inactivators of Human O6-Alkylguanine-DNA Alkyltransferase Mi-Young Chae, Kristin Swenn, Sreenivas Kanugula, M. Eileen Dolan, Anthony E. Pegg, and Robert C. Moschel pp 359 - 365; DOI: 10.1021/jm00002a018 |
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Synthesis and Structure-Activity Relationships of Phenylenebis(methylene)-Linked Bis-Tetraazamacrocycles That Inhibit HIV Replication. Effects of Macrocyclic Ring Size and Substituents on the Aromatic Linker Gary J. Bridger, Renato T. Skerlj, David Thornton, Sreenivasan Padmanabhan, Stephen A. Martellucci, Geoffrey W. Henson, Michael J. Abrams, Naohiko Yamamoto, Karen De Vreese, and et al. pp 366 - 378; DOI: 10.1021/jm00002a019 |
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Cocaine and 3.beta.-(4'-Substituted phenyl)tropane-2.beta.-carboxylic Acid Ester and Amide Analogs. New High-Affinity and Selective Compounds for the Dopamine Transporter F. Ivy Carroll, Pravin Kotian, Ali Dehghani, Jeffrey L. Gray, Michael A. Kuzemko, Karol A. Parham, Philip Abraham, Anita H. Lewin, John W. Boja, and Michael J. Kuhar pp 379 - 388; DOI: 10.1021/jm00002a020 |
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Specific Inhibition of Poly(ADP-ribose) Glycohydrolase by Adenosine Diphosphate (Hydroxymethyl)pyrrolidinediol James T. Slama, Nasreen Aboul-Ela, Deepa M. Goli, Bruce V. Cheesman, Anne M. Simmons, and Myron K. Jacobson pp 389 - 393; DOI: 10.1021/jm00002a021 |
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Book Reviews pp 394 - 394; DOI: 10.1021/jm00002a600 |
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Synthesis and Antitumor Activity of Novel Water Soluble Derivatives of Camptothecin as Specific Inhibitors of Topoisomerase I Michael J. Luzzio, Jeffrey M. Besterman, David L. Emerson, Michael G. Evans, Karen Lackey, Peter L. Leitner, Gordon McIntyre, Bradley Morton, Peter L. Myers, Michael Peel, Jay M. Sisco, Daniel D. Sternbach, Wei-Qin Tong, Ann Truesdale, David E. Uehling, Alan Vuong, and Julie Yates pp 395 - 401; DOI: 10.1021/jm00003a001 |
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7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of .delta.1 opioid receptor-mediated antinociception in mice P. S. Portoghese, F. Farouz-Grant, M. Sultana, and A. E. Takemori pp 402 - 407; DOI: 10.1021/jm00003a002 |
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Self-Assembly of a Quinobenzoxazine-Mg2+ Complex on DNA: A New Paradigm for the Structure of a Drug-DNA Complex and Implications for the Structure of the Quinolone Bacterial Gyrase-DNA Complex Jun-Yao Fan, Daekyu Sun, Hongtao Yu, Sean M. Kerwin, and Laurence H. Hurley pp 408 - 424; DOI: 10.1021/jm00003a003 |
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Impact of Polyamine Analogs on the NMDA Receptor Raymond J. Bergeron, William R. Weimar, Qianhong Wu, Jack Kramer Austin, and James S. McManis pp 425 - 428; DOI: 10.1021/jm00003a004 |
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11.beta.-Substituted Estradiol Derivatives, Potential High-Affinity Carbon-11-Labeled Probes for the Estrogen Receptor: A Structure-Affinity Relationship Study Elio Napolitano, Rita Fiaschi, Kathryn E. Carlson, and John A. Katzenellenbogen pp 429 - 434; DOI: 10.1021/jm00003a005 |
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Phosphinyl Acid-Based Bisubstrate Analog Inhibitors of Farnesyl Protein Transferase Dinesh V. Patel, Eric M. Gordon, Robert J. Schmidt, Harold N. Weller, Marian G. Young, Robert Zahler, Mariano Barbacid, Joan M. Carboni, Johnni L. Gullo-Brown, Lisa Hunihan, Carol Ricca, Simon Robinson, Bernd R. Seizinger, Anne V. Tuomari, and Veeraswamy Manne pp 435 - 442; DOI: 10.1021/jm00003a006 |
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Cosalane Analogs with Enhanced Potencies as Inhibitors of HIV-1 Protease and Integrase Mark Cushman, W. Marek Golebiewski, Yves Pommier, Abhijit Mazunder, Diane Reymen, Erik De Clercq, Lisa Grahm, and William G. Rice pp 443 - 452; DOI: 10.1021/jm00003a007 |
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2,3-Dihydro-1-benzofuran-5-ols as Analogs of .alpha.-Tocopherol That Inhibit in Vitro and ex Vivo Lipid Autoxidation and Protect Mice against Central Nervous System Trauma J. Martin Grisar, Frank N. Bolkenius, Margaret A. Petty, and Joelle Verne pp 453 - 458; DOI: 10.1021/jm00003a008 |
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Pimelautide or Trimexautide as Built-in Adjuvants Associated with an HIV-1-Derived Peptide: Synthesis and in Vivo Induction of Antibody and Virus-Specific Cytotoxic T-Lymphocyte-Mediated Response Benoit Deprez, Helene Gras-Masse, Frederic Martinon, Elisabeth Gomard, Jean-Paul Levy, and Andre Tartar pp 459 - 465; DOI: 10.1021/jm00003a009 |
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De Novo Design of Enzyme Inhibitors by Monte Carlo Ligand Generation Daniel K. Gehlhaar, Karl E. Moerder, Dominic Zichi, Christopher J. Sherman, Richard C. Ogden, and Stephan T. Freer pp 466 - 472; DOI: 10.1021/jm00003a010 |
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3-Heteroaryl-Substituted Quinuclidin-3-ol and Quinuclidin-2-ene Derivatives as Muscarinic Antagonists. Synthesis and Structure-Activity Relationships Bjoern M. Nilsson, Staffan Sundquist, Gary Johansson, Gunnar Nordvall, Gunilla Glas, Lisbeth Nilvebrant, and Uli Hacksell pp 473 - 487; DOI: 10.1021/jm00003a011 |
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5'-[4-(Pivaloyloxy)-1,3,2-dioxaphosphorinan-2-yl]-2'-deoxy-5-fluorouridine: A Membrane-Permeating Prodrug of 5-Fluoro-2'-deoxyuridylic Acid (FdUMP) David Farquhar, Roger Chen, and Saeed Khan pp 488 - 495; DOI: 10.1021/jm00003a012 |
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Amphoteric Drugs. 3. Synthesis and Antiallergic Activity of 3-[(5,11-Dihydro[1]benzoxepino[4,3-b]pyridin-11-ylidene)piperidino]propionic Acid Derivatives and Related Compounds Nobuhiko Iwasaki, Tetsuo Ohashi, Keiichi Musoh, Hiroyuki Nishino, Noriyuki Kado, Shingo Yasuda, Hideo Kato, and Yasuo Ito pp 496 - 507; DOI: 10.1021/jm00003a013 |
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N-Acyl-2-substituted-1,3-thiazolidines, a new class of non-narcotic antitussive agents: studies leading to the discovery of ethyl 2-[(2-methoxyphenoxy)methyl]-.beta.-oxothiazolidine-3-propanoate Carmelo A. Gandolfi, Roberto Di Domenico, Silvano Spinelli, Licia Gallico, Luigi Fiocchi, Andrea Lotto, Ernesto Menta, Alessandra Borghi, Carla Dalla Rosa, and Sergio Tognella pp 508 - 525; DOI: 10.1021/jm00003a014 |
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Chromophore-Modified Antitumor Anthracenediones: Synthesis, DNA Binding, and Cytotoxic Activity of 1,4-Bis[(aminoalkyl)amino]benzo[g]phthalazine-5,10-diones Carmelo A. Gandolfi, Gino Beggiolin, Ernesto Menta, Manlio Palumbo, Claudia Sissi, Silvano Spinelli, and Francis Johnson pp 526 - 536; DOI: 10.1021/jm00003a015 |
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Synthesis of Novel Thiol-Containing Citric Acid Analogs. Kinetic Evaluation of These and Other Potential Active-Site-Directed and Mechanism-Based Inhibitors of ATP Citrate Lyase Roland E. Dolle, Andy Gribble, Tracey Wilkes, Lawrence I. Kruse, Drake Eggleston, Barbara A. Saxty, Timothy N. C. Wells, and Pieter H. E. Groot pp 537 - 543; DOI: 10.1021/jm00003a016 |
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Mechanism-Based Isocoumarin Inhibitors for Human Leukocyte Elastase. Effect of the 7-Amino Substituent and 3-Alkoxy Group in 3-Alkoxy-7-amino-4-chloroisocoumarins on Inhibitory Potency John E. Kerrigan, Jozef Oleksyszyn, Chih-Min Kam, Joe Selzler, and James C. Powers pp 544 - 552; DOI: 10.1021/jm00003a017 |
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Three-Dimensional Structure of Cyclohexapeptides Containing a Phosphinic Bond in Aqueous Solution: A Template for Zinc Metalloprotease Inhibitors. A NMR And Restrained Molecular Dynamics Study Philippe Cuniasse, Isabelle Raynal, Alain Lecoq, Anasthasios Yiotakis, and Vincent Dive pp 553 - 564; DOI: 10.1021/jm00003a018 |
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(+)-cis-N-(para-, meta-, and ortho-substituted benzyl)-N-normetazocines: Synthesis and binding affinity at the [3H]-(+)-pentazocine-labeled (.sigma.1) site and quantitative structure-affinity relationship studies S. Wayne Mascarella, Xu Bai, Wanda Williams, Bethel Sine, Wayne D. Bowen, and F. Ivy Carroll pp 565 - 569; DOI: 10.1021/jm00003a019 |
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Isothiocyanate-Substituted Benzyl Ether Opioid Receptor Ligands Derived from 6.beta.-Naltrexol Ronda D. Davis and Wendel L. Nelson pp 570 - 579; DOI: 10.1021/jm00003a020 |
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Book Reviews pp 580 - 580; DOI: 10.1021/jm00003a600 |
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Inhibitors of HIV-1 Protease Containing the Novel and Potent (R)-(Hydroxyethyl)sulfonamide Isostere Michael L. Vazquez, Martin L. Bryant, Michael Clare, Gary A. DeCrescenzo, Elizabeth M. Doherty, John N. Freskos, Daniel P. Getman, Kathryn A. Houseman, Janet A. Julien, Geralyn P. Kocan, Richard A. Mueller, Huey-Sheng Shieh, William C. Stallings, Roderick A. Stegeman, and John J. Tilley pp 581 - 584; DOI: 10.1021/jm00004a001 |
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Highly .kappa. receptor-selective dynorphin A analogs with modifications in position 3 of dynorphin A(1-11)-NH2 Feng-Di T. Lung, J.-Ph. Meyer, Guigen Li, B.-S. Lou, Dagmar Stropova, Peg Davis, Henry I. Yamamura, Frank Porreca, and Victor J. Hruby pp 585 - 586; DOI: 10.1021/jm00004a002 |
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6-(4-Pyridinyl)-1H-1,2,3-triazolo[4,5-d]-pyrimidin-4(5H)-one: A Structurally Novel Competitive AMPA Receptor Antagonist Chakrapani Subramanyam, Brian Ault, David Sawutz, Edward R. Bacon, Baldev Singh, Patrick O. Pennock, Michael D. Kelly, Matthew Kraynak, Doug Krafte, and Adi Treasurywala pp 587 - 589; DOI: 10.1021/jm00004a003 |
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IAM chromatography: an in vitro screen for predicting drug membrane permeability Charles Pidgeon, Shaowei Ong, Hanlan Liu, Xiaoxing Qiu, Mary Pidgeon, Anne H. Dantzig, John Munroe, William J. Hornback, Jeffery S. Kasher, and et al. pp 590 - 594; DOI: 10.1021/jm00004a004 |
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Synthesis and Structure-Activity Relationships of Dequalinium Analogs as K+ Channel Blockers. Investigations on the Role of the Charged Heterocycle Dimitrios Galanakis, Carole A. Davis, Benedicto Del Rey Herrero, C. Robin Ganellin, Philip M. Dunn, and Donald H. Jenkinson pp 595 - 606; DOI: 10.1021/jm00004a005 |
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Structure-activity relationships of lactone ring-opened analogs of the antimalarial 1,2,4-trioxane artemisinin Gary H. Posner, David J. McGarvey, Chang Ho Oh, Nirbhay Kumar, Steven R. Meshnick, and Wanida Asawamahasadka pp 607 - 612; DOI: 10.1021/jm00004a006 |
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Synthesis and Antimalarial Activities of 12.beta.-Allyldeoxoartemisinin and Its Derivatives Yu Ming Pu and Herman Ziffer pp 613 - 616; DOI: 10.1021/jm00004a007 |
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Studies on New Acidic Azoles as Glucose-Lowering Agents in Obese, Diabetic db/db Mice Kenneth L. Kees, Thomas J. Caggiano, Kurt E. Steiner, John J. Fitzgerald, Michael J. Kates, Thomas E. Christos, John M. Kulishoff, Robin D. Moore, and Michael L. McCaleb pp 617 - 628; DOI: 10.1021/jm00004a008 |
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Molecular Similarity Matrixes and Quantitative Structure-Activity Relationships: A Case Study with Methodological Implications Romualdo Benigni, Marina Cotta-Ramusino, Fabrizio Giorgi, and Grazia Gallo pp 629 - 635; DOI: 10.1021/jm00004a009 |
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Polyiodinated Triglyceride Analogs as Potential Computed Tomography Imaging Agents for the Liver Jamey P. Weichert, Marc A. Longino, Douglas A. Bakan, Michael G. Spigarelli, Tso-sheng Chou, Susan W. Schwendner, and Raymond E. Counsell pp 636 - 646; DOI: 10.1021/jm00004a010 |
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(R)-11-Hydroxy- and (R)-11-Hydroxy-10-methylaporphine: Synthesis, Pharmacology, and Modeling of D2A and 5-HT1A Receptor Interactions Martin H. Hedberg, Anette M. Johansson, Gunnar Nordvall, Ari Yliniemela, Hong Bing Li, Arnold R. Martin, Stephan Hjorth, Lena Unelius, Staffan Sundell, and Uli Hacksell pp 647 - 658; DOI: 10.1021/jm00004a011 |
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Three-Dimensional Quantitative Structure-Activity Relationships of Sulfonamide Endothelin Inhibitors Stanley R. Krystek, John T. Hunt, Philip D. Stein, and Terry R. Stouch pp 659 - 668; DOI: 10.1021/jm00004a012 |
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Synthesis, Structure-Activity Relationships, and Pharmacological Evaluation of Pyrrolo[3,2,1-ij]quinoline Derivatives: Potent Histamine and Platelet Activating Factor Antagonism and 5-Lipoxygenase Inhibitory Properties. Potential Therapeutic Application in Asthma Dominique Paris, Michel Cottin, Patrice Demonchaux, Guy Augert, Pierre Dupassieux, Patrick Lenoir, Michael J. Peck, and Daniel Jasserand pp 669 - 685; DOI: 10.1021/jm00004a013 |
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Dual-Acting Thromboxane Receptor Antagonist/Synthase Inhibitors: Synthesis and Biological Properties of [2-Substituted-4-(3-pyridyl)-1,3-dioxan-5-yl]alkenoic Acids Alan W. Faull, Andrew G. Brewster, George R. Brown, Michael J. Smithers, and Ruth Jackson pp 686 - 694; DOI: 10.1021/jm00004a014 |
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Synthesis and Structure-Activity Relationships of Oxamic Acid and Acetic Acid Derivatives Related to L-Thyronine Naokata Yokoyama, Gordon N. Walker, Alan J. Main, James L. Stanton, Michael M. Morrissey, Charles Boehm, Allan Engle, Alan D. Neubert, Jong M. Wasvary, and et al. pp 695 - 707; DOI: 10.1021/jm00004a015 |
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Binding of 5H-Dibenzo[a,d]cycloheptene and Dibenz[b,f]oxepin Analogs of Clozapine to Dopamine and Serotonin Receptors Shawn T. Phillips, Tomas de Paulis, Jon R. Neergaard, Bruce M. Baron, Barry W. Siegel, Philip Seeman, Hubert H. M. Van Tol, Hong-Chang Guan, and Howard E. Smith pp 708 - 714; DOI: 10.1021/jm00004a016 |
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Prediction of Receptor Properties and Binding Affinity of Ligands to Benzodiazepine/GABAA Receptors Using Artificial Neural Networks Desmond J. Maddalena and Graham A. R. Johnston pp 715 - 724; DOI: 10.1021/jm00004a017 |
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C-9 and N-Substituted Analogs of cis-(3aR)-(-)-2,3,3a,4,5,9b-Hexahydro-3-propyl-1H-benz[e]indole-9-carboxamide: 5-HT1A Receptor Agonists with Various Degrees of Metabolic Stability Susanne R. Haadsma-Svensson, Kjell Svensson, Neil Duncan, Martin W. Smith, and Chiu-Hong Lin pp 725 - 734; DOI: 10.1021/jm00004a018 |
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Isolation and Characterization of a Cyclic Hydroxamic Acid from a Pollen Extract, Which Inhibits Cancerous Cell Growth in Vitro Xin Zhang, Fouad K. Habib, Margaret Ross, Ulrich Burger, Ari Lewenstein, Keith Rose, and Jean-Claude Jaton pp 735 - 738; DOI: 10.1021/jm00004a019 |
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Orally Bioavailable Benzisothiazolone Inhibitors of Human Leukocyte Elastase Dennis J. Hlasta, Chakrapani Subramanyam, Malcolm R. Bell, Philip M. Carabateas, John J. Court, Ranjit C. Desai, Marion L. Drozd, W. Mark Eickhoff, Edward W. Ferguson, Robert J. Gordon, Richard P. Dunlap, Catherine A. Franke, Albert J. Mura, Anne Rowlands, Judith A. Johnson, Virendra Kumar, Alan L. Maycock, Karl R. Mueller, Edward D. Pagani, David T. Robinson, Manohar T. Saindane, Paul J. Silver, and Sandhya Subramanian pp 739 - 744; DOI: 10.1021/jm00005a001 |
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2,4-Diamino-5-substituted-quinazolines as Inhibitors of a Human Dihydrofolate Reductase with a Site-Directed Mutation at Position 22 and of the Dihydrofolate Reductases from Pneumocystis carinii and Toxoplasma gondii Andre Rosowsky, Clara E. Mota, Sherry F. Queener, Mark Waltham, Emine Ercikan-Abali, and Joseph R. Bertino pp 745 - 752; DOI: 10.1021/jm00005a002 |
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Structure-Activity Studies of 2,3,4,4a,5,9b-Hexahydroindeno[1,2-c]pyridines as Antispermatogenic Agents for Male Contraception C. Edgar Cook, Mansukh C. Wani, Joseph M. Jump, Yue-W. Lee, Patricia A. Fail, Stephanie A. Anderson, Yu-Q. Gu, and Vladimir Petrow pp 753 - 763; DOI: 10.1021/jm00005a003 |
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Antimalarial Activity of New Dihydroartemisinin Derivatives. 6. .alpha.-Alkylbenzylic Ethers Ai Jeng Lin and Robert E. Miller pp 764 - 770; DOI: 10.1021/jm00005a004 |
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Synthesis and Anti-HIV-1 Activity of 4,5,6,7-Tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one (TIBO) Derivatives. 3 Henry J. Breslin, Michael J. Kukla, Donald W. Ludovici, Richard Mohrbacher, Winston Ho, Milton Miranda, James D. Rodgers, T. Kevin Hitchens, Gregory Leo, and et al. pp 771 - 793; DOI: 10.1021/jm00005a005 |
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Synthesis and Anti-HIV-1 Activity of 4,5,6,7-Tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one (TlBO) Derivatives. 4 Winston Ho, Michael J. Kukla, Henry J. Breslin, Donald W. Ludovici, Philip P. Grous, Craig J. Diamond, Milton Miranda, James D. Rodgers, Chih Y. Ho, and et al. pp 794 - 802; DOI: 10.1021/jm00005a006 |
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[[[(Thienylcarbonyl)alkyl]oxy]phenyl]- and [[[(Pyrrylcarbonyl)alkyl]oxy]phenyl]oxazoline Derivatives with Potent and Selective Antihuman Rhinovirus Activity Silvio Massa, Federico Corelli, Marino Artico, Antonello Mai, Rino Ragno, Antonella De Montis, Anna Giulia Loi, Simona Corrias, Maria Elena Marongiu, and Paolo La Colla pp 803 - 809; DOI: 10.1021/jm00005a007 |
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Fluorine for Hydroxy Substitution in Biogenic Amines: Asymmetric Synthesis and Biological Evaluation of Fluorine-18-Labeled .beta.-Fluorophenylalkylamines as Model Systems Marcian E. Van Dort, Yong-Woon Jung, Philip S. Sherman, Michael R. Kilbourn, and Donald M. Wieland pp 810 - 815; DOI: 10.1021/jm00005a008 |
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Synthesis of 11.beta.-[18F]Fluoro-5.alpha.-dihydrotestosterone and 11.beta.-[18F]Fluoro-19-nor-5.alpha.-dihydrotestosterone: Preparation via Halofluorination-Reduction, Receptor Binding, and Tissue Distribution Yearn Seong Choe, Pelle J. Lidstroem, Dae Yoon Chi, Thomas A. Bonasera, Michael J. Welch, and John A. Katzenellenbogen pp 816 - 825; DOI: 10.1021/jm00005a009 |
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Synthesis, Biological Evaluation, and Structure Analysis of a Series of New 1,5-Anhydrohexitol Nucleosides Ilse Verheggen, Arthur Van Aerschot, Luc Van Meervelt, Jef Rozenski, Leonard Wiebe, Robert Snoeck, Graciela Andrei, Jan Balzarini, Paul Claes, and et al. pp 826 - 835; DOI: 10.1021/jm00005a010 |
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Structural and Conformational Requirements for Human Calcitonin Activity: Design, Synthesis, and Study of Lactam-Bridged Analogs Afrodite Kapurniotu and John W. Taylor pp 836 - 847; DOI: 10.1021/jm00005a011 |
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Chemically Stable N-Methyl-4-(alkylthio)cyclophosphamide Derivatives as Prodrugs of 4-Hydroxycyclophosphamide Ki-Young Moon, Frances N. Shirota, Nesrine Baturay, and Chul-Hoon Kwon pp 848 - 851; DOI: 10.1021/jm00005a012 |
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Book Reviews pp 852 - 854; DOI: 10.1021/jm00005a600 |
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N-(1-Methyl-5-indolyl)-N'-(3-methyl-5-isothiazolyl)urea: A Novel, High-Affinity 5-HT2B Receptor Antagonist Ian T. Forbes, Graham E. Jones, Olive E. Murphy, Victoria Holland, and Gordon S. Baxter pp 855 - 857; DOI: 10.1021/jm00006a001 |
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Second Generation Leukotriene B4 Receptor Antagonists Related to SC-41930: Heterocyclic Replacement of the Methyl Ketone Pharmacophore Thomas D. Penning, Stevan W. Djuric', Julie M. Miyashiro, Stella Yu, James P. Snyder, Dale Spangler, Charles P. Anglin, Donald J. Fretland, James F. Kachur, and et al. pp 858 - 868; DOI: 10.1021/jm00006a002 |
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1-Thiomethoxsalen and 1-Thiopsoralen: Synthesis, Photobiological Properties, and Site Specific Reaction of Thiopsoralens with DNA Andreas E. Jakobs and Jacques Piette pp 869 - 874; DOI: 10.1021/jm00006a003 |
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Unsaturated Acyclic Analogs of 2'-Deoxyadenosine and Thymidine Containing Fluorine: Synthesis and Biological Activity Ze-Qi Xu, Yao-Ling Qiu, Sudhichai Chokekijchai, Hiroaki Mitsuya, and Jiri Zemlicka pp 875 - 882; DOI: 10.1021/jm00006a004 |
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Optimization of the Reaction Conditions for the Synthesis of Neoglycoprotein-AZT Monophosphate Conjugates Mirjam E. Kuipers, Pieter J. Swart, Margriet M. W. B. Hendriks, and Dirk K. F. Meijer pp 883 - 889; DOI: 10.1021/jm00006a005 |
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Three-Dimensional Quantitative Structure-Activity Relationship (QSAR) of HIV Integrase Inhibitors: A Comparative Molecular Field Analysis (CoMFA) Study K. Raghavan, John K. Buolamwini, Mark R. Fesen, Yves Pommier, Kurt W. Kohn, and John N. Weinstein pp 890 - 897; DOI: 10.1021/jm00006a006 |
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Nonpeptidic Potent HIV-1 Protease Inhibitors: (4-Hydroxy-6-phenyl-2-oxo-2H-pyran-3-yl)thiomethanes That Span P1-P2' Subsites in a Unique Mode of Binding J. V. N. Vara Prasad, Kimberly S. Para, Peter J. Tummino, Donna Ferguson, Thomas J. McQuade, Elizabeth A. Lumney, Stephen T. Rapundalo, Brain L. Batley, Gary Hingorani, and et al. pp 898 - 905; DOI: 10.1021/jm00006a007 |
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Rigid Analogs of Camptothecin as DNA Topoisomerase I Inhibitors Karen Lackey, Jeffrey M. Besterman, Wade Fletcher, Peter Leitner, Bradley Morton, and Daniel D. Sternbach pp 906 - 911; DOI: 10.1021/jm00006a008 |
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Dicationic Diarylfurans as Anti-Pneumocystis carinii Agents David W. Boykin, Arvind Kumar, Jaroslaw Spychala, Min Zhou, Richard J. Lombardy, W. David Wilson, Christine C. Dykstra, Susan K. Jones, James E. Hall, and et al. pp 912 - 916; DOI: 10.1021/jm00006a009 |
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Generation of the Neurotoxin 6-Hydroxydopamine by Peroxidase/H2O2 Oxidation of Dopamine Alessandra Napolitano, Orlando Crescenzi, Alessandro Pezzella, and Giuseppe Prota pp 917 - 922; DOI: 10.1021/jm00006a010 |
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Tryptophan-Derived NK1 Antagonists: Conformationally Constrained Heterocyclic Bioisosteres of the Ester Linkage Richard T. Lewis, Angus M. Macleod, Kevin J. Merchant, Fintan Kelleher, Ian Sanderson, Richard H. Herbert, Margaret A. Cascieri, Sharon Sadowski, Richard G. Ball, and Karst Hoogsteen pp 923 - 933; DOI: 10.1021/jm00006a011 |
