An editor's commentary on the birth of a journal Alfred Burger pp 2 - 6; DOI: 10.1021/jm00105a001 |
Synthesis and antiarrhythmic activity of .alpha.-[(diarylmethoxy)methyl]-1-piperidineethanols Milton L. Hoefle, L. T. Blouin, R. W. Fleming, S. Hastings, J. M. Hinkley, T. E. Mertz, T. J. Steffe, C. S. Stratton, and L. M. Werbel pp 7 - 12; DOI: 10.1021/jm00105a002 |
Synthesis and antiarrhythmic activity of cis-2,6-dimethyl-.alpha.,.alpha.-diaryl-1-piperidinebutanols M. L. Hoefle, L. T. Blouin, R. W. Fleming, S. Hastings, J. M. Hinkley, T. E. Mertz, T. J. Steffe, and C. S. Stratton pp 12 - 19; DOI: 10.1021/jm00105a003 |
Long-acting dihydropyridine calcium antagonists. 6. Structure-activity relationships around 4-(2,3-dichlorophenyl)-3-(ethoxycarbonyl)-2-[(2-hydroxyethoxy)methyl]-5-(methoxycarbonyl)-6-methyl-1,4-dihydropyridine David Alker, Simon F. Campbell, and Peter E. Cross pp 19 - 24; DOI: 10.1021/jm00105a004 |
(R)- and (S)-enantiomers of 11-hydroxy- and 10,11-dihydroxy-N-allylnoraporphine: synthesis and affinity for dopamine receptors in rat brain tissue John L. Neumeyer, Nora S. Kula, Ross J. Baldessarini, and Yigong Gao pp 24 - 28; DOI: 10.1021/jm00105a005 |
Fluoronaphthyridines and -quinolones as antibacterial agents. 3. Synthesis and structure-activity relationships of new 1-(1,1-dimethyl-2-fluoroethyl), 1-[1-methyl-1-(fluoromethyl)-2-fluoroethyl], and 1-[1,1-(difluoromethyl)-2-fluoroethyl] substituted derivatives P. Remuzon, D. Bouzard, P. Di Cesare, M. Essiz, J. P. Jacquet, J. R. Kiechel, B. Ledoussal, R. E. Kessler, and J. Fung-Tomc pp 29 - 37; DOI: 10.1021/jm00105a006 |
Heterocyclic quinones. XVII. A new in vivo active antineoplastic drug: 6,7-bis(1-aziridinyl)-4-[[3-(N,N-dimethylamino)propyl]amino]-5,8-quinazolinedione Sylviane Giorgi-Renault, Jean Renault, Patricia Gebel-Servolles, Michel Baron, Claude Paoletti, Suzanne Cros, Marie Christine Bissery, Francois Lavelle, and Ghanem Atassi pp 38 - 46; DOI: 10.1021/jm00105a007 |
Optimization of hydrophobic and hydrophilic substituent interactions of 2,4-diamino-5-(substituted-benzyl)pyrimidines with dihydrofolate reductase Cynthia Dias Selassie, Ren-li Li, Martin Poe, and Corwin Hansch pp 46 - 54; DOI: 10.1021/jm00105a008 |
Stereoselective reactions. XVII. Absolute structure-cytotoxic activity relationships of steganacin congeners and analogs Kiyoshi Tomioka, Tsuneo Ishiguro, Hidemichi Mizuguchi, Nobuyasu Komeshima, Kenji Koga, Shigeru Tsukagoshi, Takashi Tsuruo, Tazuko Tashiro, Seiichi Tanida, and Toyokazu Kishi pp 54 - 57; DOI: 10.1021/jm00105a009 |
Synthesis and antiviral activity of 9-alkoxypurines. 2. 9-(2,3-Dihydroxypropoxy)-, 9-(3,4-dihydroxybutoxy)-, and 9-(1,4-dihydroxybut-2-oxy)purines Stuart Bailey, Michael R. Harnden, Richard L. Jarvest, Ann Parkin, and Malcolm R. Boyd pp 57 - 65; DOI: 10.1021/jm00105a010 |
Synthesis and structure-activity relationships of benzo[b]thienylallylamine antimycotics Peter Nussbaumer, Gabor Petranyi, and Anton Stuetz pp 65 - 73; DOI: 10.1021/jm00105a011 |
Design of potent protein kinases inhibitors using the bisubstrate approach A. Ricouart, J. C. Gesquiere, A. Tartar, and C. Sergheraert pp 73 - 78; DOI: 10.1021/jm00105a012 |
(Acyloxy)alkyl carbamate prodrugs of norfloxacin Jose Alexander, Robert A. Fromtling, Judith A. Bland, Barbara A. Pelak, and Evamarie C. Gilfillan pp 78 - 81; DOI: 10.1021/jm00105a013 |
A new ionizable chromophore of 1,4-bis(alkylamino)benzo[g]phthalazine which interacts with DNA by intercalation Miquel Pons, L. Campayo, M. A. Martinez-Balbas, F. Azorin, P. Navarro, and E. Giralt pp 82 - 86; DOI: 10.1021/jm00105a014 |
Nicotinamide ethers: novel inhibitors of calcium-independent phosphodiesterase and [3H]rolipram binding Fredric J. Vinick, Nicholas A. Saccomano, B. Kenneth Koe, Jann A. Nielsen, Ian H. Williams, Peter F. Thadeio, Stanley Jung, Morgan Meltz, Jonathan Johnson Jr., Lorraine A. Lebel, Lorena L. Russo, and David Helweg pp 86 - 89; DOI: 10.1021/jm00105a015 |
4-(Tetrazolylalkyl)piperidine-2-carboxylic acids. Potent and selective N-methyl-D-aspartic acid receptor antagonists with a short duration of action Paul L. Ornstein, Darryle D. Schoepp, M. Brian Arnold, J. David Leander, David Lodge, Jonathan W. Paschal, and Tom Elzey pp 90 - 97; DOI: 10.1021/jm00105a016 |
Synthesis of water-soluble (aminoalkyl)camptothecin analogs: inhibition of topoisomerase I and antitumor activity William D. Kingsbury, Jeffrey C. Boehm, Dalia R. Jakas, Kenneth G. Holden, Sidney M. Hecht, Gregory Gallagher, Mary Jo Caranfa, Francis L. McCabe, Leo F. Faucette, Randall K. Johnson, and Robert P. Hertzberg pp 98 - 107; DOI: 10.1021/jm00105a017 |
Novel, potent aldose reductase inhibitors: 3,4-dihydro-4-oxo-3-[[5-(trifluoromethyl)-2-benzothiazolyl]methyl]-1-phthalazineacetic acid (zopolrestat) and congeners Banavara L. Mylari, Eric R. Larson, Thomas A. Beyer, William J. Zembrowski, Charles E. Aldinger, Michael F. Dee, Todd W. Siegel, and David H. Singleton pp 108 - 122; DOI: 10.1021/jm00105a018 |
Novel class of amino acid antagonists at non-N-methyl-D-aspartic acid excitatory amino acid receptors. Synthesis, in vitro and in vivo pharmacology, and neuroprotection Povl Krogsgaard-Larsen, John W. Ferkany, Elsebet O. Nielsen, Ulf Madsen, Bjarke Ebert, Joergen S. Johansen, Nils H. Diemer, Torben Bruhn, David T. Beattie, and David R. Curtis pp 123 - 130; DOI: 10.1021/jm00105a019 |
Three-dimensional structure-activity relationships and receptor mapping of N1-substituents of quinolone antibacterials Masateru Ohta and Hiroshi Koga pp 131 - 139; DOI: 10.1021/jm00105a020 |
Novel 5-HT3 antagonists. Indole oxadiazoles C. J. Swain, R. Baker, C. Kneen, J. Moseley, J. Saunders, E. M. Seward, G. Stevenson, M. Beer, J. Stanton, and K. Watling pp 140 - 151; DOI: 10.1021/jm00105a021 |
1,2,4-Triazolo[4,3-a]pyrazine derivatives with human renin inhibitory activity. 3. Synthesis and biological properties of aminodeoxystatine and difluorostatone derivatives Robert H. Bradbury and Janet E. Rivett pp 151 - 157; DOI: 10.1021/jm00105a022 |
Synthesis and antirhinovirus activity of 8-substituted analogs of 6-(dimethylamino)-9-(4-methylbenzyl)-2-(trifluoromethyl)-9H-purine James L. Kelley, James A. Linn, and J. W. T. Selway pp 157 - 160; DOI: 10.1021/jm00105a023 |
Synthesis and biological evaluation of cyclopropyl analogs of 2-amino-5-phosphonopentanoic acid Michael S. Dappen, Roberto Pellicciari, Benedetto Natalini, Joseph B. Monahan, Claudio Chiorri, and Alex A. Cordi pp 161 - 168; DOI: 10.1021/jm00105a024 |
Synthesis, antibacterial activities, and pharmacological properties of enantiomers of temafloxacin hydrochloride Daniel T. W. Chu, Carl W. Nordeen, Dwight J. Hardy, Robert N. Swanson, William J. Giardina, Andre G. Pernet, and Jacob J. Plattner pp 168 - 174; DOI: 10.1021/jm00105a025 |
Synthesis and biological evaluation of dipeptidyl and tripeptidyl polyoxin and nikkomycin analogs as anticandidal prodrugs Eduardo Krainer, Jeffrey M. Becker, and Fred Naider pp 174 - 180; DOI: 10.1021/jm00105a026 |
2-(3,4-Dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted-ethyl]-acetamides: the use of conformational analysis in the development of a novel series of potent opioid .kappa. agonists Gerard F. Costello, Roger James, John S. Shaw, Anthony M. Slater, and Neil C. J. Stutchbury pp 181 - 189; DOI: 10.1021/jm00105a027 |
Highly selective .kappa. opioid analgesics. 4. Synthesis of some conformationally restricted naphthalene derivatives with high receptor affinity and selectivity Paul R. Halfpenny, David C. Horwell, John Hughes, Christine Humblet, John C. Hunter, David C. Rees, and David Neuhaus pp 190 - 194; DOI: 10.1021/jm00105a028 |
Common stereospecificity of opioid and dopamine systems for N-butyrophenone prodine-like compounds M. A. Iorio, V. Frigeni, E. R. Bowman, L. S. Harris, E. L. May, and Mario D. Aceto pp 194 - 197; DOI: 10.1021/jm00105a029 |
Aldophosphamide acetal diacetate and structural analogs: synthesis and cytotoxicity studies Yuqiang Wang and David Farquhar pp 197 - 203; DOI: 10.1021/jm00105a030 |
Analogs of methotrexate and aminopterin with .gamma.-methylene and .gamma.-cyano substitution of the glutamate side chain: synthesis and in vitro biological activity. 40 Andre Rosowsky, Henry Bader, and James H. Freisheim pp 203 - 208; DOI: 10.1021/jm00105a031 |
Synthesis of two cyclopentenyl-3-deazapyrimidine carbocyclic nucleosides related to cytidine and uridine Richard R. Copp and Victor E. Marquez pp 208 - 212; DOI: 10.1021/jm00105a032 |
Potential anti-AIDS agents. Synthesis and antiviral activity of naphthalenesulfonic acid derivatives against HIV-1 and HIV-2 Prem Mohan, Rajendra Singh, and Masanori Baba pp 212 - 217; DOI: 10.1021/jm00105a033 |
Potential antitumor agents. 61. Structure-activity relationships for in vivo colon 38 activity among disubstituted 9-oxo-9H-xanthene-4-acetic acids Gordon W. Rewcastle, Graham J. Atwell, Li Zhuang, Bruce C. Baguley, and William A. Denny pp 217 - 222; DOI: 10.1021/jm00105a034 |
Folate analogs. 34. Synthesis and antitumor activity of non-polyglutamylatable inhibitors of dihydrofolate reductase Ann Abraham, J. J. McGuire, John Galivan, Zenia Nimec, R. L. Kisliuk, Y. Gaumont, and M. G. Nair pp 222 - 227; DOI: 10.1021/jm00105a035 |
Synthesis and biological activity of the 2-desamino and 2-desamino-2-methyl analogs of aminopterin and methotrexate Andre Rosowsky, Ronald A. Forsch, Richard G. Moran, and James H. Freisheim pp 227 - 234; DOI: 10.1021/jm00105a036 |
Nucleosides and nucleotides. 94. Radical deoxygenation of tert-alcohols in 1-(2-C-alkylpentofuranosyl)pyrimidines: synthesis of (2'S)-2'-deoxy-2'-C-methylcytidine, an antileukemic nucleoside Akira Matsuda, Kenji Takenuki, Takuma Sasaki, and Tohru Ueda pp 234 - 239; DOI: 10.1021/jm00105a037 |
Synthesis and evaluation of DNA-targeted spatially separated bis(aniline mustards) as potential alkylating agents with enhanced DNA cross-linking capability Trudi A. Gourdie, A. S. Prakash, Laurence P. G. Wakelin, Paul D. Woodgate, and William A. Denny pp 240 - 248; DOI: 10.1021/jm00105a038 |
Dopamine autoreceptor agonists as potential antipsychotics. 2. (Aminoalkoxy)-4H-1-benzopyran-4-ones Juan C. Jaen, Lawrence D. Wise, Thomas G. Heffner, Thomas A. Pugsley, and Leonard T. Meltzer pp 248 - 256; DOI: 10.1021/jm00105a039 |
A cardioselective, hydrophilic N,N,N-trimethylethanaminium .alpha.-tocopherol analog that reduces myocardial infarct size J. Martin Grisar, Margaret A. Petty, Frank N. Bolkenius, James Dow, Joseph Wagner, Eugene R. Wagner, Klaus D. Haegele, and Wybren De Jong pp 257 - 260; DOI: 10.1021/jm00105a040 |
Antidopaminergic effects of the stereoisomers of N-[(1-alkyl-2-pyrrolidinyl)methyl]-5-sulfamoylbenzamides and -2,3-dihydro-benzofuran-7-carboxamides Shu Murakami, Nobuhiro Marubayashi, Takemi Fukuda, Shuzo Takehara, and Tetsuya Tahara pp 261 - 267; DOI: 10.1021/jm00105a041 |
Dual inhibitors of thromboxane A2 synthase and 5-lipoxygenase with scavenging activity of active oxygen species (AOS). Synthesis of a novel series of (3-pyridylmethyl)benzoquinone derivatives Shigenori Ohkawa, Shinji Terao, Zenichi Terashita, Yumiko Shibouta, and Kohei Nishikawa pp 267 - 276; DOI: 10.1021/jm00105a042 |
2,3-Dihydrobenzofuran analogs of hallucinogenic phenethylamines David E. Nichols, Scott E. Snyder, Robert Oberlender, Michael P. Johnson, and Xuemei Huang pp 276 - 281; DOI: 10.1021/jm00105a043 |
