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An analysis of current methodologies for conformational searching of complex molecules Allison E. Howard and Peter A. Kollman pp 1669 - 1675; DOI: 10.1021/jm00117a001 |
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Platinum complexes with binding affinity for the estrogen receptor Norbert Knebel and Erwin Von Angerer pp 1675 - 1679; DOI: 10.1021/jm00117a002 |
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Design of rat renin inhibitory peptides Kwan Y. Hui, Eliezer J. Holtzman, Michael A. Quinones, Norman K. Hollenberg, and Edgar Haber pp 1679 - 1686; DOI: 10.1021/jm00117a003 |
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Cyclopentenylcytosine. A carbocyclic nucleoside with antitumor and antiviral properties Victor E. Marquez, Mu Ill Lim, Susan P. Treanor, Jacqueline Plowman, Matthew A. Priest, Anica Markovac, M. Sami Khan, Bashir Kaskar, and John S. Driscoll pp 1687 - 1694; DOI: 10.1021/jm00117a004 |
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Synthesis and bacterial DNA gyrase inhibitory properties of a spirocyclopropylquinolone derivative Mark P. Wentland, Robert B. Perni, Peter H. Dorff, and James B. Rake pp 1694 - 1697; DOI: 10.1021/jm00117a005 |
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Molecular requirements of the recognition site of cholinergic receptors. 27. Enantioselectivity of muscarinic antagonists. 2,2-Dicyclohexyl-5-[(dimethylamino)methyl]-1,3-oxathiolane methiodides and related 3-oxides M. Novella Romanelli, Elisabetta Teodori, Fulvio Gualtieri, Piero Angeli, and Livio Brasili pp 1698 - 1702; DOI: 10.1021/jm00117a006 |
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Molecular requirements of the recognition site of cholinergic receptors. 28. Enantioselectivity of muscarinic antagonists. Isomeric 2-cyclohexyl-2-phenyl-5-[(dimethylamino)methyl]-1,3-oxathiolane methiodides M. Novella Romanelli, Fulvio Gualtieri, Giovanni Valle, Livio Brasili, and Piero Angeli pp 1703 - 1708; DOI: 10.1021/jm00117a007 |
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Substituted benzamides with conformationally restricted side chains. 2. Indolizidine derivatives as central dopamine receptor antagonists Frank D. King, Michael S. Hadley, and Christine M. McClelland pp 1708 - 1712; DOI: 10.1021/jm00117a008 |
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Etodolac, a novel antiinflammatory agent. The syntheses and biological evaluation of its metabolites Leslie G. Humber, Eckhardt Ferdinandi, Christopher A. Demerson, Syed Ahmed, Uresh Shah, Dominick Mobilio, Joseph Sabatucci, Barbara De Lange, Francesco Labbadia, and et al. pp 1712 - 1719; DOI: 10.1021/jm00117a009 |
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3-[1-(2-Benzoxazolyl)hydrazino]propanenitrile derivatives: inhibitors of immune complex induced inflammation Fortuna Haviv, James D. Ratajczyk, Robert W. DeNet, Francis A. Kerdesky, Roland L. Walters, Steven P. Schmidt, James H. Holms, Patrick R. Young, and George W. Carter pp 1719 - 1728; DOI: 10.1021/jm00117a010 |
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Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 11. Molecular dissections of neplanocin A as potential inhibitors of S-adenosylhomocysteine hydrolase David R. Borcherding, Sunanda Narayanan, Masahide Hasobe, James G. McKee, Bradley T. Keller, and Ronald T. Borchardt pp 1729 - 1738; DOI: 10.1021/jm00117a011 |
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Thienylpyrazoloquinolines: potent agonists and inverse agonists to benzodiazepine receptors Susumu Takada, Hirohisa Shindo, Takashi Sasatani, Nobuo Chomei, Akira Matsushita, Masami Eigyo, Kazuo Kawasaki, Shunji Murata, Yukio Takahara, and Haruyuki Shintaku pp 1738 - 1745; DOI: 10.1021/jm00117a012 |
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6-Substituted 1,3,4,5-tetrahydrobenz[cd]indol-4-amines: potent serotonin agonists Michael E. Flaugh, D. L. Mullen, Ray W. Fuller, and Norman R. Mason pp 1746 - 1753; DOI: 10.1021/jm00117a013 |
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Optimizing of 2,3-diarylindenes as fluorescent estrogens. Variation of the acceptor group, ortho substitution of the 2-ring, and C-1 methylation Gregory M. Anstead and John A. Katzenellenbogen pp 1754 - 1761; DOI: 10.1021/jm00117a014 |
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Synthesis and evaluation of multisubstrate inhibitors of an oncogene-encoded tyrosine-specific protein kinase. 1 Carolyn H. Kruse, Kenneth G. Holden, M. Lynn Pritchard, John A. Feild, David J. Rieman, Russell G. Greig, and George Poste pp 1762 - 1767; DOI: 10.1021/jm00117a015 |
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Synthesis and evaluation of multisubstrate inhibitors of an oncogene-encoded tyrosine-specific protein kinase. 2 Carolyn H. Kruse, Kenneth G. Holden, Priscilla H. Offen, M. Lynn Pritchard, John A. Feild, David J. Rieman, Paul E. Bender, Blair Ferguson, Russell G. Greig, and George Poste pp 1768 - 1772; DOI: 10.1021/jm00117a016 |
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Phosphinic acid inhibitors of D-alanyl-D-alanine ligase William H. Parsons, Arthur A. Patchett, Herbert G. Bull, William R. Schoen, David Taub, Jacqueline Davidson, Patricia L. Combs, James P. Springer, Hans Gadebusch, and et al. pp 1772 - 1778; DOI: 10.1021/jm00117a017 |
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Synthesis of (aryloxy)alkylamines. I. Novel antisecretory agents with H+K+-ATPase inhibitory activity Pauline J. Sanfilippo, Maud Urbanski, Jeffery B. Press, Zoltan G. Hajos, David A. Shriver, and Cynthia K. Scott pp 1778 - 1785; DOI: 10.1021/jm00117a018 |
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Thiophene systems. 9. Thienopyrimidinedione derivatives as potential antihypertensive agents Ronald K. Russell, Jeffery B. Press, Richard A. Rampulla, James J. McNally, Robert Falotico, Joan A. Keiser, David A. Bright, and Alfonso Tobia pp 1786 - 1793; DOI: 10.1021/jm00117a019 |
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Nucleoside conjugates. 10. Synthesis and antitumor activity of 1-.beta.-D-arabinofuranosylcytosine 5'-diphosphate-1,2-dipalmitins Chung Il Hong, Seung Ho An, Louis Schliselfeld, David J. Buchheit, Alexander Nechaev, Alan J. Kirisits, and Charles R. West pp 1793 - 1798; DOI: 10.1021/jm00117a020 |
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Synthesis and antiviral evaluation of 6'-substituted aristeromycins: potential mechanism-based inhibitors of S-adenosylhomocysteine hydrolase G. V. Bindu Madhavan, Danny P. C. McGee, Robert M. Rydzewski, Richard Boehme, John C. Martin, and Ernest J. Prisbe pp 1798 - 1804; DOI: 10.1021/jm00117a021 |
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Synthesis, conformation and immunosuppressive activity of a conformationally restricted cyclosporin lactam analog Johannes D. Aebi, Dominique Guillaume, Brian E. Dunlap, and Daniel H. Rich pp 1805 - 1815; DOI: 10.1021/jm00117a022 |
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Arylformamidines with antinociceptive properties M. Gall, J. M. McCall, R. E. TenBrink, P. F. VonVoigtlander, and J. S. Mohrland pp 1816 - 1820; DOI: 10.1021/jm00117a023 |
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Effect of the CH2NH and CH2NAc peptide bond isosteres on the antagonistic and histamine releasing activities of a luteinizing hormone-releasing hormone analog Simon J. Hocart, Mary V. Nekola, and David H. Coy pp 1820 - 1824; DOI: 10.1021/jm00117a024 |
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Retro-inverso concept applied to the complete inhibitors of enkephalin-degrading enzymes J. F. Hernandez, J. M. Soleilhac, B. P. Roques, and M. C. Fournie-Zaluski pp 1825 - 1831; DOI: 10.1021/jm00117a025 |
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Phosphonoformate and phosphonoacetate derivatives of 5-substituted 2'-deoxyuridines: synthesis and antiviral activity Herfried Griengl, Walter Hayden, Gerhard Penn, Erik De Clercq, and Brigitte Rosenwirth pp 1831 - 1839; DOI: 10.1021/jm00117a026 |
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Synthesis and biological activity of some transition-state inhibitors of human renin Peter Buehlmayer, Anthony Caselli, Walter Fuhrer, Richard Goeschke, Vittorio Rasetti, Heinrich Rueger, James L. Stanton, Leoluca Criscione, and Jeanette M. Wood pp 1839 - 1846; DOI: 10.1021/jm00117a027 |
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Synthesis and in vitro activity of various derivatives of a novel thromboxane receptor antagonist, (.+-.)-(5Z)-7-[3-endo[(phenylsulfonyl)amino]bicyclo[2.2.1]hept-2-exo-yl]heptenoic acid Masayuki Narisada, Mitsuaki Ohtani, Fumihiko Watanabe, Kiyohisa Uchida, Hitoshi Arita, Masami Doteuchi, Koji Hanasaki, Hisato Kakushi, Koichi Otani, and Seijiro Hara pp 1847 - 1854; DOI: 10.1021/jm00117a028 |
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Synthesis of novel 3-substituted .beta.-carbolines as benzodiazepine receptor ligands: probing the benzodiazepine receptor pharmacophore Michael S. Allen, Timothy J. Hagen, Mark L. Trudell, Penelope W. Codding, Phil Skolnick, and James M. Cook pp 1854 - 1861; DOI: 10.1021/jm00117a029 |
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Structure-activity relationships among benextramine-related tetraamine disulfides. Chain length effect on .alpha.-adrenoreceptor blocking activity Wilma Quaglia, Livio Brasili, Gloria Cristalli, Dario Giardina, Maria T. Picchio, and Carlo Melchiorre pp 1861 - 1866; DOI: 10.1021/jm00117a030 |
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Book Reviews pp 1867 - 1868; DOI: 10.1021/jm00117a600 |
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Isoprenoid (phosphinylmethyl)phosphonates as inhibitors of squalene synthetase Scott A. Biller, Cornelia Forster, Eric M. Gordon, Thomas Harrity, William A. Scott, and Carl P. Ciosek pp 1869 - 1871; DOI: 10.1021/jm00118a001 |
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Cardiovascular effects of new water-soluble derivatives of forskolin Y. Khandelwal, K. Rajeshwari, R. Rajagopalan, Lakshmi Swamy, A. N. Dohadwalla, N. J. De Souza, and R. H. Rupp pp 1872 - 1879; DOI: 10.1021/jm00118a002 |
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Ab initio molecular electrostatic potentials of perillartine analogs: implications for sweet-taste receptor recognition Thomas J. Venanzi and Carol A. Venanzi pp 1879 - 1885; DOI: 10.1021/jm00118a003 |
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Synthesis, platelet aggregation inhibitory activity, and in vivo antithrombotic activity of new 1,4-dihydropyridines Carlos E. Sunkel, Miguel Fau de Casa-Juana, Francisco Javier Cillero, Jaime G. Priego, and M. Pilar Ortega pp 1886 - 1890; DOI: 10.1021/jm00118a004 |
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Development of conformationally constrained linear peptides exhibiting a high affinity and pronounced selectivity for .delta. opioid receptors G. Gacel, V. Dauge, P. Breuze, P. Delay-Goyet, and B. P. Roques pp 1891 - 1897; DOI: 10.1021/jm00118a005 |
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Synthesis and biological evaluation of isomeric dinucleoside monophosphates and monomethylphosphonates of 9-.beta.-D-arabinofuranosyladenine and related analogs Frederic Puech, Gilles Gosselin, Jan Balzarini, Erik De Clercq, and Jean Louis Imbach pp 1897 - 1907; DOI: 10.1021/jm00118a006 |
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Synthesis and immunological evaluation of N-terminal, noncrossreactive tachykinin antigens Witold Neugebauer, Peter Elliott, A. Claudio Cuello, and Emanuel Escher pp 1907 - 1910; DOI: 10.1021/jm00118a007 |
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Drug-induced modifications of the immune response. 12. 4,5-Dihydro-4-oxo-2-(substituted amino)-3-furancarboxylic acids and derivatives as novel antiallergic agents Robert A. Mack, Walter I. Zazulak, Lesley A. Radov, Jane E. Baer, Jeffrey D. Stewart, Philip H. Elzer, C. Richard Kinsolving, and Vassil S. Georgiev pp 1910 - 1918; DOI: 10.1021/jm00118a008 |
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Renin inhibitors containing hydrophilic groups. Tetrapeptides with enhanced aqueous solubility and nanomolar potency Mark G. Bock, Robert M. DiPardo, Ben E. Evans, Roger M. Freidinger, Kenneth E. Rittle, Linda S. Payne, Joshua Boger, Willie L. Whitter, Bruce I. LaMont, and et al. pp 1918 - 1923; DOI: 10.1021/jm00118a009 |
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A comprehensive method for determining hydrophobicity constants by reversed-phase high-performance liquid chromatography Douglas J. Minick, John H. Frenz, Mark A. Patrick, and David A. Brent pp 1923 - 1933; DOI: 10.1021/jm00118a010 |
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2-Phenylpyrroles as conformationally restricted benzamide analogs. A new class of potential antipsychotics. 2 Ineke Van Wijngaarden, Chris G. Kruse, Jan A. M. Van der Heyden, and Martin T. M. Tulp pp 1934 - 1940; DOI: 10.1021/jm00118a011 |
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Synthesis and pharmacological characterization of 1-phenyl-, 4-phenyl-, and 1-benzyl-1,2,3,4-tetrahydroisoquinolines as dopamine receptor ligands Paul S. Charifson, Steven D. Wyrick, Andrew J. Hoffman, Rosa M. Ademe Simmons, J. Phillip Bowen, Darryl L. McDougald, and Richard B. Mailman pp 1941 - 1946; DOI: 10.1021/jm00118a012 |
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Synthesis, receptor binding, and tissue distribution of (17.alpha.,20E)- and (17.alpha.,20Z)-21-[125I]Iodo-19-norpregna-1,3,5-(10),20-tetraene-3,17-diol H. Ali, J. Rousseau, M. A. Ghaffari, and J. E. Van Lier pp 1946 - 1950; DOI: 10.1021/jm00118a013 |
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A new series of ellipticine derivatives (1-(alkylamino)-9-methoxyellipticine). Synthesis, DNA binding, and biological properties Lionel Larue, Christian Rivalle, Gabriel Muzard, Claude Paoletti, Emile Bisagni, and Jacques Paoletti pp 1951 - 1956; DOI: 10.1021/jm00118a014 |
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Synthesis and antineoplastic evaluations of 1,4-bis(aminoalkanamido)-9,10-anthracenediones Sante Martelli, Maria Dzieduszycka, Barbara Stefanska, Maria Bontemps-Gracz, and Edward Borowski pp 1956 - 1959; DOI: 10.1021/jm00118a015 |
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Structure-activity analysis of a class of orally active hydroxamic acid inhibitors of leukotriene biosynthesis James B. Summers, Bruce P. Gunn, Jonathan G. Martin, Michael B. Martin, Hormoz Mazdiyasni, Andrew O. Stewart, Patrick R. Young, Jennifer B. Bouska, Andrew M. Goetze, and et al. pp 1960 - 1964; DOI: 10.1021/jm00118a016 |
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Serotonergic properties of spiroxatrine enantiomers Sham S. Nikam, Arnold R. Martin, and David L. Nelson pp 1965 - 1968; DOI: 10.1021/jm00118a017 |
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Arylpiperazine derivatives as high-affinity 5-HT1A serotonin ligands Richard A. Glennon, Noreen A. Naiman, Robert A. Lyon, and Milt Titeler pp 1968 - 1971; DOI: 10.1021/jm00118a018 |
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Syntheses and adrenergic activities of ring-fluorinated epinephrines Adeboye Adejare, Fabian Gusovsky, William Padgett, Cyrus R. Creveling, John W. Daly, and Kenneth L. Kirk pp 1972 - 1977; DOI: 10.1021/jm00118a019 |