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Synthesis and Biological Evaluation of NK1 Antagonists Derived from L-Tryptophan Angus M. MacLeod, Margaret A. Cascieri, Kevin J. Merchant, Sharon Sadowski, Sarah Hardwicke, Richard T. Lewis, D. Euan MacIntyre, Joseph M. Metzger, Tung Ming Fong, and et al. pp 934 - 941; DOI: 10.1021/jm00006a012 |
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High Affinity and Selectivity on 5-HT1A Receptor of 1-Aryl-4-[(1-tetralin)alkyl]piperazines. 2 Roberto Perrone, Francesco Berardi, Nicola A. Colabufo, Marcello Leopoldo, Vincenzo Tortorella, Francesco Fiorentini, Vincenzo Olgiati, Alberto Ghiglieri, and Stefano Govoni pp 942 - 949; DOI: 10.1021/jm00006a013 |
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Computer-Aided Molecular Modeling, Synthesis, and Biological Evaluation of 8-(Benzyloxy)-2-phenylpyrazolo[4,3-c]quinoline as a Novel Benzodiazepine Receptor Agonist Ligand C. G. Wang, T. Langer, P. G. Kamath, Z.-Q. Gu, P. Skolnick, and R. Ian Fryer pp 950 - 957; DOI: 10.1021/jm00006a014 |
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Stereoselective LSD-like Activity in a Series of d-Lysergic Acid Amides of (R)- and (S)-2-Aminoalkanes Aaron P. Monte, Danuta Marona-Lewicka, Arthi Kanthasamy, Elaine Sanders-Bush, and David E. Nichols pp 958 - 966; DOI: 10.1021/jm00006a015 |
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Quantitative structure-activity relationships of the inhibition of Pneumocystis carinii dihydrofolate reductase by 4,6-diamino-1,2-dihydro-2,2-dimethyl-1-(X-phenyl)-s-triazines Charles K. Marlowe, Cynthia Dias Selassie, and Daniel V. Santi pp 967 - 972; DOI: 10.1021/jm00006a016 |
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6-Aminoquinolones: A New Class of Quinolone Antibacterials? Violetta Cecchetti, Sergio Clementi, Gabriele Cruciani, Arnaldo Fravolini, Pier Giuseppe Pagella, Angela Savino, and Oriana Tabarrini pp 973 - 982; DOI: 10.1021/jm00006a017 |
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Amino-Substituted 2-[2-(Dimethylamino)ethyl]-1,2-dihydro-3H-dibenz[de,h]isoquinoline-1,3-diones. Synthesis, Antitumor Activity, and Quantitative Structure-Activity Relationship Salah M. Sami, Robert T. Dorr, Aniko M. Solyom, David S. Alberts, and William A. Remers pp 983 - 993; DOI: 10.1021/jm00006a018 |
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Quinazoline Antifolate Thymidylate Synthase Inhibitors: Replacement of Glutamic Acid in the C2-Methyl Series Peter R. Marsham, Ann L. Jackman, Andrew J. Barker, F. Thomas Boyle, Stephen J. Pegg, J. Michael Wardleworth, Rosemary Kimbell, Brigid M. O'Connor, A. Hilary Calvert, and Leslie R Hughes pp 994 - 1004; DOI: 10.1021/jm00006a019 |
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[[(Guaninylalkyl)phosphinico]methyl]phosphonic Acids. Multisubstrate Analog Inhibitors of Human Erythrocyte Purine Nucleoside Phosphorylase James L. Kelley, Ed W. McLean, Ronald C. Crouch, Devron R. Averett, and Joel V. Tuttle pp 1005 - 1014; DOI: 10.1021/jm00006a020 |
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Ketomethylene and (Cyanomethylene)amino Pseudopeptide Analogs of the C-Terminal Hexapeptide of Neurotensin Rosario Gonzalez-Muniz, M. Teresa Garcia-Lopez, Isabel Gomez-Monterrey, Rosario Herranz, M. Luisa Jimeno, M. Luisa Suarez-Gea, Nils L. Johansen, Kjeld Madsen, Henning Thogersen, and Peter Suzdak pp 1015 - 1021; DOI: 10.1021/jm00006a021 |
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Synthesis and Biological Activity of 7-Alkylidenecephems John D. Buynak, Kuangcong Wu, Brian Bachmann, Dipti Khasnis, Ling Hua, Hanh K. Nguyen, and Christa L. Carver pp 1022 - 1034; DOI: 10.1021/jm00006a022 |
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3-Deaza- and 7-Deaza-5'-noraristeromycin and Their Antiviral Properties Suhaib M. Siddiqi, Xing Chen, Jagadishwar Rao, Stewart W. Schneller, Satoru Ikeda, Robert Snoeck, Graciela Andrei, Jan Balzarini, and Erik De Clercq pp 1035 - 1038; DOI: 10.1021/jm00006a023 |
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Synthesis and Biological Activity of Thiazolylindolequinones, Analogs of the Natural Product BE 10988 Christopher J. Moody, Elizabeth Swann, Susan Houlbrook, Miriam A. Stephens, and Ian J. Stratford pp 1039 - 1043; DOI: 10.1021/jm00006a024 |
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Acylshikonin Analogs: Synthesis and Inhibition of DNA Topoisomerase-I Byung-Zun Ahn, Kyong-Up Baik, Gi-Ryang Kweon, Kyu Lim, and Byung-Doo Hwang pp 1044 - 1047; DOI: 10.1021/jm00006a025 |
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New Steroidal Antiinflammatory Antedrugs: Steroidal [16.alpha.,17.alpha.-d]-3'-Carbethoxyisoxazolines Taesoo Kwon, Ann S. Heiman, Ebenezer T. Oriaku, Kyoungjin Yoon, and Henry J. Lee pp 1048 - 1051; DOI: 10.1021/jm00006a026 |
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Comparison of a DSB-120 DNA interstrand crosslinked adduct with the corresponding bis-tomaymycin adduct: An example of a successful template-directed approach to drug design based upon the monoalkylating compound tomaymycin. [Erratum to document cited in CA121:195165] John A. Mountzouris, Jeh-Jeng Wang, David Thurston, and Laurence H. Hurley pp 1052 - 1052; DOI: 10.1021/jm00006a027 |
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Synthesis and Biology of 1D-3-Deoxyphosphatidylinositol: A Putative Antimetabolite of Phosphatidylinositol-3-phosphate and an Inhibitor of Cancer Cell Colony Formation Alan P. Kozikowski, James J. Kiddle, Timothy Frew, Margareta Berggren, and Garth Powis pp 1053 - 1056; DOI: 10.1021/jm00007a001 |
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Novel Thiazole Based Heterocycles as Inhibitors of LFA-1/ICAM-1 Mediated Cell Adhesion Pauline J. Sanfilippo, Michele C. Jetter, Richard Cordova, Robert A. Noe, Erika Chourmouzis, Catherine Y. Lau, and Elizabeth Wang pp 1057 - 1059; DOI: 10.1021/jm00007a002 |
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Cross-Validated R2-Guided Region Selection for Comparative Molecular Field Analysis: A Simple Method To Achieve Consistent Results Sung Jin Cho and Alexander Tropsha pp 1060 - 1066; DOI: 10.1021/jm00007a003 |
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Design, Synthesis, and Structure-Activity Relationship Studies for a New Imidazole Series of J774 Macrophage Specific Acyl-CoA:Cholesterol Acyltransferase (ACAT) Inhibitors Thomas P. Maduskuie Jr., Richard G. Wilde, Jeffrey T. Billheimer, Debra A. Cromley, Sandra Germain, Peter J. Gillies, C. Anne Higley, Alex L. Johnson, Penio Pennev, Edward J. Shimshick, and Ruth R. Wexler pp 1067 - 1083; DOI: 10.1021/jm00007a004 |
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Design and Synthesis of 1-Heteroaryl-3-(1-benzyl-4-piperidinyl)propan-1-one Derivatives as Potent, Selective Acetylcholinesterase Inhibitors Arthur A. Nagel, Dane R. Liston, Stanley Jung, Melissa Mahar, Lawrence A. Vincent, Douglas Chapin, Yuhpyng L. Chen, Sean Hubbard, Jeffrey L. Ives, and et al. pp 1084 - 1089; DOI: 10.1021/jm00007a005 |
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Thienylimidazo[2,1-b]thiazoles as Inhibitors of Mitochondrial NADH Dehydrogenase Aldo Andreani, Mirella Rambaldi, Alberto Leoni, Alessandra Locatelli, Anna Ghelli, Marina Ratta, Bruna Benelli, and Mauro Degli Esposti pp 1090 - 1097; DOI: 10.1021/jm00007a006 |
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Potent Inhibitors of Human Inosine Monophosphate Dehydrogenase Type II. Fluorine-Substituted Analogs of Thiazole-4-carboxamide Adenine Dinucleotide Andrzej Zatorski, Barry M. Goldstein, Thomas D. Colby, Jeffery P. Jones, and Krzysztof W. Pankiewicz pp 1098 - 1105; DOI: 10.1021/jm00007a007 |
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Synthesis, Topoisomerase I Inhibitory Activity, and in Vivo Evaluation of 11-Azacamptothecin Analogs David E. Uehling, Suganthini S. Nanthakumar, Dallas Croom, David L. Emerson, Peter P. Leitner, Michael J. Luzzio, Gordon McIntyre, Bradley Morton, Salvadore Profeta, and et al. pp 1106 - 1118; DOI: 10.1021/jm00007a008 |
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3-[[(Aryloxy)alkyl]piperidinyl]-1,2-Benzisoxazoles as D2/5-HT2 Antagonists with Potential Atypical Antipsychotic Activity: Antipsychotic Profile of Iloperidone (HP 873) Joseph T. Strupczewski, Kenneth J. Bordeau, Yulin Chiang, Edward J. Glamkowski, Paul G. Conway, Roy Corbett, Harold B. Hartman, Mark R. Szewczak, Carole A. Wilmot, and Grover C. Helsley pp 1119 - 1131; DOI: 10.1021/jm00007a009 |
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Mapping the Melatonin Receptor. 3. Design and Synthesis of Melatonin Agonists and Antagonists Derived from 2-Phenyltryptamines Peter J. Garratt, Rob Jones, Derek A. Tocher, and David Sugden pp 1132 - 1139; DOI: 10.1021/jm00007a010 |
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Synthesis of Two Distamycin Analogs and Their Binding Mode to d(CGCAAATTTGCG)2 in the 2:1 Solution Complexes as Determined by Two-Dimensional 1H-NMR Fabio Animati, Federico M. Arcamone, Maria Rosaria Conte, Patrizia Felicetti, Aldo Galeone, Paolo Lombardi, Luciano Mayol, Luigi G. Paloma, and Cristina Rossi pp 1140 - 1149; DOI: 10.1021/jm00007a011 |
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Novel Modified Carboxy Terminal Fragments of Neuropeptide Y with High Affinity for Y2-Type Receptors and Potent Functional Antagonism at the Y1-Type Receptor Johann J. Leban, Dennis Heyer, Antonio Landavazo, Jessica Matthews, Ann Aulabaugh, and Alejandro J. Daniels pp 1150 - 1157; DOI: 10.1021/jm00007a012 |
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Synthesis and in Vitro Activity of 17.beta.-(N-Alkyl/arylformamido and N-alkyl/arylalkyl/arylamido)-4-methyl-4-aza-3-oxo-5.alpha.-androstan-3-ones as Inhibitors of Human 5.alpha.-Reductases and Antagonists of the Androgen Receptor Xun Li, Shankar M. Singh, and Fernand Labrie pp 1158 - 1173; DOI: 10.1021/jm00007a013 |
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Search for New Purine- and Ribose-Modified Adenosine Analogs as Selective Agonists and Antagonists at Adenosine Receptors Suhaib M. Siddiqi, Kenneth A. Jacobson, John L. Esker, Mark E. Olah, Xiao-duo Ji, Neli Melman, Kamal N. Tiwari, John A. Secrist, III, Stewart W. Schneller, and et al. pp 1174 - 1188; DOI: 10.1021/jm00007a014 |
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Lipophilic, Acid-Stable, Adenosine Deaminase-Activated Anti-HIV Prodrugs for Central Nervous System Delivery. 2. 6-Halo- and 6-Alkoxy Prodrugs of 2'-.beta.-Fluoro-2',3'-dideoxyinosine Harry Ford, Maqbool Siddiqui, John S. Driscoll, Victor E. Marquez, James A. Kelley, Hiroaki Mitsuya, and Takuma Shirasaka pp 1189 - 1195; DOI: 10.1021/jm00007a015 |
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Ketanserin Analogs: The Effect of Structural Modification on 5-HT2 Serotonin Receptor Binding Abd M. Ismaiel, Kim Arruda, Milt Teitler, and Richard A. Glennon pp 1196 - 1202; DOI: 10.1021/jm00007a016 |
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7-Azetidinylquinolones as Antibacterial Agents. 3. Synthesis, Properties and Structure-Activity Relationships of the Stereoisomers Containing a 7-(3-Amino-2-methyl-1-azetidinyl) Moiety Jordi Frigola, David Vano, Antoni Torrens, Angels Gomez-Gomar, Edmundo Ortega, and Santiago Garcia-Granda pp 1203 - 1215; DOI: 10.1021/jm00007a017 |
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Synthesis of Alkyl Chain-Modified Ether Lipids and Evaluation of Their in Vitro Cytotoxicity Empar Fos, Nuria Suesa, Liset Borras, Cinta Lobato, Patrizia Banfi, Romolo A. Gambetta, Franco Zunino, David Mauleon, and Germano Carganico pp 1216 - 1228; DOI: 10.1021/jm00007a018 |
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Reductive Chemistry of the Novel Hypoxia-Selective Cytotoxin 5-[N,N-Bis(2-chloroethyl)amino]-2,4-dinitrobenzamide Brian D. Palmer, Pierre van Zijl, William A. Denny, and William R. Wilson pp 1229 - 1241; DOI: 10.1021/jm00007a019 |
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Opioid Receptor Binding Requirements for the .delta.-Selective Peptide Deltorphin I: Phe3 Replacement with Ring-Substituted and Heterocyclic Amino Acids Deborah L. Heyl, Meena Dandabathula, Kathleen R. Kurtz, and Carol Mousigian pp 1242 - 1246; DOI: 10.1021/jm00007a020 |
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Hypoxia-Selective Antitumor Agents. 11. Chlorambucil N-Oxide: A Reappraisal of Its Synthesis, Stability, and Selective Toxicity for Hypoxic Cells Moana Tercel, William R. Wilson, and William A. Denny pp 1247 - 1252; DOI: 10.1021/jm00007a021 |
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Book Reviews pp 1253 - 1254; DOI: 10.1021/jm00007a600 |
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The C-32 Triacetyl-L-rhamnose Derivative of Ascomycin: A Potent, Orally Active Macrolactone Immunosuppressant Kevin Koch, Michael F. Newborg, Douglas C. Hanson, Kelvin Cooper, Richard M. Shepard, Michael L. Biehl, Michael S. Biggers, Mukesh Ramchandani, Gary Schulte, and et al. pp 1255 - 1258; DOI: 10.1021/jm00008a001 |
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Discovery of a Novel Series of Orally Active Non-Peptide Endothelin-A (ETA) Receptor-Selective Antagonists Annette M. Doherty, William C. Patt, Jeremy J. Edmunds, Kent A. Berryman, Billy R. Reisdorph, Mark S. Plummer, Aurash Shahripour, Chet Lee, Xue-Min Cheng, and et al. pp 1259 - 1263; DOI: 10.1021/jm00008a002 |
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4,4-Disubstituted Piperidines: A New Class of NK1 Antagonists Graeme I. Stevenson, Angus M. MacLeod, Ian Huscroft, Margaret A. Cascieri, Sharon Sadowski, and Raymond Baker pp 1264 - 1266; DOI: 10.1021/jm00008a003 |
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Farnesyl Derivatives of Rigid Carboxylic Acids - Inhibitors of ras-Dependent Cell Growth Daniella Marciano, Gilad Ben-Baruch, Michal Marom, Yaakov Egozi, Roni Haklai, and Yoel Kloog pp 1267 - 1272; DOI: 10.1021/jm00008a004 |
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New (2-Methoxyphenyl)piperazine Derivatives as 5-HT1A Receptor Ligands with Reduced .alpha.1-Adrenergic Activity. Synthesis and Structure-Affinity Relationships Aurelio Orjales, Luisa Alonso-Cires, Luis Labeaga, and Reyes Corcostegui pp 1273 - 1277; DOI: 10.1021/jm00008a005 |
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N-Substituted Oxazolo[5,4-b]pyridin-2(1H)-ones: A New Class of Non-Opiate Antinociceptive Agents Marie-Claude Viaud, Patricia Jamoneau, Christine Flouzat, Jean-Guy Bizot-Espiard, Bruno Pfeiffer, Pierre Renard, Daniel-Henri Caignard, Gerard Adam, and Gerald Guillaumet pp 1278 - 1286; DOI: 10.1021/jm00008a006 |
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Synthesis and Histamine H1 Receptor Agonist Activity of a Series of 2-Phenylhistamines, 2-Heteroarylhistamines, and Analogs Christian Leschke, Sigurd Elz, Monique Garbarg, and Walter Schunack pp 1287 - 1294; DOI: 10.1021/jm00008a007 |
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Quantitative Binding Site Model Generation: Compass Applied to Multiple Chemotypes Targeting the 5-HT1A Receptor Ajay N. Jain, Nomi L. Harris, and John Y. Park pp 1295 - 1308; DOI: 10.1021/jm00008a008 |
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Determination of Receptor-Ligand Kinetic and Equilibrium Binding Constants using Surface Plasmon Resonance: Application to the lck SH2 Domain and Phosphotyrosyl Peptides M. M. Morelock, R. H. Ingraham, R. Betageri, and S. Jakes pp 1309 - 1318; DOI: 10.1021/jm00008a009 |
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Synthesis and Evaluation of Pharmacological and Pharmacokinetic Properties of Monopropyl Analogs of 5-, 7-, and 8-[[(Trifluoromethyl)sulfonyl]oxy]-2-aminotetralins: Central Dopamine and Serotonin Receptor Activity Clas Sonesson, Tjeerd Barf, Jonas Nilsson, Durk Dijkstra, Arvid Carlsson, Kjell Svensson, Martin W. Smith, Iain J. Martin, J. Neil Duncan, and et al. pp 1319 - 1329; DOI: 10.1021/jm00008a010 |
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Tricyclic Heteroaromatic Systems. Synthesis and A1 and A2a Adenosine Binding Activities of Some 1-Aryl-1,4-dihydro-3-methyl[1]benzopyrano[2,3-c]pyrazol-4-ones, 1-Aryl-4,9-dihydro-3-methyl-1H-pyrazolo[3,4-b]quinolin-4-ones, and 1-Aryl-1H-imidazo[4,5-b]quinoxalines Daniela Catarzi, Lucia Cecchi, Vittoria Colotta, Guido Filacchioni, Claudia Martini, Paolo Tacchi, and Antonio Lucacchini pp 1330 - 1336; DOI: 10.1021/jm00008a011 |
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Electrophilic N-Benzylnaltrindoles as .delta. Opioid Receptor-Selective Antagonists Vijaya L. Korlipara, Akira E. Takemori, and Philip S. Portoghese pp 1337 - 1343; DOI: 10.1021/jm00008a012 |
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Discovery and Structure-Activity Relationships of Sulfonamide ETA-Selective Antagonists Philip D. Stein, David M. Floyd, Sharon Bisaha, Joyce Dickey, Ravindar N. Girotra, Jack Z. Gougoutas, Michael Kozlowski, Ving G. Lee, Eddie C.-K. Liu, and et al. pp 1344 - 1354; DOI: 10.1021/jm00008a013 |
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Picornavirus Inhibitors: Trifluoromethyl Substitution Provides a Global Protective Effect against Hepatic Metabolism Guy D. Diana, Patrick Rudewicz, Daniel C. Pevear, Theodore J. Nitz, Suzanne C. Aldous, David J. Aldous, David T. Robinson, Tandy Draper, Frank J. Dutko, and et al. pp 1355 - 1371; DOI: 10.1021/jm00008a014 |
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Synthesis and in Vivo Evaluation of Prodrugs of 9-[2-(Phosphonomethoxy)ethoxy]adenine Halina T. Serafinowska, Ray J. Ashton, Stuart Bailey, Michael R. Harnden, Sally M. Jackson, and David Sutton pp 1372 - 1379; DOI: 10.1021/jm00008a015 |
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Cephalosporin Derivatives of Doxorubicin as Prodrugs for Activation by Monoclonal Antibody-.beta.-Lactamase Conjugates Vivekananda M. Vrudhula, Haakan P. Svensson, and Peter D. Senter pp 1380 - 1385; DOI: 10.1021/jm00008a016 |
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Conformationally Constrained Phosphotyrosyl Mimetics Designed as Monomeric src Homology 2 Domain Inhibitors Terrence R. Burke, Joseph J. Barchi, Clifford George, Gert Wolf, Steven E. Shoelson, and Xinjian Yan pp 1386 - 1396; DOI: 10.1021/jm00008a017 |
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Synthesis, Absolute Configuration, and Enantioselectivity of Antiretroviral Effect of (R)-(-)- and (S)-(+)-Cytallene. Lipase-Catalyzed Enantioselective Acylations of (.+-.)-N4-Acylcytallenes Bryan C. N. M. Jones, James V. Silverton, Claire Simons, Sreenivasulu Megati, Hisao Nishimura, Yosuke Maeda, Hiroaki Mitsuya, and Jiri Zemlicka pp 1397 - 1405; DOI: 10.1021/jm00008a018 |
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Novel Non-nucleoside Inhibitors of HIV-1 Reverse Transcriptase. 3. Dipyrido[2,3-b:2',3'-e]diazepinones John R. Proudfoot, Usha R. Patel, Suresh R. Kapadia, and Karl D. Hargrave pp 1406 - 1410; DOI: 10.1021/jm00008a019 |
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The Synthesis of N-Hydroxy-N'-phenyloctanediamide and Its Inhibitory Effect on Proliferation of AXC Rat Prostate Cancer Cells John C. Stowell, Rachel I. Huot, and Lainie Van Voast pp 1411 - 1413; DOI: 10.1021/jm00008a020 |
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Design and Synthesis of Piperidine-3-carboxamides as Human Platelet Aggregation Inhibitors [Erratum to document cited in CA122:95850] Xiaozhang Zheng, Somna R. Salgia, Walter B. Thompson, Elwood O. Dillingham, Stephen E. Bond, Zixia Feng, K. Ram Prasad, and Ram Gollamudi pp 1416 - 1416; DOI: 10.1021/jm00008a021 |
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An Evaluation of the Antirhinoviral Activity of Acylfuran Replacements for 3-Methylisoxazoles. Are 2-Acetylfurans Bioisosteres for 3-Methylisoxazoles? [Erratum to document cited in CA122:31229] Thomas R. Bailey, Guy D. Diana, John P. Mallamo, Niranjan Vescio, Tandy L. Draper, Philip M. Carabateas, Melody A. Long, Vincent L. Giranda, Frank J. Dutko, and Daniel C. Pevear pp 1416 - 1416; DOI: 10.1021/jm00008a022 |
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Book Reviews pp 1414 - 1415; DOI: 10.1021/jm00008a600 |
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Metabotropic Glutamate Receptors: Novel Targets for Drug Development Thomas Knoepfel, Rainer Kuhn, and Hans Allgeier pp 1417 - 1426; DOI: 10.1021/jm00009a001 |
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Expedient Method for the Solid-Phase Synthesis of Aspartic Acid Protease Inhibitors Directed toward the Generation of Libraries Ellen K. Kick and Jonathan A. Ellman pp 1427 - 1430; DOI: 10.1021/jm00009a002 |
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Measuring Diversity: Experimental Design of Combinatorial Libraries for Drug Discovery Eric J. Martin, Jeffrey M. Blaney, Michael A. Siani, David C. Spellmeyer, Alex K. Wong, and Walter H. Moos pp 1431 - 1436; DOI: 10.1021/jm00009a003 |
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Design, Synthesis, and Evaluation of A-, C-, and D-Ring Analogs of the Fungal Metabolite K-76 as Potential Complement Inhibitors Teodoro S. Kaufman, Ranjan P. Srivastava, Robert D. Sindelar, Susanne M. Scesney, and Henry C. Marsh pp 1437 - 1445; DOI: 10.1021/jm00009a004 |
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Evaluation of Physicochemical Parameters Important to the Oral Bioavailability of Peptide-like Compounds: Implications for the Synthesis of Renin Inhibitors Harriet W. Hamilton, Bruce A. Steinbaugh, Barbra H. Stewart, O. Helen Chan, Heidi L. Schmid, Richard Schroeder, Michael J. Ryan, Joan Keiser, Michael D. Taylor, and et al. pp 1446 - 1455; DOI: 10.1021/jm00009a005 |
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Synthesis and in Vitro Evaluation of 4-Substituted N-(1,1-Dimethylethyl)-3-oxo-4-androstene-17.beta.-carboxamides as 5.alpha.-Reductase Inhibitors and Antiandrogens Xun Li, Shankar M. Singh, Jean Cote, Sylvie Laplante, Raymonde Veilleux, and Fernand Labrie pp 1456 - 1461; DOI: 10.1021/jm00009a006 |
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2-Aralkynyl and 2-Heteroalkynyl Derivatives of Adenosine-5'-N-Ethyluronamide as Selective A2a Adenosine Receptor Agonists Gloria Cristalli, Emidio Camaioni, Sauro Vittori, Rosaria Volpini, Pier Andrea Borea, Annamaria Conti, Silvio Dionisotti, Ennio Ongini, and Angela Monopoli pp 1462 - 1472; DOI: 10.1021/jm00009a007 |
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Synthesis and Antiinflammatory Activity of Certain 5,6,7,8-Tetrahydroquinolines and Related Compounds William Calhoun, Richard P. Carlson, Roger Crossley, Louis J. Datko, Scott Dietrich, Kenneth Heatherington, Lisa A. Marshall, Peter J. Meade, Albert Opalko, and Robin G. Shepherd pp 1473 - 1481; DOI: 10.1021/jm00009a008 |
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Antitumor Activity of 9(R)-Dihydrotaxane Analogs Larry L. Klein, Leping Li, Clarence J. Maring, Clinton M. Yeung, Sheela A. Thomas, David J. Grampovnik, and Jacob J. Plattner pp 1482 - 1492; DOI: 10.1021/jm00009a009 |
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Antitumor Imidazotetrazines. 32.1 Synthesis of Novel Imidazotetrazinones and Related Bicyclic Heterocycles To Probe the Mode of Action of the Antitumor Drug Temozolomide A. S. Clark, B. Deans, M. F. G. Stevens, M. J. Tisdale, R. T. Wheelhouse, B. J. Denny, and J. A. Hartley pp 1493 - 1504; DOI: 10.1021/jm00009a010 |