Synthesis and benzodiazepine binding activity of a series of novel [1,2,4]triazolo[1,5-c]quinazolin-5(6H)-ones John E. Francis, William D. Cash, Beverly S. Barbaz, Patrick S. Bernard, Richard A. Lovell, Gerard C. Mazzenga, Robert C. Friedmann, James L. Hyun, Albert F. Braunwalder, and et al. pp 281 - 290; DOI: 10.1021/jm00105a044 |
Calcium-independent phosphodiesterase inhibitors as putative antidepressants: [3-(bicycloalkyloxy)-4-methoxyphenyl-2-imidazolidinones Nicholas A. Saccomano, Frederic J. Vinick, B. Kenneth Koe, Jann A. Nielsen, William M. Whalen, Morgan Meltz, Douglas Phillips, Peter F. Thadieo, Stanley Jung, Douglas C. Chapin, Lorraine A. Lebel, Lorena L. Russo, David L. Helweg, Jonathan L. Johnson, Jr., Jeffery L. Ives, and Ian H. Williams pp 291 - 298; DOI: 10.1021/jm00105a045 |
Antioxidant activity of probucol and its analogs in hypercholesterolemic Watanabe rabbits Simon J. T. Mao, Mark T. Yates, Ann E. Rechtin, Richard L. Jackson, and William A. Van Sickle pp 298 - 302; DOI: 10.1021/jm00105a046 |
trans-Hexahydroindolo[4,3-ab]phenanthridines ("benzergolines"), the first structural class of potent and selective dopamine D1 receptor agonists lacking a catechol group Max P. Seiler, Alexander Hagenbach, Hans Juerg Wuethrich, and Rudolf Markstein pp 303 - 307; DOI: 10.1021/jm00105a047 |
N-[(.omega.-Amino-1-hydroxyalkyl)phenyl]methanesulfonamide derivatives with class III antiarrhythmic activity Jackson B. Hester, J. Kenneth Gibson, Madeline G. Cimini, D. Edward Emmert, Paula K. Locker, Salvatore C. Perricone, Louis L. Skaletzky, Julie K. Sykes, and Bruce E. West pp 308 - 315; DOI: 10.1021/jm00105a048 |
Boron-containing thiouracil derivatives for neutron-capture therapy of melanoma Werner Tjarks and Detlef Gabel pp 315 - 319; DOI: 10.1021/jm00105a049 |
Substituted dihydrobenzopyran and dihydrobenzofuran thiazolidine-2,4-diones as hypoglycemic agents David A. Clark, Steven W. Goldstein, Robert A. Volkmann, James F. Eggler, Gerald F. Holland, Bernard Hulin, Ralph W. Stevenson, David K. Kreutter, E. Michael Gibbs, and et al. pp 319 - 325; DOI: 10.1021/jm00105a050 |
Chemical and biological studies on a series of lipid-soluble (trans-(R,R)- and -(S,S)-1,2-diaminocyclohexane)platinum(II) complexes incorporated in liposomes Abdul R. Khokhar, Salaam Al-Baker, Trellis Brown, and Roman Perez-Soler pp 325 - 329; DOI: 10.1021/jm00105a051 |
Preparation and anti-HIV activities of aurintricarboxylic acid fractions and analogs: direct correlation of antiviral potency with molecular weight Mark Cushman, Pinglang Wang, Steve H. Chang, Carl Wild, Erik De Clercq, Dominique Schols, Mark E. Goldman, and Julie A. Bowen pp 329 - 337; DOI: 10.1021/jm00105a052 |
Synthesis and anti-HIV activities of low molecular weight aurintricarboxylic acid fragments and related compounds Mark Cushman, Suseela Kanamathareddy, Erik De Clercq, Dominique Schols, Mark E. Goldman, and Julie A. Bowen pp 337 - 342; DOI: 10.1021/jm00105a053 |
A ring-enlarged oxetanocin A analog as an inhibitor HIV infectivity Christopher K. H. Tseng, Victor E. Marquez, George W. A. Milne, Ronald J. Wysocki, Hiroaki Mitsuya, Takuma Shirasaki, and John S. Driscoll pp 343 - 349; DOI: 10.1021/jm00105a054 |
A new class of HIV-1 specific 6-substituted acyclouridine derivatives: synthesis and anti-HIV-1 activity of 5- or 6-substituted analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) Hiromichi Tanaka, Masanori Baba, Hiroyuki Hayakawa, Takashi Sakamaki, Tadashi Miyasaka, Masaru Ubasawa, Hideaki Takashima, Kouichi Sekiya, Issei Nitta, Shiro Shigeta, Richard T. Walker, Jan Balzarini, and Eric De Clercq pp 349 - 357; DOI: 10.1021/jm00105a055 |
Inhibitors of cholesterol biosynthesis. 3. Tetrahydro-4-hydroxy-6-[2-(1H-pyrrol-1-yl)ethyl]-2H-pyran 2-one inhibitors of HMG-CoA reductase. 2. Effects of introducing substituents at positions three and four of the pyrrole nucleus Bruce D. Roth, C. J. Blankley, A. W. Chucholowski, E. Ferguson, M. L. Hoefle, D. F. Ortwine, R. S. Newton, C. S. Sekerke, D. R. Sliskovic, and M. W. Wilson pp 357 - 366; DOI: 10.1021/jm00105a056 |
Inhibitors of cholesterol biosynthesis. 4. trans-6-[2-(Substituted-quinolinyl)ethenyl/ethyl]tetrahydro-4-hydroxy-2H-pyran-2-ones, a novel series of HMG-CoA reductase inhibitors D. R. Sliskovic, J. A. Picard, W. H. Roark, B. D. Roth, E. Ferguson, B. R. Krause, R. S. Newton, C. Sekerke, and M. K. Shaw pp 367 - 373; DOI: 10.1021/jm00105a057 |
Disubstituted tetrahydrofurans and dioxolanes as platelet activating factor (PAF) antagonists Javier Bartroli, Elena Carceller, Manuel Merlos, Julian Garcia-Rafanell, and Javier Forn pp 373 - 386; DOI: 10.1021/jm00105a058 |
Synthesis and anticonvulsant activity of imidooxy derivatives Ivan O. Edafiogho, K. R. Scott, Jacqueline A. Moore, Vida A. Farrar, and Jesse M. Nicholson pp 387 - 392; DOI: 10.1021/jm00105a059 |
Synthesis of chiral and achiral pyranenamine derivatives. Potent agents with topical ocular antiallergic activity Charles Gluchowski, Trudy E. Bischoff, Michael E. Garst, Lester J. Kaplan, Steven W. Dietrich, Angelika S. Aswad, Mary A. Gaffney, K. Roger Aoki, Carlos Garcia, and Larry A. Wheeler pp 392 - 397; DOI: 10.1021/jm00105a060 |
(2S)-1-(Arylacetyl)-2-(aminomethyl)piperidine derivatives: novel, highly selective .kappa. opioid analgesics Vittorio Vecchietti, Antonio Giordani, Giuseppe Giardina, Roberto Colle, and Geoffrey D. Clarke pp 397 - 403; DOI: 10.1021/jm00105a061 |
Rationally designed "dipeptoid" analogs of CCK. .alpha.-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties David C. Horwell, John Hughes, John C. Hunter, Martyn C. Pritchard, Reginald S. Richardson, Edward Roberts, and Geoffrey N. Woodruff pp 404 - 414; DOI: 10.1021/jm00105a062 |
Preparation, characterization, and anticancer activity of a series of cis-PtCl2 complexes linked to anthraquinone intercalators Dan Gibson, Keria Fiorella Gean, Jehoshua Katzhendle, Raphael Ben-Shoshan, Avner Ramu, and Israel Ringel pp 414 - 420; DOI: 10.1021/jm00105a063 |
Unsaturated and carbocyclic nucleoside analogs: synthesis, antitumor and antiviral activity Shashikant Phadtare, David Kessel, Thomas H. Corbett, Harold E. Renis, Barbara E. Court, and Jiri Zemlicka pp 421 - 429; DOI: 10.1021/jm00105a064 |
Novel heteroarotinoids: synthesis and biological activity Lyle W. Spruce, Jonathan B. Gale, K. Darrell Berlin, A. K. Verma, Theodore R. Breitman, Xinhua Ji, and Dick Van der Helm pp 430 - 439; DOI: 10.1021/jm00105a065 |
Design, synthesis, and physicochemical properties of a novel, conformationally restricted 2,3-dihydro-1,3,4-thiadiazole-containing angiotensin converting enzyme inhibitor which is preferentially eliminated by the biliary route in rats Colin Bennion, Roger C. Brown, Anthony R. Cook, Carol N. Manners, David W. Payling, and David H. Robinson pp 439 - 447; DOI: 10.1021/jm00105a066 |
Non-steroidal antiandrogens. Design of novel compounds based on an infrared study of the dominant conformation and hydrogen-bonding properties of a series of anilide antiandrogens Jeffrey J. Morris, Leslie R. Hughes, Alasdair T. Glen, and Peter J. Taylor pp 447 - 455; DOI: 10.1021/jm00105a067 |
trans-3-n-propyl-L-proline is a highly favorable, conformationally restricted replacement for methionine in the C-terminal tetrapeptide of cholecystokinin. Stereoselective synthesis of 3-allyl- and 3-n-propyl-L-proline derivatives from 4-hydroxy-L-proline Mark W. Holladay, Chun Wel Lin, Catherine S. May, David S. Garvey, David G. Witte, Thomas R. Miller, Caroline A. W. Wolfram, and Alex M. Nadzan pp 455 - 457; DOI: 10.1021/jm00105a068 |
Dual antagonists of platelet-activating factor and histamine. Identification of structural requirements for dual activity of N-acyl-4-(5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)piperidines John J. Piwinski, Jesse K. Wong, Michael J. Green, Ashit K. Ganguly, M. Motasim Billah, Robert E. West, and William Kreutner pp 457 - 461; DOI: 10.1021/jm00105a069 |
Folic acid analogs lacking the 2-carbon are substrates for folylpolyglutamate synthetase and inhibit cell growth Andre Rosowsky, Ronald A. Forsch, and Richard G. Moran pp 461 - 463; DOI: 10.1021/jm00105a070 |
Relationship between tissue selectivity and lipophilicity for inhibitors of HMG-CoA reductase Bruce D. Roth, Thomas M. A. Bocan, C. John Blankley, Alexander W. Chucholowski, Paul L. Creger, Mark W. Creswell, Erika Ferguson, Roger S. Newton, Patrick O'Brien, and et al. pp 463 - 466; DOI: 10.1021/jm00105a071 |
8-(Dicyclopropylmethyl)-1,3-dipropylxanthine: a potent and selective adenosine A1 antagonist with renal protective and diuretic activities Junichi Shimada, Fumio Suzuki, Hiromi Nonaka, Akira Karasawa, Hideaki Mizumoto, Tetsuji Ohno, Kazuhiro Kubo, and Akio Ishii pp 466 - 469; DOI: 10.1021/jm00105a072 |
Design of a well-absorbed renin inhibitor Saul H. Rosenberg, Hollis D. Kleinert, Herman H. Stein, Donald L. Martin, Marcia A. Chekal, Jerome Cohen, David A. Egan, Karen A. Tricarico, and William R. Baker pp 469 - 471; DOI: 10.1021/jm00105a073 |
Book Reviews pp 471 - 478; DOI: 10.1021/jm00105a600 |
The renewed potential for folate antagonists in contemporary cancer chemotherapy E. M. Berman and Leslie M. Werbel pp 479 - 485; DOI: 10.1021/jm00106a001 |
Antineoplastic activity of didemnin congeners: nordidemnin and modified chain analogs Patrick Jouin, Joel Poncet, Marie Noelle Dufour, Andre Aumelas, Antoine Pantaloni, Suzy Cros, and Georgette Francois pp 486 - 491; DOI: 10.1021/jm00106a002 |
Potential antitumor agents. 62. Structure-activity relationships for tricyclic compounds related to the colon tumor active drug 9-oxo-9H-xanthene-4-acetic acid Gordon W. Rewcastle, Graham J. Atwell, Brian D. Palmer, Peter D. W. Boyd, Bruce C. Baguley, and William A. Denny pp 491 - 496; DOI: 10.1021/jm00106a003 |
A 3 dimensional model for 5-HT1A-receptor agonists based on stereoselective methyl-substituted and conformationally restricted analogs of 8-hydroxy-2-(dipropylamino)tetralin Charlotta Mellin, Jerk Vallgaarda, David L. Nelson, Lena Bjoerk, Hong Yu, Nils Erik Anden, Ingeborg Csoeregh, Lars Erik Arvidsson, and Uli Hacksell pp 497 - 510; DOI: 10.1021/jm00106a004 |
Molecular and crystal structures of MDL27,467A hydrochloride and quinapril hydrochloride, two ester derivatives of potent angiotensin converting enzyme inhibitors Roland J. Hausin and Penelope W. Codding pp 511 - 517; DOI: 10.1021/jm00106a005 |
Styrylpyrazoles, styrylisoxazoles, and styrylisothiazoles. Novel 5-lipoxygenase and cyclooxygenase inhibitors Daniel L. Flynn, Thomas R. Belliotti, Amal M. Boctor, David T. Connor, Catherine R. Kostlan, Donald E. Nies, Daniel F. Ortwine, Denis J. Schrier, and Jagadish C. Sircar pp 518 - 525; DOI: 10.1021/jm00106a006 |
Analysis of the in vitro antitumor activity of novel purine-6-sulfenamide, -sulfinamide, and -sulfonamide nucleosides and certain related compounds using a computer-aided receptor modeling procedure Vellarkad N. Viswanadhan, Arup K. Ghose, Naeem B. Hanna, Steven S. Matsumoto, Thomas L. Avery, Ganapathi R. Revankar, and Roland K. Robins pp 526 - 532; DOI: 10.1021/jm00106a007 |
Antiulcer agents. 5. Inhibition of gastric H+/K+-ATPase by substituted imidazo[1,2-a]pyridines and related analogs and its implication in modeling the high affinity potassium ion binding site of the gastric proton pump enzyme James J. Kaminski, Bjorn Wallmark, Carin Briving, and Britt Marie Andersson pp 533 - 541; DOI: 10.1021/jm00106a008 |