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Bis(4-hydroxyphenyl)[2-(phenoxysulfonyl)phenyl]methane: isolation and structure elucidation of a novel estrogen from commercial preparations of phenol red (phenolsulfonphthalein) Rajeshwar D. Bindal and John A. Katzenellenbogen pp 1978 - 1983; DOI: 10.1021/jm00118a020 |
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Stereochemical aspects of phenylethanolamine analogs as substrates of phenylethanolamine N-methyltransferase Gary L. Grunewald and Qizhuang Ye pp 1984 - 1986; DOI: 10.1021/jm00118a021 |
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Oral absorption of cephalosporin antibiotics. 1. Synthesis, biological properties and oral bioavailability of 7-arylacetamido-3-chloro cephalosporins in animals Stjepan Kukolja, Walter E. Wright, John F. Quay, Janice Pfeil-Doyle, Susan E. Draheim, Judith Ann Eudaly, Roderick J. Johnson, John L. Ott, Fred T. Counter, and et al. pp 1987 - 1993; DOI: 10.1021/jm00118a022 |
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Oral absorption of cephalosproin antibiotics 2. Expanded structure-activity relationships of 7-arylacetamido-3-substituted cephalosporins Janice Pfeil-Doyle, Susan E. Draheim, Stjepan Kukolja, John L. Ott, and Fred T. Counter pp 1993 - 1997; DOI: 10.1021/jm00118a023 |
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Oral absorption of cephalosporin antibiotics. 3. Synthesis and biological properties of 7.alpha.-methoxy-7.beta.-arylacetamido-3-chloro-3-cephem-4-carboxylic acids Janice Pfeil-Doyle and Stjepan Kukolja pp 1997 - 2000; DOI: 10.1021/jm00118a024 |
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9-Benzyl-6-(dimethylamino)-9H-purines with antirhinovirus activity James L. Kelley, James A. Linn, Mark P. Krochmal, and J. W. T. Selway pp 2001 - 2004; DOI: 10.1021/jm00118a025 |
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New "ofloxacin" type antibacterial agents. Incorporation of the spiro cyclopropyl group at N-1 John S. Kiely, Mel C. Schroeder, and Josephine C. Sesnie pp 2004 - 2008; DOI: 10.1021/jm00118a026 |
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Studies on antifungal agents. 23. Novel substituted 3,5-diphenyl-3-(1H-imidazol-1-ylmethyl)-2-alkylisoxazolidine derivatives George B. Mullen, Thomas R. DeCory, Jeffrey T. Mitchell, Stanley D. Allen, C. Richard Kinsolving, and Vassil S. Georgiev pp 2008 - 2014; DOI: 10.1021/jm00118a027 |
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Effects of addition of a 2-methyl group to ethyl nipecotates (.beta.-meperidines) on receptor affinities and opiate agonist/antagonist activities John A. Lawson, Alice Cheng, Joseph DeGraw, Gernot Frenking, Edward Uyeno, Lawrence Toll, and Gilda H. Loew pp 2015 - 2021; DOI: 10.1021/jm00118a028 |
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Synthesis of fluorescent muramyl dipeptide congeners. 2 C. K. Hiebert, W. C. Kopp, H. B. Richerson, and C. F. Barfknecht pp 2022 - 2024; DOI: 10.1021/jm00118a029 |
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In vitro dental plaque inhibitory properties of a series of N-[1-alkyl-4(1H)-pyridinylidene]alkylamines Mark P. Wentland, Denis M. Bailey, Ronald G. Powles, Andrew M. Slee, and David M. Sedlock pp 2024 - 2027; DOI: 10.1021/jm00118a030 |
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(S)-N-[(1-Ethyl-2-pyrrolidinyl)methyl]-5-[125I]iodo-2-methoxybenzamide hydrochloride, a new selective radioligand for dopamine D-2 receptors Tomas De Paulis, Aaron Janowsky, Robert M. Kessler, Jeffrey A. Clanton, and Howard E. Smith pp 2027 - 2033; DOI: 10.1021/jm00118a031 |
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Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists Norton P. Peet, George A. Dickerson, Abdulminium H. Abdallah, John W. Daly, and Dieter Ukena pp 2034 - 2039; DOI: 10.1021/jm00118a032 |
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Synthesis and anti-HIV activity of different sugar-modified pyrimidine and purine nucleosides Piet Herdewijn, Jan Balzarini, Masanori Baba, Rudi Pauwels, Arthur Van Aerschot, Gerard Janssen, and Erik De Clercq pp 2040 - 2048; DOI: 10.1021/jm00118a033 |
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2(1H)-Quinolinones with cardiac stimulant activity. 1. Synthesis and biological activities of (six-membered heteroaryl)-substituted derivatives Colin T. Alabaster, Andrew S. Bell, Simon F. Campbell, Peter Ellis, Christopher G. Henderson, David A. Roberts, Keith S. Ruddock, Gillian M. R. Samuels, and Mark H. Stefaniak pp 2048 - 2056; DOI: 10.1021/jm00118a034 |
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Binaltorphimine-related bivalent ligands and their .kappa. opioid receptor antagonist selectivity [Erratum to document cited in CA108(17):150771q] P. S. Portoghese, H. Nagase, A. W. Lipkowski, D. L. Larson, and A. E. Takemori pp 2056 - 2056; DOI: 10.1021/jm00118a035 |
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Excitatory amino acid neurotransmission Rodney L. Johnson and James F. Koerner pp 2057 - 2066; DOI: 10.1021/jm00119a001 |
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N-Sulfonyl imidates as a novel prodrug form for an ester function or a sulfonamide group Hans Bundgaard and Joern Drustrup Larsen pp 2066 - 2069; DOI: 10.1021/jm00119a002 |
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A photoaffinity label for the D-1 dopamine receptor, (RS)-7-[125I]iodo-8-hydroxy-3-methyl-1-(4'-azidophenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine, selectively identifies the ligand binding subunits of the receptor Nandkishore Baindur, John L. Neumeyer, Hyman B. Niznik, Natalie H. Bzowej, Kieth R. Jarvie, Phillip Seeman, Russell K. Garlick, and Joseph J. Miller pp 2069 - 2071; DOI: 10.1021/jm00119a003 |
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Modeling of .beta.-adrenoceptors based on molecular electrostatic potential studies of agonists and antagonists Nabil El Tayar, Pierre Alain Carrupt, Han Van de Waterbeemd, and Bernard Testa pp 2072 - 2081; DOI: 10.1021/jm00119a004 |
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Radioiodinated benzodiazepines: agents for mapping glial tumors Marcian E. Van Dort, Brian J. Ciliax, David L. Gildersleeve, Philip S. Sherman, Karen C. Rosenspire, Anne B. Young, Larry Junck, and Donald M. Wieland pp 2081 - 2086; DOI: 10.1021/jm00119a005 |
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Synthesis and antiviral activity of certain 4- and 4,5-disubstituted 7-[(2-hydroxyethoxy)methyl]pyrrolo[2,3-d]pyrimidines Jeffrey S. Pudlo, Naveen K. Saxena, M. Reza Nassiri, Steven R. Turk, John C. Drach, and Leroy B. Townsend pp 2086 - 2092; DOI: 10.1021/jm00119a006 |
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N-Acylphenylalanines and related compounds. A new class of oral hypoglycemic agents Hisashi Shinkai, Koji Toi, Izumi Kumashiro, Yoshiko Seto, Mariko Fukuma, Katsuaki Dan, and Shigeshi Toyoshima pp 2092 - 2097; DOI: 10.1021/jm00119a007 |
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Vinylogous carbinolamine tumor inhibitors. 23. Synthesis and antileukemic activity of bis[[(carbamoyl)oxy]methyl]-substituted pyrrolo[2,1-a]isoquinolines, pyrrolo[1,2-a]quinolines, pyrrolo[2,1-a]isobenzazepines, and pyrrolo[1,2-a]benzazepines Wayne K. Anderson, Arvela R. Heider, Natarajan Raju, and Jeffery A. Yucht pp 2097 - 2102; DOI: 10.1021/jm00119a008 |
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1,4-Dihydropyridine antagonist activities at the calcium channel: a quantitative structure-activity relationship approach Robert A. Coburn, Mark Wierzba, Mark J. Suto, Alan J. Solo, A. M. Triggle, and David J. Triggle pp 2103 - 2107; DOI: 10.1021/jm00119a009 |
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Antiallergy agents. 1. Substituted 1,8-naphthyridin-2(1H)-ones as inhibitors of SRS-A release Margaret H. Sherlock, James J. Kaminski, Wing C. Tom, Joe F. Lee, Shing Chun Wong, William Kreutner, Robert W. Bryant, and Andrew T. McPhail pp 2108 - 2121; DOI: 10.1021/jm00119a010 |
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Synthesis and .beta.-adrenergic antagonism of 2-(aryloxy)-1-(2-piperidyl)ethanols David Mauleon, Maria Dolors Pujol, and Gloria Rosell pp 2122 - 2126; DOI: 10.1021/jm00119a011 |
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A pyrimidine-based "flexible" bisubstrate analog inhibitor of human thymidylate synthase In Young Yang, R. Mark Slusher, Arthur D. Broom, T. Ueda, and Yung Chi Cheng pp 2126 - 2132; DOI: 10.1021/jm00119a012 |
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Topical nonsteroidal antipsoriatic agents. 2. 2,3-(Alkylidenedioxy)naphthalene analogs of lonapalene Michael C. Venuti, Brad E. Loe, Gordon H. Jones, and John M. Young pp 2132 - 2136; DOI: 10.1021/jm00119a013 |
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Inhibitors of cyclic AMP phosphodiesterase. 3. Synthesis and biological evaluation of pyrido and imidazolyl analogs of 1,2,3,5-tetrahydro-2-oxoimidazo[2,1-b]quinazoline Michael C. Venuti, Robert A. Stephenson, Robert Alvarez, John J. Bruno, and Arthur M. Strosberg pp 2136 - 2145; DOI: 10.1021/jm00119a014 |
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Inhibitors of cyclic AMP phosphodiesterase. 4. Synthesis and evaluation of potential prodrugs of lixazinone (N-cyclohexyl-N-methyl-4-[(1,2,3,5-tetrahydro-2-oxoimidazo[2,1-b]quinazolin-7-yl)oxy]butyramide, RS-82856) Michael C. Venuti, Robert Alvarez, John J. Bruno, Arthur M. Strosberg, Leo Gu, Hi Shi Chiang, Ian J. Massey, Nancy Chu, and John H. Fried pp 2145 - 2152; DOI: 10.1021/jm00119a015 |
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Synthesis and cognition-activating properties of some mono- and bicyclic lactam derivatives Cosimo Altomare, Angelo Carotti, Giovanni Casini, Saverio Cellamare, Marcello Ferappi, Enrico Gavuzzo, Fernando Mazza, Giancarlo Pantaleoni, and Raffaele Giorgi pp 2153 - 2158; DOI: 10.1021/jm00119a016 |
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Synthesis and structure-activity relationships of a new series of antiarrhythmic agents: monobasic derivatives of disobutamide Bipin N. Desai, Kerry W. Fowler, Robert J. Chorvat, Leo G. Frederick, Frida R. Hatley, Kurt J. Rorig, and Susan M. Garthwaite pp 2158 - 2164; DOI: 10.1021/jm00119a017 |
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Synthesis and antifolate activity of 5-methyl-5,10-dideaza analogs of aminopterin and folic acid and an alternative synthesis of 5,10-dideazatetrahydrofolic acid, a potent inhibitor of glycinamide ribonucleotide formyltransferase J. R. Piper, G. S. McCaleb, J. A. Montgomery, R. L. Kisliuk, Y. Gaumont, J. Thorndike, and F. M. Sirotnak pp 2164 - 2169; DOI: 10.1021/jm00119a018 |
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Design and synthesis of somatostatin analogs with topographical properties that lead to highly potent and specific .mu. opioid receptor antagonists with greatly reduced binding at somatostatin receptors Wieslaw Kazmierski, William S. Wire, George K. Lui, Richard J. Knapp, Jennifer E. Shook, Thomas F. Burks, Henry I. Yamamura, and Victor J. Hruby pp 2170 - 2177; DOI: 10.1021/jm00119a019 |
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Synthesis and pharmacology of trans-4-n-propyl-3,4,4a,10b-tetrahydro-2H,5H-1-benzopyrano[4,3-b]1,4-oxazin-7- and -9-ols. The significance of nitrogen pka values for central dopamine receptor activation Durk Dijkstra, Theo B. A. Mulder, Hans Rollema, Pieter G. Tepper, Jan Van der Weide, and Alan S. Horn pp 2178 - 2182; DOI: 10.1021/jm00119a020 |
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Retinobenzoic acids. 1. Structure-activity relationships of aromatic amides with retinoidal activity Hiroyuki Kagechika, Emiko Kawachi, Yuichi Hashimoto, Koichi Shudo, and Toshiyuki Himi pp 2182 - 2192; DOI: 10.1021/jm00119a021 |
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Synthesis of sulfur-containing analogs of bestatin. Inhibition of aminopeptidases by .alpha.-thiolbestatin analogs Timothy D. Ocain and Daniel H. Rich pp 2193 - 2199; DOI: 10.1021/jm00119a022 |
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Design of novel inhibitors of aminopeptidases. Synthesis of peptide-derived diamino thiols and sulfur replacement analogs of bestatin E. M. Gordon, J. D. Godfrey, N. G. Delaney, M. M. Asaad, D. Von Langen, and D. W. Cushman pp 2199 - 2211; DOI: 10.1021/jm00119a023 |
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Structure-activity relationships among analogues of pemedolac, cis-1-ethyl-1,3,4,9-tetrahydro-4-(phenylmethyl)pyrano[3,4-b]indole-1-acetic acid, a potent analgesic agent Dominick Mobilio, Leslie G. Humber, Alan H. Katz, Christopher A. Demerson, Philip Hughes, Robert Brigance, Kimberly Conway, Uresh Shah, Gail Williams, and et al. pp 2211 - 2217; DOI: 10.1021/jm00119a024 |
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Anticonvulsant activities of phenyl-substituted bicyclic 2,4-oxazolidinediones and monocyclic models. Comparison with binding to the neuronal voltage-dependent sodium channel Wayne J. Brouillette, George B. Brown, Timothy M. DeLorey, Shyam S. Shirali, and Gary L. Grunewald pp 2218 - 2221; DOI: 10.1021/jm00119a025 |
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Synthesis of (aryloxy)alkylamines. 2. Novel imidazo-fused heterocycles with calcium channel blocking and local anesthetic activity Pauline J. Sanfilippo, Maud Urbanski, Jeffery B. Press, Barry Dubinsky, and John B. Moore pp 2221 - 2227; DOI: 10.1021/jm00119a026 |
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Methotrexate analogs. 34. Replacement of the glutamate moiety in methotrexate and aminopterin by long-chain 2-aminoalkanedioic acids [Erratum to document cited in CA109(3):23348c] Andre Rosowsky, Henry Bader, William Kohler, James H. Freisheim, and Richard G. Moran pp 2227 - 2227; DOI: 10.1021/jm00119a027 |
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Synthesis and biological characterization of pyridohomotropanes. Structure-activity relationships of conformationally restricted nicotinoids [Erratum to document cited in CA108(11):94432r] David B. Kanne and Leo G. Abood pp 2227 - 2227; DOI: 10.1021/jm00119a028 |
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Book Reviews pp 2228 - 2228; DOI: 10.1021/jm00119a600 |
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Guidelines for publications in molecular modeling related to medicinal chemistry Peter Gund, David C. Barry, Jeffrey M. Blaney, and N. Claude Cohen pp 2230 - 2234; DOI: 10.1021/jm00120a001 |
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Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists B. E. Evans, K. E. Rittle, M. G. Bock, R. M. DiPardo, R. M. Freidinger, W. L. Whitter, G. F. Lundell, D. F. Veber, P. S. Anderson, and et al. pp 2235 - 2246; DOI: 10.1021/jm00120a002 |
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Antihypertensive activity in a series of 1-piperazino-3-phenylindans with potent 5-HT2-antagonistic activity Klaus P. Boegesoe, Joern Arnt, Vita Boeck, A. Vibeke Christensen, John Hyttel, and Klaus Gundertofte Jensen pp 2247 - 2256; DOI: 10.1021/jm00120a003 |
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Synthesis, absolute configuration, and molecular modeling study of etoxadrol, a potent phencyclidine-like agonist Andrew Thurkauf, Paul C. Zenk, Robert L. Balster, Everette L. May, Clifford George, F. Ivy Carroll, S. Wayne Mascarella, Kenner C. Rice, Arthur E. Jacobson, and Mariena V. Mattson pp 2257 - 2263; DOI: 10.1021/jm00120a004 |