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Phosphodiesterase Type IV Inhibition. Structure-Activity Relationships of 1,3-Disubstituted Pyrrolidines Paul L. Feldman, Marcus F. Brackeen, David J. Cowan, Brian E. Marron, Frank J. Schoenen, Jeffrey A. Stafford, Edward M. Suh, Paul L. Domanico, Dudley Rose, and et al. pp 1505 - 1510; DOI: 10.1021/jm00009a011 |
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Characterization of a Class of Peptide Boronates with Neutral P1 Side Chains as Highly Selective Inhibitors of Thrombin John J. Deadman, Said Elgendy, Christopher A. Goodwin, Donovan Green, Jehan A. Baban, Geeta Patel, Emmanuel Skordalakes, Naoyoshi Chino, Goran Claeson, and et al. pp 1511 - 1522; DOI: 10.1021/jm00009a012 |
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Probes for Narcotic Receptor-Mediated Phenomena. 20. Alteration of Opioid Receptor Subtype Selectivity of the 5-(3-Hydroxyphenyl)morphans by Application of the Message-Address Concept: Preparation of .delta.-Opioid Receptor Ligands Craig M. Bertha, Judith L. Flippen-Anderson, Richard B. Rothman, Frank Porreca, Peg Davis, Heng Xu, Karen Becketts, Xian-Yuan Cha, and Kenner C. Rice pp 1523 - 1537; DOI: 10.1021/jm00009a013 |
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Synthesis of Cluster Galactosides with High Affinity for the Hepatic Asialoglycoprotein Receptor Erik A. L. Biessen, Diana M. Beuting, Harlof C. P. F. Roelen, Gijs A. van de Marel, Jacques H. Van Boom, and Theo J. C. Van Berkel pp 1538 - 1546; DOI: 10.1021/jm00009a014 |
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Enantiomers of Diastereomeric cis-N-[1-(2-Hydroxy-2-phenylethyl)-3-methyl-4-piperidyl]-N-phenylpropanamides: Synthesis, X-ray Analysis, and Biological Activities George A. Brine, Peter A. Stark, Young Liu, F. Ivy Carroll, P. Singh, Heng Xu, and Richard B. Rothman pp 1547 - 1557; DOI: 10.1021/jm00009a015 |
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In Vitro Muscarinic Activity of Spiromuscarones and Related Analogs Edwin S. C. Wu, Ronald C. Griffith, James T. Loch, Alex Kover, Robert J. Murray, George B. Mullen, James C. Blosser, Anthony C. Machulskis, and Sally A. McCreedy pp 1558 - 1570; DOI: 10.1021/jm00009a016 |
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Phosphonates and Phosphinates: Novel Leaving Groups for Benzisothiazolone Inhibitors of Human Leukocyte Elastase Ranjit C. Desai, John C. Court, Edward Ferguson, Robert J. Gordon, Dennis J. Hlasta, Richard P. Dunlap, and Catherine A. Franke pp 1571 - 1574; DOI: 10.1021/jm00009a017 |
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Absolute Configuration of (+)-[Fluoro(hydroxyphenylphosphinyl)methyl]phosphonic Acid, a Specific Inhibitor of Na+-Gradient-Dependent Na+-Phosphate Cotransport across Renal Brush Border Membrane, by X-Ray Crystallographic Analysis of Its (-)-Quinine Salt Robert Bau, Phuong-Truc T. Pham, Gregory D. Duncan, and Charles E. McKenna pp 1575 - 1578; DOI: 10.1021/jm00009a018 |
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Discovery of .alpha.1a-Adrenergic Receptor Antagonists Based on the L-Type Ca2+ Channel Antagonist Niguldipine John M. Wetzel, Shou Wu Miao, Carlos Forray, Laurence A. Borden, Theresa A. Branchek, and Charles Gluchowski pp 1579 - 1581; DOI: 10.1021/jm00010a001 |
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Design and Evaluation of Nonpeptide Fibrinogen .gamma. Chain-Based GPIIB/IIIA Antagonists William J. Hoekstra, Mary Pat Beavers, Patricia Andrade-Gordon, Mary F. Evangelisto, Patricia M. Keane, Jeffery B. Press, Karen A. Tomko, Francis Fan, Marek Kloczewiak, and et al. pp 1582 - 1592; DOI: 10.1021/jm00010a002 |
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A Novel Pyrrolidine Analog of Histamine as a Potent, Highly Selective Histamine H3 Receptor Agonist Neng-Yang Shih, Andrew T. Lupo Jr., Robert Aslanian, Steven Orlando, John J. Piwinski, Michael J. Green, Ashit K. Ganguly, Michael A. Clark, Salvatore Tozzi, and et al. pp 1593 - 1599; DOI: 10.1021/jm00010a003 |
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Substituted (1,2-Diarylethyl)amide Acyl-CoA:Cholesterol Acyltransferase Inhibitors: Effect of Polar Groups on in Vitro and in Vivo Activity John W. Clader, Joel G. Berger, Robert E. Burrier, Harry R. Davis, Martin Domalski, Sundeep Dugar, Timothy P. Kogan, Brian Salisbury, and Wayne Vaccaro pp 1600 - 1607; DOI: 10.1021/jm00010a004 |
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A Novel Approach to Dual-Acting Thromboxane Receptor Antagonist/Synthase Inhibitors Based on the Link of 1,3-Dioxane-Thromboxane Receptor Antagonists and -Thromboxane Synthase Inhibitors Norman Ackerley, Andrew G. Brewster, George R. Brown, David S. Clarke, Alan J. Foubister, Stephen J. Griffin, Julian A. Hudson, Michael J. Smithers, and Paul R. O. Whittamore pp 1608 - 1628; DOI: 10.1021/jm00010a005 |
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Nucleoside Conjugates. 14. Synthesis and Antitumor Activity of 1-.beta.-D-Arabinofuranosylcytosine Conjugates of Ether Lipids with Improved Water Solubility Chung Hong, Alexander Nechaev, Alan J. Kirisits, Rakesh Vig, Sek-Wen Hui, and Charles R. West pp 1629 - 1634; DOI: 10.1021/jm00010a006 |
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Molecular Similarity from Atomic Electrostatic Multipole Comparisons. Application to Anti-HIV Drugs Edward M. Burgess, J. A. Ruell, Leon H. Zalkow, and Rudiger D. Haugwitz pp 1635 - 1640; DOI: 10.1021/jm00010a007 |
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Synthesis and Anti-HIV Activity of [AZT]-[TSAO-T] and [AZT]-[HEPT] Dimers as Potential Multifunctional Inhibitors of HIV-1 Reverse Transcriptase Sonsoles Velazquez, Rosa Alvarez, Ana San-Felix, Maria Luisa Jimeno, Erik De Clercq, Jan Balzarini, and Maria Jose Camarasa pp 1641 - 1649; DOI: 10.1021/jm00010a008 |
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Fluorenylalkanoic and Benzoic Acids as Novel Inhibitors of Cell Adhesion Processes in Leukocytes Gregory S. Hamilton, Richard E. Mewshaw, Carmen M. Bryant, Ying Feng, Gerda Endemann, Kip S. Madden, Jennifer E. Danczak, John Perumattam, Lawrence W. Stanton, and et al. pp 1650 - 1656; DOI: 10.1021/jm00010a009 |
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Benzophenone Derivatives: A Novel Series of Potent and Selective Inhibitors of Human Immunodeficiency Virus Type 1 Reverse Transcriptase Paul G. Wyatt, Richard C. Bethell, Nicholas Cammack, Daniel Charon, Nerina Dodic, Bernard Dumaitre, Derek N. Evans, Darren V. S. Green, Philippa L. Hopewell, and et al. pp 1657 - 1665; DOI: 10.1021/jm00010a010 |
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Antineoplastic Agents. 291. Isolation and Synthesis of Combretastatins A-4, A-5, and A-6 George R. Pettit, Sheo Bux Singh, Michael R. Boyd, Ernest Hamel, Robin K. Pettit, Jean M. Schmidt, and Fiona Hogan pp 1666 - 1672; DOI: 10.1021/jm00010a011 |
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Synthesis and Biological Properties of Water-Soluble p-Boronophenylalanine Derivatives. Relationship between Water Solubility, Cytotoxicity, and Cellular Uptake Hisao Nemoto, Jianping Cai, Satoshi Iwamoto, and Yoshinori Yamamoto pp 1673 - 1678; DOI: 10.1021/jm00010a012 |
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Synthesis of Novel Imidazobenzodiazepines as Probes of the Pharmacophore for "Diazepam-Insensitive" GABAA Receptors Puwen Zhang, Weijiang Zhang, Ruiyan Liu, Bradford Harris, Phil Skolnick, and James M. Cook pp 1679 - 1688; DOI: 10.1021/jm00010a013 |
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Dicarboxylic Acid Dipeptide Neutral Endopeptidase Inhibitors Gary M. Ksander, Raj D. Ghai, Reynalda deJesus, Clive Diefenbacher, Andrew Yuan, Carol Berry, Yumi Sakane, and Angelo Trapani pp 1689 - 1700; DOI: 10.1021/jm00010a014 |
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Buspirone Analogs as Ligands of the 5-HT1A Receptor. 1. The Molecular Structure of Buspirone and Its Two Analogs Zdzis-law Chilmonczyk, Andrzej Les, Agnieszka Wozniakowska, Jacek Cybulski, Anna E. Kozio-l, and Maria Gdaniec pp 1701 - 1710; DOI: 10.1021/jm00010a015 |
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Syntheses and Biological Properties of Chiral Fluoroalkyl Quinuclidinyl Benzilates Dale O. Kiesewetter, James V. Silverton, and William C. Eckelman pp 1711 - 1719; DOI: 10.1021/jm00010a016 |
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Structure-Activity Relationships of 9-Alkyladenine and Ribose-Modified Adenosine Derivatives at Rat A3 Adenosine Receptors Kenneth A. Jacobson, Suhaib M. Siddiqi, Mark E. Olah, Xiao-duo Ji, Neli Melman, Kamala Bellamkonda, Yacov Meshulam, Gary L. Stiles, and Hea O. Kim pp 1720 - 1735; DOI: 10.1021/jm00010a017 |
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Design, Synthesis, Biology, and Conformations of Bicyclic .alpha.-Melanotropin Analogs Carrie Haskell-Luevano, Mark D. Shenderovich, Shubh D. Sharma, Gregory V. Nikiforovich, Mac E. Hadley, and Victor J. Hruby pp 1736 - 1750; DOI: 10.1021/jm00010a018 |
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Time-Resolved Ligand Exchange Reactions: Kinetic Models for Competitive Inhibitors with Recombinant Human Renin Maurice M. Morelock, Christopher A. Pargellis, Edward T. Graham, Daniel Lamarre, and Grace Jung pp 1751 - 1761; DOI: 10.1021/jm00010a019 |
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Effects of a D-Cys6/L-Cys6 Interchange in Nonselective and Selective Vasopressin and Oxytocin Antagonists Maurice Manning, Ling Ling Cheng, Wieslaw A. Klis, Lajos Balaspiri, Aleksandra Olma, Wilbur H. Sawyer, Nga Ching Wo, and W. Y. Chan pp 1762 - 1769; DOI: 10.1021/jm00010a020 |
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S-(5'-Deoxy-5'-adenosyl)-1-aminoxy-4-(methylsulfonio)-2-cyclopentene (AdoMao): An Irreversible Inhibitor of S-Adenosylmethionine Decarboxylase with Potent in Vitro Antitrypanosomal Activity Junqing Guo, Yong Qian Wu, Donna Rattendi, Cyrus J. Bacchi, and Patrick M. Woster pp 1770 - 1777; DOI: 10.1021/jm00010a021 |
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6-Substituted 2,4-Diamino-5-methylpyrido[2,3-d]pyrimidines as Inhibitors of Dihydrofolate Reductases from Pneumocystis carinii and Toxoplasma gondii and as Antitumor Agents Aleem Gangjee, Anil Vasudevan, Sherry F. Queener, and Roy L. Kisliuk pp 1778 - 1785; DOI: 10.1021/jm00010a022 |
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Hypoxia-Selective Agents Derived from Quinoxaline 1,4-Di-N-oxides Antonio Monge, Juan A. Palop, Adela Lopez de Cerain, Virginia Senador, Francisco J. Martinez, Yolanda Sainz, Susana Narro, Estrella Garcia, Carlos de Miguel, and et al. pp 1786 - 1792; DOI: 10.1021/jm00010a023 |
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Synthesis of 4''-Deoxy Motilides: Identification of a Potent and Orally Active Prokinetic Drug Candidate Paul A. Lartey, Hugh N. Nellans, Ramin Faghih, Albert Petersen, Carla M. Edwards, Leslie Freiberg, Sherry Quigley, Kennan Marsh, Larry L Klein, and Jacob J. Plattner pp 1793 - 1798; DOI: 10.1021/jm00010a024 |
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Synthesis and Serotonergic Activity of N,N-Dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and Analogs: Potent Agonists for 5-HT1D Receptors Leslie J. Street, Raymond Baker, William B. Davey, Alexander R. Guiblin, Richard A. Jelley, Austin J. Reeve, Helen Routledge, Francine Sternfeld, Alan P. Watt, and et al. pp 1799 - 1810; DOI: 10.1021/jm00010a025 |
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Haloanilino Derivatives of Pyrimidines, Purines, and Purine Nucleoside Analogs: Synthesis and Activity against Human Cytomegalovirus Maria Medveczky, Te-Fang Yang, Joseph Gambino, Peter Medveczky, and George E. Wright pp 1811 - 1819; DOI: 10.1021/jm00010a026 |
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Inhibition of Herpes Simplex Virus Type 1 Helicase-Primase by (Dichloroanilino)purines and -pyrimidines James J. Crute, I. Robert Lehman, Joseph Gambino, Te-Fang Yang, Peter Medveczky, Mary Medveczky, Naseema N. Khan, Carel Mulder, James Monroe, and George E. Wright pp 1820 - 1825; DOI: 10.1021/jm00010a027 |
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Novel NMDA Antagonists: Replacement of the Pyridinium Ring of 6,11-Ethanobenzo[b]quinolizinium Cations with Heteroisoquinolinium Cations Virendra Kumar, Phil M. Carabateas, John A. Dority, William G. Earley, John P. Mallamo, Chakrapani Subramanyam, Lisa D. Aimone, Brian Ault, Diane L. DeHaven Hudkins, and Matthew S. Miller pp 1826 - 1830; DOI: 10.1021/jm00010a028 |
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Synthesis and Structure-Activity Relationships of Side-Chain-Substituted Analogs of the Allylamine Antimycotic Terbinafine Lacking the Central Amino Function Peter Nussbaumer, Ingrid Leitner, Karin Mraz, and Anton Stuetz pp 1831 - 1836; DOI: 10.1021/jm00010a029 |
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Design and Syntheses of Potent and Selective Dipeptide Inhibitors of Candida albicans Myristoyl-CoA:Protein N-Myristoyltransferase Balekudru Devadas, Mark E. Zupec, Sandra K. Freeman, David L. Brown, Srinivasan Nagarajan, James A. Sikorski, Charles A. McWherter, Daniel P. Getman, and Jeffrey I. Gordon pp 1837 - 1840; DOI: 10.1021/jm00011a001 |
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A-Ring Ortho-Disubstituted Aporphine Derivatives as Potential Agonists or Antagonists at Serotonergic 5-HT1A Receptors Joseph G. Cannon, Patrick T. Flaherty, Ugur Ozkutlu, and John Paul Long pp 1841 - 1845; DOI: 10.1021/jm00011a002 |
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The Cholesterol Derivative of a Triantennary Galactoside with High Affinity for the Hepatic Asialoglycoprotein Receptor: a Potent Cholesterol Lowering Agent E. A. L. Biessen, H. Broxterman, J. H. Van Boom, and Th. J. C. Van Berkel pp 1846 - 1852; DOI: 10.1021/jm00011a003 |
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Preparation and in Vitro Activities of Ethers of [D-Serine]8-cyclosporin Marcel K. Eberle, Peter Hiestand, Anne-Marie Jutzi-Eme, Francois Nuninger, and Hans R. Zihlmann pp 1853 - 1864; DOI: 10.1021/jm00011a004 |
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Prodrugs of Nitroxyl as Potential Aldehyde Dehydrogenase Inhibitors vis-a-vis Vascular Smooth Muscle Relaxants Herbert T. Nagasawa, Sagar P. Kawle, James A. Elberling, Eugene G. DeMaster, and Jon M. Fukuto pp 1865 - 1871; DOI: 10.1021/jm00011a005 |
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Carbethoxylating Agents as Inhibitors of Aldehyde Dehydrogenase Herbert T. Nagasawa, Eugene G. DeMaster, David J. W. Goon, Sagar P. Kawle, and Frances N. Shirota pp 1872 - 1876; DOI: 10.1021/jm00011a006 |
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Novel Inhibitors of Potassium Ion Channels on Human T Lymphocytes William F. Michne, Joseph W. Guiles, Adi M. Treasurywala, Laurie A. Castonguay, Carolyn A. Weigelt, Bernard Oconnor, Walter A. Volberg, Alison M. Grant, Christopher C. Chadwick, Douglas S. Krafte, and Roger J. Hill pp 1877 - 1883; DOI: 10.1021/jm00011a007 |
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Use of Medium-Sized Cycloalkyl Rings To Enhance Secondary Binding: Discovery of a New Class of Human Immunodeficiency Virus (HIV) Protease Inhibitors Karen R. Romines, Keith D. Watenpaugh, Paul K. Tomich, W. Jeffrey Howe, Jeanette K. Morris, Kristine D. Lovasz, Anne M. Mulichak, Barry C. Finzel, Janet C. Lynn, and et al. pp 1884 - 1891; DOI: 10.1021/jm00011a008 |
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Synthesis and Biological Evaluation of Novel 2,6-Diaminobenz[cd]indole Inhibitors of Thymidylate Synthase Using the Protein Structure as a Guide Michael D. Varney, Cindy L. Palmer, Judith G. Deal, Stephanie Webber, Katherine M. Welsh, Charlotte A. Bartlett, Catharine A. Morse, Ward W. Smith, and Cheryl A. Janson pp 1892 - 1903; DOI: 10.1021/jm00011a009 |
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Studies on the Monoamine Oxidase (MAO)-Catalyzed Oxidation of Phenyl-Substituted 1-Methyl-4-phenoxy-1,2,3,6-tetrahydropyridine Derivatives: Factors Contributing to MAO-A and MAO-B Selectivity You-Xiong Wang and Neal Castagnoli pp 1904 - 1910; DOI: 10.1021/jm00011a010 |
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Synthesis, Characterization, and Antimalarial Activity of the Glucuronides of the Hydroxylated Metabolites of Arteether Kumar Ramu and John K. Baker pp 1911 - 1921; DOI: 10.1021/jm00011a011 |
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Antimalarial Activity of Novel Ring-Contracted Artemisinin Derivatives Bindumadhavan Venugopalan, Chintamani P. Bapat, Pravin J. Karnik, Dipak K. Chatterjee, Natarajan Iyer, and Dogel Lepcha pp 1922 - 1927; DOI: 10.1021/jm00011a012 |
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Hypoxia-Selective Antitumor Agents. 10. Bis(nitroimidazoles) and Related Bis(nitroheterocycles): Development of Derivatives with Higher Rates of Metabolic Activation under Hypoxia and Improved Aqueous Solubility Michael P. Hay, Ho H. Lee, William R. Wilson, Peter B. Roberts, and William A. Denny pp 1928 - 1941; DOI: 10.1021/jm00011a013 |
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N4-Unsubstituted N1-Arylpiperazines as High-Affinity 5-HT1A Receptor Ligands Wilma Kuipers, Ineke van Wijngaarden, Chris G. Kruse, Marian ter Horst van Amstel, Martin Th. M. Tulp, and Adriaan P. IJzerman pp 1942 - 1954; DOI: 10.1021/jm00011a014 |
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Potent, Orally Active, Competitive N-Methyl-D-aspartate (NMDA) Receptor Antagonists Are Substrates for a Neutral Amino Acid Uptake System in Chinese Hamster Ovary Cells Jia-He Li, Christopher F. Bigge, Rufus M. Williamson, Susan A. Borosky, Mark G. Vartanian, and Daniel F. Ortwine pp 1955 - 1965; DOI: 10.1021/jm00011a015 |
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Cardioselective Antiischemic ATP-Sensitive Potassium Channel Openers. 2. Structure-Activity Studies on Benzopyranylcyanoguanidines; Modification of the Benzopyran Ring Karnail S. Atwal, Gary J. Grover, Francis N. Ferrara, Syed Z. Ahmed, Paul G. Sleph, Steven Dzwonczyk, and Diane E. Normandin pp 1966 - 1973; DOI: 10.1021/jm00011a016 |
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Three-Dimensional Quantitative Structure-Activity Relationships of Somatostatin Analogs. 1. Comparative Molecular Field Analysis of Growth Hormone Release-Inhibiting Potencies Simon J. Hocart, Vik Reddy, William A. Murphy, and David H. Coy pp 1974 - 1989; DOI: 10.1021/jm00011a017 |
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Structure-Activity Relationships of Milrinone Analogs Determined in Vitro in a Rabbit Heart Membrane Ca2+-ATPase Model Vivian Cody, Andrzej Wojtczak, Faith B. Davis, Paul J. Davis, and Susan D. Blas pp 1990 - 1997; DOI: 10.1021/jm00011a018 |
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.sigma. Ligands with Subnanomolar Affinity and Preference for the .sigma.2 Binding Site. 1. 3-(.omega.-Aminoalkyl)-1H-indoles Jens Perregaard, Ejner K. Moltzen, Eddi Meier, and Connie Sanchez pp 1998 - 2008; DOI: 10.1021/jm00011a019 |
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.sigma. Ligands with Subnanomolar Affinity and Preference for the .sigma.2 Binding Site. 2. Spiro-Joined Benzofuran, Isobenzofuran, and Benzopyran Piperidines Ejner K. Moltzen, Jens Perregaard, and Eddi Meier pp 2009 - 2017; DOI: 10.1021/jm00011a020 |
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Ocular Delivery of the .beta.-Adrenergic Antagonist Alprenolol by Sequential Bioactivation of Its Methoxime Analog Laszlo Prokai, Whei-Mei Wu, Gabor Somogyi, and Nicholas Bodor pp 2018 - 2020; DOI: 10.1021/jm00011a021 |
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DNA-Directed Alkylating Agents. 6. Synthesis and Antitumor Activity of DNA Minor Groove-Targeted Aniline Mustard Analogs of Pibenzimol. [Erratum to document cited in CA121:300815] G. Lancer Gravatt, Bruce C. Baguley, William R. Wilson, and William A. Denny pp 2022 - 2022; DOI: 10.1021/jm00011a022 |
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Book Reviews pp 2021 - 2021; DOI: 10.1021/jm00011a600 |
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Ribozymes as Human Therapeutic Agents Ralph E. Christoffersen and J. Joseph Marr pp 2023 - 2037; DOI: 10.1021/jm00012a001 |
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Thiadiazole Derivatives: Highly Potent and Specific HIV-1 Reverse Transcriptase Inhibitors Yasuaki Hanasaki, Hiroyuki Watanabe, Kimio Katsuura, Hiromitsu Takayama, Seiichiro Shirakawa, Kentaro Yamaguchi, Shin-ichiro Sakai, Katsushi Ijichi, Masatoshi Fujiwara, and et al. pp 2038 - 2040; DOI: 10.1021/jm00012a002 |
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Synthesis, Antitubulin and Antimitotic Activity, and Cytotoxicity of Analogs of 2-Methoxyestradiol, an Endogenous Mammalian Metabolite of Estradiol That Inhibits Tubulin Polymerization by Binding to the Colchicine Binding Site Mark Cushman, Hu-Ming He, John A. Katzenellenbogen, Chii M. Lin, and Ernest Hamel pp 2041 - 2049; DOI: 10.1021/jm00012a003 |
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Design and Synthesis of New Naphthalenic Derivatives as Ligands for 2-[125I]Iodomelatonin Binding Sites Michel Langlois, Beatrice Bremont, Shuren Shen, Annie Poncet, Jean Andrieux, Sames Sicsic, Isabelle Serraz, Monique Mathe-Allainmat, Pierre Renard, and Philippe Delagrange pp 2050 - 2060; DOI: 10.1021/jm00012a004 |
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Application of the Free Energy Perturbation Method to Human Carbonic Anhydrase II Inhibitors Karen A. Rossi, Kenneth M. Jr. Merz, Graham M. Smith, and John J. Baldwin pp 2061 - 2069; DOI: 10.1021/jm00012a005 |
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Investigation of the Configurational and Conformational Influences on the Hormonal Activity of 1,2-Bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamines and of their Platinum(II) Complexes. 1. Synthesis, Estradiol Receptor Affinity, and Estrogenic Activity of Diastereomeric [N-Alkyl- and N,N'-Dialkyl-1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamine]dichloroplatinum(II) Complexes Ronald Gust, Karlheinz Niebler, and Helmut Schoenenberger pp 2070 - 2079; DOI: 10.1021/jm00012a006 |
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Receptor Surface Models. 1. Definition and Construction Mathew Hahn pp 2080 - 2090; DOI: 10.1021/jm00012a007 |
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Receptor Surface Models. 2. Application to Quantitative Structure-Activity Relationships Studies Mathew Hahn and David Rogers pp 2091 - 2102; DOI: 10.1021/jm00012a008 |
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Pyridyl-Substituted Tetrahydrocyclopropa[a]naphthalenes: Highly Active and Selective Inhibitors of P450 arom Rolf W. Hartmann, Herbert Bayer, Gertrud Gruen, Tom Sergejew, Ulrike Bartz, and Markus Mitrenga pp 2103 - 2111; DOI: 10.1021/jm00012a009 |
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Synthesis and Cytotoxicity of Novel Lignans Oskar Middel, Herman J. Woerdenbag, Wim van Uden, Arjan van Oeveren, Johan F. G. A. Jansen, Ben L. Feringa, Antonius W. T. Konings, Niesko Pras, and Richard M. Kellogg pp 2112 - 2118; DOI: 10.1021/jm00012a010 |
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Hydroxamic Acids as Potent Inhibitors of Endothelin-Converting Enzyme from Human Bronchiolar Smooth Muscle Ron Bihovsky, Barry L. Levinson, Rivka C. Loewi, Paul W. Erhardt, and Mark A. Polokoff pp 2119 - 2129; DOI: 10.1021/jm00012a011 |