Synthesis, peroxidating ability, and antineoplastic evaluation of 1-[(aminoalkyl)amino]-4-hydroxy-10-imino-9-anthracenones Maria Dzieduszycka, Sante Martelli, Jolanta Tarasiuk, Jolanta Paradziej-Lukowicz, and Edward Borowski pp 541 - 546; DOI: 10.1021/jm00106a009 |
Synthesis and biological activity of bay-region metabolites of a cyclopenta-fused polycyclic aromatic hydrocarbon: benz[j]aceanthrylene R. Sangaiah, Avram Gold, K. O. Newcomb, and L. M. Ball pp 546 - 549; DOI: 10.1021/jm00106a010 |
2,4-Diamino-5-benzylpyrimidines as antibacterial agents. 14. 2,3-Dihydro-1-(2,4-diamino-5-pyrimidyl)-1H-indenes as conformationally restricted analogs of trimethoprim Joseph H. Chan and Barbara Roth pp 550 - 555; DOI: 10.1021/jm00106a011 |
Novel pyrrolo[2,3-d]pyrimidine antifolates: synthesis and antitumor activities Tetsuo Miwa, Takenori Hitaka, Hiroshi Akimoto, and Hiroaki Nomura pp 555 - 560; DOI: 10.1021/jm00106a012 |
Doxorubicin analogs incorporating chemically reactive substituents David Farquhar, Robert A. Newman, Joan E. Zuckerman, and Borje S. Andersson pp 561 - 564; DOI: 10.1021/jm00106a013 |
Phosphorus-31 NMR and chloride ion kinetics of alkylating monoester phosphoramidates Kristin M. Fries and Richard F. Borch pp 565 - 569; DOI: 10.1021/jm00106a014 |
Antimalarial polyamine analogs Michael L. Edwards, D. M. Stemerick, A. J. Bitonti, J. A. Dumont, P. P. McCann, P. Bey, and A. Sjoerdsma pp 569 - 574; DOI: 10.1021/jm00106a015 |
Synthesis and biological activity of methotrexate analogs with two acid groups and a hydrophobic aromatic ring in the side chain Andre Rosowsky, Henry Bader, and James H. Freisheim pp 574 - 579; DOI: 10.1021/jm00106a016 |
Quantitative structure-activity relationship analysis of cation-substituted polyaromatic compounds as potentiators (amplifiers) of bleomycin-mediated degradation of DNA Lucjan Strekowski, W. David Wilson, Jerzy L. Mokrosz, Maria J. Mokrosz, Donald B. Harden, Farial A. Tanious, Roman L. Wydra, and Sidney A. Crow pp 580 - 588; DOI: 10.1021/jm00106a017 |
Chemically stable, lipophilic prodrugs of phosphoramide mustard as potential anticancer agents Chul Hoon Kwon, Ki Young Moon, Nesrine Baturay, and Frances N. Shirota pp 588 - 592; DOI: 10.1021/jm00106a018 |
A new class of calcium antagonists. Synthesis and biological activity of 11-[(.omega.-aminoalkanoyl)amino]-6,6a,7,8,9,10,10a,11-octahydrodibenzo[b,e]thiepin derivatives Mikio Kurokawa, Fuminori Sato, Naonobu Hatano, Yayoi Honda, and Hitoshi Uno pp 593 - 599; DOI: 10.1021/jm00106a019 |
N-(4-Isoxazolylthiazol-2-yl)oxamic acid derivatives as potent orally active antianaphylactic agents Dario Chiarino, Giancarlo Grancini, Viviana Frigeni, Ivano Biasini, and Angelo Carenzi pp 600 - 605; DOI: 10.1021/jm00106a020 |
Synthesis and biological evaluation of 5-deazaisofolic acid, 5-deaza-5,6,7,8-tetrahydroisofolic acid, and their N9-substituted analogues Shyam K. Singh, Inderjit K. Dev, David S. Duch, Robert Ferone, Gary K. Smith, James H. Freisheim, and John B. Hynes pp 606 - 610; DOI: 10.1021/jm00106a021 |
Synthesis and biological activity of 5,11-methylenetetrahydro-5-deazahomofolic acid Aleem Gangjee, Isaac O. Donkor, Roy L. Kisliuk, Yvette Gaumont, and Janet Thorndike pp 611 - 616; DOI: 10.1021/jm00106a022 |
Novel benzamides as selective and potent gastrokinetic agents. 2. Synthesis and structure-activity relationships of 4-amino-5-chloro-2-ethoxy-N-[[4-(4-fluorobenzyl)-2-morpholinyl]methyl]benzamide citrate (AS-4370) and related compounds Shiro Kato, Toshiya Morie, Tatsuya Kon, Naoyuki Yoshida, Tadahiko Karasawa, and Junichi Matsumoto pp 616 - 624; DOI: 10.1021/jm00106a023 |
Structure-activity relationship of quinazolinedione inhibitors of calcium-independent phosphodiesterase John A. Lowe, III, Robert L. Archer, Douglas S. Chapin, John B. Cheng, David Helweg, Jonathan L. Johnson, B. Kenneth Koe, Lorraine A. Lebel, Peter F. Moore, and et al. pp 624 - 628; DOI: 10.1021/jm00106a024 |
Synthesis and anticonvulsant activity of 1-acyl-2-pyrrolidinone derivatives Hitoshi Sasaki, Yoshiyuki Mori, Junzo Nakamura, and Juichiro Shibasaki pp 628 - 633; DOI: 10.1021/jm00106a025 |
Renin inhibitory peptides. Incorporation of polar, hydrophilic end groups into an active renin inhibitory peptide template and their evaluation in a human renin-infused rat model and in conscious sodium-depleted monkeys Suvit Thaisrivongs, Donald T. Pals, Donald W. DuCharme, Steve R. Turner, Garry L. DeGraaf, Judy A. Lawson, Sally J. Couch, and Mark V. Williams pp 633 - 642; DOI: 10.1021/jm00106a026 |
Design of potent oxytocin antagonists featuring D-tryptophan at position 2 George Flouret, William Brieher, Kevin Mahan, and Laird Wilson pp 642 - 646; DOI: 10.1021/jm00106a027 |
4'-5'-Unsaturated 5'-halogenated nucleosides. Mechanism-based and competitive inhibitors of S-adenosyl-L-homocysteine hydrolase Esa T. Jarvi, James R. McCarthy, Shujaath Mehdi, Donald P. Matthews, Michael L. Edwards, Nellikunja J. Prakash, Terry L. Bowlin, Prasad S. Sunkara, and Philippe Bey pp 647 - 656; DOI: 10.1021/jm00106a028 |
Quinolone antibacterials: preparation and activity of bridged bicyclic analogues of the C7-piperazine John S. Kiely, Marland P. Hutt, Townley P. Culbertson, Ruth A. Bucsh, Donald F. Worth, Lawrence E. Lesheski, Rocco D. Gogliotti, Josephine C. Sesnie, Marjorie Solomon, and Thomas F. Mich pp 656 - 663; DOI: 10.1021/jm00106a029 |
Configuration and preferential solid-state conformations of perindoprilat (S-9780). Comparison with the crystal structures of other ACE inhibitors and conclusions related to structure-activity relationships Claudine Pascard, Jean Guilhem, Michel Vincent, Georges Remond, Bernard Portevin, and Michel Laubie pp 663 - 669; DOI: 10.1021/jm00106a030 |
Dual-action cephalosporins: cephalosporin 3'-quaternary ammonium quinolones Harry A. Albrecht, George Beskid, James G. Christenson, Joanne W. Durkin, Virve Fallat, Nafsika H. Georgopapadakou, Dennis D. Keith, Frederick M. Konzelmann, Ellen R. Lipschitz, and et al. pp 669 - 675; DOI: 10.1021/jm00106a031 |
Synthesis of halogen-substituted 1,5-benzothiazepine derivatives and their vasodilating and hypotensive activities Hirozumi Inoue, Mikihiko Konda, Tomiki Hashiyama, Hisao Otsuka, Kaoru Takahashi, Mitsunori Gaino, Tadamasa Date, Keiichi Aoe, Mikio Takeda, and et al. pp 675 - 687; DOI: 10.1021/jm00106a032 |
Muscarinic cholinergic agonists and antagonists of the 3-(3-alkyl-1,2,4-oxadiazol-5-yl)-1,2,5,6-tetrahydropyridine type. Synthesis and structure-activity relationships Per Sauerberg, Jens W. Kindtler, Lone Nielsen, Malcolm J. Sheardown, and Tage Honore pp 687 - 692; DOI: 10.1021/jm00106a033 |
Synthesis and anticancer activity of various 3'-deoxy pyrimidine nucleoside analogs, and crystal structure of 1-(3-deoxy-.beta.-D-threo-pentofuranosyl)cytosine Tai Shun Lin, Jing Hua Yang, Mao Chin Liu, Zhi Yi Shen, Yung Chi Cheng, William H. Prusoff, George I. Birnbaum, Jerzy Giziewicz, Ismail Ghazzouli, and et al. pp 693 - 701; DOI: 10.1021/jm00106a034 |
Synthesis of 3-carbamoylecgonine methyl ester analogs as inhibitors of cocaine binding and dopamine uptake Richard H. Kline, Jeremy Wright, Amy J. Eshleman, Kristine M. Fox, and Mohyee E. Eldefrawi pp 702 - 705; DOI: 10.1021/jm00106a035 |
Structure-affinity relationships of 12-sulfonyl derivatives of 5,8,8a,9,10,11,12,12a,13,13a-decahydro-6H-isoquino[2,1-g][1,6]naphthyridines at .alpha.-adrenoceptors Robin D. Clark, David B. Repke, Jacob Berger, Janis T. Nelson, Andrew T. Kilpatrick, Christine M. Brown, Alison C. MacKinnon, Ruth U. Clague, and Michael Spedding pp 705 - 717; DOI: 10.1021/jm00106a036 |
Conformationally defined neurotransmitter analogs. Selective inhibition of glutamate uptake by one pyrrolidine-2,4-dicarboxylate diastereomer Richard J. Bridges, Mark S. Stanley, Michael W. Anderson, Carl W. Cotman, and A. Richard Chamberlin pp 717 - 725; DOI: 10.1021/jm00106a037 |
Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease L. J. Browne, C. Gude, H. Rodriguez, R. E. Steele, and A. Bhatnager pp 725 - 736; DOI: 10.1021/jm00106a038 |
4'-Hydroxy-3-methoxyflavones with potent antipicornavirus activity Nadine De Meyer, Achiel Haemers, Lallan Mishra, Hrishi Kesh Pandey, L. A. C. Pieters, Dirk A. Vanden Berghe, and Arnold J. Vlietinck pp 736 - 746; DOI: 10.1021/jm00106a039 |
Synthesis and anti-HIV-1 activity of 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one (TIBO) derivatives Michael J. Kukla, Henry J. Breslin, Rudi Pauwels, Cynthia L. Fedde, Milton Miranda, Malcolm K. Scott, Ronald G. Sherrill, Alfons Raeymaekers, Jozef Van Gelder, and et al. pp 746 - 751; DOI: 10.1021/jm00106a040 |
Allosteric modifiers of hemoglobin. 1. Design, synthesis, testing, and structure-allosteric activity relationship of novel hemoglobin oxygen affinity decreasing agents Ramnarayan S. Randad, Mona A. Mahran, Ahmed S. Mehanna, and Donald J. Abraham pp 752 - 757; DOI: 10.1021/jm00106a041 |
Allosteric modifiers of hemoglobin. 2. Crystallographically determined binding sites and hydrophobic binding/interaction analysis of novel hemoglobin oxygen effectors Fred C. Wireko, Glen E. Kellogg, and Donald J. Abraham pp 758 - 767; DOI: 10.1021/jm00106a042 |
Synthesis of high specific activity (+)- and (-)-6-[18F]fluoronorepinephrine via the nucleophilic aromatic substitution reaction Yu Shin Ding, Joanna S. Fowler, S. John Gatley, Stephen L. Dewey, and Alfred P. Wolf pp 767 - 771; DOI: 10.1021/jm00106a043 |
Romazarit. A potential disease-modifying antirheumatic drug Christopher R. Self, William E. Barber, Peter J. Machin, John M. Osbond, Carey E. Smithen, Brian P. Tong, James C. Wickens, David P. Bloxham, David Bradshaw, and et al. pp 772 - 777; DOI: 10.1021/jm00106a044 |
Nucleosides and nucleotides. 96. Synthesis and antitumor activity of 5-ethynyl-1-.beta.-D-ribofuranosylimidazole-4-carboxamide (EICAR) and its derivatives Noriaki Minakawa, Takayuki Takeda, Takuma Sasaki, Akira Matsuda, and Tohru Ueda pp 778 - 786; DOI: 10.1021/jm00106a045 |
Structure-activity relationship of mutagenic aromatic and heteroaromatic nitro compounds. Correlation with molecular orbital energies and hydrophobicity Asim Kumar Debnath, Rosa L. Lopez de Compadre, Gargi Debnath, Alan J. Shusterman, and Corwin Hansch pp 786 - 797; DOI: 10.1021/jm00106a046 |
Synthesis and protein-tyrosine kinase inhibitory activities of flavonoid analogs Mark Cushman, Dhanapalan Nagarathnam, Debra L. Burg, and Robert L. Geahlen pp 798 - 806; DOI: 10.1021/jm00106a047 |
Dihydropyrimidine calcium channel blockers. 3. 3-Carbamoyl-4-aryl-1,2,3,4-tetrahydro-6-methyl-5-pyrimidinecarboxylic acid esters as orally effective antihypertensive agents Karnail S. Atwal, Brian N. Swanson, Steven E. Unger, David M. Floyd, Suzanne Moreland, Anders Hedberg, and Brian C. O'Reilly pp 806 - 811; DOI: 10.1021/jm00106a048 |
Nucleosides and nucleotides. 97. Synthesis of new broad spectrum antineoplastic nucleosides, 2'-deoxy-2'-methylidenecytidine (DMDC) and its derivatives Akira Matsuda, Kenji Takenuki, Motohiro Tanaka, Takuma Sasaki, and Tohru Ueda pp 812 - 819; DOI: 10.1021/jm00106a049 |
Structure-stability relationships of gadolinium(III) ion complexes for magnetic resonance imaging Rune Fossheim, Harald Dugstad, and Svein G. Dahl pp 819 - 826; DOI: 10.1021/jm00106a050 |
New 1-(heterocyclylalkyl)-4-(propionanilido)-4-piperidinyl methyl ester and methylene methyl ether analgesics Jerome R. Bagley, Sheela A. Thomas, Frieda G. Rudo, H. Kenneth Spencer, Brian M. Doorley, Michael H. Ossipov, Thomas P. Jerussi, Mark J. Benvenga, and Theodore Spaulding pp 827 - 841; DOI: 10.1021/jm00106a051 |