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Renin inhibitors. Dipeptide analogs of angiotensinogen utilizing a dihydroxyethylene transition-state mimic at the scissile bond to impart greater inhibitory potency Jay R. Luly, Nwe BaMaung, Jeff Soderquist, Anthony K. L. Fung, Herman Stein, Hollis D. Kleinert, Patrick A. Marcotte, David A. Egan, Barbara Bopp, and et al. pp 2264 - 2276; DOI: 10.1021/jm00120a005 |
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Renin inhibitors. Dipeptide analogs of angiotensinogen utilizing a structurally modified phenylalanine residue to impart proteolytic stability Jacob J. Plattner, Patrick A. Marcotte, Hollis D. Kleinert, Herman H. Stein, Jonathan Greer, Giorgio Bolis, Anthony K. L. Fung, Barbara A. Bopp, Jay R. Luly, and et al. pp 2277 - 2288; DOI: 10.1021/jm00120a006 |
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Synthesis and pharmacological properties of soft drug derivatives related to perhexiline Gilbert Marciniak, Dominique Decolin, Gerard Leclerc, Nicole Decker, and Jean Schwartz pp 2289 - 2296; DOI: 10.1021/jm00120a007 |
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Synthesis and anticholinesterase activity of (-)-N1-norphysostigmine, (-)-eseramine, and other N1-substituted analogs of (-)-physostigmine Qian Sheng Yu, John R. Atack, Stanley I. Rapoport, and Arnold Brossi pp 2297 - 2300; DOI: 10.1021/jm00120a008 |
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Structure-activity relationships in 1,4-benzodioxan-related compounds. Investigation on the role of the dehydrodioxane ring on .alpha.1-adrenoreceptor blocking activity Maria Pigini, Livio Brasili, Mario Giannella, Dario Giardina, Ugo Gulini, Wilma Quaglia, and Carlo Melchiorre pp 2300 - 2304; DOI: 10.1021/jm00120a009 |
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Synthesis and antiherpetic activity of (.+-.)-9-[[(Z)-2-(hydroxymethyl)cyclopropyl]methyl]guanine and related compounds Wallace T. Ashton, Laura Canning Meurer, Christine L. Cantone, A. Kirk Field, John Hannah, John D. Karkas, Richard Liou, Gool F. Patel, Helen C. Perry, and et al. pp 2304 - 2315; DOI: 10.1021/jm00120a010 |
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A quantitative structure-activity relationship analysis of some 4-aminodiphenyl sulfone antibacterial agents using linear free energy and molecular modeling methods [Erratum to document cited in CA106(19):152886p] Rosa L. Lopez de Compadre, R. A. Pearlstein, A. J. Hopfinger, and J. K. Seydel pp 2315 - 2316; DOI: 10.1021/jm00120a011 |
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Molecular Modeling in Drug Design John G. Topliss pp 2229 - 2229; DOI: 10.1021/jm00120a600 |
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Errata - Binding Orientation of Amphetamine and Norfenfluramine Analogues in the Benzonorbornene and Benzobicyclo[3.2.1]octane Ring Systems at the Active Site of Phenylethanolamine N-Methyltransferase (PNMT) Gary L. Grunewald, Kimberly M. Markovich, and Daniel J. Sall pp 2316 - 2316; DOI: 10.1021/jm00120a601 |
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Book Reviews pp 2316 - 2318; DOI: 10.1021/jm00120a602 |
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Synthesis, binding studies, and structure activity relationships of 1-aryl- and 2-aryl[1]benzopyranopyrazol-4-ones, central benzodiazepine receptor ligands Vittoria Colotta, Lucia Cecchi, Guido Filacchioni, Fabrizio Melani, Giovanna Palazzino, Claudia Martini, Gino Giannaccini, and Antonio Lucacchini pp 1 - 3; DOI: 10.1021/jm00396a001 |
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Orally active hydroxamic acid inhibitors of leukotriene biosynthesis James B. Summers, Bruce P. Gunn, Jonathan G. Martin, Hormoz Mazdiyasni, Andrew O. Stewart, Patrick R. Young, Andrew M. Goetze, Jennifer B. Bouska, Richard D. Dyer, and et al. pp 3 - 5; DOI: 10.1021/jm00396a002 |
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Iodine-125 labeled 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane: an iodinated radioligand that specifically labels the agonist high-affinity state of 5-HT2 serotonin receptors Richard A. Glennon, Mark R. Seggel, William H. Soine, Katherine Herrick-Davis, Robert A. Lyon, and Milt Titeler pp 5 - 7; DOI: 10.1021/jm00396a003 |
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Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 4. Amidines Christopher B. Chapleo, Peter L. Myers, Alan C. B. Smith, Michael R. Stillings, Ian F. Tulloch, and Donald S. Walter pp 7 - 11; DOI: 10.1021/jm00396a004 |
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Specific sequestering agents for the actinides. 16. Synthesis and initial biological testing of polydentate oxohydroxypyridinecarboxylate ligands David L. White, Patricia W. Durbin, Nylan Jeung, and Kenneth N. Raymond pp 11 - 18; DOI: 10.1021/jm00396a005 |
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Design, structure-activity, and molecular modeling studies of potent renin inhibitory peptides having N-terminal Nin-For-Trp (Ftr): angiotensinogen congeners modified by P1-P1' Phe-Phe, Sta, Leu.psi.[CH(OH)CH2]Val or Leu.psi.[CH2NH]Val substitutions Tomi K. Sawyer, Donald T. Pals, Boryeu Mao, Douglas J. Staples, Anne E. DeVaux, Linda L. Maggiora, Joseph A. Affholter, Warren Kati, David Duchamp, and et al. pp 18 - 30; DOI: 10.1021/jm00396a006 |
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Synthesis and biological properties of .alpha.-mono and .alpha.-difluoromethyl derivatives of tryptophan and 5-hydroxytryptophan D. Schirlin, F. Gerhart, J. M. Hornsperger, M. Hamon, J. Wagner, and M. J. Jung pp 30 - 36; DOI: 10.1021/jm00396a007 |
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Thyroid hormone analogs. Synthesis of 3'-substituted 3,5-diiodo-L-thyronines and quantitative structure-activity studies of in vitro and in vivo thyromimetic activities in rat liver and heart Paul D. Leeson, David Ellis, John C. Emmett, Virendra P. Shah, Graham A. Showell, and Anthony H. Underwood pp 37 - 54; DOI: 10.1021/jm00396a008 |
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Chemical aspects of metoprolol metabolism. Asymmetric synthesis and absolute configuration of the 3-[4-(1-hydroxy-2-methoxyethyl)phenoxy]-1-(isopropylamino)-2-propanols, the diastereomeric benzylic hydroxylation metabolites H. Umesha Shetty and Wendel L. Nelson pp 55 - 59; DOI: 10.1021/jm00396a009 |
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Conformational preference for the binding of biaryl substrates and inhibitors to the active site of phenylethanolamine N-methyltransferase (PNMT) Gary L. Grunewald, Anne E. Carter, Daniel J. Sall, and James A. Monn pp 60 - 65; DOI: 10.1021/jm00396a010 |
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Potent, long-acting luteinizing hormone releasing hormone antagonists containing new synthetic amino acids: N,N'-dialkyl-D-homoarginines John J. Nestor, Ram Tahilramani, Teresa L. Ho, Georgia I. McRae, and Brian H. Vickery pp 65 - 72; DOI: 10.1021/jm00396a011 |
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Ring-substituted [1,2-bis(4-hydroxyphenyl)ethylenediamine]dichloroplatinum(II) complexes: compounds with a selective effect on the hormone-dependent mammary carcinoma Johann Karl, Ronald Gust, Thilo Spruss, Martin R. Schneider, Helmut Schoenenberger, Juergen Engel, Karl Heinz Wrobel, Franz Lux, and Susanne Trebert Haeberlin pp 72 - 83; DOI: 10.1021/jm00396a012 |
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New potent antagonists of leukotrienes C4 and D4. 1. Synthesis and structure-activity relationships Hisao Nakai, Mitoshi Konno, Shunji Kosuge, Shigeru Sakuyama, Masaaki Toda, Yoshinobu Arai, Takaaki Obata, Nobuo Katsube, Tsumoru Miyamoto, and et al. pp 84 - 91; DOI: 10.1021/jm00396a013 |
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N,N-Dialkylated monophenolic trans-2-phenylcyclopropylamines: novel central 5-hydroxytryptamine-receptor agonists Lars Erik Arvidsson, Anette M. Johansson, Uli Hacksell, J. Lars G. Nilsson, Kjell Svensson, Stephan Hjorth, Tor Magnusson, Arvid Carlsson, Per Lindberg, and et al. pp 92 - 99; DOI: 10.1021/jm00396a014 |
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Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for .beta.-adrenergic blocking agents Nicholas Bodor, Alaaeldin ElKoussi, Masanobu Kano, and Toshio Nakamura pp 100 - 106; DOI: 10.1021/jm00396a015 |
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A novel class of potential central nervous system agents. 3-Phenyl-2-(1-piperazinyl)-5H-1-benzazepines Katsuhiko Hino, Yasutaka Nagai, Hitoshi Uno, Yoshinobu Masuda, Makoto Oka, and Tadahiko Karasawa pp 107 - 117; DOI: 10.1021/jm00396a016 |
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Evaluation of the side arm of (naphthylvinyl)pyridinium inhibitors of choline acetyltransferase J. F. DeBernardis, P. Gifford, M. Rizk, R. Ertel, D. J. Abraham, and J. F. Siuda pp 117 - 121; DOI: 10.1021/jm00396a017 |
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2,4-Diamino-5-benzylpyrimidines and analogs as antibacterial agents. 9. Lipophilic trimethoprim analogs as antigonococcal agents B. Roth, D. P. Baccanari, C. W. Sigel, J. P. Hubbell, J. Eaddy, J. C. Kao, M. E. Grace, and B. S. Rauckman pp 122 - 129; DOI: 10.1021/jm00396a018 |
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Evaluation of the importance of hydrophobic interactions in drug binding to dihydrofolate reductase Kazunari Taira and Stephen J. Benkovic pp 129 - 137; DOI: 10.1021/jm00396a019 |
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Potential antisecretory antidiarrheals. 1. .alpha.2-Adrenergic aromatic aminoguanidine hydrazones Barnett S. Pitzele, Alan E. Moormann, Gary W. Gullikson, David Albin, Robert G. Bianchi, Prima Palicharla, Elizabeth L. Sanguinetti, and D. Eric Walters pp 138 - 144; DOI: 10.1021/jm00396a020 |
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Effect of acyclic pyrimidines related to 9-[(1,3-dihydroxy-2-propoxy)methyl]guanine on herpes viruses Lilia M. Beauchamp, Barbara L. Serling, John E. Kelsey, Karen K. Biron, Peter Collins, John Selway, Jung-Chung Lin, and Howard J. Schaeffer pp 144 - 149; DOI: 10.1021/jm00396a021 |
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Synthesis and biological evaluation of 8-deazahomofolic acid and its tetrahydro derivative J. I. DeGraw, W. T. Colwell, V. H. Brown, M. Sato, R. L. Kisliuk, Y. Gaumont, J. Thorndike, and F. M. Sirotnak pp 150 - 153; DOI: 10.1021/jm00396a022 |
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Biologically active dihydrodiol metabolites of polycyclic aromatic hydrocarbons structurally related to the potent carcinogenic hydrocarbon 7,12-dimethylbenz[a]anthracene Ronald G. Harvey, Cecilia Cortez, Taketoshi Sugiyama, Yoshiaki Ito, Thomas W. Sawyer, and John DiGiovanni pp 154 - 159; DOI: 10.1021/jm00396a023 |
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Tertiary 3- and 4-haloalkylamine analogs of oxotremorine as prodrugs of potent muscarinic agonists Bjorn Ringdahl, Margareth Roch, and Donald J. Jenden pp 160 - 164; DOI: 10.1021/jm00396a024 |
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Dimethylsulfonium and thiolanium analogs of the muscarinic agent oxotremorine Bjorn Ringdahl pp 164 - 168; DOI: 10.1021/jm00396a025 |
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Conformational requirements of substrates for activity with phenylethanolamine N-methyltransferase Gary L. Grunewald, Qizhuang Ye, Lynda Kieffer, and James A. Monn pp 169 - 171; DOI: 10.1021/jm00396a026 |
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Leukotriene receptor antagonists. 4. Synthesis and leukotriene D4/E4 receptor antagonist activity of 4-(alkyl)acetophenone derivatives D. Mark Gapinski, Carlos R. Roman, Lynn E. Rinkema, and Jerome H. Fleisch pp 172 - 175; DOI: 10.1021/jm00396a027 |
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Cholecystokinin antagonists. Synthesis and biological evaluation of 4-substituted 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepines Mark G. Bock, Robert M. DiPardo, Ben E. Evans, Kenneth E. Rittle, Daniel F. Veber, Roger M. Freidinger, Raymond S. L. Chang, and Victor J. Lotti pp 176 - 181; DOI: 10.1021/jm00396a028 |
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Synthesis and biological evaluation of poly-.gamma.-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin M. G. Nair, N. T. Nanavati, P. Kumar, Y. Gaumont, and R. L. Kisliuk pp 181 - 185; DOI: 10.1021/jm00396a029 |
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Molecular structure of fluoxetine hydrochloride, a highly selective serotonin-uptake inhibitor David W. Robertson, Noel D. Jones, John K. Swartzendruber, Kuo S. Yang, and David T. Wong pp 185 - 189; DOI: 10.1021/jm00396a030 |
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N-(Retinoyl) amino acids. Synthesis and chemopreventive activity in vitro Y. Fulmer Shealy, Jerry L. Frye, and Leonard J. Schiff pp 190 - 196; DOI: 10.1021/jm00396a031 |
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Triazolines. 14. 1,2,3-Triazolines and triazoles. A new class of anticonvulsants. Drug design and structure-activity relationships Pankaja K. Kadaba pp 196 - 203; DOI: 10.1021/jm00396a032 |
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(Phosphinyloxy)acyl amino acid inhibitors of angiotensin converting enzyme (ACE). 1. Discovery of (S)-1-[6-amino-2-[[hydroxy(4-phenylbutyl)phosphinyl]oxy]-1-oxohexyl]-L-proline, a novel orally active inhibitor of ACE Donald S. Karanewsky, Michael C. Badia, David W. Cushman, Jack M. DeForrest, Tamara Dejneka, Melanie J. Loots, Maria G. Perri, Edward W. Petrillo, and James R. Powell pp 204 - 212; DOI: 10.1021/jm00396a033 |
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Structural factors of importance for 5-hydroxytryptaminergic activity. Conformational preferences and electrostatic potentials of 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) and some related agents Lars-Erik Arvidsson, Anders Karlen, Ulf Norinder, Lennart Kenne, Staffan Sundell, and Uli Hacksell pp 212 - 221; DOI: 10.1021/jm00396a034 |
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Studies on prodrugs. 7. Synthesis and antimicrobial activity of 3-formylquinolone derivatives Hirosato Kondo, Fumio Sakamoto, Kiyotaka Kawakami, and Goro Tsukamoto pp 221 - 225; DOI: 10.1021/jm00396a035 |
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Synthesis and antitumor activity of analogs of ifosfamide modified in the N-(2-chloroethyl) group Konrad Misiura, Ryszard W. Kinas, Wojciech J. Stec, Halina Kusnierczyk, Czeslaw Radzikowski, and Akio Sonoda pp 226 - 230; DOI: 10.1021/jm00396a036 |
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Spiro Hydantoin Aldose Reductase Inhibitors Reinhard Sarges, Rodney C. Schnur, John L. Belletire, and Michael J. Peterson pp 230 - 243; DOI: 10.1021/jm00396a037 |
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Improved delivery through biological membranes. 32. Synthesis and biological activity of brain-targeted delivery systems for various estradiol derivatives Marcus E. Brewster, Kerry S. Estes, and Nicholas Bodor pp 244 - 249; DOI: 10.1021/jm00396a038 |
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Nitrosoureido nucleosides as potential inhibitors of nucleotide biosynthesis Robert D. Elliott, H. Jeanette Thomas, Sue C. Shaddix, Doris J. Adamson, R. Wallace Brockman, James M. Riordan, and John A. Montgomery pp 250 - 254; DOI: 10.1021/jm00396a039 |