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Development of a Novel Series of Trialkoxyaryl Derivatives as Specific and Competitive Antagonists of Platelet Activating Factor Richard M. Beams, Geoffrey J. Blackwell, Michael A. Brockwell, Neil J. Cheesman, Derek A. Demaine, Lawrence G. Garland, Harold F. Hodson, Richard M. Hyde, Peter J. Islip, and et al. pp 2130 - 2137; DOI: 10.1021/jm00012a012 |
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Immunospecific Reduction of Antioligonucleotide Antibody-Forming Cells with a Tetrakis-oligonucleotide Conjugate (LJP 394), a Therapeutic Candidate for the Treatment of Lupus Nephritis David S. Jones, Paul A. Barstad, Mark J. Feild, John P. Hachmann, Merle S. Hayag, Kenneth W. Hill, G. Michael Iverson, Douglas A. Livingston, Moorthy S. Palanki, and et al. pp 2138 - 2144; DOI: 10.1021/jm00012a013 |
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Design and Synthesis of Novel Inhibitors of HIV-1 Reverse Transcriptase Helena Maruenda and Francis Johnson pp 2145 - 2151; DOI: 10.1021/jm00012a014 |
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Synthesis and Biological Evaluation of a Series of New Parenteral Optically Active 3-[[(N-Alkylpyridinium-4'-yl)thio]methyl]-2-oxaisocephems Hidetsugu Tsubouchi, Koichi Tsuji, Koichi Yasumura, Makoto Matsumoto, Takuya Shitsuta, and Hiroshi Ishikawa pp 2152 - 2157; DOI: 10.1021/jm00012a015 |
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Novel 2,4-Diamino-5-substituted-pyrrolo[2,3-d]pyrimidines as Classical and Nonclassical Antifolate Inhibitors of Dihydrofolate Reductases Aleem Gangjee, Farahnaz Mavandadi, Sherry F. Queener, and John J. McGuire pp 2158 - 2165; DOI: 10.1021/jm00012a016 |
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Comparison of the Protonation of Isophosphoramide Mustard and Phosphoramide Mustard Kevin K. Millis, Michael E. Colvin, Ellen M. Shulman-Roskes, Susan M. Ludeman, O. Michael Colvin, and Michael P. Gamcsik pp 2166 - 2175; DOI: 10.1021/jm00012a017 |
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Structure-Activity Relationship of .alpha.-Galactosylceramides against B16-Bearing Mice Masahiro Morita, Kazuhiro Motoki, Kohji Akimoto, Takenori Natori, Teruyuki Sakai, Eiji Sawa, Kazuo Yamaji, Yasuhiko Koezuka, Eiichi Kobayashi, and Hideaki Fukushima pp 2176 - 2187; DOI: 10.1021/jm00012a018 |
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Annulated Heterocyclic Bioisosteres of Norarecoline. Synthesis and Molecular Pharmacology at Five Recombinant Human Muscarinic Acetylcholine Receptors Hans Braeuner-Osborne, Bjarke Ebert, Mark R. Brann, Erik Falch, and Povl Krogsgaard-Larsen pp 2188 - 2195; DOI: 10.1021/jm00012a019 |
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Synthesis of Some 2-Aryl-1,2,4-triazolo[1,5-c][1,3]benzoxazin-5-ones as Tools To Define the Essential Pharmacophoric Descriptors of a Benzodiazepine Receptor Ligand Daniela Catarzi, Lucia Cecchi, Vittoria Colotta, Guido Filacchioni, Flavia Varano, Claudia Martini, Laura Giusti, and Antonio Lucacchini pp 2196 - 2201; DOI: 10.1021/jm00012a020 |
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Structure-Activity Relationships in the 8-Amino-6,7,8,9-tetrahydro-3H-benz[e]indole Ring System. Part 1: Effects of Substituents in the Aromatic System on Serotonin and Dopamine Receptor Subtypes Peter Stjernloef, Michael D. Ennis, Lars O. Hansson, Robert L. Hoffman, Nabil B. Ghazal, Staffan Sundell, Martin W. Smith, Kjell Svensson, Arvid Carlsson, and Hkan Wikstroem pp 2202 - 2216; DOI: 10.1021/jm00012a021 |
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Structure-Activity Relationships in the 8-Amino-6,7,8,9-tetrahydro-3H-benz[e]indole Ring System. Part 2: Effect of 8-Amino Nitrogen Substitution on Serotonin Receptor Binding and Pharmacology Michael D. Ennis, Peter Stjernloef, Robert L. Hoffman, Nabil B. Ghazal, Martin W. Smith, Kjell Svensson, Haakan Wikstroem, Susanne R. Haadsma-Svensson, and Chiu-Hong Lin pp 2217 - 2230; DOI: 10.1021/jm00012a022 |
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Irreversible Inhibitors of Nicotinic Acetylcholine Receptors: Isolation and Structural Characterization of the Biologically Active Solvolysis Products of Bipinnatin-A and Bipinnatin-C Edward G. Hyde, Arthur Boyer, Pei Tang, Yan Xu, and Stewart N. Abramson pp 2231 - 2238; DOI: 10.1021/jm00012a023 |
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Identification of 3,5-Dihydro-2-aryl-1H-pyrazolo[3,4-c]quinoline-1,4(2H)-diones as Novel High-Affinity Glycine Site N-Methyl-D-aspartate Antagonists Angus M. MacLeod, Sarah Grimwood, Cheryl Barton, Linda Bristow, Kay L. Saywell, George R. Marshall, and Richard G. Ball pp 2239 - 2243; DOI: 10.1021/jm00012a024 |
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New Analogs of Burimamide as Potent and Selective Histamine H3 Receptor Antagonists: The Effect of Chain Length Variation of the Alkyl Spacer and Modifications of the N-Thiourea Substituent Roeland C. Vollinga, Wiro M. P. B. Menge, Rob Leurs, and Hendrik Timmerman pp 2244 - 2250; DOI: 10.1021/jm00012a025 |
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2-Phenyl-4-(aminomethyl)imidazoles as Potential Antipsychotic Agents. Synthesis and Dopamine D2 Receptor Binding Andrew Thurkauf, Alan Hutchison, John Peterson, Linda Cornfield, Robin Meade, Kevin Huston, Kristine Harris, Philip C. Ross, Karen Gerber, and T. V. Ramabhadran pp 2251 - 2255; DOI: 10.1021/jm00012a026 |
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Application of 15N Nuclear Magnetic Resonance Spectroscopy to the Determination of the Stability of Aryl Nitrogen Mustards Derry E. V. Wilman, Brian D. Palmer, and William A. Denny pp 2256 - 2258; DOI: 10.1021/jm00012a027 |
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Effects of Tubercidin and its 5'-O-Methyl Ether on Adenosine Receptors and Mediator Release Functions in Mast Cells Charles G. Smith, Sung J. Lee, and Diana L. Marquardt pp 2259 - 2262; DOI: 10.1021/jm00012a028 |
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Synthesis and Biological Evaluation of Novel C-4 Aziridine-Bearing Paclitaxel (Taxol) Analogs Shu-Hui Chen, Craig Fairchild, and Byron H. Long pp 2263 - 2267; DOI: 10.1021/jm00012a029 |
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Book Reviews pp 2268 - 2272; DOI: 10.1021/jm00012a600 |
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Further Evidence Supporting the Importance of and the Restrictions on a Carbon-Centered Radical for High Antimalarial Activity of 1,2,4-Trioxanes Like Artemisinin Gary H. Posner, Dasong Wang, Jared N. Cumming, Chang Ho Oh, Andrew N. French, Annette L. Bodley, and Theresa A. Shapiro pp 2273 - 2275; DOI: 10.1021/jm00013a001 |
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Potent Inhibitors of Proteasome Mohamed Iqbal, Sankar Chatterjee, James C. Kauer, Manoj Das, Patricia Messina, Bethany Freed, William Biazzo, and Robert Siman pp 2276 - 2277; DOI: 10.1021/jm00013a002 |
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The role of charge in polyamine analog recognition Raymond J. Bergeron, James S. McManis, William R. Weimar, Kathy Schreier, Fenglan Gao, Qianhong Wu, Jackqueline Ortiz-Ocasio, Gabriel R. Luchetta, Carl Porter, and J. R. Timothy Vinson pp 2278 - 2285; DOI: 10.1021/jm00013a003 |
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Secondary Interactions Significantly Removed from the Sulfonamide Binding Pocket of Carbonic Anhydrase II Influence Inhibitor Binding Constants P. Ann Boriack, David W. Christianson, Jill Kingery-Wood, and George M. Whitesides pp 2286 - 2291; DOI: 10.1021/jm00013a004 |
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Increasing Binding Constants of Ligands to Carbonic Anhydrase by Using "Greasy Tails" Jinming Gao, Shuang Qiao, and George M. Whitesides pp 2292 - 2301; DOI: 10.1021/jm00013a005 |
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Conformationally Defined 6-s-trans-Retinoic Acid Analogs. 2. Selective Agonists for Nuclear Receptor Binding and Transcriptional Activity Muzaffar Alam, Valdimir Zhestkov, Brahma P. Sani, Pratap Venepally, Arthur A. Levin, Sonja Kazmer, Ellen Li, Andrew W. Norris, Xiao-kun Zhang, and et al. pp 2302 - 2310; DOI: 10.1021/jm00013a006 |
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Mechanism-Based Development of New Antimalarials: Synthesis of Derivatives of Artemisinin Attached to Iron Chelators Sumalee Kamchonwongpaisan, Sumpan Paitayatat, Yodhathai Thebtaranonth, Prapin Wilairat, and Yongyuth Yuthavong pp 2311 - 2316; DOI: 10.1021/jm00013a007 |
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Sequence-Dependent Drug Binding to the Minor Groove of DNA: Crystal Structure of the DNA Dodecamer d(CGCAAATTTGCG)2 Complexed with Propamidine Christine M. Nunn and Stephen Neidle pp 2317 - 2325; DOI: 10.1021/jm00013a008 |
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The Serotonin 5-HT4 Receptor. 1. Design of a New Class of Agonists and Receptor Map of the Agonist Recognition Site Karl-Heinz Buchheit, Rainer Gamse, Rudolf Giger, Daniel Hoyer, Francois Klein, Edgar Kloeppner, Hans-Juergen Pfannkuche, and Henri Mattes pp 2326 - 2330; DOI: 10.1021/jm00013a009 |
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The Serotonin 5-HT4 Receptor. 2. Structure-Activity Studies of the Indole Carbazimidamide Class of Agonists Karl-Heinz Buchheit, Rainer Gamse, Rudolf Giger, Daniel Hoyer, Francois Klein, Edgar Kloeppner, Hans-Juergen Pfannkuche, and Henri Mattes pp 2331 - 2338; DOI: 10.1021/jm00013a010 |
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Steroidal Affinity Labels of the Estrogen Receptor. 2. 17.alpha.-[(Haloacetamido)alkyl]estradiols Driss El Garrouj, Sigrid Aliau, Andre Aumelas, and Jean-Louis Borgna pp 2339 - 2348; DOI: 10.1021/jm00013a011 |
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N-Alkylated Nitrogen-in-the-Ring Sugars: Conformational Basis of Inhibition of Glycosidases and HIV-1 Replication Naoki Asano, Haruhisa Kizu, Kengo Oseki, Emiko Tomioka, Katsuhiko Matsui, Mika Okamoto, and Masanori Baba pp 2349 - 2356; DOI: 10.1021/jm00013a012 |
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Sulfonylureas and Sulfonylcarbamates as New Non-Tetrazole Angiotensin II Receptor Antagonists. Discovery of a Highly Potent Orally Active (Imidazolylbiphenylyl)sulfonylurea (HR 720) Pierre Deprez, Jacques Guillaume, Reinhard Becker, Alain Corbier, Stanislas Didierlaurent, Michel Fortin, Daniel Frechet, Gilles Hamon, Bertrand Heckmann, and et al. pp 2357 - 2377; DOI: 10.1021/jm00013a013 |
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Potent in Vitro and in Vivo Inhibitors of Platelet Aggregation Based Upon the Arg-Gly-Asp Sequence of Fibrinogen. (Aminobenzamidino)succinyl (ABAS) Series of Orally Active Fibrinogen Receptor Antagonists Jeffery A. Zablocki, Joseph G. Rico, Robert B. Garland, Thomas E. Rogers, Kenneth Williams, Lori A. Schretzman, Shashidhar A. Rao, Philippe R. Bovy, Foe S. Tjoeng, and et al. pp 2378 - 2394; DOI: 10.1021/jm00013a014 |
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Synthesis and Evaluation of 6,7-Dihydroxy-2,3,4,8,9,13b-hexahydro-1H-benzo[6,7]cyclohepta[1,2,3-ef][3]benzazepine, 6,7-Dihydroxy-1,2,3,4,8,12b-hexahydroanthr[10,4a,4-cd]azepine, and 10-(Aminomethyl)-9,10-dihydro-1,2-dihydroxyanthracene as Conformationally Restricted Analogs of .beta.-Phenyldopamine Scott E. Snyder, Felix A. Aviles-Garay, Ratna Chakraborti, David E. Nichols, Val J. Watts, and Richard B. Mailman pp 2395 - 2409; DOI: 10.1021/jm00013a015 |
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Synthesis and Opioid Activity of Conformationally Constrained Dynorphin A Analogs. 1. Conformational Constraint in the "Message" Sequence Seksiri Arttamangkul, Thomas F. Murray, Gary E. DeLander, and Jane V. Aldrich pp 2410 - 2417; DOI: 10.1021/jm00013a016 |
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Synthesis and Activity against Multidrug Resistance in Chinese Hamster Ovary Cells of New Acridone-4-carboxamides Nerina Dodic, Bernard Dumaitre, Alain Daugan, and Pascal Pianetti pp 2418 - 2426; DOI: 10.1021/jm00013a017 |
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Synthesis and Anti-HIV Activity of 1,1'-Dideoxygossypol and Related Compounds Robert E. Royer, Lorraine M. Deck, Timothy J. Vander Jagt, Francella J. Martinez, Ray G. Mills, Stephen A. Young, and David L. Vander Jagt pp 2427 - 2432; DOI: 10.1021/jm00013a018 |
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Polyanion Inhibitors of Human Immunodeficiency Virus and Other Viruses. 1. Polymerized Anionic Surfactants A. Leydet, Ph. Barthelemy, B. Boyer, G. Lamaty, J. P. Roque, A. Bousseau, M. Evers, Y. Henin, R. Snoeck, et al., S. Ikeda, D. Reymen, and E. De Clercq pp 2433 - 2440; DOI: 10.1021/jm00013a019 |
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[(Alkylamino)methyl]acrylophenones: Potent and Selective Inhibitors of the Epidermal Growth Factor Receptor Protein Tyrosine Kinase Peter Traxler, Uwe Trinks, Elisabeth Buchdunger, Helmut Mett, Thomas Meyer, Marcel Mueller, Urs Regenass, Johannes Roesel, and Nicholas Lydon pp 2441 - 2448; DOI: 10.1021/jm00013a020 |
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Orally Active .beta.-Lactam Inhibitors of Human Leukocyte Elastase. 3. Stereospecific Synthesis and Structure-Activity Relationships for 3,3-Dialkylazetidin-2-ones Paul E. Finke, Shrenik K. Shah, Daniel S. Fletcher, Bonnie M. Ashe, Karen A. Brause, Gilbert O. Chandler, Pam S. Dellea, Karen M. Hand, Alan L. Maycock, and et al. pp 2449 - 2462; DOI: 10.1021/jm00013a021 |
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Novel Steroidal Inhibitors of Human Cytochrome P45017.alpha.-Hydroxylase-C17,20-lyase): Potential Agents for the Treatment of Prostatic Cancer Gerard A. Potter, S. Elaine Barrie, Michael Jarman, and Martin G. Rowlands pp 2463 - 2471; DOI: 10.1021/jm00013a022 |
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(Piperidinylalkoxy)chromones: Novel Antihistamines with Additional Antagonistic Activity against Leukotriene D4 Ming-Qiang Zhang, Yasushi Wada, Fumiyasu Sato, and Henk Timmerman pp 2472 - 2477; DOI: 10.1021/jm00013a023 |
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Use of .beta.-Methylphenylalanine (.beta.MeF) Residues To Probe the Nature of the Interaction of Substance P with Its Receptor: Effects of .beta.MeF-Containing Substance P Analogs on Rabbit Iris Smooth Muscle Contraction David M. Birney, Derek C. Cole, Craig E. Crosson, Brenda F. Kahl, Bart W. Neff, Ted W. Reid, Kaijun Ren, and Robert D. Walkup pp 2478 - 2482; DOI: 10.1021/jm00013a024 |
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Synthesis and Evaluation of 6,11-Ethanohexahydrobenzo[b]quinolizidines: A New Class of Noncompetitive N-Methyl-D-aspartate Antagonists Chakrapani Subramanyam, John P. Mallamo, Gary M. Pilling, William G. Earley, Philip M. Carabateas, Joseph R. Wetzel, Diane DeHaven-Hudkins, Timothy Allen, and Rudolph K. Kullnig pp 2483 - 2489; DOI: 10.1021/jm00013a025 |
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Book Reviews pp 2490 - 2490; DOI: 10.1021/jm00013a600 |
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Toward Improved Anti-HIV Chemotherapy: Therapeutic Strategies for Intervention with HIV Infections Erik De Clercq pp 2491 - 2517; DOI: 10.1021/jm00014a001 |
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Synthesis, Resolution, and Biological Evaluation of the Four Stereoisomers of 4-Methylglutamic Acid: Selective Probes of Kainate Receptors Zi-Qiang Gu, David P. Hesson, Jeffrey C. Pelletier, Maria-Luisa Maccecchini, Li-Ming Zhou, and Phil Skolnick pp 2518 - 2520; DOI: 10.1021/jm00014a002 |
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New Orally Active Serine Protease Inhibitors Kazuhiko Senokuchi, Hisao Nakai, Yoshisuke Nakayama, Yoshihiko Odagaki, Katsuhito Sakaki, Masashi Kato, Toru Maruyama, Toru Miyazaki, Hidenori Ito, Koumei Kamiyasu, Soon-ih Kim, Masanori Kawamura, and Nobuyuki Hamanaka pp 2521 - 2523; DOI: 10.1021/jm00014a003 |
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5-Methyl-1-(3-pyridylcarbamoyl)-1,2,3,5-tetrahydropyrrolo[2,3-f]indole: A Novel 5-HT2C/5-HT2B Receptor Antagonist with Improved Affinity, Selectivity, and Oral Activity Ian T. Forbes, Peter Ham, Deborah H. Booth, Roger T. Martin, Mervyn Thompson, Gordon S. Baxter, Thomas P. Blackburn, Alison Glen, Guy A. Kennett, and Martyn D. Wood pp 2524 - 2530; DOI: 10.1021/jm00014a004 |
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Synthesis and Antibacterial Activity of Some Novel 1-Substituted 1,4-Dihydro-4-oxo-7-pyridinyl-3-quinolinecarboxylic Acids. Potent Antistaphylococcal Agents Michael Reuman, Sol J. Daum, Baldev Singh, Mark P. Wentland, Robert B. Perni, Patrick Pennock, Philip M. Carabateas, Monte D. Gruett, Manohar T. Saindane, Peter H. Dorff, Susan A. Coughlin, David M. Sedlock, James B. Rake, and George Y. Lesher pp 2531 - 2540; DOI: 10.1021/jm00014a005 |
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Cyclic Variations of 3-Quinolinecarboxamides and Effects on Antiherpetic Activity Mark P. Wentland, John A. Carlson, Peter H. Dorff, Suzanne C. Aldous, Robert B. Perni, Dorothy C. Young, Maureen G. Woods, Susan D. Kingsley, Kathryn A. Ryan, David Rosi, Marion L. Drozd, and Frank J. Dutko pp 2541 - 2545; DOI: 10.1021/jm00014a006 |
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Novel and Potent Adenosine 3',5'-Cyclic Phosphate Phosphodiesterase III Inhibitors: Thiazolo[4,5-b][1,6]naphthyridin-2-ones Baldev Singh, Edward R. Bacon, George Y. Lesher, Shaughnessy Robinson, Patrick O. Pennock, Donald C. Bode, Edward D. Pagani, Ross G. Bentley, Mary J. Connell, Linda T. Hamel, and Paul J. Silver pp 2546 - 2550; DOI: 10.1021/jm00014a007 |
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4,5-Dihydro-3-(methanesulfonamidophenyl)-1-phenyl-1H-2,4-benzodiazepines: A Novel Class III Antiarrhythmic Agents Robert E. Johnson, Paul J. Silver, Russell Becker, Nancy C. Birsner, Eric A. Bohnet, G. Maurice Briggs, Carl A. Busacca, Paul Canniff, Philip M. Carabateas, Thomas D'Ambra, Ronald L. Dundore, Jen-Sen Dung, Christopher C. Chadwick, Alan M. Ezrin, William Gorczyca, Peter G. Habeeb, Patrick Horan, Douglas S. Krafte, Gary M. Pelling, Bernard O'Connor, Manohar T. Saindane, Donald C. Schlegel, Gerald P. Stankus, John Swestock, and Walter A. Volberg pp 2551 - 2556; DOI: 10.1021/jm00014a008 |
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Novel Inhibitors of the Nuclear Factor of Activated T Cells (NFAT)-Mediated Transcription of .beta.-Galactosidase: Potential Immunosuppressive and Antiinflammatory Agents William F. Michne, Joseph D. Schroeder, Joseph W. Guiles, Adi M. Treasurywala, Carolyn A. Weigelt, Mary F. Stansberry, Elizabeth McAvoy, Chandra R. Shah, Elizabeth Bump, and et al. pp 2557 - 2569; DOI: 10.1021/jm00014a009 |
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Inhibition of Matrix Metalloproteinases by Hydroxamates Containing Heteroatom-Based Modifications of the P1' Group Madhusudhan R. Gowravaram, Jeffrey S. Johnson, Daniel Delecki, Ewell R. Cook, Bruce E. Tomczuk, Arup K. Ghose, Alan M. Mathiowetz, John C. Spurlino, Byron Rubin, Douglas L. Smith, Tricia Pulvino, and Robert C. Wahl pp 2570 - 2581; DOI: 10.1021/jm00014a010 |
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Synthesis and Structure-Activity Relationships of 6-Heterocyclic-Substituted Purines as Inactivation Modifiers of Cardiac Sodium Channels Kimberly G. Estep, Kurt A. Josef, Edward R. Bacon, Philip M. Carabateas, Squire Rumney IV, Garry M. Pilling, Douglas S. Krafte, Walter A. Volberg, Kathleen Dillon, Nancy Dugrenier, G. Maurice Briggs, Paul C. Canniff, William P. Gorczyca, Gerald P. Stankus, and Alan M. Ezrin pp 2582 - 2595; DOI: 10.1021/jm00014a011 |
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1,1-Bisphosphonate Squalene Synthase Inhibitors: Interplay Between the Isoprenoid Subunit and the Diphosphate Surrogate David R. Magnin, John K. Dickson Jr., Janette V. Logan, R. Michael Lawrence, Ying Chen, Richard B. Sulsky, Carl P. Ciosek Jr., Scott A. Biller, Thomas W. Harrity, Kern G. Jolibois, Lori K. Kunselman, Lois C. Rich, and Dorothy A. Slusarchyk pp 2596 - 2605; DOI: 10.1021/jm00014a012 |
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Specific Sequestering Agents for the Actinides. 28. Synthesis and Initial Evaluation of Multidentate 4-Carbamoyl-3-hydroxy-1-methyl-2(1H)-pyridinone Ligands for in Vivo Plutonium(IV) Chelation Jide Xu, Birgitta Kullgren, Patricia W. Durbin, and Kenneth N. Raymond pp 2606 - 2614; DOI: 10.1021/jm00014a013 |
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2,4-Diaminopyrido[3,2-d]pyrimidine Inhibitors of Dihydrofolate Reductase from Pneumocystis carinii and Toxoplasma gondii Andre Rosowsky, Ronald A. Forsch, and Sherry F. Queener pp 2615 - 2620; DOI: 10.1021/jm00014a014 |
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Structure-Activity Relationships for Inhibition of Type 1 and 2 Human 5.alpha.-Reductase and Human Adrenal 3.beta.-Hydroxy-.DELTA.5-steroid Dehydrogenase/3-Keto-.DELTA.5-steroid Isomerase by 6-Azaandrost-4-en-3-ones: Optimization of the C17 Substituent Stephen V. Frye, Curt D. Haffner, Patrick R. Maloney, Roger N. Hiner, George F. Dorsey, Robert A. Noe, Rayomand J. Unwalla, Kenneth W. Batchelor, H. Neal Bramson, J. Darren Stuart, Stephanie L. Schweiker, John Van Arnold, D. Mark Bickett, Marcia L. Moss, Gaochoa Tian, Frank W. Lee, Timothy K. Tippin, Michael K. James, Mary K. Grizzle, James E. Long, and Dallas K. Croom pp 2621 - 2627; DOI: 10.1021/jm00014a015 |
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Novel 1,2-Dithiins: Synthesis, Molecular Modeling Studies, and Antifungal Activity Donald E. Bierer, Jeffrey M. Dener, Larisa G. Dubenko, R. Eric Gerber, Joane Litvak, Stefan Peterli, Patricia Peterli-Roth, Thien V. Truong, Guohua Mao, and Barr E. Bauer pp 2628 - 2648; DOI: 10.1021/jm00014a016 |
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Gonadotropin-Releasing Hormone Antagonists: Novel Members of the Azaline B Family Jean E. Rivier, Guangcheng Jiang, John Porter, Carl Hoeger, A. Grey Craig, Anne Corrigan, Wylie Vale, and Catherine L. Rivier pp 2649 - 2662; DOI: 10.1021/jm00014a017 |
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Synthesis of Carbon-11-, Fluorine-18-, and Iodine-125-Labeled GABAA-Gated Chloride Ion Channel Blockers: Substituted 5-tert-Butyl-2-phenyl-1,3-dithianes and -dithiane Oxides Scott E. Snyder, Akito Kume, Yong-Woon Jung, Stephen E. Connor, Philip S. Sherman, Roger L. Albin, Donald M. Wieland, and Michael R. Kilbourn pp 2663 - 2671; DOI: 10.1021/jm00014a018 |
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Synthesis and Biological Evaluation of 5-Fluoro-2'-deoxyuridine Phosphoramidate Analogs Kristin M. Fries, Carolyn Joswig, and Richard F. Borch pp 2672 - 2680; DOI: 10.1021/jm00014a019 |
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Prediction of Drug Binding Affinities by Comparative Binding Energy Analysis Angel R. Ortiz, M. Teresa Pisabarro, Federico Gago, and Rebecca C. Wade pp 2681 - 2691; DOI: 10.1021/jm00014a020 |
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Novel, Potent, and Selective 5-HT3 Receptor Antagonists Based on the Arylpiperazine Skeleton: Synthesis, Structure, Biological Activity, and Comparative Molecular Field Analysis Studies Maurizio Anzini, Andrea Cappelli, Salvatore Vomero, Gianluca Giorgi, Thierry Langer, Michel Hamon, Nacera Merahi, Boris M. Emerit, Alfredo Cagnotto, Malgorzata Skorupska, Tiziana Mennini, and Julia C. Pinto pp 2692 - 2704; DOI: 10.1021/jm00014a021 |