Synthesis and biological evaluation of a series of 1,1-dichloro-2,2,3-triarylcyclopropanes as pure antiestrogens Billy W. Day, Robert A. Magarian, Pramod T. Jain, J. Thomas Pento, Gorgin K. Mousissian, and Karen L. Meyer pp 842 - 851; DOI: 10.1021/jm00106a052 |
Synthesis and biological activity of D3-trishomocubyl-4-amines Douglas W. Oliver, Theodor G. Dekker, Friedrich O. Snyckers, and Theunis G. Fourie pp 851 - 854; DOI: 10.1021/jm00106a053 |
Synthesis, receptor binding, and tissue distribution of 7.alpha.- and 11.beta.-substituted (17.alpha.,20E)- and (17.alpha.,20Z)-21-[125I]iodo-19-norpregna-1,3,5(10),20-tetraene-3,17-diols H. Ali, J. Rousseau, M. A. Ghaffari, and Johan E. Van Lier pp 854 - 860; DOI: 10.1021/jm00106a054 |
Synthesis of high specific activity 6-[18F]fluorodopamine for positron emission tomography studies of sympathetic nervous tissue Yu Shin Ding, Joanna S. Fowler, S. John Gatley, Stephen L. Dewey, Alfred P. Wolf, and David J. Schlyer pp 861 - 863; DOI: 10.1021/jm00106a055 |
Hydrophobicity parameters for platinum complexes Jean Pierre Souchard, Tam T. B. Ha, S. Cros, and Neil P. Johnson pp 863 - 864; DOI: 10.1021/jm00106a056 |
Book Reviews pp 864 - 868; DOI: 10.1021/jm00106a600 |
Reevaluating equilibrium and kinetic binding parameters for lipophilic drugs based on a structural model for drug interactions with biological membranes R. Preston Mason, David G. Rhodes, and Leo G. Herbette pp 869 - 877; DOI: 10.1021/jm00107a001 |
Synthesis and resolution of (.+-.)-7-chloro-8-hydroxy-1-(3'-iodophenyl)-3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine (TISCH): a high affinity and selective iodinated ligand for CNS D1 dopamine receptor Sumalee Chumpradit, Mei Pung Kung, Jeffrey J. Billings, and Hank F. Kung pp 877 - 883; DOI: 10.1021/jm00107a002 |
Synthesis and ligand binding of cocaine isomers at the cocaine receptor F. Ivy Carroll, Anita H. Lewin, Philip Abraham, Karol Parham, John W. Boja, and Michael J. Kuhar pp 883 - 886; DOI: 10.1021/jm00107a003 |
Renin inhibitors containing conformationally restricted P1-P1' dipeptide mimetics Peter D. Williams, Debra S. Perlow, Linda S. Payne, M. Katherine Holloway, Peter K. S. Siegl, Terry W. Schorn, Robert J. Lynch, John J. Doyle, John F. Strouse, and et al. pp 887 - 900; DOI: 10.1021/jm00107a004 |
Syntheses and in vitro evaluation of water-soluble "cationic metalloporphyrin-ellipticine" molecules having a high affinity for DNA Li Ding, Guita Etemad-Moghadam, Suzy Cros, Christian Auclair, and Bernard Meunier pp 900 - 906; DOI: 10.1021/jm00107a005 |
Fluorocarbocyclic nucleosides: synthesis and antiviral activity of 2'- and 6'-fluorocarbocyclic 2'-deoxyguanosines Alan D. Borthwick, Barrie E. Kirk, Keith Biggadike, Anne M. Exall, Suzanne Butt, Stanley M. Roberts, David J. Knight, Jonathan A. V. Coates, and D. Michael Ryan pp 907 - 914; DOI: 10.1021/jm00107a006 |
N-(5-fluorobenzothiazol-2-yl)-2-guanidinothiazole-4-carboxamide. A novel, systemically active antitumor agent effective against 3LL Lewis Lung carcinoma Rodney C. Schnur, Anton F. J. Fliri, Shama Kajiji, and Vincent A. Pollack pp 914 - 918; DOI: 10.1021/jm00107a007 |
Synthesis and smooth muscle relaxant activity of a new series of potassium channel activators: 3-amido-1,1-dimethylindan-2-ols Derek R. Buckle, Jonathan R. S. Arch, Colin Edge, Keith A. Foster, Catherine S. V. Houge-Frydrych, Ivan L. Pinto, David G. Smith, John F. Taylor, Stephen G. Taylor, and et al. pp 919 - 926; DOI: 10.1021/jm00107a008 |
A new class of calcium antagonists. 2. Synthesis and biological activity of 11-[4-[4-(4-fluorophenyl)-1-piperazinyl]butyryl]amino]-6,11-dihydrodibenzo[b,e]thiepin maleate and related compounds Mikio Kurokawa, Fuminori Sato, Iwao Fujiwara, Naonobu Hatano, Yayoi Honda, Takayuki Yoshida, Shunsuke Naruto, Junichi Mastumoto, and Hitoshi Uno pp 927 - 934; DOI: 10.1021/jm00107a009 |
Modeling alcohol metabolism with the DARC/CALPHI system Christiane Mercier, Veronique Fabart, Yves Sobel, and Jacques Emile Dubois pp 934 - 942; DOI: 10.1021/jm00107a010 |
Specific bradycardic agents. 2. Heteroaromatic modifications in the side chain of specific bradycardic benzazepinones: chemistry, pharmacology, and structure-activity relationships Andreas Bomhard, Manfred Reiffen, Joachim Heider, Manfred Psiorz, and Christian Lillie pp 942 - 947; DOI: 10.1021/jm00107a011 |
Potential antipsychotic agents. 9. Synthesis and stereoselective dopamine D-2 receptor blockade of a potent class of substituted (R)-N-[(1-benzyl-2-pyrrolidinyl)methyl]benzamides. Relations to other side chain congeners Thomas Hoegberg, Peter Stroem, Tomas De Paulis, Birgitta Stensland, Ingeborg Csoeregh, Kerstin Lundin, Haakan Hall, and Sven Ove Oegren pp 948 - 955; DOI: 10.1021/jm00107a012 |
Synthesis and siderophore activity of albomycin-like peptides derived from N5-acetyl-N5-hydroxy-L-ornithine E. Kurt Dolence, Chia En Lin, Marvin J. Miller, and Shelley M. Payne pp 956 - 968; DOI: 10.1021/jm00107a013 |
Synthesis and siderophore and antibacterial activity of N5-acetyl-N5-hydroxyl-L-ornithine derived siderophore-.beta.-lactam conjugates: iron transport mediated drug delivery E. Kurt Dolence, Albert A. Minnick, Chia En Lin, Marvin J. Miller, and Shelley M. Payne pp 968 - 978; DOI: 10.1021/jm00107a014 |
Quinazoline antifolates inhibiting thymidylate synthase: 4-thio-substituted analogs Timothy J. Thornton, Terence R. Jones, Ann L. Jackman, Anthony Flinn, Breda M. O'Connor, Peter Warner, and A. Hilary Calvert pp 978 - 984; DOI: 10.1021/jm00107a015 |
Synthesis and antitumor activity of structural analogs of the epipodophyllotoxins Larry L. Klein, Clinton M. Yeung, Daniel T. Chu, Edith J. McDonald, Jacob J. Clement, and Jacob J. Plattner pp 984 - 992; DOI: 10.1021/jm00107a016 |
Relationships between the structure of taxol analogs and their antimitotic activity Francoise Gueritte-Voegelein, Daniel Guenard, Francois Lavelle, Marie Therese Le Goff, Lydie Mangatal, and Pierre Potier pp 992 - 998; DOI: 10.1021/jm00107a017 |
Nucleosides and nucleotides. 95. Improved synthesis of 1-(2-azido-2-deoxy-.beta.-D-arabinofuranosyl)cytosine (Cytarazid) and -thymine. Inhibitory spectrum of Cytarazid on the growth of various human tumor cells in vitro Akira Matsuda, Johji Yasuoka, Takuma Sasaki, and Tohru Ueda pp 999 - 1002; DOI: 10.1021/jm00107a018 |
Synthesis of 2-exo- and 2-endo-mecamylamine analogs. Structure-activity relationships for nicotinic antagonism in the central nervous system John A. Suchocki, Everette L. May, Thomas J. Martin, Clifford George, and Billy R. Martin pp 1003 - 1010; DOI: 10.1021/jm00107a019 |
A highly specific aldose reductase inhibitor, ethyl 1-benzyl-3-hydroxy-2(5H)-oxopyrrole-4-carboxylate and its congeners Banavara L. Mylari, Thomas A. Beyer, and Todd W. Siegel pp 1011 - 1018; DOI: 10.1021/jm00107a020 |
A potential radioiodinated ligand for androgen receptor: 7.alpha.-methyl-17.alpha.-[2'-(E)-iodovinyl]-19-nortestosterone Mohammad Salman and Gary C. Chamness pp 1019 - 1024; DOI: 10.1021/jm00107a021 |
Perfluorinated analogs of poison ivy allergens. Synthesis and skin tolerogenic activity in mice Rossana Fraginals, Marcel Schaeffer, Jean Luc Stampf, and Claude Benezra pp 1024 - 1027; DOI: 10.1021/jm00107a022 |
Indazolinones, a new series of redox-active 5-lipoxygenase inhibitors with built-in selectivity and oral activity P. Bruneau, C. Delvare, M. P. Edwards, and R. M. McMillan pp 1028 - 1036; DOI: 10.1021/jm00107a023 |
Water-soluble cholesteryl-containing phosphorothioate monogalactosides: synthesis, properties, and use in lowering blood cholesterol by directing plasma lipoproteins to the liver Harlof C. P. F. Roelen, Martin K. Bijsterbosch, Hille F. Bakkeren, Theo J. C. Van Berkel, Herman J. M. Kempen, Marinus Buytenhek, Gijs A. Van der Marel, and Jacques H. Van Boom pp 1036 - 1042; DOI: 10.1021/jm00107a024 |
N6-Substituted adenosine receptor agonists: potential antihypertensive agents B. K. Trivedi, C. J. Blankley, J. A. Bristol, H. W. Hamilton, W. C. Patt, W. J. Kramer, S. A. Johnson, R. F. Bruns, D. M. Cohen, and M. J. Ryan pp 1043 - 1049; DOI: 10.1021/jm00107a025 |
Studies on (H+-K+)-ATPase inhibitors of gastric acid secretion. Prodrugs of 2-[(2-pyridinylmethyl)sulfinyl]benzimidazole proton-pump inhibitors John C. Sih, Wha bin Im, Andre Robert, David R. Graber, and David P. Blakeman pp 1049 - 1062; DOI: 10.1021/jm00107a026 |
Effect of fluorine substitution on the adrenergic properties of 3-(tert-butylamino)-1-(3,4-dihydroxyphenoxy)-2-propanol Adeboye Adejare, Jun Ying Nie, David Hebel, L. Ellen Brackett, Oksoon Choi, Fabian Gusovsky, William L. Padgett, John W. Daly, Cyrus R. Creveling, and Kenneth L. Kirk pp 1063 - 1068; DOI: 10.1021/jm00107a027 |
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents Nicholas J. Hrib, John G. Jurcak, Francis P. Huger, Cheri L. Errico, and Robert W. Dunn pp 1068 - 1072; DOI: 10.1021/jm00107a028 |
Muscarinic receptor binding and activation of second messengers by substituted N-methyl-N-[4-(1-azacycloalkyl)-2-butynyl]acetamides Barton J. Bradbury, Jesse Baumgold, Robert Paek, Udai Kammula, Jeff Zimmet, and Kenneth A. Jacobson pp 1073 - 1079; DOI: 10.1021/jm00107a029 |
Isomeric monomethyl ether derivatives of (RS)-9,10-dihydroxyaporphine ("isoapomorphine") as possible products of metabolism by catechol-O-methyltransferase Joseph G. Cannon and Pang Qijie pp 1079 - 1082; DOI: 10.1021/jm00107a030 |
The enantiomeric specificity of the antihypertensive activity of 1-(phenylthio)-2-aminopropane, a synthetic substrate analog for dopamine .beta.-monooxygenase Heath H. Herman, Philip A. Husain, James E. Colbert, Margaret M. Schweri, Stanley H. Pollock, Lydia C. Fowler, and Sheldon W. May pp 1082 - 1085; DOI: 10.1021/jm00107a031 |
Tetrahydropyridyloxadiazoles: semi-rigid muscarinic ligands Graham A. Showell, Tracey L. Gibbons, Clare O. Kneen, Angus M. MacLeod, Kevin Merchant, John Saunders, Stephen B. Freedman, Shailendra Patel, and Raymond Baker pp 1086 - 1094; DOI: 10.1021/jm00107a032 |
Identification and exploitation of the .sigma.-opiate pharmacophore Richard A. Glennon, J. Doyle Smith, Abd M. Ismaiel, Mahmoud El-Ashmawy, George Battaglia, and James B. Fischer pp 1094 - 1098; DOI: 10.1021/jm00107a033 |
Antinociceptive (aminoalkyl)indoles Malcolm R. Bell, Thomas E. D'Ambra, Virendra Kumar, Michael A. Eissenstat, John L. Herrmann Jr., Joseph R. Wetzel, David Rosi, Richard E. Philion, Sol J. Daum, and et al. pp 1099 - 1110; DOI: 10.1021/jm00107a034 |
Synthesis and structure-activity relationship of new cephalosporins with amino heterocycles at C-7. Dependence of the antibacterial spectrum and .beta.-lactamase stability on the pKa of the C-7 heterocycle F. Jung, C. Delvare, D. Boucherot, A. Hamon, N. Ackerley, and M. J. Betts pp 1110 - 1116; DOI: 10.1021/jm00107a035 |
A comparative NMR study between the macrolide antibiotic roxithromycin and erythromycin A with different biological properties Josyane Gharbi-Benarous, Marcel Delaforge, Christophe K. Jankowski, and Jean Pierre Girault pp 1117 - 1125; DOI: 10.1021/jm00107a036 |
Carboxylic acids and tetrazoles as isosteric replacements for sulfate in cholecystokinin analogs Jefferson W. Tilley, Waleed Danho, Kathleen Lovey, Rolf Wagner, Joseph Swistok, Raymond Makofske, Joseph Michalewsky, Joseph Triscari, David Nelson, and Sally Weatherford pp 1125 - 1136; DOI: 10.1021/jm00107a037 |