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The preparation, antischistosomal and antitumor activity of hycanthone and some of its congeners. Evidence for the mode of action of hycanthone Sydney Archer, Livia Pica-Mattoccia, Donato Cioli, Ahmad Seyed-Mozaffari, and Abdel Hadi Zayed pp 254 - 260; DOI: 10.1021/jm00396a040 |
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Heterocyclic quinones with potential antitumor activity. 2. Synthesis and antitumor activity of some benzimidazole-4,7-dione derivatives Ippolito Antonini, Francesco Claudi, Gloria Cristalli, Palmarisa Franchetti, Mario Grifantini, and Sante Martelli pp 260 - 264; DOI: 10.1021/jm00396a041 |
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Cholecystokinin antagonists. Synthesis and biological evaluation of 3-substituted 1,4-benzodiazepin-2-amines Mark G. Bock, Robert M. DiPardo, Ben E. Evans, Kenneth E. Rittle, Roger M. Freidinger, Raymond S. L. Chang, and Victor J. Lotti pp 264 - 268; DOI: 10.1021/jm00396a042 |
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Synthesis and antiviral properties of (E)-5-(2-bromovinyl)-2'-deoxycytidine-related compounds A. Stanley Jones, Jon R. Sayers, Richard T. Walker, and Erik De Clercq pp 268 - 271; DOI: 10.1021/jm00396a043 |
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N6-(Arylalkyl)adenosines. Identification of N6-(9-fluorenylmethyl)adenosine as a highly potent agonist for the adenosine A2 receptor B. K. Trivedi, J. A. Bristol, R. F. Bruns, S. J. Haleen, and R. P. Steffen pp 271 - 273; DOI: 10.1021/jm00396a044 |
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Novel degradation products from the treatment of salinomycin and narasin with formic acid Jennie L. Wells, Jon Bordner, Paul Bowles, and James W. McFarland pp 274 - 276; DOI: 10.1021/jm00396a045 |
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Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships [Erratum to document cited in CA107(17):154217r] Bruce E. Maryanoff, David F. McComsey, Joseph F. Gardocki, Richard P. Shank, Michael J. Costanzo, Samuel O. Nortey, Craig R. Schneider, and Paulette E. Setler pp 276 - 276; DOI: 10.1021/jm00396a046 |
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Book Reviews pp 277 - 280; DOI: 10.1021/jm00396a600 |
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Application of the message-address concept in the design of highly potent and selective non-peptide .delta. opioid receptor antagonists P. S. Portoghese, M. Sultana, H. Nagase, and A. E. Takemori pp 281 - 282; DOI: 10.1021/jm00397a001 |
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Novel type of potential anticancer agents derived from chrysophanol and emodin. Some structure-activity relationship studies Masao Koyama, T. Ross Kelly, and Kyoichi A. Watanabe pp 283 - 284; DOI: 10.1021/jm00397a002 |
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Renin inhibitors. Design and synthesis of a new class of conformationally restricted analogs of angiotensinogen Hing L. Sham, Giorgio Bolis, Herman H. Stein, Stephen W. Fesik, Patrick A. Marcotte, Jacob J. Plattner, Cheryl A. Rempel, and Jonathan Greer pp 284 - 295; DOI: 10.1021/jm00397a003 |
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Analgesic dipeptide derivatives. 4. Linear and cyclic analogs of the analgesic compounds arginyl-2-[(o-nitrophenyl)sulfenyl]tryptophan and lysyl-2-[(o-nitrophenyl)sulfenyl]tryptophan M. Teresa Garcia-Lopez, Rosario Gonzalez-Muniz, M. Teresa Molinero, and Joaquin Del Rio pp 295 - 300; DOI: 10.1021/jm00397a004 |
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Crystal structures and pharmacologic activities of 1,4-dihydropyridine calcium channel antagonists of the isobutyl methyl 2,6-dimethyl-4-(substituted phenyl)-1,4-dihydropyridine-3,5-dicarboxylate (nisoldipine) series R. Fossheim, A. Joslyn, A. J. Solo, E. Luchowski, A. Rutledge, and D. J. Triggle pp 300 - 305; DOI: 10.1021/jm00397a005 |
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Conformational analysis and structural comparisons of (1R,3S)-(+)- and (1S,3R)-(-)-tefludazine, (S)-(+)- and (R)-(-)-octoclothepin, and (+)-dexclamol in relation to dopamine receptor antagonism and amine-uptake inhibition Tommy Liljefors and Klaus P. Boegesoe pp 306 - 312; DOI: 10.1021/jm00397a006 |
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(R)-(-)-10-Methyl-11-hydroxyaporphine: a highly selective serotonergic agonist Joseph G. Cannon, Prem Mohan, Jacek Bojarski, John Paul Long, Ranbir K. Bhatnagar, Paul A. Leonard, Jan R. Flynn, and Tapan K. Chatterjee pp 313 - 318; DOI: 10.1021/jm00397a007 |
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(Acyloxy)alkyl carbamates as novel bioreversible prodrugs for amines: increased permeation through biological membranes Jose Alexander, Robyn Cargill, Stuart R. Michelson, and Harvey Schwam pp 318 - 322; DOI: 10.1021/jm00397a008 |
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Nitrosoimidazoles: highly bactericidal analogs of 5-nitroimidazole drugs William J. Ehlhardt, Bernard B. Beaulieu, and Peter Goldman pp 323 - 329; DOI: 10.1021/jm00397a009 |
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Synthesis and evaluation of 5-amino-1-.beta.-D-ribofuranosyl-1,2,4-triazole-3-carboxamidine and certain related nucleosides as inhibitors of purine nucleoside phosphorylase Yogesh S. Sanghvi, Naeem B. Hanna, Steven B. Larson, James M. Fujitaki, Randall C. Willis, Roberts A. Smith, Roland K. Robins, and Ganapathi R. Revankar pp 330 - 335; DOI: 10.1021/jm00397a010 |
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Synthesis and antiviral activity of various 3'-azido analogs of pyrimidine deoxyribonucleosides against human immunodeficiency virus (HIV-1, HTLV-III/LAV) Tai Shun Lin, Ji Yu Guo, Raymond F. Schinazi, Chung K. Chu, Jia Ning Xiang, and William H. Prusoff pp 336 - 340; DOI: 10.1021/jm00397a011 |
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Novel DNA groove binding alkylators: design, synthesis, and biological evaluation Krzysztof Krowicki, Jan Balzarini, Erik De Clercq, Robert A. Newman, and J. William Lown pp 341 - 345; DOI: 10.1021/jm00397a012 |
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Design and synthesis of a series of combined vasodilator-.beta.-adrenoceptor antagonists based on 6-arylpyridazinones R. A. Slater, W. Howson, G. T. G. Swayne, E. M. Taylor, and D. R. Reavill pp 345 - 351; DOI: 10.1021/jm00397a013 |
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Synthesis and biological activity of the four stereoisomers of 6-[4-[3-[[2-hydroxy-3-[4-[2-(cyclopropylmethoxy)ethyl]phenoxy]propyl]amino]-propionamido]phenyl]-5-methyl-4,5-dihydro-3(2H)-pyridazinone, a combined vasodilator and .beta.-adrenoceptor antagonist W. Howson, J. Kitteringham, J. Mistry, M. B. Mitchell, R. Novelli, R. A. Slater, and G. T. G. Swayne pp 352 - 356; DOI: 10.1021/jm00397a014 |
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Molecular complexes of thyroid hormone tyrosyl rings with aromatic donors. Possible relationship to receptor protein interactions Kun Chae and James D. McKinney pp 357 - 362; DOI: 10.1021/jm00397a015 |
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6-[18F]fluorometaraminol. A radiotracer for in vivo mapping of adrenergic nerves of the heart Suresh G. Mislankar, David L. Gildersleeve, Donald M. Wieland, Christopher C. Massin, G. Keith Mulholland, and Steven A. Toorongian pp 362 - 366; DOI: 10.1021/jm00397a016 |
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Quantitative structure-activity relationships for the inhibition of Escherichia coli dihydrofolate reductase by 5-(substituted benzyl)-2,4-diaminopyrimidines Renli Li and Martin Poe pp 366 - 370; DOI: 10.1021/jm00397a017 |
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N-Aryl 3-halogenated azetidin-2-ones and benzocarbacephems, inhibitors of .beta.-lactamases Roger Joyeau, Huguette Molines, Roger Labia, and Michel Wakselman pp 370 - 374; DOI: 10.1021/jm00397a018 |
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Investigation of the structural parameters involved in the .mu. and .delta. opioid receptor discrimination of linear enkephalin-related peptides G. Gacel, J. M. Zajac, P. Delay-Goyet, V. Dauge, and B. P. Roques pp 374 - 383; DOI: 10.1021/jm00397a019 |
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Toward the synthesis of isozyme-specific enzyme inhibitors. Potent inhibitors of rat methionine adenosyltransferases. Effect of one-atom elongation of the ribose-P.alpha. bridge in two covalent adducts of L-methionine and .beta.,.gamma.-imido-ATP Francis Kappler, Vivekananda M. Vrudhula, and Alexander Hampton pp 384 - 389; DOI: 10.1021/jm00397a020 |
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Adenosine deaminase inhibitors. Synthesis and biological activities of deaza analogs of erythro-9-(2-hydroxy-3-nonyl)adenine Gloria Cristalli, Palmarisa Franchetti, Mario Grifantini, Sauro Vittori, Giulio Lupidi, Francesca Riva, Teresa Bordoni, Cristina Geroni, and M. Antonietta Verini pp 390 - 393; DOI: 10.1021/jm00397a021 |
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Synthesis and biological activities of 4-O-(difluoromethyl)-5-substituted-uracil nucleoside analogs Juergen Reefschlaeger, Claus Dietmar Pein, and Dieter Cech pp 393 - 397; DOI: 10.1021/jm00397a022 |
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1-Amino-substituted 4-methyl-5H-pyrido[4,3-b]indoles (.gamma.-carbolines) as tricyclic analogs of ellipticines: a new class of antineoplastic agents Emile Bisagni, Nguyen Chi Hung, Alain Pierre, Odile Pepin, Paul De Cointet, and Pierre Gros pp 398 - 405; DOI: 10.1021/jm00397a023 |
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Synthesis and biological evaluations of certain 2-halo-2'-substituted derivatives of 9-.beta.-D-arabinofuranosyladenine John A. Secrist, Anita T. Shortnacy, and John A. Montgomery pp 405 - 410; DOI: 10.1021/jm00397a024 |
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Structure-activity relationship in PAF-acether. 4. Synthesis and biological activities of carboxylate isosteres Boguslaw Wichrowski, Simone Jouquey, Colette Broquet, Francoise Heymans, Jean Jacques Godfroid, Jeanne Fichelle, and Manuel Worcel pp 410 - 415; DOI: 10.1021/jm00397a025 |
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Dehydro ketomethylene and ketomethylene analogs of substance P: synthesis and biological activity Ariel Ewenson, Ralph Laufen, Michael Chorev, Zvi Selinger, and Chaim Gilon pp 416 - 421; DOI: 10.1021/jm00397a026 |
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Angiotensin-converting enzyme inhibitors. 2. Perhydroazepin-2-one derivatives Hiroaki Yanagisawa, Sadao Ishihara, Akiko Ando, Takuro Kanazaki, Shuichi Miyamoto, Hiroyuki Koike, Yasuteru Iijima, Kiyoshi Oizumi, Yoichi Matsushita, and Tadashi Hata pp 422 - 428; DOI: 10.1021/jm00397a027 |
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Synthesis of spin traps specific for hydroxyl radical Gerald M. Rosen and Marvin J. Turner pp 428 - 432; DOI: 10.1021/jm00397a028 |
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Conformationally defined adrenergic agents. 13. Conformational and steric aspects of the inhibition of phenylethanolamine N-methyltransferase by benzylamines Gary L. Grunewald, Daniel J. Sall, and James A. Monn pp 433 - 444; DOI: 10.1021/jm00397a029 |
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(8.beta.)-Ergoline-8-carboxylic acid cycloalkyl esters as serotonin antagonists: structure-activity study William L. Garbrecht, Gifford Marzoni, Kathleen R. Whitten, and Marlene L. Cohen pp 444 - 448; DOI: 10.1021/jm00397a030 |
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Inhibition of murine thymidylate synthase and human dihydrofolate reductase by 5,8-dideaza analogs of folic acid and aminopterin John B. Hynes, Shirish A. Patil, Alenka Tomazic, Arvind Kumar, Alpana Pathak, Xuehai Tan, Xianqiang Li, Manohar Ratnam, Tavner J. Delcamp, and James H. Freisheim pp 449 - 454; DOI: 10.1021/jm00397a031 |
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Synthesis and potential antipsychotic activity of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines Horace A. DeWald, Nicholas W. Beeson, Fred M. Hershenson, Lawrence D. Wise, David A. Downs, Thomas G. Heffner, Linda L. Coughenour, and Thomas A. Pugsley pp 454 - 461; DOI: 10.1021/jm00397a032 |
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Imidazole-pyridine bioisosterism: comparison of the inotropic activities of pyridine- and imidazole-substituted 6-phenyldihydropyridazinone cardiotonics David W. Robertson, Joseph H. Krushinski, G. Don Pollock, and J. Scott Hayes pp 461 - 465; DOI: 10.1021/jm00397a033 |
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Pyrido[2,1-b]quinazolinecarboxamide derivatives as platelet activating factor antagonists Jefferson W. Tilley, Barbara Burghardt, Charles Burghardt, Thomas F. Mowles, Franz Josef Leinweber, Larry Klevans, Richard Young, Gerry Hirkaler, Kenneth Fahrenholtz, and et al. pp 466 - 472; DOI: 10.1021/jm00397a034 |
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Cardioactivity and solid-state structure of two 4-isoxazolyldihydropyridines related to the 4-aryldihydropyridine calcium-channel blockers John I. McKenna, Ludwig Schlicksupp, Nicholas R. Natale, Roger D. Willett, Bruce E. Maryanoff, and Stephen F. Flaim pp 473 - 476; DOI: 10.1021/jm00397a035 |
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Pumiliotoxin alkaloids: relationship of cardiotonic activity to sodium channel activity and phosphatidylinositol turnover J. W. Daly, E. McNeal, F. Gusovsky, F. Ito, and L. E. Overman pp 477 - 480; DOI: 10.1021/jm00397a036 |
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4-N-Hydroxy-L-2,4-diaminobutyric acid. A strong inhibitor of glutamine synthetase Shinji Fushiya, Kazutoshi Maeda, Toshihiko Funayama, and Shigeo Nozoe pp 480 - 483; DOI: 10.1021/jm00397a037 |
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Synthesis and antiviral evaluation of carbocyclic analogs of 2'-azido- and 2'-amino-2'-deoxycytidine Tai Shun Lin, Xiao Hui Zhang, Zi Hou Wang, and W. H. Prusoff pp 484 - 486; DOI: 10.1021/jm00397a038 |
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2-Methyl-1,3-dioxaazaspiro[4.5]decanes as novel muscarinic cholinergic agonists John Saunders, Graham A. Showell, Roger J. Snow, Raymond Baker, Elizabeth A. Harley, and Stephen B. Freedman pp 486 - 491; DOI: 10.1021/jm00397a039 |
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Book Reviews-Writing the Laboratory Notebook Stephen T. Ross, and Stuart R. Suter pp 491 - 491; DOI: 10.1021/jm00397a600 |
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Book Reviews pp 491 - 498; DOI: 10.1021/jm00397a601 |
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Acetohydroxamic acids as potent, selective, orally active 5-lipoxygenase inhibitors William P. Jackson, Peter J. Islip, Geoffrey Kneen, Ashley Pugh, and Peter J. Wates pp 499 - 500; DOI: 10.1021/jm00398a001 |
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9-(Trans-2'-trans-3'-dihydroxycyclopent-4'-enyl) derivatives of adenine and 3-deazaadenine: potent inhibitors of bovine liver S-adenosylhomocysteine hydrolase Sunandra R. Narayanan, Bradley T. Keller, David R. Borcherding, Stephen A. Scholtz, and R. T. Borchardt pp 500 - 503; DOI: 10.1021/jm00398a002 |