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Amino Acid Side Chain Descriptors for Quantitative Structure-Activity Relationship Studies of Peptide Analogs Elizabeth R. Collantes and William J. Dunn pp 2705 - 2713; DOI: 10.1021/jm00014a022 |
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Synthesis and Biochemical Evaluation of Adenosylspermidine, a Nucleoside-Polyamine Adduct Inhibitor of Spermidine Synthase John R. Lakanen, Anthony E. Pegg, and James K. Coward pp 2714 - 2727; DOI: 10.1021/jm00014a023 |
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Novel Angiotensin II Receptor Antagonists. Design, Synthesis, and in Vitro Evaluation of Dibenzo[a,d]cycloheptene and Dibenzo[b,f]oxepin Derivatives. Searching for Bioisosteres of Biphenyltetrazole Using a Three-Dimensional Search Technique Ryuichi Kiyama, Tsunetoshi Honma, Kunio Hayashi, Masayoshi Ogawa, Mariko Hara, Masafumi Fujimoto, and Toshio Fujishita pp 2728 - 2741; DOI: 10.1021/jm00014a024 |
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Solid-State Nuclear Magnetic Resonance Analysis of the Conformation of an Inhibitor Bound to Thermolysin Denise D. Beusen, Lynda M. McDowell, Ursula Slomczynska, and Jacob Schaefer pp 2742 - 2747; DOI: 10.1021/jm00014a025 |
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Reversible Inhibitors of the Gastric (H+/K+)-ATPase. 4. Identification of an Inhibitor with an Intermediate Duration of Action Colin A. Leach, Thomas H. Brown, Robert J. Ife, David J. Keeling, Michael E. Parsons, Colin J. Theobald, and Kenneth J. Wiggall pp 2748 - 2762; DOI: 10.1021/jm00014a026 |
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Reversible Inhibitors of the Gastric (H+/K+)-ATPase. 5. Substituted 2,4-Diaminoquinazolines and Thienopyrimidines Robert J. Ife, Thomas H. Brown, Peter Blurton, David J. Keeling, Colin A. Leach, Malcolm L. Meeson, Michael E. Parsons, and Colin J. Theobald pp 2763 - 2773; DOI: 10.1021/jm00014a027 |
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11.beta.-Substituted Estradiol Derivatives. 2. Potential Carbon-11- and Iodine-Labeled Probes for the Estrogen Receptor Elio Napolitano, Rita Fiaschi, Kathryn E. Carlson, and John A. Katzenellenbogen pp 2774 - 2779; DOI: 10.1021/jm00014a028 |
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[(Biaryloxy)alkyl]isoxazoles: Picornavirus Inhibitors Joseph W. Guiles, Guy D. Diana, and Daniel C. Pevear pp 2780 - 2783; DOI: 10.1021/jm00014a029 |
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Analysis of a 29 Full Factorial Chemical Library S. Stanley Young and Douglas M. Hawkins pp 2784 - 2788; DOI: 10.1021/jm00014a030 |
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Synthesis, Pharmacologic Activity, and Structure-Activity Relationships of a Series of Propafenone-Related Modulators of Multidrug Resistance Peter Chiba, Sabine Burghofer, Elisabeth Richter, Barbara Tell, Andrea Moser, and Gerhard Ecker pp 2789 - 2793; DOI: 10.1021/jm00014a031 |
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Synthesis and Pharmacological Evaluation of 2'-Hydroxychalcones and Flavones as Inhibitors of Inflammatory Mediators Generation J. F. Ballesteros, M. J. Sanz, A. Ubeda, M. A. Miranda, S. Iborra, M. Paya, and M. J. Alcaraz pp 2794 - 2797; DOI: 10.1021/jm00014a032 |
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Book Reviews pp 2798 - 2798; DOI: 10.1021/jm00014a600 |
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Technetium-99m-Labeled HOE 140: A Potential Bradykinin B2 Receptor Imaging Agent Wilhelm Stahl, Gerhard Breipohl, Ludwig Kuhlmann, Axel Steinstraesser, Hermann J. Gerhards, and Bernward A. Schoelkens pp 2799 - 2801; DOI: 10.1021/jm00015a001 |
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5,7-Dihydro-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-6H-pyrrolo[3,2-f]-1,2-benzisoxazol-6-one: A Potent and Centrally-Selective Inhibitor of Acetylcholinesterase Anabella Villalobos, Todd W. Butler, Douglas S. Chapin, Yuhpyng L. Chen, Steven B. DeMattos, Jeffrey L. Ives, Shawn B. Jones, Dane R. Liston, Arthur A. Nagel, and et al. pp 2802 - 2808; DOI: 10.1021/jm00015a002 |
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Structure-activity relationships of the potent combined endothelinA/endothelinB receptor antagonist Ac-DDip16-Leu-Asp-Ile-Ile-Trp21 (PD 142893): development of endothelinB receptor selective antagonists Wayne L. Cody, John X. He, Patricia L. DePue, Lisa A. Waite, Daniele M. Leonard, Andrea M. Sefler, James S. Kaltenbronn, Stephen J. Haleen, Donnelle M. Walker, Michael A. Flynn, Kathleen M. Welch, Elwood E. Reynolds, and Annette M. Doherty pp 2809 - 2819; DOI: 10.1021/jm00015a003 |
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Synthesis and Structure-Activity Relationships of Stilbene Retinoid Analogs Substituted with Heteroaromatic Carboxylic Acids Richard L. Beard, Diana F. Colon, Samuel J. Gillett, Elizabeth Henry, Deborah K. Marler, Tae Song, Lydia Denys, Michael E. Garst, Taghreed Arefieg, and et al. pp 2820 - 2829; DOI: 10.1021/jm00015a004 |
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Synthesis, Structure, and Pharmacological Evaluation of the Stereoisomers of Furnidipine Ramon Alajarin, Juan J. Vaquero, Julio Alvarez-Builla, Manuel Pastor, Carlos Sunkel, Miguel Fau de Casa-Juana, Jaime Priego, Peter R. Statkow, Julia Sanz-Aparicio, and Isabel Fonseca pp 2830 - 2841; DOI: 10.1021/jm00015a005 |
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Synthesis, Structure Elucidation, and Biochemical Evaluation of 7.alpha.- and 7.beta.-Arylaliphatic-Substituted Androst-4-ene-3,17-diones as Inhibitors of Aromatase Jill M. O'Reilly, Naiyin Li, William L. Duax, and Robert W. Brueggemeier pp 2842 - 2850; DOI: 10.1021/jm00015a006 |
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Syntheses, Calcium Channel Agonist-Antagonist Modulation Activities, and Voltage-Clamp Studies of Isopropyl 1,4-Dihydro-2,6-dimethyl-3-nitro- 4-pyridinylpyridine-5-carboxylate Racemates and Enantiomers Dean Vo, Wandikayi C. Matowe, Manian Ramesh, Nadeem Iqbal, Michael W. Wolowyk, Susan E. Howlett, and Edward E. Knaus pp 2851 - 2859; DOI: 10.1021/jm00015a007 |
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Synthesis and Antiviral Activity of 6-Benzyl Analogs of 1-[(2-Hydroxyethoxy)methyl]-5-(phenylthio)thymine (HEPT) as Potent and Selective Anti-HIV-1 Agents Hiromichi Tanaka, Hideaki Takashima, Masaru Ubasawa, Kouichi Sekiya, Naoko Inouye, Masanori Baba, Shiro Shigeta, Richard T. Walker, Erik De Clercq, and Tadashi Miyasaka pp 2860 - 2865; DOI: 10.1021/jm00015a008 |
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Peptide Mimetics of Thyrotropin-Releasing Hormone Based on a Cyclohexane Framework: Design, Synthesis, and Cognition-Enhancing Properties Gary L. Olson, Ho-Chuen Cheung, Elliot Chiang, Vincent S. Madison, Jerry Sepinwall, George P. Vincent, Andrew Winokur, and Keith A. Gary pp 2866 - 2879; DOI: 10.1021/jm00015a009 |
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Cardioselective Ammonium, Phosphonium, and Sulfonium Analogs of .alpha.-Tocopherol and Ascorbic Acid That Inhibit in Vitro and ex Vivo Lipid Peroxidation and Scavenge Superoxide Radicals J. Martin Grisar, Gilbert Marciniak, Frank N. Bolkenius, Joelle Verne-Mismer, and Eugene R. Wagner pp 2880 - 2886; DOI: 10.1021/jm00015a010 |
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(E)-4-{2-[[3-(Indol-5-yl)-1-oxo-2-butenyl]amino]phenoxy}butyric Acid Derivatives: A New Class of Steroid 5.alpha.-Reductase Inhibitors in the Rat Prostate. 1 Toshiaki Kumazawa, Hitoshi Takami, Nobuyuki Kishibayashi, Akio Ishii, Yoshitomo Nagahara, Noriaki Hirayama, and Hiroyuki Obase pp 2887 - 2892; DOI: 10.1021/jm00015a011 |
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Design and Synthesis of Renin Inhibitors: Incorporation of Transition-State Isostere Side Chains That Span from the S1 to the S3 Binding Pockets and Examination of P3-Modified Renin Inhibitors Aurash Shahripour, James S. Kaltenbronn, Elizabeth A. Lunney, Bruce A. Steinbaugh, James M. Hamby, Harriet W. Hamilton, Tomi K. Sawyer, Christine Humblet, Annette M. Doherty, and et al. pp 2893 - 2905; DOI: 10.1021/jm00015a012 |
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Farnesyl Diphosphate-Based Inhibitors of Ras Farnesyl Protein Transferase Dinesh V. Patel, Robert J. Schmidt, Scott A. Biller, Eric M. Gordon, Simon S. Robinson, and Veeraswamy Manne pp 2906 - 2921; DOI: 10.1021/jm00015a013 |
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Reduced-Size Antagonists of Luteinizing Hormone-Releasing Hormone Active in Vitro Anna Janecka, Tomasz Janecki, Cyril Bowers, and Karl Folkers pp 2922 - 2924; DOI: 10.1021/jm00015a014 |
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4-Diazinyl- and 4-Pyridinylimidazoles: Potent Angiotensin II Antagonists. A Study of Their Activity and Computational Characterization J. S. Harmat Nicholas, Raffaello Giorgi, Fabrizio Bonaccorsi, Guido Cerbai, Spartaco M. Colombani, Anna R. Renzetti, Rocco Cirillo, Alessandro Subissi, Giuliano Alagona, and et al. pp 2925 - 2937; DOI: 10.1021/jm00015a015 |
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Balanced AT1/AT2 Receptor Antagonists. 4. XR510 and Related 5-(3-Amidopropanoyl)imidazoles Possessing Equal Affinity for the AT1 and AT2 Receptors Mimi L. Quan, Andrew T. Chiu, Christopher D. Ellis, Pancras C. Wong, Ruth R. Wexler, and Pieter B. M. W. M. Timmermans pp 2938 - 2945; DOI: 10.1021/jm00015a016 |
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5-Methyl-6-phenyl-1,3,5,6-tetrahydro-3,6-methano-1,5-benzodiazocine-2,4- dione (BA 41899): Representative of a Novel Class of Purely Calcium-Sensitizing Agents Peter Herold, Joachim W. Herzig, Paul Wenk, Thomas Leutert, Paul Zbinden, Walter Fuhrer, Stefan Stutz, Karl Schenker, Max Meier, and Greti Rihs pp 2946 - 2954; DOI: 10.1021/jm00015a017 |
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Novel Hexakis(areneisonitrile)technetium(I) Complexes as Radioligands Targeted to the Multidrug Resistance P-Glycoprotein Lee W. Herman, Vijay Sharma, James F. Kronauge, Eva Barbarics, Lisa A. Herman, and David Piwnica-Worms pp 2955 - 2963; DOI: 10.1021/jm00015a018 |
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(.+-.)-(Z)-2-(Aminomethyl)-1-phenylcyclopropanecarboxamide Derivatives as a New Prototype of NMDA Receptor Antagonists Satoshi Shuto, Hironao Takada, Daisuke Mochizuki, Ryuichi Tsujita, Yukako Hase, Shizuka Ono, Nobuko Shibuya, and Akira Matsuda pp 2964 - 2968; DOI: 10.1021/jm00015a019 |
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Flexible 1-[(2-Aminoethoxy)alkyl]-3-ar(o)yl(thio)ureas as Novel Acetylcholinesterase Inhibitors. Synthesis and Biochemical Evaluation Jean-Louis Vidaluc, Francis Calmel, Dennis C. H. Bigg, Elisabeth Carilla, and Mike Briley pp 2969 - 2973; DOI: 10.1021/jm00015a020 |
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Effect of Lipophilicity at N-1 on Activity of Fluoroquinolones against Mycobacteria Thomas E. Renau, Joseph P. Sanchez, Martin A. Shapiro, Julie A. Dever, Stephen J. Gracheck, and John M. Domagala pp 2974 - 2977; DOI: 10.1021/jm00015a021 |
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Synthesis and .sigma. Binding Properties of 2'-Substituted 5,9.alpha.-Dimethyl-6,7-benzomorphans Richmond Danso-Danquah, Xu Bai, X. Zhang, S. Wayne Mascarella, Wanda Williams, Bethel Sine, Wayne D. Bowen, and F. Ivy Carroll pp 2978 - 2985; DOI: 10.1021/jm00015a022 |
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Synthesis and .sigma. Binding Properties of 1'- and 3'-Halo- and 1',3'-Dihalo-N-normetazocine Analogs Richmond Danso-Danquah, Xu Bai, X. Zhang, S. Wayne Mascarella, Wanda Williams, Bethel Sine, Wayne D. Bowen, and F. Ivy Carroll pp 2986 - 2989; DOI: 10.1021/jm00015a023 |
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Antineoplastic Agents. 291. Isolation and Synthesis of Combretastatins A-4, A-5, and A-6. [Erratum to document cited in CA122:290568] George R. Pettit, Sheo Bux Singh, Michael R. Boyd, Ernest Hamel, Robin K. Pettit, Jean M. Schmidt, and Fiona Hogan pp 2994 - 2994; DOI: 10.1021/jm00015a024 |
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Book Reviews pp 2990 - 2993; DOI: 10.1021/jm00015a600 |
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Synthetic chemical diversity: solid phase synthesis of libraries of C2 symmetric inhibitors of HIV protease containing diamino diol and diamino alcohol cores Gary T. Wang, Sam Li, Norman Wideburg, Grant A. Krafft, and Dale J. Kempf pp 2995 - 3002; DOI: 10.1021/jm00016a001 |
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Anti-AIDS (Acquired Immune Deficiency Syndrome) Agents. 17. New Brominated Hexahydroxybiphenyl Derivatives as Potent Anti-HIV Agents Lan Xie, Jing-Xi Xie, Yoshiki Kashiwada, L. Mark Cosentino, Shwu-Huey Liu, Rekha B. Pai, Yung-Chi Cheng, and Kuo-Hsiung Lee pp 3003 - 3008; DOI: 10.1021/jm00016a002 |
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PLS Analysis of Distance Matrixes To Detect Nonlinear Relationships between Biological Potency and Molecular Properties Yvonne C. Martin, C. Thomas Lin, Chandanie Hetti, and Jerry DeLazzer pp 3009 - 3015; DOI: 10.1021/jm00016a003 |
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Synthesis and in Vitro and in Vivo Antitumor Activity of a Series of Trans Platinum Antitumor Complexes Lloyd R. Kelland, F. J. Barnard, Iona G. Evans, Barry A. Murrer, Brian R. C. Theobald, Sandra B. Wyer, Phyllis M. Goddard, Mervyn Jones, Melanie Valenti, and et al. pp 3016 - 3024; DOI: 10.1021/jm00016a004 |
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Synthesis and Antitumor Activity of Various 6-Demethylmitomycins and 6-Demethyl-6-halomitomycins Hitoshi Arai, Tadashi Ashizawa, Katsushige Gomi, Motomichi Kono, Hiromitsu Saito, and Masaji Kasai pp 3025 - 3033; DOI: 10.1021/jm00016a005 |
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Antihyperglycemic N-Sulfonyl-1a,2,6,6a-tetrahydro-1H,4H-[1,3]dioxepino[5,6-b]azirines: Synthesis, X-ray Structure Analysis, Conformational Behavior, Quantitative Stroposcopic Pulse Radiolysis, and Quantitative Structure-Activity Relationships Miljenko Dumic, Mladen Vinkovic, Darko Filic, Blanka Jamnicky, Mirela Eskinja, and Boris Kamenar pp 3034 - 3042; DOI: 10.1021/jm00016a006 |
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Bisimidazoacridones and Related Compounds: New Antineoplastic Agents with High Selectivity against Colon Tumors Wieslaw M. Cholody, Lidia Hernandez, Lawrence Hassner, Dominic A. Scudiero, Draginja B. Djurickovic, and Christopher J. Michejda pp 3043 - 3052; DOI: 10.1021/jm00016a007 |
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Diamine and Triamine Analogs and Derivatives as Inhibitors of Deoxyhypusine Synthase: Synthesis and Biological Activity Young Bok Lee, Myung Hee Park, and J. E. Folk pp 3053 - 3061; DOI: 10.1021/jm00016a008 |
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Synthesis and Biological Evaluation of a Series of Substituted Benzo[a]phenanthridines as Agonists at D1 and D2 Dopamine Receptors Timm A. Knoerzer, Val J. Watts, David E. Nichols, and Richard B. Mailman pp 3062 - 3070; DOI: 10.1021/jm00016a009 |
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Synthesis and Biological Evaluation of 14-Alkoxymorphinans. 11. 3-Hydroxycyprodime and Analogs: Opioid Antagonist Profile in Comparison to Cyprodime Helmut Schmidhammer, Herwig K. Jennewein, Roland Krassnig, John R. Traynor, Dinesh Patel, Katrina Bell, Gudrun Froschauer, Karin Mattersberger, Christine Jachs-Ewinger, and et al. pp 3071 - 3077; DOI: 10.1021/jm00016a010 |
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Aziridine Analogs of [[trans-(Epoxysuccinyl)-L-leucyl]amino]-4-guanidinobutane (E-64) as Inhibitors of Cysteine Proteases Valeri Martichonok, Celine Plouffe, Andrew C. Storer, Robert Menard, and J. Bryan Jones pp 3078 - 3085; DOI: 10.1021/jm00016a011 |
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Chemistry and Biology of the 2.beta.-Alkyl-3.beta.-phenyl Analogs of Cocaine: Subnanomolar Affinity Ligands That Suggest a New Pharmacophore Model at the C-2 Position Alan P. Kozikowski, M. K. Eddine Saiah, Kenneth M. Johnson, and John S. Bergmann pp 3086 - 3093; DOI: 10.1021/jm00016a012 |
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Aminoalkylindoles: Structure-Activity Relationships of Novel Cannabinoid Mimetics Michael A. Eissenstat, Malcolm R. Bell, Thomas E. D'Ambra, E. John Alexander, Sol J. Daum, James H. Ackerman, Monte D. Gruett, Virendra Kumar, Kimberly G. Estep, and et al. pp 3094 - 3105; DOI: 10.1021/jm00016a013 |
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Novel, Potent, and Orally Active Substance P Antagonists: Synthesis and Antagonist Activity of N-Benzylcarboxamide Derivatives of Pyrido[3,4-b]pyridine Hideaki Natsugari, Yoshinori Ikeura, Yutaka Kiyota, Yuji Ishichi, Takenori Ishimaru, Osamu Saga, Hideo Shirafuji, Toshimasa Tanaka, Izumi Kamo, and et al. pp 3106 - 3120; DOI: 10.1021/jm00016a014 |
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On the Quantitative Structure-Activity Relationships of Meta-Substituted (S)-Phenylpiperidines, a Class of Preferential Dopamine D2 Autoreceptor Ligands: Modeling of Dopamine Synthesis and Release in Vivo by Means of Partial Least Squares Regression Lars O. Hansson, Nicholas Waters, Susanna Holm, and Clas Sonesson pp 3121 - 3131; DOI: 10.1021/jm00016a015 |
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Synthesis and dopaminergic activity of pyridine analogs of 5-hydroxy-2-(di-n-propylamino)tetralin Shelly A. Glase, Ann E. Corbin, Thomas A. Pugsley, Thomas G. Heffner, and Lawrence D. Wise pp 3132 - 3137; DOI: 10.1021/jm00016a016 |
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(1S,2S)-1-(4-Hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)-1-propanol: A Potent New Neuroprotectant Which Blocks N-Methyl-D-Aspartate Responses B. L. Chenard, J. Bordner, T. W. Butler, L. K. Chambers, M. A. Collins, D. L. De Costa, M. F. Ducat, M. L. Dumont, C. B. Fox, and et al. pp 3138 - 3145; DOI: 10.1021/jm00016a017 |
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Design and Synthesis of Potent Retinoid X Receptor Selective Ligands That Induce Apoptosis in Leukemia Cells Marcus F. Boehm, Lin Zhang, Lin Zhi, Michael R. McClurg, Elain Berger, Murriel Wagoner, Dale E. Mais, Carla M. Suto, Peter J. A. Davies, and et al. pp 3146 - 3155; DOI: 10.1021/jm00016a018 |
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Synthesis and Biological Evaluation of Radioiodinated Phospholipid Ether Stereoisomers Mark A. Rampy, Anatoly N. Pinchuk, Jamey P. Weichert, R. W. Scott Skinner, Susan J. Fisher, Richard L. Wahl, Milton D. Gross, and Raymond E. Counsell pp 3156 - 3162; DOI: 10.1021/jm00016a019 |
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A Novel Type of Retinoic Acid Receptor Antagonist: Synthesis and Structure-Activity Relationships of Heterocyclic Ring-Containing Benzoic Acid Derivatives Hiroyuki Yoshimura, Mitsuo Nagai, Shigeki Hibi, Kouichi Kikuchi, Shinya Abe, Takayuki Hida, Seiko Higashi, Ieharu Hishinuma, and Takashi Yamanaka pp 3163 - 3173; DOI: 10.1021/jm00016a020 |
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Potent Inhibitors of Acyl-CoA:Cholesterol Acyltransferase. Structure-Activity Relationships of Novel N-(4-Oxo-8-chromanyl) amides Ken-ichiro Kataoka, Tatsuki Shiota, Takumi Takeyasu, Tsutomu Mochizuki, Keiko Taneda, Mikio Ota, Hirofumi Tanabe, and Hisao Yamaguchi pp 3174 - 3186; DOI: 10.1021/jm00016a021 |
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2,6-Disubstituted Aryl Carboxylic Acids, Leaving Groups "Par Excellence" for Benzisothiazolone Inhibitors of Human Leukocyte Elastase. [Erratum to document cited in CA121:230709] Chakrapani Subramanyam, Malcolm R. Bell, Philip Carabateas, John J. Court, John A. Jr. Dority, Edward Ferguson, Robert Gordon, Dennis J. Hlasta, Virendra Kumar, and et al. pp 3188 - 3188; DOI: 10.1021/jm00016a022 |
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Book Reviews pp 3187 - 3187; DOI: 10.1021/jm00016a600 |
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4-Aza-3-oxo-5.alpha.-androst-1-ene-17.beta.-N-arylcarboxamides as Dual Inhibitors of Human Type 1 and Type 2 Steroid 5.alpha.-Reductases. Dramatic Effect of N-Aryl Substituents on Type 1 and Type 2 5.alpha.-Reductase Inhibitory Potency Raman K. Bakshi, Gary H. Rasmusson, Gool F. Patel, Ralph T. Mosley, Benedict Chang, Kenneth Ellsworth, Georgianna S. Harris, and Richard L. Tolman pp 3189 - 3192; DOI: 10.1021/jm00017a001 |
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Vinyl Sulfones as Mechanism-Based Cysteine Protease Inhibitors James T. Palmer, David Rasnick, Jeffrey L. Klaus, and Dieter Bromme pp 3193 - 3196; DOI: 10.1021/jm00017a002 |
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Keto/Enol Epoxy Steroids as HIV-1 Tat Inhibitors: Structure-Activity Relationships and Pharmacophore Localization William F. Michne, Joseph D. Schroeder, Thomas R. Bailey, Helmut C. Neumann, Debra Cooke, Dorothy C. Young, Joseph V. Hughes, Susan D. Kingsley, Kathryn A. Ryan, Henry S. Putz, Lucinda J. Shaw, and Frank J. Dutko pp 3197 - 3206; DOI: 10.1021/jm00017a003 |
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(Aryloxy)methylsilane Derivatives as New Cholesterol Biosynthesis Inhibitors: Synthesis and Hypocholesterolemic Activity of a New Class of Squalene Epoxidase Inhibitors Jean-Pierre Gotteland, Isabelle Brunel, Fabrice Gendre, Jerome Desire, Andre Delhon, Didier Junquero, Philippe Oms, and Serge Halazy pp 3207 - 3216; DOI: 10.1021/jm00017a004 |
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Structure-Based Inhibitors of Influenza Virus Sialidase. A Benzoic Acid Lead with Novel Interaction Sangeeta Singh, Marek J. Jedrzejas, Gillian M. Air, Ming Luo, W. Graeme Laver, and Wayne J. Brouillette pp 3217 - 3225; DOI: 10.1021/jm00017a005 |
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9-Substituted acridine derivatives with long half-life and potent antitumor activity: synthesis and structure-activity relationships Tsann-Long Su, Ting-Chao Chou, Joong Young Kim, Jai-Tung Huang, Grazyna Ciszewska, Wu-Yun Ren, Grenys M. Otter, Francis M. Sirotnak, and Kyoichi A. Watanabe pp 3226 - 3235; DOI: 10.1021/jm00017a006 |
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Cardioselective Anti-Ischemic ATP-Sensitive Potassium Channel Openers. 3. Structure-Activity Studies on Benzopyranyl Cyanoguanidines; Modification of the Cyanoguanidine Portion Karnail S. Atwal, Gary J. Grover, Syed Z. Ahmed, Paul G. Sleph, Steven Dzwonczyk, Anne J. Baird, and Diane E. Normandin pp 3236 - 3245; DOI: 10.1021/jm00017a007 |
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A Check on Rational Drug Design: Crystal Structure of a Complex of Human Immunodeficiency Virus Type 1 Protease with a Novel .gamma.-Turn Mimetic Inhibitor Susan S. Hoog, Baoguang Zhao, Evon Winborne, Seth Fisher, David W. Green, Renee L. DesJarlais, Kenneth A. Newlander, James F. Callahan, Sherin S. Abdel-Meguid, Michael L. Moore, and William F. Huffman pp 3246 - 3252; DOI: 10.1021/jm00017a008 |