Neoglycoproteins as carriers for antiviral drugs: synthesis and analysis of protein-drug conjugates Grietje Molema, Robert W. Jansen, Jan Visser, Piet Herdewijn, Frits Moolenaar, and Dirk K. F. Meijer pp 1137 - 1141; DOI: 10.1021/jm00107a038 |
Synthesis and biological activity of 5-amino- and 5-hydroxyquinolones, and the overwhelming influence of the remote N1-substituent in determining the structure-activity relationship John M. Domagala, Alex J. Bridges, Townley P. Culbertson, Laura Gambino, Susan E. Hagen, Gregory Karrick, Kenneth Porter, Joseph P. Sanchez, Josephine A. Sesnie, and et al. pp 1142 - 1154; DOI: 10.1021/jm00107a039 |
Synthesis and biological activity of 5-alkyl-1,7,8-trisubstituted-6-fluoroquinoline-3-carboxylic acids Susan E. Hagen, John M. Domagala, Carl L. Heifetz, and Judith Johnson pp 1155 - 1161; DOI: 10.1021/jm00107a040 |
.beta.-Substituted .beta.-phenylpropionyl chymotrypsins. Structural and stereochemical features in stable acyl enzymes Peter E. Reed and John A. Katzenellenbogen pp 1162 - 1176; DOI: 10.1021/jm00107a041 |
Biologically active taxol analogs with deleted A-ring side chain substituents and variable C-2' configurations Charles S. Swindell, Nancy E. Krauss, Susan B. Horwitz, and Israel Ringel pp 1176 - 1184; DOI: 10.1021/jm00107a042 |
Positional effects of sulfation in hirudin and hirudin PA related anticoagulant peptides Marguerite H. Payne, John L. Krstenansky, Mark T. Yates, and Simon J. T. Mao pp 1184 - 1187; DOI: 10.1021/jm00107a043 |
Adenosine deaminase inhibitors: synthesis and structure activity relationships of imidazole analogs of erythro-9-(2-hydroxy-3-nonyl)adenine Gloria Cristalli, Alessandra Eleuteri, Palmarisa Franchetti, Mario Grifantini, Sauro Vittori, and Giulio Lupidi pp 1187 - 1192; DOI: 10.1021/jm00107a044 |
Synthesis and copper-dependent antimycoplasmal activity of amides and amidines derived from 2-amino-1,10-phenanthroline Marcel A. H. De Zwart, Henricus M. M. Bastiaans, Henk Van der Goot, and Hendrik Timmerman pp 1193 - 1201; DOI: 10.1021/jm00107a045 |
1H-Imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists Philip J. M. Van Galen, Peter Nissen, Ineke Van Wijngaarden, Adriaan P. Ijzerman, and Willem Soudijn pp 1202 - 1206; DOI: 10.1021/jm00107a046 |
Dual-function radiosensitizers. .alpha.-[[(2-Bromoethyl)amino]methyl]-2-nitro-1H-imidazole-1-ethanol and related compounds: preparation via an aziridine equivalent Mark J. Suto, Michael A. Stier, and Leslie M. Werbel pp 1207 - 1209; DOI: 10.1021/jm00107a047 |
Triazolobenzo- and triazolothienodiazepines as potent antagonists of platelet activating factor Armin Walser, Thomas Flynn, Carl Mason, Herman Crowley, Catherine Maresca, Bob Yaremko, and Margaret O'Donnell pp 1209 - 1221; DOI: 10.1021/jm00107a048 |
Effect of hydroxyl group configuration in hydroxyethylamine dipeptide isosteres on HIV protease inhibition. Evidence for multiple binding modes Daniel H. Rich, Chong Qing Sun, J. V. N. Vara Prasad, Ahammadunny Pathiasseril, Mihaly V. Toth, Garland R. Marshall, Michael Clare, Richard A. Mueller, and Kathryn Houseman pp 1222 - 1225; DOI: 10.1021/jm00107a049 |
L-687,908, a potent hydroxyethylene containing HIV protease inhibitor Joseph P. Vacca, J. P. Guare, S. J. DeSolms, W. M. Sanders, E. A. Giuliani, S. D. Young, P. L. Darke, I. S. Sigal, W. A. Schleif, and et al. pp 1225 - 1228; DOI: 10.1021/jm00107a050 |
Benzocycloalkyl amines as novel C-termini for HIV protease inhibitors Terry A. Lyle, Catherine M. Wiscount, James P. Guare, Wayne J. Thompson, Paul S. Anderson, Paul L. Darke, Joan A. Zugay, Emilio A. Emini, William A. Schleif, and et al. pp 1228 - 1230; DOI: 10.1021/jm00107a051 |
Design and conformational analysis of several highly potent bradykinin receptor antagonists Donald J. Kyle, Jennifer A. Martin, Stephen G. Farmer, and Ronald M. Burch pp 1230 - 1233; DOI: 10.1021/jm00107a052 |
Book Reviews pp 1233 - 1234; DOI: 10.1021/jm00107a600 |
Peptide leukotrienes: current status of research A. Shaw and R. D. Krell pp 1235 - 1242; DOI: 10.1021/jm00108a001 |
Kynurenic acid derivatives. Structure-activity relationships for excitatory amino acid antagonism and identification of potent and selective antagonists at the glycine site on the N-methyl-D-aspartate receptor Paul D. Leeson, Raymond Baker, Robert W. Carling, Neil R. Curtis, Kevin W. Moore, Brian J. Williams, Alan C. Foster, Angus E. Donald, John A. Kemp, and George R. Marshall pp 1243 - 1252; DOI: 10.1021/jm00108a002 |
Synthesis and pharmacological evaluation of a major metabolite of ameltolide, a potent anticonvulsant David W. Robertson, E. E. Beedle, Joseph H. Krushinski, Ronald R. Lawson, C. John Parli, Brian Potts, and J. David Leander pp 1253 - 1257; DOI: 10.1021/jm00108a003 |
New inhibitors of human renin that contain novel replacements at the P2 site Annette M. Doherty, James S. Kaltenbronn, James P. Hudspeth, Joseph T. Repine, William H. Roark, Ila Sircar, Frank J. Tinney, Cleo J. Connolly, John C. Hodges, and et al. pp 1258 - 1271; DOI: 10.1021/jm00108a004 |
Morphine 6-glucuronide and morphine 3-glucuronide as molecular chameleons with unexpected lipophilicity Pierre Alain Carrupt, Bernard Testa, Antoine Bechalany, Nabil El Tayar, Patrick Descas, and Daniel Perrissoud pp 1272 - 1275; DOI: 10.1021/jm00108a005 |
Conformationally constrained renin inhibitory peptides: cyclic (3-1)-1-(carboxymethyl)-L-prolyl-L-phenylalanyl-L-histidinamide as a conformational restriction at the P2-P4 tripeptide portion of the angiotensinogen template Suvit Thaisrivongs, James R. Blinn, Donald T. Pals, and Steve R. Turner pp 1276 - 1282; DOI: 10.1021/jm00108a006 |
Novel indole-2-carboxylates as ligands for the strychnine-insensitive N-methyl-D-aspartate-linked glycine receptor Nancy M. Gray, Michael S. Dappen, Brian K. Cheng, Alexis A. Cordi, John P. Biesterfeldt, William F. Hood, and Joseph B. Monahan pp 1283 - 1292; DOI: 10.1021/jm00108a007 |
Role of the spacer in conferring .kappa. opioid receptor selectivity to bivalent ligands related to norbinaltorphimine P. S. Portoghese, A. Garzon-Aburbeh, H. Nagase, C. E. Lin, and A. E. Takemori pp 1292 - 1296; DOI: 10.1021/jm00108a008 |
Synthesis and properties of some peptide analogs of actinomycin D Anthony B. Mauger, Oswald A. Stuart, and Edward Katz pp 1297 - 1301; DOI: 10.1021/jm00108a009 |
Interaction of GTP derivatives with cellular and oncogenic ras-p21 proteins Timothy Noonan, Neal Brown, Lech Dudycz, and George Wright pp 1302 - 1307; DOI: 10.1021/jm00108a010 |
Synthesis and biochemical evaluation of baclofen analogs locked in the baclofen solid-state conformation Andre Mann, Thierry Boulanger, Barbara Brandau, Francois Durant, Guy Evrard, Michel Heaulme, Eric Desaulles, and Camille Georges Wermuth pp 1307 - 1313; DOI: 10.1021/jm00108a011 |
Optical isomers of rocastine and close analogs: synthesis and H1 antihistaminic activity of its enantiomers and their structural relationship to the classical antihistamines Mark C. Sleevi, Albert D. Cale, Thomas W. Gero, Larry W. Jaques, William J. Welstead, Ashby F. Johnson, Brian F. Kilpatrick, Iulia Demian, Joseph C. Nolan, and Herndon Jenkins pp 1314 - 1328; DOI: 10.1021/jm00108a012 |
Synthesis and aromatase inhibitory activity of novel 1-(4-aminophenyl)-3-azabicyclo[3.1.0]hexane- and -[3.1.1]heptane-2,4-diones Jaroslav Stanek, Alex Alder, Daniel Bellus, Ajay S. Bhatnagar, Albert Haeusler, and Klaus Schieweck pp 1329 - 1334; DOI: 10.1021/jm00108a013 |
2-Alkoxyadenosines: potent and selective agonists at the coronary artery A2 adenosine receptor Masayuki Ueeda, Robert D. Thompson, Luis H. Arroyo, and Ray A. Olsson pp 1334 - 1339; DOI: 10.1021/jm00108a014 |
2-Aralkoxyadenosines: potent and selective agonists at the coronary artery A2 adenosine receptor Masayuki Ueeda, Robert D. Thompson, Luis H. Arroyo, and Ray A. Olsson pp 1340 - 1344; DOI: 10.1021/jm00108a015 |
Inhibition of human placental aromatase by novel homologated 19-oxiranyl and 19-thiiranyl steroids Wayne E. Childers, James V. Silverton, James T. Kellis, Larry E. Vickery, and Cecil H. Robinson pp 1344 - 1349; DOI: 10.1021/jm00108a016 |
Function of negative charge in the "address domain" of deltorphins L. H. Lazarus, S. Salvadori, V. Santagada, R. Tomatis, and W. E. Wilson pp 1350 - 1355; DOI: 10.1021/jm00108a017 |
New dibenzothiadiazepine derivatives with antidepressant activities Danilo Giannotti, Giovanni Viti, Piero Sbraci, Vittorio Pestellini, Giovanna Volterra, Franco Borsini, Alessandro Lecci, Alberto Meli, Paolo Dapporto, and Paola Paoli pp 1356 - 1362; DOI: 10.1021/jm00108a018 |
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 4. Effect of various side-chain substituents on therapeutic activity against anticholinesterase intoxication Dane A. Goff, Gary A. Koolpe, Andrew B. Kelson, Huynh M. Vu, Dorris L. Taylor, Clifford D. Bedford, Ralph N. Harris, H. A. Mussalam, and Irwin Koplovitz pp 1363 - 1368; DOI: 10.1021/jm00108a019 |
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 5. Structure-activity relationships for side-chain nitro-, sulfone-, amino-, and aminosulfonyl-substituted analogs for therapy against anticholinesterase intoxication Gary A. Koolpe, Steven M. Lovejoy, Dane A. Goff, Kuei Ying Lin, Doris S. Leung, Clifford D. Bedford, Ralph N. Harris, H. A. Musallam, and Irwin Koplovitz pp 1368 - 1376; DOI: 10.1021/jm00108a020 |
In vitro evaluation of phosphocholine and quaternary ammonium containing lipids as novel anti-HIV agents Karen L. Meyer, Canino J. Marasco, Susan L. Morris-Natschke, Khalid S. Ishaq, Claude Piantadosi, and Louis S. Kucera pp 1377 - 1383; DOI: 10.1021/jm00108a021 |
Receptor-based design of novel dihydrofolate reductase inhibitors: benzimidazole and indole derivatives Kwasi A. Ohemeng and Barbara Roth pp 1383 - 1394; DOI: 10.1021/jm00108a022 |
Synthesis and anti-HIV activity of 2-, 3-, and 4-substituted analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) Hiromichi Tanaka, Masanori Baba, Masaru Ubasawa, Hideaki Takashima, Kouichi Sekiya, Issei Nitta, Shiro Shigeta, Richard T. Walker, Erik De Clercq, and Tadashi Miyasaka pp 1394 - 1399; DOI: 10.1021/jm00108a023 |
Synthesis of potential dual-acting radiation sensitizer antineoplastic agents: 2,2-dimethylphosphoraziridines containing 2-nitroimidazoles or other electron-affinic moieties Michael E. Perlman, Joseph A. Dunn, Thomas A. Piscitelli, Julie Earle, William C. Rose, Galen L. Wampler, Joan E. MacDiarmid, and Thomas J. Bardos pp 1400 - 1407; DOI: 10.1021/jm00108a024 |
Synthesis and evaluation of novel ether lipid nucleoside conjugates for anti-HIV-1 activity Claude Piantadosi, Canio J. Marasco Jr., Susan L. Morris-Natschke, Karen L. Meyer, Fatma Gumus, Jefferson R. Surles, Khalid S. Ishaq, Louis S. Kucera, Nathan Iyer, and et al. pp 1408 - 1414; DOI: 10.1021/jm00108a025 |
Synthesis and antiviral activity of enantiomeric forms of cyclobutyl nucleoside analogs Gregory S. Bisacchi, Abbe Braitman, Christopher W. Cianci, Junius M. Clark, A. Kirk Field, Moira E. Hagen, Deborah R. Hockstein, Mary F. Malley, Toomas Mitt, and et al. pp 1415 - 1421; DOI: 10.1021/jm00108a026 |
2-Acetylpyridine thiosemicarbazones. 13. Derivatives with antifilarial activity Daniel L. Klayman, Ai J. Lin, John W. McCall, Shao Yin Wang, Simon Townson, Max Grogl, and Kenneth E. Kinnamon pp 1422 - 1425; DOI: 10.1021/jm00108a027 |