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7-Substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials John M. Domagala, Susan E. Hagen, Carl L. Heifetz, Marland P. Hutt, Thomas F. Mich, Joseph P. Sanchez, and Ashok K. Trehan pp 503 - 506; DOI: 10.1021/jm00398a003 |
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Synthesis and biological characterization of pyridohomotropanes. Structure-activity relationships of conformationally restricted nicotinoids David B. Kanne and Leo G. Abood pp 506 - 509; DOI: 10.1021/jm00398a004 |
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Effects of D-amino acid substitution on antagonist activities of angiotensin II analogs J. Samanen, D. Narindray, W. Adams, T. Cash, T. Yellin, and D. Regoli pp 510 - 516; DOI: 10.1021/jm00398a005 |
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2,4-Diamino-6,7-dimethoxyquinazolines. 4. 2-[4-(Substituted oxyethoxy)piperidino] derivatives as .alpha.1-adrenoceptor antagonists and antihypertensive agents Simon F. Campbell, John C. Danilewicz, Colin W. Greengrass, and Rhona M. Plews pp 516 - 520; DOI: 10.1021/jm00398a006 |
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Structure-activity relationships for drugs binding to the agonist and antagonist states of the primary morphine receptor B. Vernon Cheney pp 521 - 531; DOI: 10.1021/jm00398a007 |
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New inhibitors of human renin that contain novel Leu-Val replacements. Examination of the P1 site Jay R. Luly, Giorgio Bolis, Nwe BaMaung, Jeff Soderquist, Joseph F. Dellaria, Herman Stein, Jerome Cohen, Thomas J. Perun, Jonathan Greer, and Jacob J. Plattner pp 532 - 539; DOI: 10.1021/jm00398a008 |
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Enantiomeric effects of homologs of disoxaril on the inhibitory activity against human rhinovirus-14 Guy D. Diana, Michael J. Otto, Adi M. Treasurywala, Mark A. McKinlay, Richard C. Oglesby, Edward G. Maliski, Michael G. Rossmann, and Thomas J. Smith pp 540 - 544; DOI: 10.1021/jm00398a009 |
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Synthesis, pharmacology, and molecular modeling studies of semirigid, nicotinic agonists James A. Waters, Charles E. Spivak, Mark Hermsmeier, Janardan S. Yadav, Rong F. Liang, and Tamara M. Gund pp 545 - 554; DOI: 10.1021/jm00398a010 |
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Synthesis and analgesic properties of N-substituted trans-4a-aryldecahydroisoquinolines Dennis M. Zimmerman, Buddy E. Cantrell, John K. Swartzendruber, Noel D. Jones, Laura G. Mendelsohn, J. David Leander, and Rodney C. Nickander pp 555 - 560; DOI: 10.1021/jm00398a011 |
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Synthesis and biological activity of ketomethylene-containing nonapeptide analogs of snake venom angiotensin converting enzyme inhibitors Ronald G. Almquist, W. R. Chao, A. K. Judd, C. Mitoma, D. J. Rossi, R. E. Panasevich, and R. J. Matthews pp 561 - 567; DOI: 10.1021/jm00398a012 |
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Clofazimine analogs active against a clofazimine-resistant organism John F. O'Sullivan, Michael L. Conalty, and Norman E. Morrison pp 567 - 572; DOI: 10.1021/jm00398a013 |
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Analogs of [(triethylsilyl)ethynyl]estradiol as potential antifertility agents Richard H. Peters, David F. Crowe, Mitchell A. Avery, Wesley K. M. Chong, and Masato Tanabe pp 572 - 576; DOI: 10.1021/jm00398a014 |
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Derivatives of the muscarinic agent N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide Bjoern M. Nilsson, Bjoern Ringdahl, and Uli Hacksell pp 577 - 582; DOI: 10.1021/jm00398a015 |
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One- and two-dimensional proton NMR, fluorescence and molecular modeling studies on the tomaymycin-d(ATGCAT)2 adduct. Evidence for two covalent adducts with opposite orientations and stereochemistries at the covalent linkage site Steve Cheatham, Alan Kook, Laurence H. Hurley, Mary D. Barkley, and William Remers pp 583 - 590; DOI: 10.1021/jm00398a016 |
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Stereoelectronic factors influencing the biological activity and DNA interaction of synthetic antitumor agents modeled on CC-1065 M. A. Warpehoski, I. Gebhard, R. C. Kelly, W. C. Krueger, L. H. Li, J. P. McGovren, M. D. Prairie, N. Wicnienski, and W. Wierenga pp 590 - 603; DOI: 10.1021/jm00398a017 |
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Synthesis of arginine-vasopressins, modified in positions 1 and 2, as antagonists of the vasopressor response to the parent hormone Bernard Lammek, Piotr Rekowski, Gotfryd Kupryszewski, Per Melin, and Ulf Ragnarsson pp 603 - 606; DOI: 10.1021/jm00398a018 |
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6-(Alkylamino)-9-benzyl-9H-purines. A new class of anticonvulsant agents James L. Kelley, Mark P. Krochmal, James A. Linn, Ed W. McLean, and Francis E. Soroko pp 606 - 612; DOI: 10.1021/jm00398a019 |
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8-Aryl- and 8-cycloalkyl-1,3-dipropylxanthines: further potent and selective antagonists for A1-adenosine receptors M. T. Shamim, D. Ukena, W. L. Padgett, O. Hong, and J. W. Daly pp 613 - 617; DOI: 10.1021/jm00398a020 |
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Atypical antipsychotic agents: patterns of activity in a series of 3-substituted 2-pyridinyl-1-piperazine derivatives James S. New, Joseph P. Yevich, Davis L. Temple, Kimberly B. New, Sharon M. Gross, R. Francis Schlemmer, Michael S. Eison, Duncan P. Taylor, and Leslie A. Riblet pp 618 - 624; DOI: 10.1021/jm00398a021 |
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Inhibition of porcine pepsin by two substrate analogs containing statine. The effect of histidine at the P2 subsite on the inhibition of aspartic proteinases Juergen Maibaum and Daniel H. Rich pp 625 - 629; DOI: 10.1021/jm00398a022 |
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2-Ethynylbenzenealkanamines. A new class of calcium entry blockers J. R. Carson, H. R. Almond, M. D. Brannan, R. J. Carmosin, S. F. Flaim, A. Gill, M. M. Gleason, S. L. Keely, D. W. Ludovici, and et al. pp 630 - 636; DOI: 10.1021/jm00398a023 |
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Regio- and stereochemical studies on the .alpha.-carbon oxidation of (S)-nicotine by cytochrome P-450 model systems Lisa A. Peterson and Neal Castagnoli pp 637 - 640; DOI: 10.1021/jm00398a024 |
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Structure-affinity relationships of arylquinolizines at .alpha.-adrenoceptors Joel R. Huff, John J. Baldwin, S. Jane DeSolms, James P. Guare, Cecilia A. Hunt, William C. Randall, William S. Sanders, Steven J. Smith, Joseph P. Vacca, and Matthew M. Zrada pp 641 - 645; DOI: 10.1021/jm00398a025 |
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Arteether, a new antimalarial drug: synthesis and antimalarial properties A. Brossi, B. Venugopalan, L. Dominguez Gerpe, H. J. C. Yeh, J. L. Flippen-Anderson, P. Buchs, X. D. Luo, W. Milhous, and W. Peters pp 645 - 650; DOI: 10.1021/jm00398a026 |
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Synthesis and anticandidal properties of polyoxin L analogs containing .alpha.-amino fatty acids R. K. Khare, Jeffrey M. Becker, and Fred R. Naider pp 650 - 656; DOI: 10.1021/jm00398a027 |
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Development of a new physicochemical model for brain penetration and its application to the design of centrally acting H2 receptor histamine antagonists Rodney C. Young, Robert C. Mitchell, Thomas H. Brown, C. Robin Ganellin, Robin Griffiths, Martin Jones, Kishore K. Rana, David Saunders, Ian R. Smith, and et al. pp 656 - 671; DOI: 10.1021/jm00398a028 |
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Renin inhibitors containing .psi.[CH2O] pseudopeptide inserts Ruth E. Ten Brink, Donald T. Pals, Douglas W. Harris, and Garland A. Johnson pp 671 - 677; DOI: 10.1021/jm00398a029 |
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Design of potent cyclic gonadotropin releasing hormone antagonists J. Rivier, G. Kupryszewski, J. Varga, J. Porter, C. Rivier, M. Perrin, A. Hagler, S. Struthers, A. Corrigan, and W. Vale pp 677 - 682; DOI: 10.1021/jm00398a030 |
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5-Methyl-2-pyrrolidone analogs of oxotremorine as selective muscarinic agonists Bjoern Ringdahl pp 683 - 688; DOI: 10.1021/jm00398a031 |
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6- and 8-Hydroxy-3,4-dihydro-3-(dipropylamino)-2H-1-benzopyrans. Dopamine agonists with autoreceptor selectivity Lawrence D. Wise, Horace A. DeWald, Elma S. Hawkins, Donna M. Reynolds, Thomas G. Heffner, Leonard T. Meltzer, and Thomas A. Pugsley pp 688 - 691; DOI: 10.1021/jm00398a032 |
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Synthesis and pharmacological characterization of a series of leukotriene analogs with antagonist and agonist activities Peter R. Bernstein, Edward P. Vacek, Edward J. Adams, David W. Snyder, and Robert D. Krell pp 692 - 696; DOI: 10.1021/jm00398a033 |
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Potential anticancer agents. 5-(N-Substituted-aminocarbonyl)- and 5-(N-substituted-aminothiocarbonyl)-5,6,7,8-tetrahydrofolic acids Carroll Temple, Robert D. Elliott, and John A. Montgomery pp 697 - 700; DOI: 10.1021/jm00398a034 |
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Additions and Corrections-Synthesis, Binding Studies, and Structure-Activity Relationships of 1-Aryl- and 2-Aryl[1]benzopyranopyrazol-4-ones, Central Benzodiazepine Receptor Ligands Vittoria Colotta, Lucia Cecchi, Guido Filacchioni, Fabrizio Melani, Giovanna Palazzino, and Anotonio Lucacchini pp 700 - 700; DOI: 10.1021/jm00398a600 |
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New human renin inhibitors containing an unnatural amino acid, norstatine Kinji Iizuka, Tetsuhide Kamijo, Tetsuhiro Kubota, Kenji Akahane, Hideaki Umeyama, and Yoshiaki Kiso pp 701 - 704; DOI: 10.1021/jm00399a001 |
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.beta.-Substituted phenethylamines as high-affinity mechanism-based inhibitors of dopamine .beta.-hydroxylase Lawrence I. Kruse, Carl Kaiser, Walter E. DeWolf, Pamela A. Chambers, Paula J. Goodhart, Mildred Ezekiel, and Eliot H. Ohlstein pp 704 - 706; DOI: 10.1021/jm00399a002 |
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Potential antitumor agents. 54. Chromophore requirements for in vivo antitumor activity among the general class of linear tricyclic carboxamides Brian D. Palmer, Gordon W. Rewcastle, Graham J. Atwell, Bruce C. Baguley, and William A. Denny pp 707 - 712; DOI: 10.1021/jm00399a003 |
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1,2,4-Trioxanes as potential antimalarial agents John A. Kepler, Abraham Philip, Y. W. Lee, Matthew C. Morey, and F. Ivy Carroll pp 713 - 716; DOI: 10.1021/jm00399a004 |
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Synthesis and copper-dependent antimycoplasmal activity of 1-amino-3-(2-pyridyl)isoquinoline derivatives. 1. Amides Marcel A. H. De Zwart, Henk Van der Goot, and Henk Timmerman pp 716 - 722; DOI: 10.1021/jm00399a005 |
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Using shape complementarity as an initial screen in designing ligands for a receptor binding site of known three-dimensional structure Renee L. DesJarlais, Robert P. Sheridan, George L. Seibel, J. Scott Dixon, Irwin D. Kuntz, and R. Venkataraghavan pp 722 - 729; DOI: 10.1021/jm00399a006 |
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Bile acids with a cyclopropyl-containing side chain. 3. Separation, identification, and properties of all four stereoisomers of 3.alpha.,7.beta.-dihydroxy-22,23-methylene-5.beta.-cholan-24-oic acid Roberto Pellicciari, Benedetto Natalini, Sergio Cecchetti, Barry Porter, Aldo Roda, Brunella Grigolo, and Renzo Balducci pp 730 - 736; DOI: 10.1021/jm00399a007 |
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The importance of residues 2 (arginine) and 6 (histidine) in high-affinity angiotensin II antagonists J. Samanen, E. Brandeis, D. Narindray, W. Adams, T. Cash, T. Yellin, and D. Regoli pp 737 - 741; DOI: 10.1021/jm00399a008 |
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Design, synthesis, and biological activity of a peptide mimic of vasopressin William M. Bryan, Judith C. Hempel, William F. Huffman, Garland R. Marshall, Michael L. Moore, Joanne Silvestri, Frans L. Stassen, James S. Stefankiewicz, Lynn Sulat, and R. Lee Webb pp 742 - 744; DOI: 10.1021/jm00399a009 |
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Iodine-125-labeled 8-phenylxanthine derivatives: antagonist radioligands for adenosine A1 receptors Joel Linden, Amrat Patel, Craig Q. Earl, Rebecca H. Craig, and Susan M. Daluge pp 745 - 751; DOI: 10.1021/jm00399a010 |
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Photoaffinity labeling adenosine A1 receptors with an antagonist iodine-125-labeled aryl azide derivative of 8-phenylxanthine Craig Q. Earl, Amrat Patel, Rebecca H. Craig, Susan M. Daluge, and Joel Linden pp 752 - 756; DOI: 10.1021/jm00399a011 |
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Sulfur derivatives of 2-oxopropanal oxime as reactivators of organophosphate-inhibited acetylcholinesterase in vitro: synthesis and structure-reactivity relationships Francoise Degorre, Daniel Kiffer, and Francois Terrier pp 757 - 763; DOI: 10.1021/jm00399a012 |
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Methotrexate analogs. 31. Meta and ortho isomers of aminopterin, compounds with a double bond in the side chain, and a novel analog modified at the .alpha.-carbon: chemical and in vitro biological studies Andre Rosowsky, Henry Bader, Ronald A. Forsch, Richard G. Moran, and James H. Freisheim pp 763 - 768; DOI: 10.1021/jm00399a013 |
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New actinomycin D analogs as superior chemotherapeutic agents against primary and advanced colon tumors and colon xenografts in nude mice Sisir K. Sengupta, Yuri Kogan, Christine Kelly, and Josephine Szabo pp 768 - 774; DOI: 10.1021/jm00399a014 |
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Potential antitumor agents. 55. 6-Phenylphenanthridine-4-carboxamides: a new class of DNA-intercalating antitumor agents Graham J. Atwell, Bruce C. Baguley, and William A. Denny pp 774 - 779; DOI: 10.1021/jm00399a015 |
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Synthesis and antiulcer activity of 5,11-dihydro[1]benzoxepino[3,4-b]pyridines Toshiaki Kumazawa, Hiroyuki Harakawa, Hiroyuki Obase, Yoshimasa Oiji, Hiroshi Tanaka, Katsuichi Shuto, Akio Ishii, Tetsuo Oka, and Nobuhiro Nakamizo pp 779 - 785; DOI: 10.1021/jm00399a016 |
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Synthesis and intramolecular hydrogen bonding and biochemical studies of clitocine, a naturally occurring exocyclic amino nucleoside Randall J. Moss, Charles R. Petrie, Rich B. Meyer, L. Dee Nord, Randall C. Willis, Roberts A. Smith, Steven B. Larson, Ganesh D. Kini, and Roland K. Robins pp 786 - 790; DOI: 10.1021/jm00399a017 |
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Synthesis and biological properties of actinomycin D chromophoric analogs substituted at carbon 7 with aziridine and cyclopropyl functions Raj K. Sehgal, Bijan Almassian, David P. Rosenbaum, Ruth Zadrozny, and Sisir K. Sengupta pp 790 - 793; DOI: 10.1021/jm00399a018 |