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Unusual Single-Stranded Polyribonucleotides as Potent Anti-HIV Agents Arthur D. Broom, Vijai K. Agrawal, Mayoka G. Tutonda, Heidi D. Fain, and Robert W. Buckheit pp 3253 - 3257; DOI: 10.1021/jm00017a009 |
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Preparation and anti-HIV-1 activity of Thio Analogues of Dichydroalkoxybenzyloxopyrimidines Antonello Mai, Marino Artico, Gianluca Sbardella, Silvio Massa, Anna Giulia Loi, Enzo Tramontano, Patrizia Scano, and Paolo La Colla pp 3258 - 3263; DOI: 10.1021/jm00017a010 |
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Novel Zinc Chelators with Dual Activity in the Inhibition of the .kappa.B Site-Binding Proteins, HIV-EP1 and NF-.kappa.B Masami Otsuka, Mikako Fujita, Tsutomu Aoki, Shunsuke Ishii, Yukio Sugiura, Tadashi Yamamoto, and Jun-ichiro Inoue pp 3264 - 3270; DOI: 10.1021/jm00017a011 |
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Semisynthetic Chemical Modification of the Antifungal Lipopeptide Echinocandin B (ECB): Structure-Activity Studies of the Lipophilic and Geometric Parameters of Polyarylated Acyl Analogs of ECB Manuel Debono, William W. Turner, Lisa LaGrandeur, Fred J. Burkhardt, Jeffrey S. Nissen, Kimberly K. Nichols, Michael J. Rodriguez, Mark J. Zweifel, Douglas J. Zeckner, and et al. pp 3271 - 3281; DOI: 10.1021/jm00017a012 |
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Synthesis of (Dialkylamino)alkyl-Disubstituted Pyrimido[5,6,1-de]acridines, a Novel Group of Anticancer Agents Active on a Multidrug Resistant Cell Line Ippolito Antonini, Donatella Cola, Paolo Polucci, Maria Bontemps-Gracz, Edward Borowski, and Sante Martelli pp 3282 - 3286; DOI: 10.1021/jm00017a013 |
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Partial GABAA Receptor Agonists. Synthesis and in Vitro Pharmacology of a Series of Nonannulated Analogs of 4,5,6,7-Tetrahydroisoxazolo[4,5-c]pyridin-3-ol Bente Frolund, Uffe Kristiansen, Lotte Brehm, Annette B. Hansen, Povl Krogsgaard-Larsen, and Erik Falch pp 3287 - 3296; DOI: 10.1021/jm00017a014 |
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Phosphinic Acid Analogs of GABA. 1. New Potent and Selective GABAB Agonists Wolfgang Froestl, Stuart J. Mickel, Roger G. Hall, Georg von Sprecher, Dietrich Strub, Peter A. Baumann, Felix Brugger, Conrad Gentsch, Joachim Jaekel, and et al. pp 3297 - 3312; DOI: 10.1021/jm00017a015 |
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Phosphinic Acid Analogs of GABA. 2. Selective, Orally Active GABAB Antagonists Wolfgang Froestl, Stuart J. Mickel, Georg von Sprecher, Peter J. Diel, Roger G. Hall, Ludwig Maier, Dietrich Strub, Vito Melillo, Peter A. Baumann, and et al. pp 3313 - 3331; DOI: 10.1021/jm00017a016 |
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Non-Peptide Fibrinogen Receptor Antagonists. 7. Design and Synthesis of a Potent, Orally Active Fibrinogen Receptor Antagonist Mark E. Duggan, Adel M. Naylor-Olsen, James J. Perkins, Paul S. Anderson, Charles T.-C. Chang, Jacquelynn J. Cook, Robert J. Gould, Nathan C. Ihle, George D. Hartman, and et al. pp 3332 - 3341; DOI: 10.1021/jm00017a017 |
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Design of Potent Non-Thiourea H3-Receptor Histamine Antagonists C. Robin Ganellin, S. Kiumars Hosseini, Yasmin S. Khalaf, Wasyl Tertiuk, Jean-Michel Arrang, Monique Garbarg, Xavier Ligneau, and Jean-Charles Schwartz pp 3342 - 3350; DOI: 10.1021/jm00017a018 |
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The Histamine H1-Receptor Antagonist Binding Site. A Stereoselective Pharmacophoric Model Based upon (Semi-)Rigid H1-Antagonists and Including a Known Interaction Site on the Receptor Anton M. ter Laak, Jennifer Venhorst, Gabrielle M. Donne-Op den Kelder, and Hendrik Timmerman pp 3351 - 3360; DOI: 10.1021/jm00017a019 |
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The Role of Water Molecules in the Structure-Based Design of (5-Hydroxynorvaline)-2-cyclosporin: Synthesis, Biological Activity, and Crystallographic Analysis with Cyclophilin A Vincent Mikol, Christos Papageorgiou, and Xaver Borer pp 3361 - 3367; DOI: 10.1021/jm00017a020 |
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Conformational Effects on Retinoid Receptor Selectivity. 2. Effects of Retinoid Bridging Group on Retinoid X Receptor Activity and Selectivity Marcia I. Dawson, Ling Jong, Peter D. Hobbs, James F. Cameron, Wan-ru Chao, Michaela Pfahl, Mi-Ock Lee, Braham Shroot, and Magnus Pfahl pp 3368 - 3383; DOI: 10.1021/jm00017a021 |
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Modification of Receptor Selectivity and Functional Activity in Cholecystokinin Peptoid Ligands Milana Dezube, Elizabeth E. Sugg, Larry S. Birkemo, Dallas K. Croom, Robert W. Dougherty Jr., Gregory N. Ervin, Mary K. Grizzle, Michael K. James, Michael F. Johnson, and et al. pp 3384 - 3390; DOI: 10.1021/jm00017a022 |
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Nucleosides and Nucleotides. 141. Chemical Stability of a New Antitumor Nucleoside, 2'-C-Cyano-2'-deoxy-1-.beta.-D-arabino-pentofuranosylcytosine (CNDAC) in Alkaline Medium: Formation of 2'-C-Cyano-2'-deoxy-1-.beta.-D-ribo-pentofuranosylcytosine (CNDC) and Its Antitumor Activity Atsushi Azuma, Kenji Hanaoka, Atsushi Kurihara, Tomowo Kobayashi, Seiji Miyauchi, Naoki Kamo, Motohiro Tanaka, Takuma Sasaki, and Akira Matsuda pp 3391 - 3397; DOI: 10.1021/jm00017a023 |
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Structure-Activity Relationships of Unsaturated Analogs of Valproic Acid Jan Palaty and Frank S. Abbott pp 3398 - 3406; DOI: 10.1021/jm00017a024 |
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Synthesis and Cytotoxicity of Water-Soluble Ambrosin Prodrug Candidates Elzbieta Hejchman, Rudiger D. Haugwitz, and Mark Cushman pp 3407 - 3410; DOI: 10.1021/jm00017a025 |
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Synthesis and Evaluation of Some 10-Mono- and 2',10-Diesters of 10-Deacetylpaclitaxel Koppaka V. Rao, Rajendra S. Bhakuni, James Johnson, and Ravi Oruganti pp 3411 - 3414; DOI: 10.1021/jm00017a026 |
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.alpha.- and .beta.-Adrenoceptors: From the Gene to the Clinic. Part 1. Molecular Biology and Adrenoceptor Subclassification J. Paul Hieble, William Bondinell, and Robert R. Ruffolo pp 3415 - 3444; DOI: 10.1021/jm00018a001 |
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(5aR,11bS)-4,5,5a,6,7,11b-Hexahydro-2-propyl-3-thia-5-azacyclopent-1-ena[c]phenanthrene-9,10-diol (A-86929): a potent and selective dopamine D1 agonist that maintain behavioral efficacy following repeated administration and characterization of its diacetyl prodrug (ABT-431) Michael R. Michaelides, Yufeng Hong, Stanley DiDomenico, Karen E. Asin, Donald R. Britton, Chun Wel Lin, Michael Williams, and Kazumi Shiosaki pp 3445 - 3447; DOI: 10.1021/jm00018a002 |
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Antidiabetic agents: a new class of reversible carnitine palmitoyltransferase I inhibitors Robert C. Anderson, Michael Balestra, Philip A. Bell, Rhonda O. Deems, William S. Fillers, James E. Foley, James D Fraser, William R. Mann, Markus Rudin, and Edwin B. Villhauer pp 3448 - 3450; DOI: 10.1021/jm00018a003 |
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Synthesis and Ligand Binding Study of 3.beta.-(4'-Substituted phenyl)-2.beta.-(heterocyclic)tropanes Pravin Kotian, Philip Abraham, Anita H. Lewin, S. Wayne Mascarella, John W. Boja, Michael J. Kuhar, and F. Ivy Carroll pp 3451 - 3453; DOI: 10.1021/jm00018a004 |
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Cyclic lactam .alpha.-melanotropin analogs of Ac-Nle4-cyclo[Asp5,D-Phe7,Lys10]-.alpha.-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors Victor J. Hrubu, Dongsi Lu, Shubh D. Sharma, Ana de L. Castrucci, Robert A. Kesterson, Fahad A. Al-Obeidi, Mac E. Hadley, and Roger D. Cone pp 3454 - 3461; DOI: 10.1021/jm00018a005 |
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Synthesis Using a Fmoc-Based Strategy and Biological Activities of Some Reduced Peptide Bond Pseudopeptide Analogs of Dynorphin A Jean-Philippe Meyer, Peg Davis, Katharine B. Lee, Frank Porreca, Henry I. Yamamura, and Victor J. Hruby pp 3462 - 3468; DOI: 10.1021/jm00018a006 |
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Functionally selective M1 muscarinic agonists. 3. Side chain and azacycles contributing to functional muscarinic selectivity among pyrazinylazacycles John S. Ward, Leander Merrit, David O. Calligaro, Frank P. Bymaster, Harlan E. Shannon, Barry D. Sawyer, Charles H. Mitch, Jack B. Deeter, Steven C. Peters, and et al. pp 3469 - 3481; DOI: 10.1021/jm00018a007 |
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Tyrosine kinase inhibitors. 5. Synthesis and structure-activity relationships for 4-[(phenylmethyl)amino]- and 4-(phenylamino)quinazolines as potent adenosine 5'-triphosphate binding site inhibitors of the tyrosine kinase domain of the epidermal growth factor receptor. Gordon W. Rewcastle, William A. Denny, Alexander J. Bridges, Hairong Zhou, Donna R. Cody, Amy McMichael, and David W. Fry pp 3482 - 3487; DOI: 10.1021/jm00018a008 |
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Novel Acridine-Triazenes as Prototype Combilexins: Synthesis, DNA Binding, and Biological Activity Adrian W. McConnaughie and Terence C. Jenkins pp 3488 - 3501; DOI: 10.1021/jm00018a009 |
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The Squalestatins: Synthesis and Biological Activity of Some C3-Modified Analogs; Replacement of a Carboxylic Acid or Methyl Ester with an Isoelectronic Heterocyclic Functionality Mark J. Bamford, Chuen Chan, Andrew P. Craven, Brian W. Dymock, Darren Green, Richard A. Henson, Barrie E. Kirk, Michael G. Lester, Panayiotis A. Procopiou, and et al. pp 3502 - 3513; DOI: 10.1021/jm00018a010 |
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Novel Antagonists of Platelet-Activating Factor. 1. Synthesis and Structure-Activity Relationships of Benzodiazepine and Benzazepine Derivatives of 2-Methyl-1-phenylimidazo[4,5-c]pyridine M. Jonathan Fray, Kelvin Cooper, M. John Parry, Kenneth Richardson, and John Steele pp 3514 - 3523; DOI: 10.1021/jm00018a011 |
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Novel Antagonists of Platelet-Activating Factor. 2. Synthesis and Structure-Activity Relationships of Potent and Long-Acting Heterofused [1,5]Benzodiazepine and [1,4]Diazepine Derivatives of 1-Phenyl-2-methylimidazo[4,5-c]pyridine M. Jonathan Fray, David J. Bull, Kelvin Cooper, M. John Parry, and Mark H. Stefaniak pp 3524 - 3535; DOI: 10.1021/jm00018a012 |
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Synthesis and Quantitative Structure-Activity Relationship of Dequalinium Analogs as K+ Channel Blockers: Investigations on the Role of the Substituent at Position 4 of the Quinoline Ring Dimitrios Galanakis, Julie A. D. Calder, C. Robin Ganellin, Clive S. Owen, and Philip M. Dunn pp 3536 - 3546; DOI: 10.1021/jm00018a013 |
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Discovery of Potent Cyclic GMP Phosphodiesterase Inhibitors. 2-Pyridyl- and 2-Imidazolylquinazolines Possessing Cyclic GMP Phosphodiesterase and Thromboxane Synthesis Inhibitory Activities Sung J. Lee, Yoshitaka Konishi, Dingwei T. Yu, Tamara A. Miskowski, Christopher M. Riviello, Orest T. Macina, Manton R. Frierson, Kigen Kondo, Masafumi Sugitani, and et al. pp 3547 - 3557; DOI: 10.1021/jm00018a014 |
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Synthesis and antiviral activity of benzyl-substituted imidazo[1,5-a]-1,3,5-triazine (5,8-diaza-7,9-dideazapurine) derivatives Bozenna Golankiewicz, Piot Januszczyk, Satoru Ikeda, Jan Balzarini, and Erik De Clercq pp 3558 - 3565; DOI: 10.1021/jm00018a015 |
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Computer-Aided Design and Synthesis of 5-Substituted Tryptamines and Their Pharmacology at the 5-HT1D Receptor: Discovery of Compounds with Potential Anti-Migraine Properties Janet Buckingham, Robert C. Glen, Alan P. Hill, Richard M. Hyde, Graeme R. Martin, Alan D. Robertson, John A. Salmon, and Patrick M. Woollard pp 3566 - 3580; DOI: 10.1021/jm00018a016 |
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2-[N'-(3-Arylallylidene)hydrazino]adenosines Showing A2a Adenosine Agonist Properties and Vasodilation Activity Monica Viziano, Ennio Ongini, Anna Conti, Cristina Zocchi, Monica Seminati, and Donato Pocar pp 3581 - 3585; DOI: 10.1021/jm00018a017 |
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Novel Benzo[b]quinolizinium Cations as Uncompetitive N-Methyl-D-aspartic Acid (NMDA) Antagonists: The Relationship between log D and Agonist Independent (Closed) NMDA Channel Block William G. Earley, Virendra Kumar, John P. Mallamo, Chakrapani Subramanyam, John A. Dority, Matthew S. Miller, Diane L. DeHaven-Hudkins, Lisa D. Aimone, Michael D. Kelly, and Brian Ault pp 3586 - 3592; DOI: 10.1021/jm00018a018 |
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Effect of a Chiral 4-Alkyl Substituent in Hallucinogenic Amphetamines Robert Oberlender, P. V. Ramachandran, Michael P. Johnson, Xuemei Huang, and David E. Nichols pp 3593 - 3601; DOI: 10.1021/jm00018a019 |
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Synthesis and serotonergic activity of arylpiperazide derivatives of serotonin: potent agonists for 5-HT1D receptors Michel Perez, Catherine Fourrier, Isabelle Sigogneau, Petrus J. Pauwels, Christiane Palmier, Gareth W. John, Jean-Pierre Valentin, and Serge Halazy pp 3602 - 3607; DOI: 10.1021/jm00018a020 |
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Selective Inhibitors of Candida albicans Dihydrofolate Reductase: Activity and Selectivity of 5-(Arylthio)-2,4-diaminoquinazolines Joseph H. Chan, Jean S. Hong, Lee F. Kuyper, David P. Baccanari, Suzanne S. Joyner, Robert L. Tansik, Christine M. Boytos, and Sharon K. Rudolph pp 3608 - 3616; DOI: 10.1021/jm00018a021 |
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Peptidomimetic inhibitors of herpes simplex virus ribonucleotide reductase: a new class of antiviral agents Neil Moss, Pierre Beaulieu, Jean-Simon Duceppe, Jean-Marie Ferland, Jean Gauthier, Elsie Ghiro, Sylvie Goulet, Louis Grenier, Montse Llinas-Brunet, Raymond Plante, Dominik Wernic, and Robert Deziel pp 3617 - 3623; DOI: 10.1021/jm00018a022 |
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Structure-Based Design of Novel HIV Protease Inhibitors: Carboxamide-Containing 4-Hydroxycoumarins and 4-Hydroxy-2-pyrones as Potent Nonpeptidic Inhibitors Suvit Thaisrivongs, Keith D. Watenpaugh, W. Jeffrey Howe, Paul K. Tomich, Lester A. Dolak, Kong-Teck Chong, Che-Shen C. Tomich, Alfredo G. Tomasselli, Steve R. Turner, and et al. pp 3624 - 3637; DOI: 10.1021/jm00018a023 |
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Synthesis and Evaluation of Terbenzimidazoles as Topoisomerase I Inhibitors Qun Sun, Barbara Gatto, Chiang Yu, Angela Liu, Leroy F. Liu, and Edmond J. LaVoie pp 3638 - 3644; DOI: 10.1021/jm00018a024 |
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Synthesis and Evaluation of 5-Amino-5,6,7,8-tetrahydroquinolinones as Potential Agents for the Treatment of Alzheimer's Disease David M. Fink, Gina M. Bores, Richard C. Effland, Francis P. Huger, Barbara E. Kurys, Douglas K. Rush, and David E. Selk pp 3645 - 3651; DOI: 10.1021/jm00018a025 |
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Stereoisomers of N-[1-(2-Hydroxy-2-phenylethyl)-3-methyl-4-piperidyl]- N-phenylpropanamide: Synthesis, Stereochemistry, Analgesic Activity, and Opioid Receptor Binding Characteristics Zhi-Xian Wang, You-Cheng Zhu, Wen-Qiao Jin, Xin-Jian Chen, Jie Chen, Ru-Yun Ji, and Zhi-Qiang Chi pp 3652 - 3659; DOI: 10.1021/jm00018a026 |
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Nonclassical 2,4-diamino-6-(aminomethyl)-5,6,7,8-tetrahydroquinazoline antifolates: synthesis and biological activities Aleem Gangjee, Nurulain Zaveri, Mohi Kothare, and Sherry F. Queener pp 3660 - 3668; DOI: 10.1021/jm00018a027 |
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Decapeptide agonists of human C5a: the relationship between conformation and neutrophil response Sam D. Sanderson, Leonid Kirnarsky, Simon A. Sherman, Shawn M. Vogen, Om Prakash, Julia A. Ember, Angela M. Finch, and Stephen M. Taylor pp 3669 - 3675; DOI: 10.1021/jm00018a028 |
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8-Amino-3-benzyl-1,2,4-triazolo[4,3-a]pyrazines. Synthesis and anticonvulsant activity. James L. Kelley, James A. Linn, Donald D. Bankston, Christopher J. Burchall, Francis E. Soroko, and Barrett R. Cooper pp 3676 - 3679; DOI: 10.1021/jm00018a029 |
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Book Reviews pp 3680 - 3680; DOI: 10.1021/jm00018a600 |
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.alpha.- and .beta.-Adrenoceptors: From the Gene to the Clinic. 2. Structure-Activity Relationships and Therapeutic Applications Robert R. Ruffolo, William Bondinell, and J. Paul Hieble pp 3681 - 3716; DOI: 10.1021/jm00019a001 |
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1-Aminoindan-1,5-dicarboxylic Acid: A Novel Antagonist at Phospholipase C-Linked Metabotropic Glutamate Receptors Roberto Pellicciari, Roberto Luneia, Gabriele Costantino, Maura Marinozzi, Benedetto Natalini, Palle Jakobsen, Anders Kanstrup, Grazia Lombardi, Flavio Moroni, and Christian Thomsen pp 3717 - 3719; DOI: 10.1021/jm00019a002 |
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Synthesis of 1,4,7,8,9,10-hexahydro-9-methyl-6-nitropyrido[3,4-f]-quinoxaline-2,3-dione and related quinoxalinediones: characterization of .alpha.-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (and N-methyl-D-aspartate) receptor and anticonvulsant activity Christopher F. Bigge, Thomas C. Malone, Peter A. Boxer, Carrie B. Nelson, Daniel F. Ortwine, Robert Schelkun, Daniel M. Retz, Leonard J. Lescosky, Susan A. Borosky, and et al. pp 3720 - 3740; DOI: 10.1021/jm00019a003 |
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Potent and orally active angiotensin II receptor antagonists with equal affinity for human AT1 and AT2 subtypes Linda L. Chang, Wallace T. Ashton, Kelly L. Flanagan, Tsing-Bau Chen, Stacey S. O'Malley, Gloria J. Zingaro, Salah D. Kivlighn, Peter K. S. Siegl, Victor J. Lotti, and et al. pp 3741 - 3758; DOI: 10.1021/jm00019a004 |
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Derivatives of 5-[[1-4(4-carboxybenzyl)imidazolyl]methylidene]hydantoins as orally active angiotensin II receptor antagonists Jeremy J. Edmunds, Sylvester Klutchko, James M. Hamby, Amy M. Bunker, Cleo J. C. Connolly, R. Thomas Winters, John Quin, III, Ila Sircar, John C. Hodges, and et al. pp 3759 - 3771; DOI: 10.1021/jm00019a005 |
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New Spiropiperidines as Potent and Selective Non-Peptide Tachykinin NK2 Receptor Antagonists Paul W. Smith, Anthony W. J. Cooper, Richard Bell, Isabel J. M. Beresford, Paul M. Gore, Andrew B. McElroy, John M. Pritchard, Victoria Saez, Neil R. Taylor, and et al. pp 3772 - 3779; DOI: 10.1021/jm00019a006 |
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Tyrosine kinase inhibitors. 7. 7-amino-4-(phenylamino)- and 7-amino-4-[(phenylmethyl)amino]pyrido[4,3-d]pyrimidines: a new class of inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor Andrew M. Thompson, Alexander J. Bridges, David W. Fry, Alan J. Kraker, and William A. Denny pp 3780 - 3788; DOI: 10.1021/jm00019a007 |
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Synthesis, antitumor activity, and chemical properties of silaplatin and related platinum(II) and platinum(IV) complexes derived from .beta.-silyl amines Wayne K. Anderson, Ravindra Kasliwal, D. Michael Houston, Yueh-sha Wang, Ven L. Narayanan, Rudiger D. Haugwitz, and Jacqueline Plowman pp 3789 - 3797; DOI: 10.1021/jm00019a008 |
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Effect of bridge region variation on antifolate and antitumor activity of classical 5-substituted 2,4-diaminofuro[2,3-d]pyrimidines Aleem Gangjee, Rajesh Devraj, John J. McGuire, and Roy L. Kisliuk pp 3798 - 3805; DOI: 10.1021/jm00019a009 |
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Inhibition of the oncogene product p185erbB-2 in vitro and in vivo by geldanamycin and dihydrogeldanamycin derivatives R. C. Schnur, M. L. Corman, R. J. Gallaschun, B. A. Cooper, M. F. Dee, J. L. Doty, M. L. Muzzi, J. D. Moyer, C. I. DiOrio, and et al. pp 3806 - 3812; DOI: 10.1021/jm00019a010 |
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erbB-2 oncogene inhibition by geldanamycin derivatives: synthesis, mechanism of action, and structure-activity relationships R. C. Schnur, M. L. Corman, R. J. Gallaschun, B. A. Cooper, M. F. Dee, J. L. Doty, M. L. Muzzi, C I. DiOrio, E. G. Barbacci, and et al. pp 3813 - 3820; DOI: 10.1021/jm00019a011 |
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Novel cytotoxic 3'-(tert-Butyl) 3'-diphenyl analogs of paclitaxel and docetaxel Syed M. Ali, Michael Z. Hoemann, Jeffrey Aube, Lester A. Mitscher, Gunda I. Georg, Randy McCall, and Lalith R. Jayasinghe pp 3821 - 3828; DOI: 10.1021/jm00019a012 |
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Furanfurin and Thiophenfurin: Two Novel Tiazofurin Analogs. Synthesis, Structure, Antitumor Activity, and Interactions with Inosine Monophosphate Dehydrogenase Palmarisa Franchetti, Loredana Cappellacci, Mario Grifantini, Anna Barzi, Giuseppe Nocentini, Hongyoan Yang, Ayrn O'Connor, Hiremagalur N. Jayaram, Christopher Carrell, and Barry M. Goldstein pp 3829 - 3837; DOI: 10.1021/jm00019a013 |
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Synthesis and Structure-Activity Relationships of Analogs of 2'-Deoxy-2'-(3-methoxybenzamido)adenosine, a Selective Inhibitor of Trypanosomal Glycosomal Glyceraldehyde-3-phosphate Dehydrogenase Serge Van Calenbergh, Christophe L. M. J. Verlinde, Johanna Soenens, Andre De Bruyn, Mia Callens, Norbert M. Blaton, Oswald M. Peeters, Piet Herdewijn, Jef Rozenski, and Wim G. J. Hol pp 3838 - 3849; DOI: 10.1021/jm00019a014 |
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Inhibition of uridine phosphorylase: synthesis and structure-activity relationships of aryl-substituted 5-benzyluracils and 1-[(2-hydroxyethoxy)methyl]-5-benzyluracils. G. Faye Orr, David L. Musso, G. Evan Boswell, James L. Kelley, Suzanne S. Joyner, Stephen T. Davis, and David P. Baccanari pp 3850 - 3856; DOI: 10.1021/jm00019a015 |
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1-Phenyl-3-amino-1,2,3,4-tetrahydronaphthalenes and Related Derivatives as Ligands for the Neuromodulatory .sigma.3 Receptor: Further Structure-Activity Relationships Steven D. Wyrick, Raymond G. Booth, Andrew M. Myers, Constance E. Owens, Ehren C. Bucholtz, Phillip C. Hooper, Nora S. Kula, Ross J. Baldessarini, and Richard B. Mailman pp 3857 - 3864; DOI: 10.1021/jm00019a016 |
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Quantitative structural activity relationship study of bis-tetraazacyclic compounds. A novel series of HIV-1 and HIV-2 inhibitors Heidi C. Joao, Karen De Vreese, Rudi Pauwels, Erik De Clercq, Geoff W. Henson, and Gary J. Bridger pp 3865 - 3873; DOI: 10.1021/jm00019a017 |
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Inhibition of Monoamine Oxidase-B by 5H-Indeno[1,2-c]pyridazines: Biological Activities, Quantitative Structure-Activity Relationships (QSARs) and 3D-QSARs Silvia Kneubuehler, Ulrike Thull, Cosimo Altomare, Vincenco Carta, Patrick Gaillard, Pierre-Alain Carrupt, Angelo Carotti, and Bernard Testa pp 3874 - 3883; DOI: 10.1021/jm00019a018 |