Synthesis and antiretrovirus properties of 5'-isocyano-5'-deoxythymidine,5'-isocyano-2',5'-dideoxyuridine,3'-azido-5'-isocyano-3',5'-dideoxythymidine, and 3'-azido-5'-isocyano-2',3',5'-trideoxyuridine Johann Hiebl, Erich Zbiral, Jan Balzarini, and Erik De Clercq pp 1426 - 1430; DOI: 10.1021/jm00108a028 |
1,3,8-Trisubstituted xanthines. Effects of substitution pattern upon adenosine receptor A1/A2 affinity Ronald H. Erickson, Roger N. Hiner, Scott W. Feeney, Paul R. Blake, Waclaw J. Rzeszotarski, Rickey P. Hicks, Diane G. Costello, and Mary E. Abreu pp 1431 - 1435; DOI: 10.1021/jm00108a029 |
Crystal, solution, and molecular modeling structural properties and muscarinic antagonist activity of azaprophen F. Ivy Carroll, Philip Abraham, S. Wayne Mascarella, P. Singh, Charles G. Moreland, S. S. Sankar, Yong Wha Kwon, and David J. Triggle pp 1436 - 1440; DOI: 10.1021/jm00108a030 |
Thienotriazolodiazepines as platelet-activating factor antagonists. Steric limitations for the substituent in position 2 Armin Walser, Thomas Flynn, Carl Mason, Herman Crowley, Catherine Maresca, and Margaret O'Donnell pp 1440 - 1446; DOI: 10.1021/jm00108a031 |
Synthesis and in vitro biological activity of new deaza analogs of folic acid, aminopterin, and methotrexate with an L-ornithine side chain Andre Rosowsky, Ronald A. Forsch, Henry Bader, and James H. Freisheim pp 1447 - 1454; DOI: 10.1021/jm00108a032 |
Recognition of cholinergic agonists by the muscarinic receptor. 2. Pilocarpine Jerome M. Schulman, Rosalie C. Peck, and Raymond L. Disch pp 1455 - 1459; DOI: 10.1021/jm00108a033 |
Synthesis and structure-activity studies of alkyl-substituted .gamma.-butyrolactones and .gamma.-thiobutyrolactones: ligands for the picrotoxin receptor Daniel J. Canney, Katherine D. Holland, Jeffrey A. Levine, Ann C. McKeon, James A. Ferrendelli, and Douglas F. Covey pp 1460 - 1467; DOI: 10.1021/jm00108a034 |
New derivatives of kanamycin B obtained by modifications and substitutions in position 6''. 1. Synthesis and microbiological evaluation A. Van Schepdael, J. Delcourt, M. Mulier, R. Busson, L. Verbist, H. J. Vanderhaeghe, M. P. Mingeot-Leclercq, P. M. Tulkens, and P. J. Claes pp 1468 - 1475; DOI: 10.1021/jm00108a035 |
New derivatives of kanamycin B obtained by modifications and substitutions in position 6''. 2. In vitro and computer-aided toxicological evaluation with respect to interactions with phosphatidylinositol M. P. Mingeot-Leclercq, A. Van Schepdael, R. Brasseur, R. Busson, H. J. Vanderhaeghe, P. J. Claes, and P. M. Tulkens pp 1476 - 1482; DOI: 10.1021/jm00108a036 |
New derivatives of kanamycin B obtained by combined modifications in positions 1 and 6". Synthesis, microbiological properties, and in vitro and computer-aided toxicological evaluation A. Van Schepdael, R. Busson, H. J. Vanderhaeghe, P. J. Claes, L. Verbist, M. P. Mingeot-Leclercq, R. Brasseur, and P. M. Tulkens pp 1483 - 1492; DOI: 10.1021/jm00108a037 |
Quinazolineacetic acids and related analogs as aldose reductase inhibitors Michael S. Malamas and Jane Millen pp 1492 - 1503; DOI: 10.1021/jm00108a038 |
Novel caffeic acid derivatives: extremely potent inhibitors of 12-lipoxygenase Hidetsura Cho, Masaru Ueda, Mie Tamaoka, Mikiko Hamaguchi, Kazuo Aisaka, Yoshinobu Kiso, Teruyoshi Inoue, Ryoko Ogino, Toshio Tatsuoka, and et al. pp 1503 - 1505; DOI: 10.1021/jm00108a039 |
Quinazolinone cholecystokinin-B receptor ligands Melvin J. Yu, K. Jeff Thrasher, Jefferson R. McCowan, Norma R. Mason, and Laurane G. Mendelsohn pp 1505 - 1508; DOI: 10.1021/jm00108a040 |
Specific anti-HIV-1 acyclonucleosides which cannot be phosphorylated: synthesis of some deoxy analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine Hiromichi Tanaka, Masanori Baba, Shigeru Saito, Tadashi Miyasaka, Hideaki Takashima, Kouichi Sekiya, Masaru Ubasawa, Issei Nitta, Richard T. Walker, and et al. pp 1508 - 1511; DOI: 10.1021/jm00108a041 |
Novel synthesis and biochemical properties of an [125I]-labeled photoaffinity probe for thromboxane A2/prostaglandin H2 receptors Dale E. Mais, Nancy L. Bowling, Timothy A. True, Masao Naka, Thomas A. Morinelli, John E. Oatis, Nobuyuki Hamanaka, and Perry V. Halushka pp 1511 - 1514; DOI: 10.1021/jm00108a042 |
1-(Carboxybenzyl)imidazole-5-acrylic acids: potent and selective angiotensin II receptor antagonists Joseph Weinstock, Richard M. Keenan, James Samanen, Judith Hempel, Joseph A. Finkelstein, Robert G. Franz, Dimitri E. Gaitanopoulos, Gerald R. Girard, John G. Gleason, and et al. pp 1514 - 1517; DOI: 10.1021/jm00108a043 |
Synthesis and pharmacology of the enantiomers of cis-7-hydroxy-3-methyl-2-(dipropylamino)tetralin [Erratum to document cited in CA113(21):190865h] Anette M. Johansson, Karin Fredriksson, Uli Hacksell, Cor J. Grol, Kjell Svensson, Arvid Carlsson, and Staffan Sundell pp 1517 - 1517; DOI: 10.1021/jm00108a044 |
Book Reviews pp 1518 - 1520; DOI: 10.1021/jm00108a600 |
S-Adenosyl-L-homocysteine hydrolase as a target for antiviral chemotherapy Michael S. Wolfe and Ronald T. Borchardt pp 1521 - 1530; DOI: 10.1021/jm00109a001 |
Novel site-directed affinity ligands for GABA-gated chloride channels: synthesis, characterization, and molecular modeling of 1-(isothiocyanatophenyl)-4-tert-butyl-2,6,7-trioxabicyclo[2.2.2]octanes Brian R. De Costa, Anita H. Lewin, Kenner C. Rice, Phil Skolnick, and Joyce A. Schoenheimer pp 1531 - 1538; DOI: 10.1021/jm00109a002 |
Benzyloxazolidine-2,4-diones as potent hypoglycemic agents Robert L. Dow, Bruce M. Bechle, Thomas T. Chou, David A. Clark, Bernard Hulin, and Ralph W. Stevenson pp 1538 - 1544; DOI: 10.1021/jm00109a003 |
(Benzoylphenyl)piperidines: a new class of immunomodulators Francois D. Bellamy, Jean B. Chazan, Pierre Dodey, Patrick Dutartre, Khan Ou, Marc Pascal, and Jacques Robin pp 1545 - 1552; DOI: 10.1021/jm00109a004 |
DNA-directed alkylating agents. 4. 4-Anilinoquinoline-based minor groove directed aniline mustards G. Lance Gravatt, Bruce C. Baguley, William R. Wilson, and William A. Denny pp 1552 - 1560; DOI: 10.1021/jm00109a005 |
5-Lipoxygenase inhibitors: the synthesis and structure-activity relationships of a series of 1-phenyl-3-pyrazolidinones Dennis J. Hlasta, Francis B. Casey, Edward W. Ferguson, Sally J. Gangell, Martha R. Heimann, Edward P. Jaeger, Rudolph K. Kullnig, and Robert J. Gordon pp 1560 - 1570; DOI: 10.1021/jm00109a006 |
The synthesis and potassium channel blocking activity of some (4-methanesulfonamidophenoxy)propanolamines as potential class III antiarrhythmic agents Sean P. Connors, Paul D. Dennis, Edward W. Gill, and Derek A. Terrar pp 1570 - 1577; DOI: 10.1021/jm00109a007 |
Phosphonate-containing inhibitors of tyrosine-specific protein kinases Terrence R. Burke, Zhen Hong Li, Joseph B. Bolen, and Victor E. Marquez pp 1577 - 1581; DOI: 10.1021/jm00109a008 |
Structure-activity studies on a potent antagonist to organophosphate-induced toxicity Joseph G. Cannon, M. Fethi Sahin, Ranbir K. Bhatnagar, Jan R. Flynn, and John Paul Long pp 1582 - 1584; DOI: 10.1021/jm00109a009 |
Aminoalkynyldithianes. A new class of calcium channel blockers Theodore C. Adams, Andrea C. Dupont, J. Paul Carter, James F. Kachur, Maria E. Guzewska, W. Janusz Rzeszotarski, Stephen G. Farmer, Lalita Noronha-Blob, and Carl Kaiser pp 1585 - 1593; DOI: 10.1021/jm00109a010 |
Quinazoline antifolate thymidylate synthase inhibitors: heterocyclic benzoyl ring modifications Peter R. Marsham, Leslie R. Hughes, Ann L. Jackman, Anthony J. Hayter, John Oldfield, J. Michael Wardleworth, Joel A. M. Bishop, Brigid M. O'Connor, and A. Hilary Calvert pp 1594 - 1605; DOI: 10.1021/jm00109a011 |
Escherichia coli mediated biosynthesis and in vitro anti-HIV activity of lipophilic 6-halo-2',3'-dideoxypurine nucleosides Kunichika Murakami, Takuma Shirasaka, Hidetoshi Yoshioka, Eiji Kojima, Shizuko Aoki, Harry Ford, John S. Driscoll, James A. Kelley, and Hiroaki Mitsuya pp 1606 - 1612; DOI: 10.1021/jm00109a012 |
Synthesis and in vitro evaluation of 2,3-dimethoxy-5-(fluoroalkyl)-substituted benzamides: high-affinity ligands for CNS dopamine D2 receptors John E. Bishop, Chester A. Mathis, John M. Gerdes, John M. Whitney, Allison M. Eaton, and Richard B. Mailman pp 1612 - 1624; DOI: 10.1021/jm00109a013 |
Synthesis and biological activity of new halo-steroidal antiestrogens Charles Levesque, Yves Merand, Jean Marc Dufour, Claude Labrie, and Fernand Labrie pp 1624 - 1630; DOI: 10.1021/jm00109a014 |
Synthesis and anthelmintic activity of 3'-benzoylurea derivatives of 6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole Robert J. Weikert, Stanford Bingham, Mark A. Emanuel, Elizabeth B. Fraser-Smith, David G. Loughhead, Peter H. Nelson, and Anthony L. Poulton pp 1630 - 1633; DOI: 10.1021/jm00109a015 |
Synthesis and antimalarial activity of 2-aziridinyl- and 2,3-bis(aziridinyl)-1,4-naphthoquinonyl sulfonate and acylate derivatives Tai Shun Lin, Li Ya Zhu, Shi Ping Xu, Alan A. Divo, and Alan C. Sartorelli pp 1634 - 1639; DOI: 10.1021/jm00109a016 |
Fluorinated sugar analogs of potential anti-HIV-1 nucleosides Jai Tung Huang, Ling Ching Chen, Liben Wang, Moon Hwan Kim, James A. Warshaw, Donald Armstrong, Qing Yu Zhu, Ting Chao Chou, Kyoichi A. Watanabe, and et al. pp 1640 - 1646; DOI: 10.1021/jm00109a017 |
Potential anti-AIDS drugs. Lipophilic, adenosine deaminase-activated prodrugs Joseph J. Barchi, Victor E. Marquez, John S. Driscoll, Harry Ford, Hiroaki Mitsuya, Takuma Shirasaka, Shizuko Aoki, and James A. Kelley pp 1647 - 1655; DOI: 10.1021/jm00109a018 |
Synthesis and structure-activity relationships of deltorphins analogs Severo Salvadori, Mauro Marastoni, Gianfranco Balboni, Pier Andrea Borea, Michele Morari, and Roberto Tomatis pp 1656 - 1661; DOI: 10.1021/jm00109a019 |
Synthesis and pharmacological examination of 1-(3-methoxy-4-methylphenyl)-2-aminopropane and 5-methoxy-6-methyl-2-aminoindan: similarities to 3,4-(methylenedioxy)methamphetamine (MDMA) Michael P. Johnson, Stewart P. Frescas, Robert Oberlender, and David E. Nichols pp 1662 - 1668; DOI: 10.1021/jm00109a020 |
Using theoretical descriptors in quantitative structure-activity relationships: some toxicological indices Leland Y. Wilson and George R. Famini pp 1668 - 1674; DOI: 10.1021/jm00109a021 |
Compounds from Danshen. Part 4. Structure-activity relationship of miltirone, an active central benzodiazepine receptor ligand isolated from Salvia miltiorrhiza Bunge (Danshen) Hson Mou Chang, Kuk Ying Chui, Fan Wah Lau Tan, Yun Yang, Zeng Pei Zhong, Chi Ming Lee, Hing Leung Sham, and Henry N. C. Wong pp 1675 - 1692; DOI: 10.1021/jm00109a022 |
Synthesis of the 2-amino-4-phosphonobutanoic acid analogs (E)- and (Z)-2-amino-2,3-methano-4-phosphonobutanoic acid and their evaluation as inhibitors of hippocampal excitatory neurotransmission Heather B. Kroona, Nancy L. Peterson, James F. Koerner, and Rodney L. Johnson pp 1692 - 1699; DOI: 10.1021/jm00109a023 |
Anesthetic steroid mobility in model membrane preparations examined by high-resolution proton and deuterium NMR spectroscopy Alexandros Makriyannis, Christine M. DiMeglio, and Stephen W. Fesik pp 1700 - 1703; DOI: 10.1021/jm00109a024 |
Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene D4 receptor antagonists. 4. Addition of chromone moiety enhances leukotriene D4 receptor binding affinity Fu Chih Huang, Robert A. Galemmo, Gregory B. Poli, Keith S. Learn, Mathew M. Morrissette, William H. Johnson, William P. Dankulich, Henry F. Campbell, Gilbert W. Carnathan, and Richard G. Van Inwegen pp 1704 - 1707; DOI: 10.1021/jm00109a025 |