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Studies on scavengers of active oxygen species. 1. Synthesis and biological activity of 2-O-alkylascorbic acids Kaneyoshi Kato, Shinji Terao, Norio Shimamoto, and Minoru Hirata pp 793 - 798; DOI: 10.1021/jm00399a019 |
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Flavins as potential antimalarials. 1. 10-(halophenyl)-3-methylflavins William B. Cowden, Ian A. Clark, and Nicholas H. Hunt pp 799 - 801; DOI: 10.1021/jm00399a020 |
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Inhibition of copper-dependent amine oxidases by some hydrazides of pyrrol-1-ylbenzoic and pyrrol-1-ylphenylacetic acids Marino Artico, Federico Corelli, Silvio Massa, Giorgio Stefancich, Luciana Avigliano, Olivia Befani, Giordana Marcozzi, Stefania Sabatini, and Bruno Mondovi pp 802 - 806; DOI: 10.1021/jm00399a021 |
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Approaches to protection against nerve agent poisoning. (Naphthylvinyl)pyridine derivatives as potential antidotes Allan P. Gray, Robert D. Platz, Theresa R. Henderson, Timothy C. P. Chang, Kazuyuki Takahashi, and Kenneth L. Dretchen pp 807 - 814; DOI: 10.1021/jm00399a022 |
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Chemistry and positive inotropic effect of pelrinone and related derivatives. A novel class of 2-methylpyrimidones as inotropic agents Jehan Bagli, T. Bogri, B. Palameta, S. Rakhit, S. Peseckis, J. McQuillan, and D. K. H. Lee pp 814 - 823; DOI: 10.1021/jm00399a023 |
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Synthesis and evaluation of 3-substituted analogs of 1,2,3,4-tetrahydroisoquinoline as inhibitors of phenylethanolamine N-methyltransferase Gary L. Grunewald, Daniel J. Sall, and James A. Monn pp 824 - 830; DOI: 10.1021/jm00399a024 |
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Highly selective .kappa. opioid analgesics. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide and N-[(2-aminocyclohexyl)aryloxy]acetamide derivatives Colin R. Clark, Paul R. Halfpenny, Raymond G. Hill, David C. Horwell, John Hughes, Terry C. Jarvis, David C. Rees, and David Schofield pp 831 - 836; DOI: 10.1021/jm00399a025 |
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Binaltorphimine-related bivalent ligands and their .kappa. opioid receptor antagonist selectivity P. S. Portoghese, H. Nagase, A. W. Lipkowski, D. L. Larson, and A. E. Takemori pp 836 - 841; DOI: 10.1021/jm00399a026 |
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3-Phenoxypyridine 1-oxides as anticonvulsant agents Michael R. Pavia, Charles P. Taylor, Fred M. Hershenson, Sandra J. Lobbestael, and Donald E. Butler pp 841 - 847; DOI: 10.1021/jm00399a027 |
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Synthesis, molecular modeling, DNA binding, and antitumor properties of some substituted amidoanthraquinones David A. Collier and Stephen Neidle pp 847 - 857; DOI: 10.1021/jm00399a028 |
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Synthesis and evaluation of neoplastic cell growth inhibition of 1-N-alkylamide analogs of glycero-3-phosphocholine Michael H. Marx, Claude Piantadosi, Alessandro Noseda, Larry W. Daniel, and Edward J. Modest pp 858 - 863; DOI: 10.1021/jm00399a029 |
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Synthesis, resolution, and absolute configuration of the isomers of the neuronal excitant 1-amino-1,3-cyclopentanedicarboxylic acid Kenneth Curry, M. J. Peet, D. S. K. Magnuson, and H. McLennan pp 864 - 867; DOI: 10.1021/jm00399a030 |
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N,N-Di-n-propylserotonin: binding at serotonin binding sites and a comparison with 8-hydroxy-2-(di-n-propylamino)tetralin Richard A. Glennon, Milt Titeler, Robert A. Lyon, and R. M. Slusher pp 867 - 870; DOI: 10.1021/jm00399a031 |
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Peptide derivatives of primaquine as potential antimalarial agents Abraham Philip, John A. Kepler, Bernadette H. Johnson, and F. Ivy Carroll pp 870 - 874; DOI: 10.1021/jm00399a032 |
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Synthesis and pharmacological activity of angiotensin-converting enzyme inhibitors: N-(mercaptoacyl)-4-substituted-(S)-prolines Elizabeth M. Smith, Gerald F. Swiss, Bernard R. Neustadt, Elijah H. Gold, Jane A. Sommer, Arthur D. Brown, Peter J. S. Chiu, Rosa Moran, Edmund J. Sybertz, and Thomas Baum pp 875 - 885; DOI: 10.1021/jm00399a033 |
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Resolution of the non steroidal antiandrogen 4'-cyano-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methyl-3'-(trifluoromethyl)propionanilide and the determination of the absolute configuration of the active enantiomer Howard Tucker and Glynne J. Chesterson pp 885 - 887; DOI: 10.1021/jm00399a034 |
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Book Reviews pp 887 - 892; DOI: 10.1021/jm00399a600 |
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Analogs of .gamma.-hydroxybutyric acid. Synthesis and binding studies Jean Jacques Bourguignon, Angele Schoenfelder, Martine Schmitt, Camille Georges Wermuth, Viviane Hechler, Brigitte Charlier, and Michel Maitre pp 893 - 897; DOI: 10.1021/jm00400a001 |
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Synthesis of diethylenetriaminepentaacetic acid conjugated inulin and utility for cellular uptake of liposomes Herbert Essien, J. Y. Lai, and Karl J. Hwang pp 898 - 901; DOI: 10.1021/jm00400a002 |
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Antihypertensive thiadiazoles. 1. Synthesis of some 2-aryl-5-hydrazino-1,3,4-thiadiazoles with vasodilator activity Stephen Turner, Malcolm Myers, Brian Gadie, Anthony J. Nelson, Robin Pape, John F. Saville, John C. Doxey, and Timothy L. Berridge pp 902 - 906; DOI: 10.1021/jm00400a003 |
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Antihypertensive thiadiazoles. 2. Vasodilator activity of some 2-aryl-5-guanidino-1,3,4-thiadiazoles Stephen Turner, Malcolm Myers, Brian Gadie, Stafford A. Hale, Alan Horsley, Anthony J. Nelson, Robin Pape, John F. Saville, John C. Doxey, and Timothy L. Berridge pp 906 - 913; DOI: 10.1021/jm00400a004 |
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Homoallylic amines related to zimeldine. Comparative study on neuronal serotonin and norepinephrine reuptake based on conformational analysis Thomas Hoegberg, Svante B. Ross, Peter Stroem, Gary L. Grunewald, Mary W. Creese, and Jeffrey D. Bunce pp 913 - 919; DOI: 10.1021/jm00400a005 |
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Novel calcium antagonists. Synthesis and structure-activity relationship studies of benzothiazoline derivatives Koji Yamamoto, Masanobu Fujita, Keizo Tabashi, Yoichi Kawashima, Eishin Kato, Masayuki Oya, Tadashi Iso, and Junichi Iwao pp 919 - 930; DOI: 10.1021/jm00400a006 |
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Synthesis and pharmacological evaluation of 5,6-exo-epoxy-7-oxabicyclo[2.2.1]heptane derivatives Jagabandhu Das, Truc Vu, Don N. Harris, and Martin L. Ogletree pp 930 - 935; DOI: 10.1021/jm00400a007 |
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Studies directed toward ascertaining the active conformation of 1,4-dihydropyridine calcium entry blockers George Rovnyak, Niels Andersen, Jack Gougoutas, Anders Hedberg, S. David Kimball, Mary Malley, Suzanne Moreland, Michael Porubcan, and Andrew Pudzianowski pp 936 - 944; DOI: 10.1021/jm00400a008 |
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Indoline analogs of idazoxan: potent .alpha.2-antagonists and .alpha.1-agonists Gay P. Fagan, Christopher B. Chapleo, Anthony C. Lane, Malcolm Myers, Alan G. Roach, Colin F. C. Smith, Michael R. Stillings, and Anthony P. Welbourn pp 944 - 948; DOI: 10.1021/jm00400a009 |
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Melanin concentrating hormone analogs: contraction of the cyclic structure. 1. Agonist activity Michal Lebl, Victor J. Hruby, Ana M. de L. Castrucci, Maria A. Visconti, and Mac E. Hadley pp 949 - 954; DOI: 10.1021/jm00400a010 |
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Nonsteroidal antiandrogens. Synthesis and structure-activity relationships of 3-substituted derivatives of 2-hydroxypropionanilides Howard Tucker, J. W. Crook, and G. J. Chesterson pp 954 - 959; DOI: 10.1021/jm00400a011 |
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Peripherally acting enkephalin analogs. 1. Polar pentapeptides George W. Hardy, Lawrence A. Lowe, Pang Yih Sang, Dean S. A. Simpkin, Samuel Wilkinson, Rhonda L. Follenfant, and Terence W. Smith pp 960 - 966; DOI: 10.1021/jm00400a012 |
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Synthesis and biological activity of CCK26-33-related analogs modified in position 31 I. Marseigne, A. Dor, D. Begue, M. Reibaud, J. L. Zundel, J. C. Blanchard, D. Pelaprat, and B. P. Roques pp 966 - 970; DOI: 10.1021/jm00400a013 |
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Analogs of aminoglutethimide based on 1-phenyl-3-azabicyclo[3.1.0]hexane-2,4-dione: selective inhibition of aromatase activity Martin G. Rowlands, Michael A. Bunnett, Allan B. Foster, Michael Jarman, Jaroslav Stanek, and Ernst Schweizer pp 971 - 976; DOI: 10.1021/jm00400a014 |
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Coupling products of amino acids to penicillin V and cephalothin: synthesis and susceptibility to carboxypeptidases and lysosomal enzymes Z. Bounkhala, C. Renard, R. Baurain, J. Marchand-Brynaert, L. Ghosez, and P. M. Tulkens pp 976 - 983; DOI: 10.1021/jm00400a015 |
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Quinolone antibacterial agents. Synthesis and structure-activity relationships of 8-substituted quinoline-3-carboxylic acids and 1,8-naphthyridine-3-carboxylic acids Joseph P. Sanchez, John M. Domagala, Susan E. Hagen, Carl L. Heifetz, Marland P. Hutt, Jeffry B. Nichols, and Ashok K. Trehan pp 983 - 991; DOI: 10.1021/jm00400a016 |
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1-Substituted 7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids. New quantitative structure activity relationships at N1 for the quinolone antibacterials John M. Domagala, Carl L. Heifetz, Marland P. Hutt, Thomas F. Mich, Jeffry B. Nichols, Marjorie Solomon, and Donald F. Worth pp 991 - 1001; DOI: 10.1021/jm00400a017 |
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Potential anticonvulsants. 11. Synthesis and anticonvulsant activity of spiro[1,3-dioxolane-2,3'-indolin]-2'-ones and structural analogs Milind Rajopadhye and Frank D. Popp pp 1001 - 1005; DOI: 10.1021/jm00400a018 |
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9-(2-Fluorobenzyl)-6-(alkylamino)-9H-purines. A new class of anticonvulsant agents James L. Kelley, Mark P. Krochmal, James A. Linn, Ed W. McLean, and Francis E. Soroko pp 1005 - 1009; DOI: 10.1021/jm00400a019 |
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N-Terminal requirements of small peptide anticoagulants based on hirudin 54-65 Thomas J. Owen, John L. Krstenansky, Mark T. Yates, and Simon J. T. Mao pp 1009 - 1011; DOI: 10.1021/jm00400a020 |
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[1,2,4]Triazolo[4,3-a]quinoxalin-4-amines: a new class of A1 receptor selective adenosine antagonists Bharat K. Trivedi and Robert F. Bruns pp 1011 - 1014; DOI: 10.1021/jm00400a021 |
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Structure-activity profile of a series of novel triazoloquinazoline adenosine antagonists John E. Francis, William D. Cash, Stacy Psychoyos, Geetha Ghai, Paul Wenk, Robert C. Friedmann, Charlotte Atkins, Vivian Warren, Patricia Furness, and et al. pp 1014 - 1020; DOI: 10.1021/jm00400a022 |
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Asymmetrical bisintercalators as potential antitumor agents P. Leon, C. Garbay-Jaureguiberry, B. Lambert, J. B. Le Pecq, and B. P. Roques pp 1021 - 1026; DOI: 10.1021/jm00400a023 |
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Ara-tiazofurin: conservation of structural features in an unusual thiazole nucleoside Barry M. Goldstein, David T. Mao, and Victor E. Marquez pp 1026 - 1031; DOI: 10.1021/jm00400a024 |
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2,4-Diamino-6,7-dimethoxyquinoline derivatives as .alpha.1-adrenoceptor antagonists and antihypertensive agents Simon F. Campbell, J. David Hardstone, and Michael J. Palmer pp 1031 - 1035; DOI: 10.1021/jm00400a025 |
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1,3-Diamino-6,7-dimethoxyisoquinoline derivatives as potential .alpha.1-adrenoceptor antagonists Jon Bordner, Simon F. Campbell, Michael J. Palmer, and Michael S. Tute pp 1036 - 1039; DOI: 10.1021/jm00400a026 |
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Dopamine D-2 receptor imaging radiopharmaceuticals: synthesis, radiolabeling and in vitro binding of (R)-(+)- and (S)-(-)-3-iodo-2-hydroxy-6-methoxy-N-[(1-ethyl-2-pyrrolidinyl)methyl]benzamide Hank F. Kung, Ravindra Kasliwal, Sangren Pan, Mei Ping Kung, Robert H. Mach, and Yu Zhi Guo pp 1039 - 1043; DOI: 10.1021/jm00400a027 |
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Synthesis and biodistribution of 99mTc-labeled piperidinyl bis(aminoethanethiol) complexes: potential brain perfusion imaging agents for single photon emission computed tomography S. M. N. Efange, Hank F. Kung, J. J. Billings, and M. Blau pp 1043 - 1047; DOI: 10.1021/jm00400a028 |
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Potential antitumor agents. 56. Minimal DNA-intercalating ligands as antitumor drugs: phenylquinoline-8-carboxamides Graham J. Atwell, Claudia D. Bos, Bruce C. Baguley, and William A. Denny pp 1048 - 1052; DOI: 10.1021/jm00400a029 |
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(Acyloxy)benzophenones and (acyloxy)-4-pyrones. A new class of inhibitors of human neutrophil elastase Masateru Miyano, James R. Deason, Akira Nakao, Michael A. Stealey, Clara I. Villamil, Daniel D. Sohn, and Richard A. Mueller pp 1052 - 1061; DOI: 10.1021/jm00400a030 |
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Book Reviews pp 1061 - 1062; DOI: 10.1021/jm00400a600 |
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Nucleosides and nucleotides. 83. Design, synthesis, and antineoplastic activity of 2'-deoxy-2'-methylidenecytidine Kenji Takenuki, Akira Matsuda, Tohru Ueda, Takuma Sasaki, Akihiro Fujii, and Keiji Yamagami pp 1063 - 1064; DOI: 10.1021/jm00401a001 |
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(.+-.)-4-tert-Butyl-3-cyano-1-(4-ethynylphenyl)-2,6,7-trioxabicyclo[2.2.2]octane: synthesis of a remarkably potent GABAA receptor antagonist Christopher J. Palmer, Loretta M. Cole, and John E. Casida pp 1064 - 1066; DOI: 10.1021/jm00401a002 |
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Novel antihypertensives targeted at dopamine .beta.-monooxygenase: turnover-dependent cofactor depletion by phenylaminoethylselenide Sheldon W. May, Kandatege Wimalasena, Heath H. Herman, Lydia C. Fowler, Melanie C. Ciccarello, and Stanley H. Pollock pp 1066 - 1068; DOI: 10.1021/jm00401a003 |
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Mapping of the .beta.2-adrenoceptor on Chang liver cells. Differences between high- and low-affinity receptor states G. M. Donne-Op den Kelder, T. Bultsma, H. Timmerman, and B. Rademaker pp 1069 - 1079; DOI: 10.1021/jm00401a004 |