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Synthesis and anticonvulsant activity of N-Benzylpyrrolo[2,3-d]-, -pyrazolo[3,4-d]-, and -triazolo[4,5-d]pyrimidines: imidazole ring-modified analogs of 9-(2-Fluorobenzyl)-6-(methylamino)-9H-purine James L. Kelley, Ronda G. Davis, Ed W. McLean, Robert C. Glen, Francis E. Soroko, and Barrett R. Cooper pp 3884 - 3888; DOI: 10.1021/jm00019a019 |
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Book Reviews pp 3889 - 3890; DOI: 10.1021/jm00019a600 |
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A New Paclitaxel Photoaffinity Analog with a 3-(4-Benzoylphenyl)propanoyl Probe for Characterization of Drug-Binding Sites on Tubulin and P-Glycoprotein Iwao Ojima, Olivier Duclos, Gyorgy Dorman, Bruno Simonot, Glenn D. Prestwich, Srinivasa Rao, Keith A. Lerro, and Susan B. Horwitz pp 3891 - 3894; DOI: 10.1021/jm00020a001 |
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Antiinflammatory 4,5-Diarylpyrroles. 2. Activity as a Function of Cyclooxygenase-2 Inhibition Wendell Wilkie Wilkerson, Robert A. Copeland, Maryanne Covington, and James M. Trzaskos pp 3895 - 3901; DOI: 10.1021/jm00020a002 |
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Pyrazinoic Acid Esters with Broad Spectrum in Vitro Antimycobacterial Activity Michael H. Cynamon, Rayomand Gimi, Ferenc Gyenes, Cindy A. Sharpe, Kathryn E. Bergmann, Hye Jung Han, Livia B. Gregor, Radha Rapolu, Gregorio Luciano, and John T. Welch pp 3902 - 3907; DOI: 10.1021/jm00020a003 |
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Resolution and in Vitro and Initial in Vivo Evaluation of Isomers of Iodine-125-Labeled 1-Azabicyclo[2.2.2]oct-3-yl .alpha.-Hydroxy-.alpha.-(1-iodo-1-propen-3-yl)-.alpha.-phenylacetate: A High-Affinity Ligand for the Muscarinic Receptor Daniel W. McPherson, Carla R. Lambert, Kristi Jahn, Virendar Sood, Robert C. McRee, Barry Zeeberg, Richard C. Reba, and Furn F. Knapp pp 3908 - 3917; DOI: 10.1021/jm00020a004 |
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Synthesis and Antifungal Activity of New Azole Derivatives Containing an N-Acylmorpholine Ring Javier Bartroli, Enric Turmo, Monica Alguero, Eulalia Boncompte, Maria L. Vericat, Julian Garcia-Rafanell, and Javier Forn pp 3918 - 3932; DOI: 10.1021/jm00020a005 |
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Novel 4'-Substituted and 4',4''-Disubstituted 3.alpha.-(Diphenylmethoxy)tropane Analogs as Potent and Selective Dopamine Uptake Inhibitors Amy Hauck Newman, Richard H. Kline, Andrew C. Allen, Sari Izenwasser, Clifford George, and Jonathan L. Katz pp 3933 - 3940; DOI: 10.1021/jm00020a006 |
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Mononucleoside Phosphotriester Derivatives with S-Acyl-2-thioethyl Bioreversible Phosphate-Protecting Groups: Intracellular Delivery of 3'-Azido-2',3'-dideoxythymidine 5'-Monophosphate Isabelle Lefebvre, Christian Perigaud, Alain Pompon, Anne-Marie Aubertin, Jean-Luc Girardet, Andre Kirn, Gilles Gosselin, and Jean-Louis Imbach pp 3941 - 3950; DOI: 10.1021/jm00020a007 |
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Chiral Dioxolane Inhibitors of Leukotriene Biosynthesis: Structure-Activity Relationships and Syntheses Using Asymmetric Dihydroxylation Graham C. Crawley and Malcolm T. Briggs pp 3951 - 3956; DOI: 10.1021/jm00020a008 |
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Synthesis and Anti-DNA Viral Activities in Vitro of Certain 2,4-Disubstituted- 7-(2-deoxy-2-fluoro-.beta.-D-arabinofuranosyl)pyrrolo[2,3-d]pyrimidine Nucleosides Birendra K. Bhattacharya, Joshua O. Ojwang, Robert F. Rando, John H. Huffman, and Ganapathi R. Revankar pp 3957 - 3966; DOI: 10.1021/jm00020a009 |
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Pseudodipeptide Inhibitors of Protein Farnesyltransferase S. Jane deSolms, Albert A. Deana, Elizabeth A. Giuliani, Samuel L. Graham, Nancy E. Kohl, Scott D. Mosser, Allen I. Oliff, David L. Pompliano, Elaine Rands, and et al. pp 3967 - 3971; DOI: 10.1021/jm00020a010 |
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Peptidyl .alpha.-ketoheterocyclic inhibitors of human neutrophil elastase. 3. In vitro and in vivo potency of a series of peptidyl .alpha.-ketobenzoxazoles Philip D. Edwards, Mark A. Zottola, Matthew Davis, Joseph Williams, and Paul A. Tuthill pp 3972 - 3982; DOI: 10.1021/jm00020a011 |
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Cyclization-Activated Prodrugs: N-(Substituted 2-hydroxyphenyl and 2-hydroxypropyl)carbamates Based on Ring-Opened Derivatives of Active Benzoxazolones and Oxazolidinones as Mutual Prodrugs of Acetaminophen Alain Vigroux, Michel Bergon, and Chantal Zedde pp 3983 - 3994; DOI: 10.1021/jm00020a012 |
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Novel Deltorphin Heptapeptide Analogs with Potent .delta. Agonist, .delta. Antagonist, or Mixed .mu. Antagonist/.delta. Agonist Properties Yusuke Sasaki and Takako Chiba pp 3995 - 3999; DOI: 10.1021/jm00020a013 |
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Ribose-Modified Adenosine Analogs as Potential Partial Agonists for the Adenosine Receptor Eleonora M. van der Wenden, Jacobien K. von Frijtag Drabbe Kuenzel, Ron A. A. Mathot, Meindert Danhof, Adriaan P. IJzerman, and Willem Soudijn pp 4000 - 4006; DOI: 10.1021/jm00020a014 |
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Synthesis and Antiviral Activity of 8-Aza Analogs of Chiral [2-(Phosphonomethoxy)propyl]guanines Palmarisa Franchetti, Ghassan Abu Sheikha, Loredana Cappellacci, Mario Grifantini, Antonella De Montis, Giovanna Piras, Anna Giulia Loi, and Paolo La Colla pp 4007 - 4013; DOI: 10.1021/jm00020a015 |
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Synthesis of Tight Binding Inhibitors and Their Action on the Proprotein-Processing Enzyme Furin Herbert Angliker pp 4014 - 4018; DOI: 10.1021/jm00020a016 |
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Synthesis and Biological Evaluation of N6-Cycloalkyl Derivatives of 1-Deazaadenine Nucleosides: A New Class of Anti-Human Immunodeficiency Virus Agents Gloria Cristalli, Sauro Vittori, Alessandra Eleuteri, Rosaria Volpini, Emidio Camaioni, Giulio Lupidi, Naheed Mahmood, Francesca Bevilacqua, and Giorgio Palu pp 4019 - 4025; DOI: 10.1021/jm00020a017 |
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New Antihistamines: Substituted Piperazine and Piperidine Derivatives as Novel H1-Antagonists Magid Abou-Gharbia, John A. Moyer, Susan T. Nielsen, Michael Webb, and Usha Patel pp 4026 - 4032; DOI: 10.1021/jm00020a018 |
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Synthesis and Anticonvulsant Activity of Enaminones. 3. Investigations on 4'-, 3'-, and 2'-Substituted and Polysubstituted Anilino Compounds, Sodium Channel Binding Studies, and Toxicity Evaluations1,2 K. R. Scott, Gary O. Rankin, James P. Stables, Mariano S. Alexander, Ivan O. Edafiogho, Vida A. Farrar, Kymberle R. Kolen, Jacqueline A. Moore, Lyndia D. Sims, and Ahn D. Tonnu pp 4033 - 4043; DOI: 10.1021/jm00020a019 |
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Characterization of Potent and Selective Antagonists at Postsynaptic 5-HT1A Receptors in a Series of N4-Substituted Arylpiperazines Jean-Louis Peglion, Herve Canton, Karin Bervoets, Valerie Audinot, Mauricette Brocco, Alain Gobert, Sylvie Le Marouille-Girardon, and Mark J. Millan pp 4044 - 4055; DOI: 10.1021/jm00020a020 |
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Design, synthesis, and structure-activity Relationships of a new series of .alpha.-adrenergic agonists: spiro[(1,3-diazacycylpent-1-ent)-5,2'-(1',2',3',4'-tetrahydronaphthalene)] Alex A. Cordi, Jean-Michel Lacoste, Jean-Jacques Descombes, Christine Courchay, Paul M. Vanhoutte, Michel Laubie, and Tony J. Verbeuren pp 4056 - 4069; DOI: 10.1021/jm00020a021 |
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Synthesis, X-ray Crystallography, and Pharmacokinetics of Novel Azomethine Prodrugs of (R)-.alpha.-Methylhistamine: Highly Potent and Selective Histamine H3 Receptor Agonists Michael Krause, Agnes Rouleau, Holger Stark, Peter Luger, Ralph Lipp, Monique Garbarg, Jean-Charles Schwartz, and Walter Schunack pp 4070 - 4079; DOI: 10.1021/jm00020a022 |
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A Molecular Dynamics Approach to Receptor Mapping: Application to the 5HT3 and .beta.2-Adrenergic Receptors Paul R. Gouldson, Peter J. Winn, and Christopher A. Reynolds pp 4080 - 4086; DOI: 10.1021/jm00020a023 |
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In Vivo and in Vitro Studies on the Neurotoxic Potential of 6-Hydroxydopamine Analogs Su Ma, Lorrie Lin, R. Raghavan, Pat Cohenour, Peter Y. T. Lin, Jennifer Bennett, Russell J. Lewis, Eric L. Enwall, Richard Kostrzewa, and et al. pp 4087 - 4097; DOI: 10.1021/jm00020a024 |
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Design, Synthesis, and Antiviral Activity of Certain 2,5,6-Trihalo-1-(.beta.-D-ribofuranosyl)benzimidazoles Leroy B. Townsend, Rodrigo V. Devivar, Steven R. Turk, M. Reza Nassiri, and John C. Drach pp 4098 - 4105; DOI: 10.1021/jm00020a025 |
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Synthesis and Antiproliferative and Antiviral Activity of 2'-Deoxy-2'-fluoroarabinofuranosyl Analogs of the Nucleoside Antibiotics Toyocamycin and Sangivamycin Steven H. Krawczyk, M. Reza Nassiri, Louis S. Kucera, Earl R. Kern, Roger G. Ptak, Linda L. Wotring, John C. Drach, and Leory B. Townsend pp 4106 - 4114; DOI: 10.1021/jm00020a026 |
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Synthesis and Evaluation of Certain Thiosangivamycin Analogs as Potential Inhibitors of Cell Proliferation and Human Cytomegalovirus Steven H. Krawczyk, Thomas E. Renau, M. Reza Nassiri, Allison C. Westerman, Linda L. Wotring, John C. Drach, and Leroy B. Townsend pp 4115 - 4119; DOI: 10.1021/jm00020a027 |
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Synthesis and Antimalarial Activities of Several Fluorinated Artemisinin Derivatives Yu Ming Pu, Daniel S. Torok, Herman Ziffer, Xing-Qing Pan, and Steven R. Meshnick pp 4120 - 4124; DOI: 10.1021/jm00020a028 |
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Development of a Potent Thrombin Receptor Ligand Dong-Mei Feng, Daniel F. Veber, Thomas M. Connolly, Cindra Condra, Mei-Jy Tang, and Ruth F. Nutt pp 4125 - 4130; DOI: 10.1021/jm00020a029 |
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1-(Fluorobenzyl)-4-amino-1H-1,2,3-triazolo[4,5-c]pyridines: Synthesis and Anticonvulsant Activity James L. Kelley, Cecilia S. Koble, Ronda G. Davis, Ed W. McLean, Francis E. Soroko, and Barrett R. Cooper pp 4131 - 4134; DOI: 10.1021/jm00020a030 |
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Probing the Hydrophobic Pocket of the Active Site of Aromatase with 4-Phenoxy-7.alpha.-(phenylthio)-4-androstene-3,17-dione Xing-Ping Liu, Didier M. Lambert, and Yusuf J. Abul-Hajj pp 4135 - 4138; DOI: 10.1021/jm00020a031 |
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Book Reviews pp 4139 - 4140; DOI: 10.1021/jm00020a600 |
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Therapeutic Approaches Related to Amyloid-.beta. Peptide and Alzheimer's Disease Dale B. Schenk, Russell E. Rydel, Patrick May, Sheila Little, Jill Panetta, Ivan Lieberburg, and Sukanto Sinha pp 4141 - 4154; DOI: 10.1021/jm00021a001 |
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Alkane-6,8-diol: Inhibitor of Tumor Promotion in Two-Stage Carcinogenesis in Mouse Skin Shigeyasu Motohashi, Toshihiro Akihisa, Toshitake Tamura, Norio Tokutake, Michio Takido, and Ken Yasukawa pp 4155 - 4156; DOI: 10.1021/jm00021a002 |
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Phenoxypropylamines: A New Series of Squalene Synthase Inhibitors George R. Brown, Roger J. Butlin, Steven Chapman, M. Allan Eakin, Alan J. Foubister, Susan Freeman, David Griffiths, Peter J. Harrison, Michael C. Johnson, and et al. pp 4157 - 4160; DOI: 10.1021/jm00021a003 |
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Synthesis of Novel 2,4-Diaminopyrrolo[2,3-d]pyrimidines with Antioxidant, Neuroprotective, and Antiasthma Activity Gordon L. Bundy, Donald E. Ayer, Lee S. Banitt, Kenneth L. Belonga, Stephen A. Mizsak, John R. Palmer, James M. Tustin, Jia En Chin, Edward D. Hall, and et al. pp 4161 - 4163; DOI: 10.1021/jm00021a004 |
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Cyclosporin Analogs Modified in the 3,7,8-Positions: Substituent Effects on Peptidylprolyl Isomerase Inhibition and Immunosuppressive Activity Are Nonadditive Ming-Kuan Hu, Alison Badger, and Daniel H. Rich pp 4164 - 4170; DOI: 10.1021/jm00021a005 |
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Hydroxylated Aromatic Inhibitors of HIV-1 Integrase Terrence R. Jr. Burke, Mark Fesen, Abhijit Mazumder, Jessie Yung, Jian Wang, Adelaide M. Carothers, Dezider Grunberger, John Driscoll, Yves Pommier, and Kurt Kohn pp 4171 - 4178; DOI: 10.1021/jm00021a006 |
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Effective Inhibitors of Hemagglutination by Influenza Virus Synthesized from Polymers Having Active Ester Groups. Insight into Mechanism of Inhibition Mathai Mammen, Georg Dahmann, and George M. Whitesides pp 4179 - 4190; DOI: 10.1021/jm00021a007 |
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Esters of 3-Pyridylacetic Acid That Combine Potent Inhibition of 17.alpha.-Hydroxylase/C17,20-Lyase (Cytochrome P45017.alpha.) with Resistance to Esterase Hydrolysis Martin G. Rowlands, S. Elaine Barrie, Ferdinand Chan, John Houghton, Michael Jarman, Raymond McCague, and Gerard A. Potter pp 4191 - 4197; DOI: 10.1021/jm00021a008 |
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Piperazinylalkyl Heterocycles as Potential Antipsychotic Agents Malcolm K. Scott, Ellen W. Baxter, Debra J. Bennett, Robert E. Boyd, Paul S. Blum, Ellen E. Codd, Michael J. Kukla, Elizabeth Malloy, Bruce E. Maryanoff, and et al. pp 4198 - 4210; DOI: 10.1021/jm00021a009 |
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N-Aryl-N'-Benzylpiperazines as Potential Antipsychotic Agents Allen B. Reitz, Ellen W. Baxer, Debra J. Bennett, Ellen E. Codd, Alfonzo D. Jordan, Elizabeth A. Malloy, Bruce E. Maryanoff, Mark E. McDonnell, Marta E. Ortegon, and et al. pp 4211 - 4222; DOI: 10.1021/jm00021a010 |
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Antifungal Agents. 9. 3-Aryl-4-[.alpha.-(1H-imidazol-1-yl)arylmethyl]pyrroles: A New Class of Potent Anti-Candida Agents Marino Artico, Roberto Di Santo, Roberta Costi, Silvio Massa, Augusta Retico, Marco Artico, Germana Apuzzo, Giovanna Simonetti, and Vittorio Strippoli pp 4223 - 4233; DOI: 10.1021/jm00021a011 |
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Synthesis and Antitumor Activity of 4- and 5-Substituted Derivatives of Isoquinoline-1-carboxaldehyde Thiosemicarbazone Mao-Chin Liu, Tai-Shun Lin, Philip Penketh, and Alan C. Sartorelli pp 4234 - 4243; DOI: 10.1021/jm00021a012 |
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2-Substituted Penems with Amino Acid-Related Side Chains: Synthesis and Antibacterial Activity of a New Series of .beta.-Lactam Antibiotics Maria Altamura, Enzo Perrotta, Piero Sbraci, Vittorio Pestellini, Federico Arcamone, Giuseppe Cascio, Laura Lorenzi, Giuseppe Satta, Grazia Morandotti, and Roberta Sperning pp 4244 - 4256; DOI: 10.1021/jm00021a013 |
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Microsphere Formation in a Series of Derivatized .alpha.-Amino Acids: Properties, Molecular Modeling, and Oral Delivery of Salmon Calcitonin Andrea Leone-Bay, Campbell McInnes, NaiFang Wang, Frenel DeMorin, Doug Achan, Christine Lercara, Donald Sarubbi, Susan Haas, Jeffery Press, and et al. pp 4257 - 4262; DOI: 10.1021/jm00021a014 |
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N-Acylated .alpha.-Amino Acids as Novel Oral Delivery Agents for Proteins Andrea Leone-Bay, Noemi Santiago, Douglas Achan, Kirin Chaudhary, Frenel DeMorin, Lise Falzarano, Susan Haas, Suraj Kalbag, David Kaplan, and et al. pp 4263 - 4269; DOI: 10.1021/jm00021a015 |
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L-O-(2-Malonyl)tyrosine: A New Phosphotyrosyl Mimetic for the Preparation of Src Homology 2 Domain Inhibitory Peptides Bin Ye, Miki Akamatsu, Steven E. Shoelson, Gert Wolf, Sophie Giorgetti-Peraldi, Xinjian Yan, Peter P. Roller, and Terrence R. Burke pp 4270 - 4275; DOI: 10.1021/jm00021a016 |
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Identification of efficient pentapeptide substrates for the tyrosine kinase pp60c-src Shrikumar A. Nair, Moon H. Kim, Stephen D. Warren, Sun Choi, Zhou Songyang, Lewis C. Cantley, and David G. Hangauer pp 4276 - 4283; DOI: 10.1021/jm00021a017 |
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(.+-.)-(Aminoalkyl)benzazepine Analogs: Novel Dopamine D1 Receptor Antagonists Jamshed H. Shah, Sari Izenwasser, Beth Geter-Douglass, Jeffrey M. Witkin, and Amy Hauck Newman pp 4284 - 4293; DOI: 10.1021/jm00021a018 |
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Improving the Affinity and Selectivity of a Nonpeptide Series of Cholecystokinin-B/Gastrin Receptor Antagonists Based on the Dibenzobicyclo[2.2.2]octane Skeleton S. Barret Kalindjian, Ildiko M. Buck, Julia R. Cushnir, David J. Dunstone, Martin L. Hudson, Caroline M. R. Low, Iain M. McDonald, Michael J. Pether, Katherine I. M. Steel, and Matthew J. Tozer pp 4294 - 4302; DOI: 10.1021/jm00021a019 |
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A Series of N4-Imidoethyl Derivatives of 1-(2,3-Dihydro-1,4-benzodioxin-5-yl)piperazine as 5-HT1A Receptor Ligands: Synthesis and Structure-Affinity Relationships B. J. van Steen, I. van Wijngaarden, M. Th. M. Tulp, and W. Soudijn pp 4303 - 4308; DOI: 10.1021/jm00021a020 |
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Structure-Activity Relationships of Cyclic Pentapeptide Endothelin A Receptor Antagonists Takehiro Fukami, Toshio Nagase, Kagari Fujita, Takashi Hayama, Kenji Niiyama, Toshiaki Mase, Shigeru Nakajima, Takahiro Fukuroda, Toshihiko Saeki, and et al. pp 4309 - 4324; DOI: 10.1021/jm00021a021 |
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Structure-Taste Correlations in Sweet Dihydrochalcone, Sweet Dihydroisocoumarin, and Bitter Flavone Compounds Whanchul Shin, Seung Jun Kim, Jung Mi Shin, and Sung-Hou Kim pp 4325 - 4331; DOI: 10.1021/jm00021a022 |
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Mechanism of Inhibition of Poly(ADP-ribose) Glycohydrolase by Adenosine Diphosphate (Hydroxymethyl)pyrrolidinediol James T. Slama, Nasreen Aboul-Ela, and Myron K. Jacobson pp 4332 - 4336; DOI: 10.1021/jm00021a023 |
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Synthesis of Isoornithines and Methylputrescines. An Evaluation of Their Inhibitory Effects on Ornithine Decarboxylase Gerardo Aizencang, Rosalia B. Frydman, Sergio Giorgieri, Luis Sambrotta, Liliana Guerra, and Benjamin Frydman pp 4337 - 4341; DOI: 10.1021/jm00021a024 |
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Book Reviews pp 4342 - 4342; DOI: 10.1021/jm00021a600 |
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Nitric Oxide: A New Paradigm for Second Messengers James F. Kerwin, Jack R. Lancaster, and Paul L. Feldman pp 4343 - 4362; DOI: 10.1021/jm00022a001 |
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Drug Leads from Combinatorial Phosphodiester Libraries Peter W. Davis, Timothy A. Vickers, Laura Wilson-Lingardo, Jacqueline R. Wyatt, Charles J. Guinosso, Yogesh S. Sanghvi, Elizabeth A. DeBaets, Oscar L. Acevedo, P. Dan Cook, and David J. Ecker pp 4363 - 4366; DOI: 10.1021/jm00022a002 |
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Synthesis and Structure-Activity Relationships of Substituted 1,4-Dihydroquinoxaline-2,3-diones: Antagonists of N-Methyl-D-aspartate (NMDA) Receptor Glycine Sites and Non-NMDA Glutamate Receptors John F. W. Keana, Sunil M. Kher, Sui Xiong Cai, Christian M. Dinsmore, Anne G. Glenn, J. Guastella, Jin-Cheng Huang, Victor Ilyin, Yixin Lu, and et al. pp 4367 - 4379; DOI: 10.1021/jm00022a003 |
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Enhanced D1 Affinity in a Series of Piperazine Ring Substituted 1-Piperazino-3-Arylindans with Potential Atypical Antipsychotic Activity Klaus P. Bogeso, Jorn Arnt, Kristen Frederiksen, Hans Otto Hansen, John Hyttel, and Henrik Pedersen pp 4380 - 4392; DOI: 10.1021/jm00022a004 |
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Pyrrolo[2,1-c][1,4]benzothiazines: Synthesis, Structure-Activity Relationships, Molecular Modeling Studies, and Cardiovascular Activity Giuseppe Campiani, Antonio Garofalo, Isabella Fiorini, Maurizio Botta, Vito Nacci, Andrea Tafi, Alberto Chiarini, Roberta Budriesi, Giancarlo Bruni, and Maria R. Romeo pp 4393 - 4410; DOI: 10.1021/jm00022a005 |
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Synthetic and Structure/Activity Studies on Acid-Substituted 2-Arylphenols: Discovery of 2-[2-Propyl-3-[3-[2-ethyl-4-(4-fluorophenyl)-5-hydroxyphenoxy]- propoxy]phenoxy]benzoic Acid, a High-Affinity Leukotriene B4 Receptor Antagonist J. Scott Sawyer, Nicholas J. Bach, S. Richard Baker, Ronald F. Baldwin, Peter S. Borromeo, Sandra L. Cockerham, Jerome H. Fleisch, Paul Floreancig, Larry L. Froelich, and et al. pp 4411 - 4432; DOI: 10.1021/jm00022a006 |
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A 3-Amino-4-hydroxy-3-cyclobutene-1,2-dione-Containing Glutamate Analog Exhibiting High Affinity to Excitatory Amino Acid Receptors Philip C. M. Chan, Robert J. Roon, James F. Koerner, Nicholas J. Taylor, and John F. Honek pp 4433 - 4438; DOI: 10.1021/jm00022a007 |
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Kynurenic Acid Derivatives Inhibit the Binding of Nerve Growth Factor (NGF) to the Low-Affinity p75 NGF Receptor Juan C. Jaen, Edgardo Laborde, Ruth A. Bucsh, Bradley W. Caprathe, Roderick J. Sorenson, James Fergus, Katharyn Spiegel, James Marks, Melvin R. Dickerson, and Robert E. Davis pp 4439 - 4445; DOI: 10.1021/jm00022a008 |
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Structure-Activity Study of Tripeptide Thrombin Inhibitors Using .alpha.-Alkyl Amino Acids and Other Conformationally Constrained Amino Acid Substitutions Robert T. Shuman, Robert B. Rothenberger, Charles S. Campbell, Gerald F. Smith, Donetta S. Gifford-Moore, Jonathan W. Paschal, and Paul D. Gesellchen pp 4446 - 4453; DOI: 10.1021/jm00022a009 |
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Quantitative Structure-Activity Relationships (QSARs) of N-Terminus Fragments of NK1 Tachykinin Antagonists: A Comparison of Classical QSARs and Three-Dimensional QSARs from Similarity Matrixes David C. Horwell, William Howson, Michael Higginbottom, Dorica Naylor, Giles S. Ratcliffe, and Sophie Williams pp 4454 - 4462; DOI: 10.1021/jm00022a010 |
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Structure-Based Design of Nonpeptidic HIV Protease Inhibitors from a Cyclooctylpyranone Lead Structure Karen R. Romines, Keith D. Watenpaugh, W. Jeffrey Howe, Paul K. Tomich, Kristine D. Lovasz, Jeanette K. Morris, Musiri N. Janakiraman, Janet C. Lynn, Miao-Miao Horng, and et al. pp 4463 - 4473; DOI: 10.1021/jm00022a011 |
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Synthesis of substituted 1-norbornylamines with antiviral activity. A. Garcia Martinez, E. Teso Vilar, A. Garcia Fraile, S. de la Cerero, M. E. Rodriguez Herrero, P. Martinez Ruiz, L. R. Subramanian, and A. Garcia Gancedo pp 4474 - 4477; DOI: 10.1021/jm00022a012 |