Conformational properties of semirigid antipsychotic drugs: the pharmacophore for dopamine D2 antagonist activity Mark Froimowitz and Sten Raemsby pp 1707 - 1714; DOI: 10.1021/jm00109a026 |
Role of spacer and address components in peptidomimetic .delta.-opioid receptor antagonists related to naltrindole P. S. Portoghese, H. Nagase, K. E. MaloneyHuss, C. E. Lin, and A. E. Takemori pp 1715 - 1720; DOI: 10.1021/jm00109a027 |
Synthesis and hypocholesterolemic activity of 6,7-dihydro-4H-pyrazolo[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-diones, novel inhibitors of acylCoA: cholesterol O-acyltransferase Scott D. Larsen, Charles H. Spilman, Frank P. Bell, Dac M. Dinh, Esther Martinborough, and Gracella J. Wilson pp 1721 - 1727; DOI: 10.1021/jm00109a028 |
Synthesis and receptor binding of N-substituted tropane derivatives. High-affinity ligands for the cocaine receptor Richard A. Milius, Jayanta K. Saha, Bertha K. Madras, and John L. Neumeyer pp 1728 - 1731; DOI: 10.1021/jm00109a029 |
Synthesis, hydrolysis rates, supercomputer modeling, and antibacterial activity of bicyclic tetrahydropyridazinones Louis N. Jungheim, Donald B. Boyd, Joseph M. Indelicato, Carol E. Pasini, David A. Preston, and William E. Alborn pp 1732 - 1739; DOI: 10.1021/jm00109a030 |
Synthesis and quantitative structure-activity relationship analysis of 2-(aryl or heteroaryl)quinolin-4-amines, a new class of anti-HIV-1 agents Lucjan Strekowski, Jerzy L. Mokrosz, Vidya A. Honkan, Agnieszka Czarny, Marek T. Cegla, Roman L. Wydra, Steven E. Patterson, and Raymond F. Schinazi pp 1739 - 1746; DOI: 10.1021/jm00109a031 |
Synthesis and bioactivity of N.omega.-hydroxyarginine: a possible intermediate in the biosynthesis of nitric oxide from arginine Guillermo C. Wallace and Jon M. Fukuto pp 1746 - 1748; DOI: 10.1021/jm00109a032 |
Novel time-dependent inhibitors of human placental aromatase Joseph P. Burkhart, Norton P. Peet, C. Lee Wright, and J. O'Neal Johnston pp 1748 - 1750; DOI: 10.1021/jm00109a033 |
Imidazo[4,5-b]quinoxaline cyanines as neurokinin antagonists Kenneth C. Appell, Bruce E. Babb, Ramanuj Goswami, Patricia L. Hall, Kristine B. Lawrence, Margaret E. Logan, Rose Przyklek-Elling, Bruce E. Tomczuk, Bhaskar R. Venepalli, and John M. Yanni pp 1751 - 1753; DOI: 10.1021/jm00109a034 |
The agonist pharmacophore of the benzodiazepine receptor. Synthesis of a selective anticonvulsant/anxiolytic Hernando Diaz-Arauzo, Gary E. Evoniuk, Phil Skolnick, and James M. Cook pp 1754 - 1756; DOI: 10.1021/jm00109a035 |
An approach to the design of receptor-type-selective nonpeptide antagonists of peptidergic receptors: .delta. opioid antagonists Philip S. Portoghese pp 1757 - 1762; DOI: 10.1021/jm00110a001 |
Dexamethasone 21-(.beta.-isothiocyanatoethyl)thio ether: a new affinity label for glucocorticoid receptors Susana Lopez and S. Stoney Simons pp 1762 - 1767; DOI: 10.1021/jm00110a002 |
Synthesis and antiviral activity of 5-heteroaryl-substituted 2'-deoxyuridines P. Wigerinck, R. Snoeck, P. Claes, E. De Clercq, and P. Herdewijn pp 1767 - 1772; DOI: 10.1021/jm00110a003 |
Substituent effect on the stereochemistry of H2-receptor antagonists of the phenylformamidine series. A conformation-dependent mode of interaction with the H2 receptor Arturo Donetti, Harold M. M. Bastiaans, Klaas Kramer, Giuseppe Bietti, Enzo Ceeda, Enrica Dubini, Maurizio Mondoni, Aalt Bast, and Hendrik Timmerman pp 1772 - 1776; DOI: 10.1021/jm00110a004 |
Synthesis, conformational properties, and antibody recognition of peptides containing .beta.-turn mimetics based on .alpha.-alkylproline derivatives Mark G. Hinds, John H. Welsh, David M. Brennand, J. Fisher, Martin J. Glennie, Nigel G. J. Richards, David L. Turner, and John A. Robinson pp 1777 - 1789; DOI: 10.1021/jm00110a005 |
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 1. (.+-.)-(3-Pyridinylbicycloheptyl)alkanoic acids Shripad S. Bhagwat, Candido Gude, David S. Cohen, Warren Lee, Patricia Furness, and Frank H. Clarke pp 1790 - 1797; DOI: 10.1021/jm00110a006 |
Structure/activity and molecular modeling studies of the lophotoxin family of irreversible nicotinic receptor antagonists Stewart N. Abramson, Jacqueline A. Trischman, Dianne M. Tapiolas, Edward E. Harold, William Fenical, and Palmer Taylor pp 1798 - 1804; DOI: 10.1021/jm00110a007 |
New isomeric classes of topically active ocular hypotensive carbonic anhydrase inhibitors: 5-substituted thieno[2,3-b]thiophene-2-sulfonamides and 5-substituted thieno[3,2-b]thiophene-2-sulfonamides John D. Prugh, George D. Hartman, Pierre J. Mallorga, Brian M. McKeever, Stuart R. Michelson, Mark A. Murcko, Harvey Schwam, Robert L. Smith, John M. Sondey, and et al. pp 1805 - 1818; DOI: 10.1021/jm00110a008 |
Flavins as potential antimalarials. 2. 3-Methyl-10-(substituted-phenyl)flavins William B. Cowden, Peter K. Halladay, Ross B. Cunningham, Nicholas H. Hunt, and Ian A. Clark pp 1818 - 1822; DOI: 10.1021/jm00110a009 |
Topographically designed analogs of [cyclic] [D-Pen2,D-Pen5]enkephalin Victor J. Hruby, Geza Toth, Catherine A. Gehrig, Lung Fa Kao, Richard Knapp, George K. Lui, Henry I. Yamamura, Thomas H. Kramer, P. Davis, and Thomas F. Burks pp 1823 - 1830; DOI: 10.1021/jm00110a010 |
Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study and antiviral activity Yvette Henin, Catherine Gouyette, Olivier Schwartz, Jean Claude Debouzy, Jean Michel Neumann, and Huynh Dinh Tam pp 1830 - 1837; DOI: 10.1021/jm00110a011 |
Oxidation of dihydropyridine calcium channel blockers and analogs by human liver cytochrome P-450 IIIA4 F. Peter Guengerich, William R. Brian, Masahiko Iwasaki, Marie Agnes Sari, Catharina Baeaernhielm, and Peder Berntsson pp 1838 - 1844; DOI: 10.1021/jm00110a012 |
Synthesis and anticonvulsant activity of 2-iminohydantoins Chul Hoon Kwon, Muhammad Tahir Iqbal, and John N. D. Wurpel pp 1845 - 1849; DOI: 10.1021/jm00110a013 |
Pyrimido[5,4-b]indole derivatives. 1. A new class of potent and selective .alpha.1 adrenoceptor ligands Filippo Russo, Giuseppe Romeo, Salvatore Guccione, and Antonio De Blasi pp 1850 - 1854; DOI: 10.1021/jm00110a014 |
Binding of substituted and conformationally restricted derivatives of N-(3-phenyl-n-propyl)-1-phenyl-2-aminopropane at .sigma.-receptors Richard A. Glennon, Abd M. Ismaiel, J. Doyle Smith, Mamoun Yousif, Mahmoud El-Ashmawy, J. L. Herndon, James B. Fischer, Kathleen J. Burke Howie, and Alfred C. Server pp 1855 - 1859; DOI: 10.1021/jm00110a015 |
1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents John A. Lowe, III, Thomas F. Seeger, Arthur A. Nagel, Harry R. Howard, Patricia A. Seymour, James H. Heym, Frank E. Ewing, Michael E. Newman, Anne W. Schmidt, and et al. pp 1860 - 1866; DOI: 10.1021/jm00110a016 |
Radiosynthesis of .sigma. receptor ligands for positron emission tomography: carbon-11 and fluorine-18 labeled guanidines Alan A. Wilson, Robert F. Dannals, Hayden T. Ravert, Mark S. Sonders, Eckard Weber, and Henry N. Wagner pp 1867 - 1870; DOI: 10.1021/jm00110a017 |
Streptonigrin and related compounds. 5. Synthesis and evaluation of some isoquinoline analogs Koppaka V. Rao and Joseph W. Beach pp 1871 - 1879; DOI: 10.1021/jm00110a018 |
2'-Deoxy-2'-methylenecytidine and 2'-deoxy-2',2'-difluorocytidine 5'-diphosphates: potent mechanism-based inhibitors of ribonucleotide reductase C. H. Baker, J. Banzon, J. M. Bollinger, J. Stubbe, V. Samano, M. J. Robins, B. Lippert, E. Jarvi, and R. Resvick pp 1879 - 1884; DOI: 10.1021/jm00110a019 |
FTIR spectral study of intramolecular hydrogen bonding in thromboxane A2 receptor antagonist S-145 and related compounds. 3. Conformation and activity of S-145 analogs Mamoru Takasuka, Masumi Yamakawa, and Mitsuaki Ohtani pp 1885 - 1891; DOI: 10.1021/jm00110a020 |
Naphtho and benzo analogs of the .kappa. opioid agonist trans-(.+-.)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzeneacetamide Jeremiah P. Freeman, Eric T. Michalson, Stan V. D'Andrea, Lubomir Baczynskyj, Philip F. VonVoigtlander, R. A. Lahti, Martin W. Smith, Charles F. Lawson, Terrence A. Scahill, and et al. pp 1891 - 1896; DOI: 10.1021/jm00110a021 |
Tyrphostins. II. Heterocyclic and .alpha.-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases Aviv Gazit, Nir Osherov, Israel Posner, Pnina Yaish, Enrique Poradosu, Chaim Gilon, and Alexander Levitzki pp 1896 - 1907; DOI: 10.1021/jm00110a022 |
Linear discriminant and multiple regression analyses of anticoccidial triazines James W. McFarland, Christopher B. Cooper, and Deborah M. Newcomb pp 1908 - 1911; DOI: 10.1021/jm00110a023 |
Isoprenyl phosphinylformates: new inhibitors of squalene synthetase Scott A. Biller, Cornelia Forster, Eric M. Gordon, Thomas Harrity, Lois C. Rich, Joseph Marretta, and Carl P. Ciosek pp 1912 - 1914; DOI: 10.1021/jm00110a024 |
Targeting renal dipeptidase (dehydropeptidase I) for inactivation by mechanism-based inactivators Yong Qian Wu and Shahriar Mobashery pp 1914 - 1916; DOI: 10.1021/jm00110a025 |
Book Reviews pp 1916 - 1924; DOI: 10.1021/jm00110a600 |
Design of enzyme inhibitors using iterative protein crystallographic analysis Krzysztof Appelt, Russell J. Bacquet, Charlotte A. Bartlett, Carol L. J. Booth, Stephan T. Freer, Mary Ann M. Fuhry, Michael R. Gehring, Steven M. Herrmann, Eleanor F. Howland, and et al. pp 1925 - 1934; DOI: 10.1021/jm00111a001 |
Renin inhibitors containing esters at the P2-position. Oral activity in a derivative of methyl aminomalonate Joseph T. Repine, Richard J. Himmelsbach, John C. Hodges, James S. Kaltenbronn, Ila Sircar, Richard W. Skeean, Sean T. Brennan, Timothy R. Hurley, Elizabeth Lunney, and et al. pp 1935 - 1943; DOI: 10.1021/jm00111a002 |
Structural studies on tazobactam Carol A. Toomer, Carl H. Schwalbe, Neil S. Ringan, Peter A. Lambert, Philip R. Lowe, and Ving J. Lee pp 1944 - 1947; DOI: 10.1021/jm00111a003 |
Additional nucleotide derivatives of mitosenes. Synthesis and activity against parental and multidrug resistant L1210 leukemia Bhashyam S. Iyengar, Robert T. Dorr, and William A. Remers pp 1947 - 1951; DOI: 10.1021/jm00111a004 |
Synthetic approaches to the guanosine and xanthosine analogs 5-amino-3-.beta.-D-ribofuranosylpyrazolo[3,4-e][1,3]oxazin-7-one and 3-.beta.-D-ribofuranosylpyrazolo[3,4-e][1,3]oxazine-5,7-dione and studies of their antitumor potential Ruiming Zou, Vladimir G. Beylin, Michael P. Groziak, Linda L. Wotring, and Leroy B. Townsend pp 1951 - 1959; DOI: 10.1021/jm00111a005 |
Synthesis and biological evaluation of quinocarcin derivatives: thioalkyl-substituted quinones and hydroquinones Hiromitsu Saito, Tadashi Hirata, Masaji Kasai, Kazuhisa Fujimoto, Tadashi Ashizawa, Makoto Morimoto, and Akira Sato pp 1959 - 1966; DOI: 10.1021/jm00111a006 |
Persistent binding of fatty acyl derivatives of naltrexamine to opioid receptors P. S. Portoghese, A. Garzon-Aburbeh, and D. L. Larson pp 1966 - 1969; DOI: 10.1021/jm00111a007 |
Lipopeptides containing 2-(palmitoylamino)-6,7-bis(palmitoyloxy)heptanoic acid: synthesis, stereospecific stimulation of B-lymphocytes and macrophages and adjuvanticity in vivo and in vitro Joerg Metzger, Guenther Jung, Wolfgang G. Bessler, Petra Hoffmann, Marianne Strecker, Albrecht Lieberknecht, and Ulrich Schmidt pp 1969 - 1974; DOI: 10.1021/jm00111a008 |