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Occurrence and pharmacological significance of metabolic ortho-hydroxylation of 5- and 8-hydroxy-2-(di-n-propylamino)tetralin Haakan Wikstroem, Thomas Elebring, Gerd Hallnemo, Bengt Andersson, Kjell Svensson, Arvid Carlsson, and Hans Rollema pp 1080 - 1084; DOI: 10.1021/jm00401a005 |
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Protoberberine alkaloids as antimalarials Jonathan L. Vennerstrom and Daniel L. Klayman pp 1084 - 1087; DOI: 10.1021/jm00401a006 |
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Graphics computer-aided receptor mapping as a predictive tool for drug design: development of potent, selective, and stereospecific ligands for the 5-HT1A receptor Marcel F. Hibert, Maurice W. Gittos, Derek N. Middlemiss, Anis K. Mir, and John R. Fozard pp 1087 - 1093; DOI: 10.1021/jm00401a007 |
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Synthesis and interaction with uridine phosphorylase of 5'-deoxy-4',5-difluorouridine, a new prodrug of 5-fluorouracil Sudhir Ajmera, Ashok R. Bapat, Peter V. Danenberg, and Edic Stephanian pp 1094 - 1098; DOI: 10.1021/jm00401a008 |
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Synthesis and oral antiallergic activity of carboxylic acids derived from imidazo[2,1-c][1,4]benzoxazines, imidazo[1,2-a]quinolines, imidazo[1,2-a]quinoxalines, imidazo[1,2-a]quinoxalinones, pyrrolo[1,2-a]quinoxalinones, pyrrolo[2,3-a]quinoxalinones, and imidazo[2,1-b]benzothiazoles Ian R. Ager, Alan C. Barnes, Geoffrey W. Danswan, Peter W. Hairsine, David P. Kay, Peter D. Kennewell, Saroop S. Matharu, Peter Miller, Peter Robson, and et al. pp 1098 - 1115; DOI: 10.1021/jm00401a009 |
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6-(Alkylamino)-3-aryl-1,2,4-triazolo[3,4-a]phthalazines. A new class of benzodiazepine receptor ligands Giorgio Tarzia, Emilio Occelli, Emilio Toja, Domenico Barone, Nerina Corsico, Licia Gallico, and Franco Luzzani pp 1115 - 1123; DOI: 10.1021/jm00401a010 |
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Terminal bifunctional retinoids. Synthesis and evaluations related to cancer chemopreventive activity Y. Fulmer Shealy, Charles A. Krauth, James M. Riordan, and Brahma P. Sani pp 1124 - 1130; DOI: 10.1021/jm00401a011 |
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Central dopaminergic and 5-hydroxytryptaminergic effects of C(3)-methylated derivatives of 8-hydroxy-2-(di-n-propylamino)tetralin Charlotta Mellin, Lena Bjoerk, Anders Karlen, Anette M. Johansson, Staffan Sundell, Lennart Kenne, David L. Nelson, Nils Erik Anden, and Uli Hacksell pp 1130 - 1140; DOI: 10.1021/jm00401a012 |
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Linear free energy relationship studies of enzyme active site binding: thymidylate synthase George Chang, Douglas Schwepler, Charles J. Decedue, Jan Balzarini, Erik De Clercq, and Mathias P. Mertes pp 1141 - 1147; DOI: 10.1021/jm00401a013 |
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Angiotensin-converting enzyme inhibitors. Mercaptan, carboxyalkyl dipeptide, and phosphinic acid inhibitors incorporating 4-substituted prolines John Krapcho, Chester Turk, David W. Cushman, James R. Powell, Jack M. DeForrest, Ervin R. Spitzmiller, Donald S. Karanewsky, Mark Duggan, George Rovnyak, and et al. pp 1148 - 1160; DOI: 10.1021/jm00401a014 |
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Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis Tiiu Ojasoo, Jean Christophe Dore, Jacques Gilbert, and Jean Pierre Raynaud pp 1160 - 1169; DOI: 10.1021/jm00401a015 |
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Tricyclic compounds as selective antimuscarinics. 2. Structure-activity relationships of M1-selective antimuscarinics related to pirenzepine Wolfgang G. Eberlein, Wolfhard W. Engel, Guenter Trummlitz, Guenther Schmidt, and Rudolf Hammer pp 1169 - 1174; DOI: 10.1021/jm00401a016 |
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Derivatives of 2-methylenepropane-1,3-diol as new antagonists of platelet activating factor Gunnar Grue-Soerensen, Inger Mann Nielsen, and Christian Kaergaard Nielsen pp 1174 - 1178; DOI: 10.1021/jm00401a017 |
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Adenosine receptor agonists: synthesis and biological evaluation of 1-deaza analogs of adenosine derivatives Gloria Cristalli, Palmarisa Franchetti, Mario Grifantini, Sauro Vittori, Karl Norbert Klotz, and Martin J. Lohse pp 1179 - 1183; DOI: 10.1021/jm00401a018 |
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Synthetic polyamine analogs as antineoplastics Raymond J. Bergeron, Allen H. Neims, James S. McManis, Thomas R. Hawthorne, John R. T. Vinson, Rita Bortell, and Michael J. Ingeno pp 1183 - 1190; DOI: 10.1021/jm00401a019 |
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An examination of O-2-isocephems as orally absorbable antibiotics Harold Mastalerz, Marcel Menard, Vivianne Vinet, James Desiderio, Joan Fung-Tomc, Robert Kessler, and Yuan Tsai pp 1190 - 1196; DOI: 10.1021/jm00401a020 |
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Synthesis of ethyl 2-(4-chlorophenyl)-5-(2-furyl)-4-oxazoleacetate, a hypolipidemic agent, and related compounds Tamon Moriya, Masahiko Seki, Seiichi Takabe, Kazuo Matsumoto, Kohki Takashima, Tetsuji Mori, Akio Odawara, and Shigeyuki Takeyama pp 1197 - 1204; DOI: 10.1021/jm00401a021 |
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Synthesis and hypolipidemic activity of 2-substituted isobutyric acid derivatives Shinichi Morishita, Takashi Saito, Yasuharu Hirai, Masamichi Shoji, Yasuhiro Mishima, and Masato Kawakami pp 1205 - 1209; DOI: 10.1021/jm00401a022 |
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Chemical synthesis and biological activities of 5-deazaaminopterin analogs bearing substituent(s) at the 5- and/or 7-position(s) Tsann Long Su, Jai Tung Huang, Ting Chao Chou, Glenys M. Otter, Francis M. Sirotnak, and Kyoichi A. Watanabe pp 1209 - 1215; DOI: 10.1021/jm00401a023 |
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Substituted 2-[(2-benzimidazolylsulfinyl)methyl]anilines as potential inhibitors of H+/K+ ATPase Gilbert W. Adelstein, Chung H. Yen, Richard A. Haack, Stella Yu, Gary Gullikson, Doreen V. Price, Charles Anglin, Dennis L. Decktor, Henry Tsai, and Robert H. Keith pp 1215 - 1220; DOI: 10.1021/jm00401a024 |
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(Imidazo[1,2-a]pyrimidin-2-yl)phenylmethanones and related compounds as potential nonsedative anxiolytics Stephen Clements-Jewery, Geoffrey Danswan, Colin R. Gardner, Saroop S. Matharu, Robert Murdoch, W. Roger Tully, and Robert Westwood pp 1220 - 1226; DOI: 10.1021/jm00401a025 |
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The acylating potential of .gamma.-lactam antibacterials: base hydrolysis of bicyclic pyrazolidinones Joseph M. Indelicato and Carol E. Pasini pp 1227 - 1230; DOI: 10.1021/jm00401a026 |
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Molecular basis for bleomycin amplification: conformational and stereoelectronic effects in unfused amplifiers Lucjan Strekowski, Jerzy L. Mokrosz, Farial A. Tanious, Rebecca A. Watson, Donald Harden, Maria Mokrosz, W. Daniel Edwards, and W. David Wilson pp 1231 - 1240; DOI: 10.1021/jm00401a027 |
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Synthesis and testing of quinone-based bis(2,2-dimethyl-1-aziridinyl)phosphinyl carbamates as radiation-potentiating antitumor agents Shoufang Zhang, Julie Earle, Joan MacDiarmid, and Thomas J. Bardos pp 1240 - 1244; DOI: 10.1021/jm00401a028 |
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Synthesis and analgesic activity of pemedolac [cis-1-ethyl-1,3,4,9-tetrahydro-4-(phenylmethyl)pyrano[3,4-b]indole-1-acetic acid] Alan H. Katz, Christopher A. Demerson, Chia Cheng Shaw, Andre A. Asselin, Leslie G. Humber, Kimberly M. Conway, Gregory Gavin, Charles Guinosso, Norman P. Jensen, and et al. pp 1244 - 1250; DOI: 10.1021/jm00401a029 |
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Potential sweetening agents of plant origin. 13. An intensely sweet dihydroflavonol derivative based on a natural product lead compound N. P. Dhammika Nanayakkara, Raouf A. Hussain, John M. Pezzuto, D. Doel Soejarto, and A. Douglas Kinghorn pp 1250 - 1253; DOI: 10.1021/jm00401a030 |
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2,4-Dihydro-3H-1,2,4-triazole-3-thiones as potential antidepressant agents John M. Kane, Mark W. Dudley, Stephen M. Sorensen, and Francis P. Miller pp 1253 - 1258; DOI: 10.1021/jm00401a031 |
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Facile N-oxygenation of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine by the flavin-containing monooxygenase. A convenient synthesis of tritiated [methyl-3H]-4-phenyl-2,3-dihydropyridinium species John R. Cashman pp 1258 - 1261; DOI: 10.1021/jm00401a032 |
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C-Nor-9,11-secoestranes as modified estrogens and fertility regulation Kasturi Lal, Indra Sharma, A. K. Agarwal, Anila Agnihotri, and Suprabhat Ray pp 1261 - 1264; DOI: 10.1021/jm00401a033 |
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Book Reviews pp 1264 - 1268; DOI: 10.1021/jm00401a600 |
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Oxidants, oxidant drugs, and malaria Jonathan L. Vennerstrom and John W. Eaton pp 1269 - 1277; DOI: 10.1021/jm00402a001 |
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(.+-.)-9-Amino-1,2,3,4-tetrahydroacridin-1-ol. A potential Alzheimer's disease therapeutic of low toxicity Gregory M. Shutske, Frank A. Pierrat, Michael L. Cornfeldt, Mark R. Szewczak, Francis P. Huger, Gina M. Bores, Vahram Haroutunian, and Kenneth L. Davis pp 1278 - 1279; DOI: 10.1021/jm00402a002 |
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Methyl mercapturate episulfonium ion: a model reactive metabolite of dihaloethanes James G. Henkel and George S. Amato pp 1279 - 1282; DOI: 10.1021/jm00402a003 |
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N6-[2-(3,5-dimethoxyphenyl)-2-(2-methylphenyl)ethyl]adenosine and its uronamide derivatives. Novel adenosine agonists with both high affinity and high selectivity for the adenosine A2 receptor Alexander J. Bridges, Robert F. Bruns, Daniel F. Ortwine, Steven R. Priebe, Deedee L. Szotek, and Bharat K. Trivedi pp 1282 - 1285; DOI: 10.1021/jm00402a004 |
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Nonisomerizable analogs of (Z)- and (E)-4-hydroxytamoxifen. Synthesis and endocrinological properties of substituted diphenylbenzocycloheptenes Raymond McCague, Guy Leclercq, and V. Craig Jordan pp 1285 - 1290; DOI: 10.1021/jm00402a005 |
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Electrophysiologic and antiarrhythmic activities of 4-amino-N-[2-(diethylamino)ethyl]-3,5-dimethylbenzamide, a sterically hindered procainamide analog David W. Robertson, E. E. Beedle, Harve Wilson, C. John Parli, Jeffrey K. Smallwood, and Mitchell I. Steinberg pp 1290 - 1295; DOI: 10.1021/jm00402a006 |
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Synthesis and antitumor activity of quaternary ellipticine glycosides, a series of novel and highly active antitumor agents Tadashi Honda, Mika Kato, Minako Inoue, Tetsuo Shimamoto, Keiyuu Shima, Toshihiro Nakanishi, Takako Yoshida, and Teruhisa Noguchi pp 1295 - 1305; DOI: 10.1021/jm00402a007 |
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Dinucleotide analogs as inhibitors of thymidine kinase, thymidylate kinase and ribonucleotide reductase Lawrence C. Davies, John A. Stock, S. Elaine Barrie, Rosanne M. Orr, and Kenneth R. Harrap pp 1305 - 1308; DOI: 10.1021/jm00402a008 |
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Synthesis of the tumorigenic 3,4-dihydrodiol metabolites of dibenz[a,j]anthracene and 7,14-dimethyldibenz[a,j]anthracene Ronald G. Harvey, Cecilia Cortez, Thomas W. Sawyer, and John DiGiovanni pp 1308 - 1312; DOI: 10.1021/jm00402a009 |
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Heterocyclic muscarinic agonists. Synthesis and biological activity of some bicyclic sulfonium arecoline bioisosteres Per Sauerberg, Erik Falch, Eddi Meier, Hanne L. Lemboel, and Povl Krogsgaard-Larsen pp 1312 - 1316; DOI: 10.1021/jm00402a010 |
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2,3-Diarylindenes and 2,3-diarylindenones: synthesis, molecular structure, photochemistry, estrogen receptor binding affinity, and comparisons with related triarylethylenes Gregory M. Anstead, Robert J. Altenbach, Scott R. Wilson, and John A. Katzenellenbogen pp 1316 - 1326; DOI: 10.1021/jm00402a011 |
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Methotrexate analog. 32. Chain extension, .alpha.-carboxyl deletion, and .gamma. carboxyl replacement by sulfonate and phosphate. Effect on enzyme binding and cell-growth inhibition Andre Rosowsky, Ronald A. Forsch, Richard G. Moran, William Kohler, and James H. Freisheim pp 1326 - 1331; DOI: 10.1021/jm00402a012 |
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Methotrexate analogs. 33. N.delta.-Acyl-N.alpha.-(4-amino-4-deoxypteroyl)-L-ornithine derivatives. Synthesis and in vitro antitumor activity Andre Rosowsky, Henry Bader, Carol A. Cucchi, Richard G. Moran, William Kohler, and James H. Freisheim pp 1332 - 1337; DOI: 10.1021/jm00402a013 |
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Methotrexate analogs. 34. Replacement of the glutamate moiety in methotrexate and aminopterin by long-chain 2-aminoalkanedioic acids Andre Rosowsky, Henry Bader, William Kohler, James H. Freisheim, and Richard G. Moran pp 1338 - 1344; DOI: 10.1021/jm00402a014 |
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Stereochemical studies on medicinal agents. 31. Only one pharmacophore is required for the .kappa. opioid antagonist selectivity of norbinaltorphimine P. S. Portoghese, H. Nagase, and A. E. Takemori pp 1344 - 1347; DOI: 10.1021/jm00402a015 |
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7-Aminoquinolines. A novel class of agents active against herpes viruses Mohamed Nasr, John C. Drach, Sandra H. Smith, Charles Shipman, and J. H. Burckhalter pp 1347 - 1351; DOI: 10.1021/jm00402a016 |
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Synthesis and antiviral activity of novel N-substituted derivatives of acyclovir Jerzy Boryski, Bozenna Golankiewicz, and Erik De Clercq pp 1351 - 1355; DOI: 10.1021/jm00402a017 |
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cis-4-Carboxy-6-(mercaptomethyl)-3,4,5,6-tetrahydropyrimidin-2(1H)-one, a potent inhibitor of mammalian dihydroorotase Jerry L. Adams, Thomas D. Meek, Shau Ming Mong, Randall K. Johnson, and Brian W. Metcalf pp 1355 - 1359; DOI: 10.1021/jm00402a018 |
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21-[18F]fluoro-16.alpha.-ethyl-19-norprogesterone. Synthesis and target tissue selective uptake of a progestin receptor-based radiotracer for positron emission tomography Martin G. Pomper, John A. Katzenellenbogen, Michael J. Welch, James W. Brodack, and Carla J. Mathias pp 1360 - 1363; DOI: 10.1021/jm00402a019 |
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Cardiotonic agents. Synthesis and inotropic activity of a series of isoquinolin-3-ol derivatives Ramesh M. Kanojia, Jeffery B. Press, O. William Lever, Louella Williams, James J. McNally, Alfonso J. Tobia, Robert Falotico, and John B. Moore pp 1363 - 1368; DOI: 10.1021/jm00402a020 |