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The Synthesis, Structure-Activity, and Structure-Side Effect Relationships of a Series of 8-Alkoxy- and 5-Amino-8-alkoxyquinolone Antibacterial Agents Joseph P. Sanchez, Rocco D. Gogliotti, John M. Domagala, Stephen J. Gracheck, Michael D. Huband, Josephine A. Sesnie, Michael A. Cohen, and Martin A. Shapiro pp 4478 - 4487; DOI: 10.1021/jm00022a013 |
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Hypoxia-Selective Agents Derived from 2-Quinoxalinecarbonitrile 1,4-Di-N-oxides. 2 Antonio Monge, Francisco J. Martinez-Crespo, Adela Lopez de Cerain, Juan A. Palop, Susana Narro, Virginia Senador, Ana Marin, Yolanda Sainz, Mercedes Gonzalez, and et al. pp 4488 - 4494; DOI: 10.1021/jm00022a014 |
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5-Arylthio Substituted 2-Amino-4-oxo-6-methylpyrrolo[2,3-d]pyrimidine Antifolates as Thymidylate Synthase Inhibitors and Antitumor Agents Aleem Gangjee, Rajesh Devraj, John J. McGuire, and Roy L. Kisliuk pp 4495 - 4502; DOI: 10.1021/jm00022a015 |
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Topoisomerase II-Mediated DNA Cleavage by Adocia- and Xestoquinones from the Philippine Sponge Xestospongia sp. Gisela P. Concepcion, Tommaso A. Foderaro, Glenn S. Eldredge, Emil Lobkovsky, Jon Clardy, Louis R. Barrows, and Chris M. Ireland pp 4503 - 4507; DOI: 10.1021/jm00022a016 |
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New Orally Active Serine Protease Inhibitors: Structural Requirements for Their Good Oral Activity Kazuhiko Senokuchi, Hisao Nakai, Yoshisuke Nakayama, Yoshihiko Odagaki, Katsuhito Sakaki, Masashi Kato, Toru Maruyama, Toru Miyazaki, Hidenori Ito, and et al. pp 4508 - 4517; DOI: 10.1021/jm00022a017 |
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Steroidal Spiro-.gamma.-lactones That Inhibit 17.beta.-Hydroxysteroid Dehydrogenase Activity in Human Placental Microsomes Kay Mane Sam, Serge Auger, Van Luu-The, and Donald Poirier pp 4518 - 4528; DOI: 10.1021/jm00022a018 |
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1.alpha.,25-Dihydroxyvitamin D3 Analogs Featuring Aromatic and Heteroaromatic Rings: Design, Synthesis, and Preliminary Biological Testing Gary H. Posner, Zhengong Li, M. Christina White, Victoria Vinader, Kazuhiro Takeuchi, Sandra E. Guggino, Patrick Dolan, and Thomas W. Kensler pp 4529 - 4537; DOI: 10.1021/jm00022a019 |
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Thiopyranol[2,3,4-c,d]indoles as Inhibitors of 5-Lipoxygenase, 5-Lipoxygenase-Activating Protein, and Leukotriene C4 Synthase John H. Hutchinson, Stella Charleson, Jilly F. Evans, Jean-Pierre Falgueyret, Karst Hoogsteen, Tom R. Jones, Stacia Kargman, Dwight Macdonald, Cyril S. McFarlane, and et al. pp 4538 - 4547; DOI: 10.1021/jm00022a020 |
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Neurosteroid Analogs. 3. The Synthesis and Electrophysiological Evaluation of Benz[e]indene Congeners of Neuroactive Steroids Having the 5.beta.-Configuration Mingcheng Han, Yuefei Hu, Charles F. Zorumski, and Douglas F. Covey pp 4548 - 4556; DOI: 10.1021/jm00022a021 |
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.alpha.-Hydroxy Phosphinyl-Based Inhibitors of Human Renin Dinesh V. Patel, Katherine Rielly-Gauvin, Denis E. Ryono, Charles A. Free, W. Lynn Rogers, Sandra A. Smith, Jack M. DeForrest, Robert S. Oehl, and Edward W. Petrillo pp 4557 - 4569; DOI: 10.1021/jm00022a022 |
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1,2-Diarylcyclopentenes as Selective Cyclooxygenase-2 Inhibitors and Orally Active Anti-inflammatory Agents James J. Li, Gary D. Anderson, Earl G. Burton, J. Nita Cogburn, Joe T. Collins, Danny J. Garland, Susan A. Gregory, Horng-Chih Huang, Peter C. Isakson, and et al. pp 4570 - 4578; DOI: 10.1021/jm00022a023 |
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Y1 and Y2 Receptor Selective Neuropeptide Y Analogs: Evidence for a Y1 Receptor Subclass Dean A. Kirby, Steven C. Koerber, John M. May, Cristin Hagaman, Mary Jane Cullen, Mary Ann Pelleymounter, and Jean E. Rivier pp 4579 - 4586; DOI: 10.1021/jm00022a024 |
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Structure-Activity Relationships of Cytotoxic Cholesterol-Modified DNA Duplexes Michael W. Reed, Eugeny Lukhtanov, Vladimir Gorn, Deborah D. Lucas, James H. Zhou, S. Balakrishna Pai, Yung-chi Cheng, and Rich B. Meyer pp 4587 - 4596; DOI: 10.1021/jm00022a025 |
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Inhibition of E-Selectin-, ICAM-1-, and VCAM-1-Mediated Cell Adhesion by Benzo[b]thiophene-, Benzofuran-, Indole-, and Naphthalene-2-carboxamides: Identification of PD 144795 as an Antiinflammatory Agent Diane H. Boschelli, James B. Kramer, Sonya S. Khatana, Roderick J. Sorenson, David T. Connor, Mark A. Ferin, Clifford D. Wright, Mark E. Lesch, Kathleen Imre, and et al. pp 4597 - 4614; DOI: 10.1021/jm00022a026 |
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Prospects for Improved Antidepressants C. L. E. Broekkamp, D. Leysen, B. W. M. M. Peeters, and R. M. Pinder pp 4615 - 4633; DOI: 10.1021/jm00023a001 |
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1-[1-[4-[(N-Acetyl-4-piperidinyl)oxy]-2- methoxybenzoyl]piperidin-4-yl]-4H-3,1- benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist. Peter D. Williams, Bradley V. Clineschmidt, Jill M. Erb, Roger M. Freidinger, Maribeth T. Guidotti, Edward V. Lis, Joseph M. Pawluczyk, Douglas J. Pettibone, Duane R. Reiss, and et al. pp 4634 - 4636; DOI: 10.1021/jm00023a002 |
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A Novel Strategy for Improving Ligand Selectivity in Receptor-Based Drug Design Manuel Pastor and Gabriele Cruciani pp 4637 - 4647; DOI: 10.1021/jm00023a003 |
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Design, Synthesis, and Structure-Activity Relationship of Novel Dinucleotide Analogs as Agents against Herpes and Human Immunodeficiency Viruses Gholam H. Hakimelahi, Ali A. Moosavi-Movahedi, Majid M. Sadeghi, Shwu-Chen Tsay, and Jih Ru Hwu pp 4648 - 4659; DOI: 10.1021/jm00023a004 |
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Differences in Backbone Structure between Angiotensin II Agonists and Type I Antagonists John M. Matsoukas, George Agelis, Amal Wahhab, John Hondrelis, Dimitris Panagiotopoulos, Raghav Yamdagni, Qiao Wu, Thomas Mavromoustakos, Hernani L. S. Maia, and et al. pp 4660 - 4669; DOI: 10.1021/jm00023a005 |
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4-(Heteroarylthio)-2-biphenylyltetrazoles as Nonpeptide Angiotensin II Antagonists Mark H. Norman, H. David Smith, C. Webster Andrews, Flora L. M. Tang, Conrad L. Cowan, and Robert P. Steffen pp 4670 - 4678; DOI: 10.1021/jm00023a006 |
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A New Series of Pyridinone Derivatives as Potent Non-Nucleoside Human Immunodeficiency Virus Type 1 Specific Reverse Transcriptase Inhibitors Valerie Dolle, E. Fan, Chi Hung Nguyen, Anne-Marie Aubertin, Andre Kirn, Marie Line Andreola, Gordon Jamieson, Laura Tarrago-Litvak, and Emile Bisagni pp 4679 - 4686; DOI: 10.1021/jm00023a007 |
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A Novel Class of Cyclic .beta.-Dicarbonyl Leaving Groups and Their Use in the Design of Benzisothiazolone Human Leukocyte Elastase Inhibitors Dennis J. Hlasta, James H. Ackerman, John J. Court, Robert P. Farrell, Judith A. Johnson, James L. Kofron, David T. Robinson, Timothy G. Talomie, Richard P. Dunlap, and Catherine A. Franke pp 4687 - 4692; DOI: 10.1021/jm00023a008 |
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Inhibition of the EGF-Stimulated Cellular Proliferation of ER 22 Cells by Hydroxybiphenyl Derivatives Marie-Emmanuelle Million, Janine Boiziau, Fabienne Parker, Bruno Tocque, Bernard P. Roques, and Christiane Garbay pp 4693 - 4703; DOI: 10.1021/jm00023a009 |
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Evidence for a Carbocation Intermediate during Conversion of Bipinnatin-A and -C into Irreversible Inhibitors of Nicotinic Acetylcholine Receptors Edward G. Hyde, Stacy M. Thornhill, Arthur J. Boyer, and Stewart N. Abramson pp 4704 - 4709; DOI: 10.1021/jm00023a010 |
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Synthesis and Antimicrobial and Toxicological Studies of Amino Acid and Peptide Derivatives of Kanamycin A and Netilmicin S. Kotretsou, M. P. Mingeot-Leclercq, V. Constantinou-Kokotou, R. Brasseur, M. P. Georgiadis, and P. M. Tulkens pp 4710 - 4719; DOI: 10.1021/jm00023a011 |
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Topographical modification of melanotropin peptide analogs with .beta.-methyltryptophan isomers at position 9 leads to differential potencies and prolonged biological activities Carrie Haskell-Luevano, Lakmal W. Boteju, Hiroto Miwa, Chris Dickinson, Ira Gantz, Tadataka Yamada, Mac E. Hadley, and Victor J. Hruby pp 4720 - 4729; DOI: 10.1021/jm00023a012 |
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A Concerted Study Using Binding Measurements, X-ray Structural Data, and Molecular Modeling on the Stereochemical Features Responsible for the Affinity of 6-Arylpyrrolo[2,1-d][1,5]benzothiazepines toward Mitochondrial Benzodiazepine Receptors Alessandro Dalpiaz, Valerio Bertolasi, Pier Andrea Borea, Vito Nacci, Isabella Fiorini, Giuseppe Campiani, Tiziana Mennini, Cristina Manzoni, Ettore Novellino, and Giovanni Greco pp 4730 - 4738; DOI: 10.1021/jm00023a013 |
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New Drug Developments for Opportunistic Infections in Immunosuppressed Patients: Pneumocystis carinii Sherry F. Queener pp 4739 - 4759; DOI: 10.1021/jm00024a001 |
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N-[(1-Butyl-4-piperidinyl)methyl]-3,4- dihydro-2H-[1,3]oxazino[3,2-a]indole- 10-carboxamide hydrochloride: the first potent and selective 5-HT4 receptor antagonist amide with oral activity. Laramie M. Gaster, Graham F. Joiner, Frank D. King, Paul A. Wyman, Jonathan M. Sutton, Sharon Bingham, Elizabeth S. Ellis, Gareth J. Sanger, and Kay A. Wardle pp 4760 - 4763; DOI: 10.1021/jm00024a002 |
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Synthesis and Characterization of a Highly Potent and Effective Antagonist of Retinoic Acid Receptors Alan T. Johnson, Elliott S. Klein, Samuel J. Gillett, Liming Wang, Tae K. Song, Mary E. Pino, and Roshantha A. S. Chandraratna pp 4764 - 4767; DOI: 10.1021/jm00024a003 |
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Preparation of (R)-(+)-N-[3-[5-[(4-Fluorophenyl)methyl]-2-thienyl]-1-methyl-2-propynyl]-N-hydroxyurea (ABT-761), a second-generation 5-lipoxygenase inhibitor. Clint D. W. Brooks, Andrew O. Stewart, Anwer Basha, Pramila Bhatia, James D. Ratajczyk, Jonathan G. Martin, Richard A. Craig, Teodozyj Kolasa, Jennifer B. Bouska, Carmine Lanni, Richard R. Harris, Peter E. Malo, George W. Carter, and Randy L. Bell pp 4768 - 4775; DOI: 10.1021/jm00024a004 |
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(E)-8-Benzylidene Derivatives of 2-Methyl-5-(3-hydroxyphenyl)morphans: Highly Selective Ligands for the .sigma.2 Receptor Subtype Craig M. Bertha, Bertold J. Vilner, Mariena V. Mattson, Wayne D. Bowen, Karen Becketts, Heng Xu, Richard B. Rothman, Judith L. Flippen-Anderson, and Kenner C. Rice pp 4776 - 4785; DOI: 10.1021/jm00024a005 |
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Selective and Potent Monoamine Oxidase Type B Inhibitors: 2-Substituted 5-Aryltetrazoles Derivatives Luc Lebreton, Olivier Curet, Salah Gueddari, Fathi Mazouz, Suzanne Bernard, Claude Burstein, and Rene Milcent pp 4786 - 4792; DOI: 10.1021/jm00024a006 |
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Identification of a Series of 3-(Benzyloxy)-1-azabicyclo[2.2.2]octane Human NK1 Antagonists Christopher J. Swain, Eileen M. Sewart, Margaret A. Cascieri, Tung M. Fong, Richard Herbert, D Euan MacIntyre, Kevin J. Merchant, Simon N. Owen, Andrew P. Owens, and et al. pp 4793 - 4805; DOI: 10.1021/jm00024a007 |
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N-3-Substituted Pyrimidinones as Potent, Orally Active, AT1 Selective Angiotensin II Receptor Antagonists Aldo Salimbeni, Renato Canevotti, Fabio Paleari, Davide Poma, Saturnino Caliari, Francesco Fici, Rocco Cirillo, Anna R. Renzetti, Alessandro Subissi, and et al. pp 4806 - 4820; DOI: 10.1021/jm00024a008 |
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Synthesis and Structure-Activity Relationships of Acetylcholinesterase Inhibitors: 1-Benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine Hydrochloride and Related Compounds Hachiro Sugimoto, Youichi Iimura, Yoshiharu Yamanishi, and Kiyomi Yamatsu pp 4821 - 4829; DOI: 10.1021/jm00024a009 |
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Novel Non-nucleoside Inhibitors of Human Immunodeficiency Virus Type 1 (HIV-1) Reverse Transcriptase. 4. 2-Substituted Dipyridodiazepinones as Potent Inhibitors of Both Wild-Type and Cysteine-181 HIV-1 Reverse Transcriptase Enzymes John R. Proudfoot, Karl D. Hargrave, Suresh R. Kapadia, Usha R. Patel, Karl G. Grozinger, Daniel W. McNeil, Ernest Cullen, Mario Cardozo, Liang Tong, and et al. pp 4830 - 4838; DOI: 10.1021/jm00024a010 |
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Novel Non-nucleoside Inhibitors of Human Immunodeficiency Virus Type 1 Reverse Transcriptase. 5. 4-Substituted and 2,4-Disubstituted Analogs of Nevirapine Terence A. Kelly, John R. Proudfoot, Daniel W. McNeil, Usha R. Patel, Eva David, Karl D. Hargrave, Peter M. Grob, Mario Cardozo, Atul Agarwal, and Julian Adams pp 4839 - 4847; DOI: 10.1021/jm00024a011 |
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Design and Synthesis of Conformationally Constrained Analogs of 4-(3-Butoxy-4-methoxybenzyl)imidazolidin-2-one (Ro 20-1724) as Potent Inhibitors of cAMP-Specific Phosphodiesterase Marcus F. Brackeen, Jeffrey A. Stafford, David J. Cowan, Peter J. Brown, Paul L. Domanico, Paul L. Feldman, Dudley Rose, Alan B. Strickland, James M. Veal, and Margrith Verghese pp 4848 - 4854; DOI: 10.1021/jm00024a012 |
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The Intracellular Receptor and Signal Transducers and Activators of Transcription Factor Superfamilies: Novel Targets for Small-Molecule Drug Discovery Jonathan Rosen, Adrienne Day, Todd K. Jones, E. Tracy Turner Jones, Alex M. Nadzan, and Robert B. Stein pp 4855 - 4874; DOI: 10.1021/jm00025a001 |
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Substituted 2-azaspiro[5.3]nonan-1-ones as potent cholesterol absorption inhibitors: defining a binding conformation for SCH 48461 Sundeep Dugar, John W. Clader, Tze-Ming Chan, and Harry Davis pp 4875 - 4877; DOI: 10.1021/jm00025a002 |
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Nonsteroidal progesterone receptor ligands. 1. 3-Aryl-1-benzoyl-1,4,5,6- tetrahydropyridazines. Donald W. Combs, Kimberly Reese, and Audrey Phillips pp 4878 - 4879; DOI: 10.1021/jm00025a003 |
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Nonsteroidal Progesterone Receptor Ligands. 2. High-Affinity Ligands with Selectivity for Bone Cell Progesterone Receptors Donald W. Combs, Kimberly Reese, Lyndon A. M. Cornelius, Joseph W. Gunnet, Ellen V. Cryan, Kay S. Granger, Jerold J. Jordan, and Keith T. Demarest pp 4880 - 4884; DOI: 10.1021/jm00025a004 |
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(3SR,4aRS,6SR,8aRS)-6-(1H-Tetrazol-5-yl)decahydroisoquinoline-3-carboxylic Acid, a Novel, Competitive, Systemically Active NMDA and AMPA Receptor Antagonist Paul L. Ornstein, M. Brian Arnold, Nancy K. Allen, J. David Leander, Joseph P. Tizzano, David Lodge, and Darryle D. Schoepp pp 4885 - 4890; DOI: 10.1021/jm00025a005 |
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Synthesis of N,N'-Substituted Piperazine and Homopiperazine Derivatives with Polyamine-like Actions at N-Methyl-D-aspartate Receptors Li-Ming Zhou, Xiao-Shu He, Guiying Li, Brian R. de Costa, and Phil Skolnick pp 4891 - 4896; DOI: 10.1021/jm00025a006 |
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Cyclooxygenase-2 Inhibitors. Synthesis and Pharmacological Activities of 5-Methanesulfonamido-1-indanone Derivatives Chun-Sing Li, W. Cameron Black, Chi-Chung Chan, Anthony W. Ford-Hutchinson, Jacques-Yves Gauthier, Robert Gordon, Daniel Guay, Stacia Kargman, Cheuk K. Lau, and et al. pp 4897 - 4905; DOI: 10.1021/jm00025a007 |
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Structure-Activity Relationship of Omeprazole and Analogs as Helicobacter pylori Urease Inhibitors Thomas C. Kuehler, Jan Fryklund, Nils-ke Bergman, Jessica Weilitz, Adrian Lee, and Haakan Larsson pp 4906 - 4916; DOI: 10.1021/jm00025a008 |
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3D-Quantitative Structure-Activity Relationships of Human Immunodeficiency Virus Type-1 Proteinase Inhibitors: Comparative Molecular Field Analysis of 2-Heterosubstituted Statine Derivatives-Implications for the Design of Novel Inhibitors Romano T. Kroemer, Peter Ettmayer, and Peter Hecht pp 4917 - 4928; DOI: 10.1021/jm00025a009 |
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Phenethylthiazolethiourea (PETT) Compounds, a New Class of HIV-1 Reverse Transcriptase Inhibitors. 1. Synthesis and Basic Structure-Activity Relationship Studies of PETT Analogs Frank W. Bell, Amanda S. Cantrell, Marita Hoegberg, S. Richard Jaskunas, Nils Gunnar Johansson, Christopher L. Jordan, Michael D. Kinnick, Peter Lind, John M. Morin Jr., and et al. pp 4929 - 4936; DOI: 10.1021/jm00025a010 |
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Synthesis and Biological Evaluation of Substituted Flavones as Gastroprotective Agents Jeffrey J. Ares, Pamela E. Outt, Jared L. Randall, Peter D. Murray, Pamela S. Weisshaar, Linda M. O'Brien, Beth L. Ems, Sunil V. Kakodkar, Gary R. Kelm, and et al. pp 4937 - 4943; DOI: 10.1021/jm00025a011 |
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The Furoxan System as a Useful Tool for Balancing "Hybrids" with Mixed .alpha.1-Antagonist and NO-like Vasodilator Activities Roberta Fruttero, Donatella Boschi, Antonella Di Stilo, and Alberto Gasco pp 4944 - 4949; DOI: 10.1021/jm00025a012 |
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1-Phenyl-3-(aminomethyl)pyrroles as Potential Antipsychotic Agents. Synthesis and Dopamine Receptor Binding Andrew Thurkauf, Jun Yuan, Nathan Chen, Jan W. F. Wasley, Robin Meade, Kristine Harris Woodruff, Kevin Huston, and Philip C. Ross pp 4950 - 4952; DOI: 10.1021/jm00025a013 |
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Computational Methods to Predict Binding Free Energy in Ligand-Receptor Complexes Ajay and Mark A. Murcko pp 4953 - 4967; DOI: 10.1021/jm00026a001 |
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Structure-Based Design of Sulfonamide-Substituted Non-Peptidic HIV Protease Inhibitors Harvey I. Skulnick, Paul D. Johnson, W. Jeffrey Howe, Paul K. Tomich, Kong-Teck Chong, Keith D. Watenpaugh, Musiri N. Janakiraman, Lester A. Dolak, James P. McGrath, and et al. pp 4968 - 4971; DOI: 10.1021/jm00026a002 |
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Introduction of a conformational switching element on a pyrrolidine ring. Synthesis and evaluation of methyl (R*,R*)-(.+-.)-3-acetyl-4-[3- (cyclopentyloxy)-4-methoxyphenyl]-3- methyl-1-pyrrolidinecarboxylate, a potent and selective inhibitor of cAMP-specific phosphodiesterase. Jeffrey A. Stafford, James M. Veal, Paul L. Feldman, Nicole L. Valvano, Philip G. Baer, Marcus F. Brackeen, E. Sloan Brawley, Kevin M. Connolly, Paul L. Domanico, and et al. pp 4972 - 4975; DOI: 10.1021/jm00026a003 |
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Rational Design and Synthesis of Small Molecule, Non-oligosaccharide Selectin Inhibitors: (.alpha.-D-Mannopyranosyloxy)biphenyl-Substituted Carboxylic Acids Timothy P. Kogan, Brian Dupre, Karin M. Keller, Ian L. Scott, Huong Bui, Robert V. Market, Pamela J. Beck, Jennifer A. Voytus, B. Mitch Revelle, and Delores Scott pp 4976 - 4984; DOI: 10.1021/jm00026a004 |
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Discovery of an Orally Bioavailable NK1 Receptor Antagonist, (2S,3S)-(2-Methoxy-5-tetrazol-1-ylbenzyl)(2-phenylpiperidin-3-yl)amine (GR203040), with Potent Antiemetic Activity Peter Ward, Duncan R. Armour, David E. Bays, Brian Evans, Gerard M. P. Giblin, Nicola Heron, Tania Hubbard, Kai Liang, David Middlemiss, and et al. pp 4985 - 4992; DOI: 10.1021/jm00026a005 |
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Synthesis, Structure-Affinity Relationships, and Biological Activities of Ligands Binding to Retinoic Acid Receptor Subtypes Bruno Charpentier, Jean-Michel Bernardon, Jacques Eustache, Corinne Millois, Bernard Martin, Serge Michel, and Braham Shroot pp 4993 - 5006; DOI: 10.1021/jm00026a006 |
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Identification, Characterization and Pharmacological Profile of Three Metabolites of (R)-(+)-1,2,3,6-Tetrahydro-4-phenyl-1-[(3-phenylcyclohexen-1-yl)methyl]p yridine (CI-1007), a Dopamine Autoreceptor Agonist and Potential Antipsychotic Agent Jon L. Wright, Dennis M. Downing, M. Rose Feng, Roger N. Hayes, Thomas G. Heffner, Robert G. MacKenzie, Leonard T. Meltzer, Thomas A. Pugsley, and Lawrence D. Wise pp 5007 - 5014; DOI: 10.1021/jm00026a007 |
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Chemistry and Antimicrobial Activity of Caryoynencin Analogs Masahiko Yamaguchi, Hyeon-Joo Park, Shinji Ishizuka, Kenji Omata, and Masahiro Hirama pp 5015 - 5022; DOI: 10.1021/jm00026a008 |
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New .alpha.-Thiol Dipeptide Dual Inhibitors of Angiotensin-I-Converting Enzyme and Neutral Endopeptidase EC 3.4.24.11 Cynthia A. Fink, Ying Qiao, Carol J. Berry, Yumi Sakane, Rajendra D. Ghai, and Angelo J. Trapani pp 5023 - 5030; DOI: 10.1021/jm00026a009 |
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In Vitro Antimalarial Activity of Chalcones and Their Derivatives Rongshi Li, Xiaowu Chen, Baoqing Gong, Jose N. Dominguez, Eugene Davidson, Gary Kurzban, Robert E. Miller, Edwin O. Nuzum, Philip J. Rosenthal, and et al. pp 5031 - 5037; DOI: 10.1021/jm00026a010 |
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Structure-Activity Relationships of the Antimalarial Agent Artemisinin. 2. Effect of Heteroatom Substitution at O-11: Synthesis and Bioassay of N-Alkyl-11-aza-9-desmethylartemisinins Mitchell A. Avery, Jason D. Bonk, Wesley K. M. Chong, Sanjiv Mehrotra, Robert Miller, Wilbur Milhous, D. Keith Goins, Sridhar Venkatesan, Christy Wyandt, and et al. pp 5038 - 5044; DOI: 10.1021/jm00026a011 |
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Syntheses and Antimalarial Activities of N-Substituted 11-Azaartemisinins Daniel S. Torok, Herman Ziffer, Steven R. Meshnick, Xing-Qing Pan, and Arba Ager pp 5045 - 5050; DOI: 10.1021/jm00026a012 |
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Optimization of Alkylating Agent Prodrugs Derived from Phenol and Aniline Mustards: A New Clinical Candidate Prodrug (ZD2767) for Antibody-Directed Enzyme Prodrug Therapy Caroline J. Springer, Robert Dowell, Philip J. Burke, Elma Hadley, D. Huw Davies, David C. Blakey, Roger G. Melton, and Ion Niculescu-Duvaz pp 5051 - 5065; DOI: 10.1021/jm00026a013 |
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Novel Inhibitors for Multidrug Resistance: 1,3,5-Triazacycloheptanes Hiroyuki Sawanishi, Shinya Wakusawa, Rieko Murakami, Hiromi Muramatsu, Hirokazu Suzuki, Akemi Takashima, Tatsuo Aizawa, and Ken-ichi Miyamoto pp 5066 - 5070; DOI: 10.1021/jm00026a014 |
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Book Reviews pp 5071 - 5071; DOI: 10.1021/jm00026a600 |