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Conformationally constrained renin inhibitory peptides: .gamma.-lactam-bridged dipeptide isostere as conformational restriction Suvit Thaisrivongs, Donald T. Pals, Steve R. Turner, and Lisa T. Kroll pp 1369 - 1376; DOI: 10.1021/jm00402a021 |
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Synthesis and renin inhibitory activity of angiotensinogen analogs having dehydrostatine, Lue.psi.[CH2S]Val, or Lue.psi.[CH2SO] Val at the Pt, P1' cleavage site Clark W. Smith, Hossain H. Saneii, Tomi K. Sawyer, Donald T. Pals, Terrence A. Scahill, Bharat V. Kamdar, and Judy A. Lawson pp 1377 - 1382; DOI: 10.1021/jm00402a022 |
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Polycyclic aryl- and heteroarylpiperazinyl imides as 5-HT1A receptor ligands and potential anxiolytic agents: synthesis and structure-activity relationship studies Magid Abou-Gharbia, Usha R. Patel, Michael B. Webb, John A. Moyer, Terrance H. Andree, and Eric A. Muth pp 1382 - 1392; DOI: 10.1021/jm00402a023 |
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Synthesis and dopamine agonist and antagonist effects of (R)-(-)- and (S)-(+)-11-hydroxy-N-n-propylnoraporphine Yigong Gao, Rushi Zong, Alexander Campbell, Nora S. Kula, Ross J. Baldessarini, and John L. Neumeyer pp 1392 - 1396; DOI: 10.1021/jm00402a024 |
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The hypothetical active site lattice. An approach to modelling active sites from data on inhibitor molecules Arthur M. Doweyko pp 1396 - 1406; DOI: 10.1021/jm00402a025 |
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Synthesis and serotonin receptor affinities of a series of enantiomers of .alpha.-methyltryptamines: evidence for the binding conformation of tryptamines at serotonin 5-HT1B receptors David E. Nichols, David H. Lloyd, Michael P. Johnson, and Andrew J. Hoffman pp 1406 - 1412; DOI: 10.1021/jm00402a026 |
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The absolute configurations and pharmacological activities of the optical isomers of fluoxetine, a selective serotonin-uptake inhibitor David W. Robertson, Joseph H. Krushinski, Ray W. Fuller, and J. David Leander pp 1412 - 1417; DOI: 10.1021/jm00402a027 |
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Importance of the N-terminal domain of the type II angiotensin antagonist sarmesin for receptor blockade John Matsoukas, Paul Cordopatis, Urania Belte, Mahesh H. Goghari, Renee C. Ganter, Kevin J. Franklin, and Graham J. Moore pp 1418 - 1421; DOI: 10.1021/jm00402a028 |
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Synthesis and structure-activity relationships of 2-sulfonamido-1,3,4,6,7,11b.alpha.-hexahydro-2H-benzo[a]quinolizines as .alpha.2-adrenoceptor antagonists Terence J. Ward, John F. White, Norman Lattimer, Keith F. Rhodes, Shobna Sharma, and John F. Waterfall pp 1421 - 1426; DOI: 10.1021/jm00402a029 |
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Synthesis and antineoplastic activity of 5-aryl-2,3-dihydropyrrolo[2,1-b]thiazole-6,7-dimethanol 6,7-bis(isopropylcarbamates) Iraj Lalezari and Edward L. Schwartz pp 1427 - 1429; DOI: 10.1021/jm00402a030 |
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Dopamine receptor modulation by conformationally constrained analogs of Pro-Leu-Gly-NH2 Kuo Long Yu, G. Rajakumar, Lalit K. Srivastava, Ram K. Mishra, and Rodney L. Johnson pp 1430 - 1436; DOI: 10.1021/jm00402a031 |
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Synthetic aci-reductones. 3,4-Dihydroxy-2H-1-benzopyran-2-ones and their cis- and trans-4a,5,6,7,8,8a-hexahydro diastereomers. Antiaggregatory, antilipidemic, and redox properties compared to the 4-substituted 2-hydroxytetronic acids Donald T. Witiak, Sung K. Kim, Ashok K. Tehim, Kent D. Sternitzke, Richard L. McCreery, Sung U. Kim, Dennis R. Feller, Karl J. Romstedt, Vaijinath S. Kamanna, and Howard A. I. Newman pp 1437 - 1445; DOI: 10.1021/jm00402a032 |
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Predictive structure-activity relationships in a series of pyranoquinoline derivatives. A new primate model for the identification of antiallergic activity Ken J. Gould, Carol N. Manners, David W. Payling, John L. Suschitzky, and Edward Wells pp 1445 - 1453; DOI: 10.1021/jm00402a033 |
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4-Hydroxy-3-quinolinecarboxamides with antiarthritic and analgesic activities Francois Clemence, Odile Le Martret, Francoise Delevallee, Josette Benzoni, Alain Jouanen, Simone Jouquey, Michel Mouren, and Roger Deraedt pp 1453 - 1462; DOI: 10.1021/jm00402a034 |
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Affinity and selectivity of the optical isomers of 3-quinuclidinyl benzilate and related muscarinic antagonists W. Janusz Rzeszotarski, Daniel W. McPherson, John W. Ferkany, William J. Kinnier, Lalita Noronha-Blob, and Alicja Kirkien-Rzeszotarski pp 1463 - 1466; DOI: 10.1021/jm00402a035 |
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Preparation of 7-oxaaporphine derivatives and evaluation of their dopaminergic activity Carlo Banzatti, Nicola Carfagna, Roberto Commisso, Franco Heidempergher, Lorenzo Pegrassi, and Piero Melloni pp 1466 - 1471; DOI: 10.1021/jm00402a036 |
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Synthesis and estrogen receptor selectivity of 1,1-bis(4-hydroxyphenyl)-2-(p-halophenyl)ethylenes Peter C. Ruenitz, Jerome R. Bagley, and Nitin T. Nanavati pp 1471 - 1475; DOI: 10.1021/jm00402a037 |
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1-(2,3-Anhydro-.beta.-D-lyxofuranosyl)cytosine derivatives as potential inhibitors of the human immunodeficiency virus Thomas R. Webb, Hiroaki Mitsuya, and Samuel Broder pp 1475 - 1479; DOI: 10.1021/jm00402a038 |
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Syntheses and gastric acid antisecretory properties of the H2-receptor antagonist N-[3-[3-(1-piperidinylmethyl)phenoxy]propyl]thieno[3,4-d]isothiazol-3-amine 1,1-dioxide and related derivatives Arthur A. Santilli, Anthony C. Scotese, Robert L. Morris, Guy A. Schiehser, Daniel M. Teller, Susan T. Nielsen, and Donald P. Strike pp 1480 - 1486; DOI: 10.1021/jm00402a039 |
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Dicarbavasopressin antagonist analogs exhibit reduced in vivo agonist activity Michael L. Moore, Christine Albrightson, Bridget Brickson, Heidemarie G. Bryan, Nancy Caldwell, James F. Callahan, Jonathan Foster, Lewis B. Kinter, Kenneth A. Newlander, and et al. pp 1487 - 1489; DOI: 10.1021/jm00403a001 |
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Dimeric 1,4-dihydropyridines as calcium channel antagonists Alan F. Joslyn, Elizabeth Luchowski, and David J. Triggle pp 1489 - 1492; DOI: 10.1021/jm00403a002 |
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Decomposition of N-(2-chloroethyl)-N-nitrosocarbamoyl amino acid amides Helga Suli-Vargha, Jozsef Bodi, Miomir Meszaros, and Kalman Medzihradszky pp 1492 - 1495; DOI: 10.1021/jm00403a003 |
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N2-Phenyldeoxyguanosine: a novel selective inhibitor of herpes simplex thymiding kinase Federico Focher, Catherine Hildebrand, Stephen Freese, Giovanni Ciarrocchi, Timothy Noonan, Stefano Sangalli, Neal Brown, Silvio Spadari, and George Wright pp 1496 - 1500; DOI: 10.1021/jm00403a004 |
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Synthesis and antiviral activity of certain 4-substituted and 2,4-disubstituted 7-[(2-hydroxyethoxy)methyl]pyrrolo[2,3-d]pyrimidines Naveen K. Saxena, Brenda M. Hagenow, Gail Genzlinger, Steven R. Turk, John C. Drach, and Leroy B. Townsend pp 1501 - 1506; DOI: 10.1021/jm00403a005 |
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Synthesis and thromboxane A2 antagonist activity of N-benzyltrimetoquinol analogs Marc W. Harrold, Barbara Grajzl, Yangmee Shin, Karl J. Romstedt, Dennis R. Feller, and Duane D. Miller pp 1506 - 1512; DOI: 10.1021/jm00403a006 |
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Ergolines as selective 5-HT1 agonists John S. Ward, Ray W. Fuller, Leander Merritt, Harold D. Snoddy, Jonathan W. Paschal, Norman R. Mason, and J. S. Horng pp 1512 - 1519; DOI: 10.1021/jm00403a007 |
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Semisynthetic pyrrolizidine alkaloid N-oxide antitumor agents. Esters of heliotridine Leon H. Zalkow, Jan A. Glinski, Leslie T. Gelbaum, David Moore, Deborah Melder, and Garth Powis pp 1520 - 1526; DOI: 10.1021/jm00403a008 |
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Benzothiopyranoindazoles, a new class of chromophore modified anthracenedione anticancer agents. Synthesis and activity against murine leukemias H. D. Hollis Showalter, Mario M. Angelo, Ellen M. Berman, Gerald D. Kanter, Daniel F. Ortwine, Suzanne G. Ross-Kesten, Anthony D. Sercel, William R. Turner, Leslie M. Werbel, and et al. pp 1527 - 1539; DOI: 10.1021/jm00403a009 |
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Enantiomers of 7-(2,3-epoxypropoxy)actinomycin D as dual-action DNA-acting antitumor agents Sisir K. Sengupta, David P. Rosenbaum, Raj K. Sehgal, Bijan Almassian, and Joanne Blondin pp 1540 - 1547; DOI: 10.1021/jm00403a010 |
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Substituted benzamides. 1. Potential nondopaminergic antagonists of chemotherapy-induced nausea and emesis Ivo Monkovic, David Willner, Michael A. Adam, Myron Brown, R. R. Crenshaw, Carl E. Fuller, Peter F. Juby, George M. Luke, John A. Matiskella, and Thomas A. Montzka pp 1548 - 1558; DOI: 10.1021/jm00403a011 |
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Stereoisomers of allenic amines as inactivators of monoamine oxidase type B. Stereochemical probes of the active site Roger A. Smith, Robert L. White, and Allen Krantz pp 1558 - 1566; DOI: 10.1021/jm00403a012 |
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1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine analogs. Inactivation of monoamine oxidase by conformationally rigid analogs of N,N-dimethylcinnamylamine Charles K. Hiebert and Richard B. Silverman pp 1566 - 1570; DOI: 10.1021/jm00403a013 |
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Synthesis, configuration, and evaluation of two conformationally restrained analogs of phencyclidine Brian R. De Costa, Clifford George, Terrence R. Burke, Michael F. Rafferty, Patricia C. Contreras, Stephen J. Mick, Arthur E. Jacobson, and Kenner C. Rice pp 1571 - 1575; DOI: 10.1021/jm00403a014 |
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Nucleosides of 1,4-thiazin-3-one and derivatives as tetrahedral intermediate analogs of enzymes in pyrimidine nucleoside metabolism E. Ted Marcus, Afaf Gundy, Corey H. Levenson, and Rich B. Meyer pp 1575 - 1579; DOI: 10.1021/jm00403a015 |
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Nucleotide derivatives of 2,7-diaminomitosene Bhashyam S. Iyengar, Robert T. Dorr, William A. Remers, and Charles D. Kowal pp 1579 - 1585; DOI: 10.1021/jm00403a016 |
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Asymmetric synthesis and properties of the enantiomers of the antibacterial agent 7-(3-aminopyrrolidin-1-yl)-1-(2,4-difluorophenyl)-1,4-dihydro-6-fluoro-4-oxo-1,8-naphthyridine-3-carboxylic acid hydrochloride Terry Rosen, Daniel T. W. Chu, Isabella M. Lico, Prabhavathi B. Fernandes, Linus Shen, Saul Borodkin, and Andre G. Pernet pp 1586 - 1590; DOI: 10.1021/jm00403a017 |
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Imidazo[1,2-a]pyrimidines and imidazo[1,2-a]pyrazines: the role of nitrogen position in inotropic activity Wayne A. Spitzer, Frantz Victor, G. Don Pollock, and J. Scott Hayes pp 1590 - 1595; DOI: 10.1021/jm00403a018 |
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Deletion sequences of salmon calcitonin that retain the essential biological and conformational features of the intact molecule Richard M. Epand, Raquel F. Epand, Alan R. Stafford, and Ronald C. Orlowski pp 1595 - 1598; DOI: 10.1021/jm00403a019 |
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Design, synthesis, and properties of (4S)-7-(4-amino-2-substituted-pyrrolidin-1-yl)quinolone-3-carboxylic acids Terry Rosen, Daniel T. W. Chu, Isabella M. Lico, Prabhavathi B. Fernandes, Kennan Marsh, Linus Shen, Valerie G. Cepa, and Andre G. Pernet pp 1598 - 1611; DOI: 10.1021/jm00403a020 |
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Conformations of complexes between mitomycins and decanucleotides. 3. Sequence specificity, binding at C-10, and mitomycin analogs William A. Remers, Shashidhar N. Rao, Timothy P. Wunz, and Peter A. Kollman pp 1612 - 1620; DOI: 10.1021/jm00403a021 |
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Dopamine autoreceptor agonists as potential antipsychotics. 1. (Aminoalkoxy)anilines Juan C. Jaen, Lawrence D. Wise, Thomas G. Heffner, Thomas A. Pugsley, and Leonard T. Meltzer pp 1621 - 1625; DOI: 10.1021/jm00403a022 |
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Synthesis, pharmacological action, and receptor binding affinity of the enantiomeric 1-(1-phenyl-3-methylcyclohexyl)piperidines Andrew Thurkauf, Paul Hillery, Mariena V. Mattson, Arthur E. Jacobson, and Kenner C. Rice pp 1625 - 1628; DOI: 10.1021/jm00403a023 |
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Studies on some derivatives of oxamniquine Wageeh El-Hamouly, Livia Pica-Mattoccia, Donato Cioli, Herbert M. Schwartz, and Sydney Archer pp 1629 - 1631; DOI: 10.1021/jm00403a024 |
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Synthesis and evaluation of tylosin-related macrolides modified at the aldehyde function: a new series of orally effective antibiotics Herbert A. Kirst, John E. Toth, Manuel Debono, Kevin E. Willard, Brenda A. Truedell, John L. Ott, Fred T. Counter, Anna M. Felty-Duckworth, and Robert S. Pekarek pp 1631 - 1641; DOI: 10.1021/jm00403a025 |
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Nucleosides. 150. Synthesis and some biological properties of 5-monofluoromethyl, 5-difluoromethyl, and 5-trifluoromethyl derivatives of 2'-deoxyuridine and 2'-deoxy-2'-fluoro-.beta.-D-arabinofuranosyluracil Jasenka Matulic-Adamic, Kiyobumi Takahashi, Ting Chao Chou, Hakan Gadler, Richard W. Price, Kyoichi A. Watanabe, A. R. Venugopala Reddy, and Thomas I. Kalman pp 1642 - 1647; DOI: 10.1021/jm00403a026 |
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Substrate analog inhibitors of the IgA1 proteinases from Neisseria gonorrhoeae James Burton, Stephen G. Wood, Mary Lynch, and Andrew G. Plaut pp 1647 - 1651; DOI: 10.1021/jm00403a027 |
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Soft drugs. 7. Soft .beta.-blockers for systemic and ophthalmic use Nicholas Bodor, Alaaeldin A. El-Koussi, Masanobu Kano, and Mohamed M. Khalifa pp 1651 - 1656; DOI: 10.1021/jm00403a028 |
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Effects of sulfur-containing analogs of stearic acid on growth and fatty acid biosynthesis in the protozoan Crithidia fasciculata Mohammad D. Rahman, David L. Ziering, Sara J. Mannarelli, Karen L. Swartz, Ded Shih Huang, and Robert A. Pascal pp 1656 - 1659; DOI: 10.1021/jm00403a029 |
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2-(2-Aryl-2-oxoethylidene)-1,2,3,4-tetrahydropyridines. Novel isomers of 1,4-dihydropyridine calcium channel blockers Michael D. Taylor, Edward W. Badger, Robert P. Steffen, Stephen J. Haleen, Thomas A. Pugsley, Yu Hsin Shih, and Ronald E. Weishaar pp 1659 - 1664; DOI: 10.1021/jm00403a030 |
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Book Reviews pp 1665 - 1668; DOI: 10.1021/jm00403a600 |