Quantitative structure-activity relationships of antitumor guanidinothiazolecarboxamides with survival enhancement for therapy in the 3LL Lewis lung carcinoma model Rodney C. Schnur, Randall J. Gallaschun, David H. Singleton, Martin Grissom, Donald E. Sloan, Peter Goodwin, Patricia A. McNiff, Anton F. J. Fliri, F. Michael Mangano, and et al. pp 1975 - 1982; DOI: 10.1021/jm00111a009 |
2-[(Arylmethyl)amino]-2-methyl-1,3-propanediol DNA intercalators. An examination of the effects of aromatic ring variation on antitumor activity and DNA binding Kenneth W. Bair, C. Webster Andrews, Richard L. Tuttle, Vincent C. Knick, Michael Cory, and David D. McKee pp 1983 - 1990; DOI: 10.1021/jm00111a010 |
Computer simulation of the binding of saframycin A to d(GATGCATC)2 G. Craig Hill and William A. Remers pp 1990 - 1998; DOI: 10.1021/jm00111a011 |
New .alpha.-amino phosphonic acid derivatives of vinblastine: chemistry and antitumor activity Gilbert Lavielle, Patrick Hautefaye, Corinne Schaeffer, Jean A. Boutin, Claude A. Cudennec, and Alain Pierre pp 1998 - 2003; DOI: 10.1021/jm00111a012 |
Novel cerebroprotective agents with central nervous system stimulating activity. 1. Synthesis and pharmacology of the 1-amino-7-hydroxyindan derivatives Yasuo Oshiro, Youji Sakurai, Tatsuyoshi Tanaka, Hiraki Ueda, Tetsuro Kikuchi, and Katura Tottori pp 2004 - 2013; DOI: 10.1021/jm00111a013 |
Novel cerebroprotective agents with central nervous system stimulating activity. 2. Synthesis and pharmacology of the 1-(acylamino)-7-hydroxyindan derivatives Yasuo Oshiro, Youji Sakurai, Tatsuyoshi Tanaka, Tetsuro Kikuchi, Tsuyoshi Hirose, and Katsura Tottori pp 2014 - 2023; DOI: 10.1021/jm00111a014 |
Octoclothepin enantiomers. A reinvestigation of their biochemical and pharmacological activity in relation to a new receptor-interaction model for dopamine D-2 receptor antagonists Klaus P. Boegesoe, Tommy Liljefors, Joern Arnt, John Hyttel, and Henrik Pedersen pp 2023 - 2030; DOI: 10.1021/jm00111a015 |
Neurochemistry of aging. 2. Design, synthesis and biological evaluation of halomethyl analogs of choline with high affinity choline transport inhibitory activity Jehangir S. Mistry, Donald J. Abraham, Alan P. Kozikowski, and Israel Hanin pp 2031 - 2036; DOI: 10.1021/jm00111a016 |
An NMR and theoretical study of the conformation and internal flexibility of butaclamol hydrochloride Marco G. Casarotto, David J. Craik, Edward J. Lloyd, and Ashton C. Partridge pp 2036 - 2043; DOI: 10.1021/jm00111a017 |
NMR studies of the conformational interconversion of butaclamol in solution Marco G. Casarotto, David J. Craik, and Edward J. Lloyd pp 2043 - 2049; DOI: 10.1021/jm00111a018 |
Electron-deficient isoalloxazines: model systems for disulfide prodrug formation John R. Cashman and Yan Liu pp 2049 - 2055; DOI: 10.1021/jm00111a019 |
Direct prediction of dissociation constants (pKa's) of clonidine-like imidazolines, 2-substituted imidazoles and 1-methyl-2-substituted-imidazoles from 3D structures using a comparative molecular field analysis (CoMFA) approach Ki H. Kim and Yvonne C. Martin pp 2056 - 2060; DOI: 10.1021/jm00111a020 |
2-(Oxadiazolyl)- and 2-(thiazolyl)imidazo[1,2-a]pyrimidines as agonists and inverse agonists at benzodiazepine receptors W. Roger Tully, Colin R. Gardner, Roger J. Gillespie, and Robert Westwood pp 2060 - 2067; DOI: 10.1021/jm00111a021 |
Identification and synthesis of a receptor binding site of human anaphylatoxin C5a Megumi Kawai, David A. Quincy, Benjamin Lane, Karl W. Mollison, Jay R. Luly, and George W. Carter pp 2068 - 2071; DOI: 10.1021/jm00111a022 |
Evaluation of desferrithiocin and its synthetic analogs as orally effective iron chelators Raymond J. Bergeron, Jan Wiegand, John B. Dionis, Majia Egli-Karmakka, Joerg Frei, Alica Huxley-Tencer, and Heinrich H. Peter pp 2072 - 2078; DOI: 10.1021/jm00111a023 |
Computer simulation of the binding of naphthyridinomycin and cyanocycline A to DNA G. Craig Hill, Timothy P. Wunz, Neil E. MacKenzie, Paul R. Gooley, and William A. Remers pp 2079 - 2088; DOI: 10.1021/jm00111a024 |
Improvement in potency of an oxytocin antagonist after systematic substitutions with L-tryptophan George Flouret, William Brieher, Tadeusz Majewski, Kevin Mahan, and Laird Wilson pp 2089 - 2094; DOI: 10.1021/jm00111a025 |
Stereospecific synthesis of (R)- and (S)-S-adenosyl-1,8-diamino-3-thiooctane, a potent inhibitor of polyamine biosynthesis. Comparison of asymmetric induction vs enantiomeric synthesis Chin Liu and James K. Coward pp 2094 - 2101; DOI: 10.1021/jm00111a026 |
Gastrin releasing peptide antagonists with improved potency and stability David C. Heimbrook, Walfred S. Saari, Nancy L. Balishin, Thorsten W. Fisher, Arthur Friedman, David M. Kiefer, Nicola S. Rotberg, John W. Wallen, and Allen Oliff pp 2102 - 2107; DOI: 10.1021/jm00111a027 |
Determination of dissociation constants of high affinity (pM) human renin inhibitors: application to analogs of ditekiren (U-71,038) D. E. Epps, R. A. Poorman, F. Mandel, and H. J. Schostarez pp 2107 - 2112; DOI: 10.1021/jm00111a028 |
Synthesis of a series of nitrothiophenes with basic or electrophilic substituents and evaluation as radiosensitizers and as bioreductively activated cytotoxins Michael D. Threadgill, Paul Webb, Peter O'Neill, Matthew A. Naylor, Miriam A. Stephens, Ian J. Stratford, Shirley Cole, Gerald E. Adams, and E. Martin Fielden pp 2112 - 2120; DOI: 10.1021/jm00111a029 |
Relative structure-inhibition analyses of the N-benzoyl and N-(phenylsulfonyl) amino acid aldose reductase inhibitors Jack DeRuiter, R. Alan Davis, Vinay G. Wandrekar, and Charles A. Mayfield pp 2120 - 2126; DOI: 10.1021/jm00111a030 |
Synthesis and in vivo photodynamic activity of some bacteriochlorin derivatives against bladder tumors in rodents Alan R. Morgan, Greta M. Garbo, Rick W. Keck, Steven H. Selman, and Dimitris Skalkos pp 2126 - 2133; DOI: 10.1021/jm00111a031 |
Functionalized congener approach to muscarinic antagonists: analogs of pirenzepine Yishai Karton, Barton J. Bradbury, Jesse Baumgold, Robert Paek, and Kenneth A. Jacobson pp 2133 - 2145; DOI: 10.1021/jm00111a032 |
2-Phenylindole-linked [2-(aminoalkyl)pyridine]dichloroplatinum(II): complexes with a selective action on estrogen receptor positive mammary tumors Norbert G. Knebel and Erwin Von Angerer pp 2145 - 2152; DOI: 10.1021/jm00111a033 |
3-O-Alkylascorbic acids as free-radical quenchers: synthesis and inhibitory effect on lipid peroxidation Yasunori Nihro, Hideki Miyataka, Tadamitsu Sudo, Hitoshi Matsumoto, and Toshio Satoh pp 2152 - 2157; DOI: 10.1021/jm00111a034 |
4-Hydroxythiazole inhibitors of 5-lipoxygenase Francis A. J. Kerdesky, James H. Holms, Jimmie L. Moore, Randy L. Bell, Richard D. Dyer, George W. Carter, and Dee W. Brooks pp 2158 - 2165; DOI: 10.1021/jm00111a035 |
Synthesis of an (iodovinyl)misonidazole derivative for hypoxia imaging Joseph E. Biskupiak, John R. Grierson, Janet S. Rasey, Gary V. Martin, and Kenneth A. Krohn pp 2165 - 2168; DOI: 10.1021/jm00111a036 |
Syntheses of 5,7,8- and 5,6,7-trioxygenated 3-alkyl-3',4'-dihydroxyflavones and their inhibitory activities against arachidonate 5-lipoxygenase Tokunaru Horie, Hideaki Tominaga, Yasuhiko Kawamura, Takahiko Hada, Natsuo Ueda, Yumi Amano, and Shozo Yamamoto pp 2169 - 2176; DOI: 10.1021/jm00111a037 |
(Methoxyalkyl)thiazoles: a new series of potent, selective, and orally active 5-lipoxygenase inhibitors displaying high enantioselectivity T. Geoffrey C. Bird, Pierre Bruneau, Graham C. Crawley, Martin P. Edwards, Stephen J. Foster, Jean Marc Girodeau, John F. Kingston, and Rodger M. McMillan pp 2176 - 2186; DOI: 10.1021/jm00111a038 |
Novel thiophene-, pyrrole-, furan-, and benzene carboxamidotetrazoles as potential antiallergy agents Michael D. Mullican, Roderick J. Sorenson, David T. Connor, David O. Thueson, John A. Kennedy, and Mary Carol Conroy pp 2186 - 2194; DOI: 10.1021/jm00111a039 |
Synthesis and antiviral and cytostatic properties of 3'-deoxy-3'-fluoro- and 2'-azido-3'-fluoro-2',3'-dideoxy-D-ribofuranosides of natural heterocyclic bases I. A. Mikhailopulo, N. E. Poopeiko, T. I. Prikota, G. G. Sivets, E. I. Kvasyuk, J. Balzarini, and Erik De Clercq pp 2195 - 2202; DOI: 10.1021/jm00111a040 |
Design, synthesis, and pharmacological evaluation of ultrashort- to long-acting opioid analgesics Paul L. Feldman, Michael K. James, Marcus F. Brackeen, Joanne M. Bilotta, Suzanne V. Schuster, Avis P. Lahey, Michael W. Lutz, M. Ross Johnson, and H. Jeff Leighton pp 2202 - 2208; DOI: 10.1021/jm00111a041 |
Quinazoline antifolate thymidylate synthase inhibitors: bridge modifications and conformationally restricted analogs in the C2-methyl series Peter R. Marsham, Ann L. Jackman, Anthony J. Hayter, Melanie R. Daw, Jayne L. Snowden, Brigid M. O'Connor, Joel A. M. Bishop, A. Hilary Calvert, and Leslie R. Hughes pp 2209 - 2218; DOI: 10.1021/jm00111a042 |
Verapamil analog with restricted molecular flexibility Silvia Dei, M. Novella Romanelli, Serena Scapecchi, Elisabetta Teodori, Alberto Chiarini, and Fulvio Gualtieri pp 2219 - 2225; DOI: 10.1021/jm00111a043 |
Purine and 1-deazapurine ribonucleosides and deoxyribonucleosides: synthesis and biological activity Gloria Cristalli, Sauro Vittori, Alessandra Eleuteri, Mario Grifantini, Rosaria Volpini, Giulio Lupidi, Laura Capolongo, and Enrico Pesenti pp 2226 - 2230; DOI: 10.1021/jm00111a044 |
Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones Karl D. Hargrave, John R. Proudfoot, Karl G. Grozinger, Ernest Cullen, Suresh R. Kapadia, Usha R. Patel, Victor U. Fuchs, Scott C. Mauldin, Jana Vitous, and et al. pp 2231 - 2241; DOI: 10.1021/jm00111a045 |
Synthesis and antidopaminergic activity of some 3-(aminomethyl)tetralones as analogs of butyrophenone Lourdes Cortizo, Lourdes Santana, Enrique Ravina, Francisco Orallo, Jose A. Fontenla, Elena Castro, Jose M. Calleja, and Maria L. De Ceballos pp 2242 - 2247; DOI: 10.1021/jm00111a046 |
Calcium channel blocking and positive inotropic activities of ethyl 5-cyano-1,4-dihydro-6-methyl-2-[(phenylsulfonyl)methyl]-4-aryl-3-pyridinecarboxylate and analogs. Synthesis and structure-activity relationships Ila Sircar, Eva K. Gregor, K. R. Anderson, Stehen J. Haleen, Yu Hsin Shih, Ronald E. Weishaar, Robert P. Steffen, Thomas A. Pugsley, and M. D. Taylor pp 2248 - 2260; DOI: 10.1021/jm00111a047 |
Synthesis and biological evaluation of substituted benzenesulfonamides as novel potent membrane-bound phospholipase A2 inhibitors Hitoshi Oinuma, Tadanobu Takamura, Takashi Hasegawa, Kenichi Nomoto, Toshihiko Naitoh, Yoshiharu Daiku, Sachiyuki Hamano, Hiroshi Kakisawa, and Norio Minami pp 2260 - 2267; DOI: 10.1021/jm00111a048 |
Fluorescent markers for hypoxic cells: a study of nitroaromatic compounds, with fluorescent heterocyclic side chains, that undergo bioreductive binding Richard J. Hodgkiss, Gareth W. Jones, Anthony Long, Richard W. Middleton, John Parrick, Michael R. L. Stratford, Peter Wardman, and George D. Wilson pp 2268 - 2274; DOI: 10.1021/jm00111a049 |
Nucleic acid related compounds. 65. New syntheses of 1-(.beta.-D-arabinofuranosyl)-5(E)-(2-iodovinyl)uracil (IVAraU) from vinylsilane precursors. Radioiodine uptake as a marker for thymidine kinase herpes viral infections Morris J. Robins, Stefano Manfredini, Steven G. Wood, R. James Wanklin, Bruce A. Rennie, and Stephen L. Sacks pp 2275 - 2280; DOI: 10.1021/jm00111a050 |
Structure activity relationship for mitomycin C and mitomycin A analogs Kenneth R. Kunz, Bhashyam S. Iyengar, Robert T. Dorr, David S. Alberts, and William A. Remers pp 2281 - 2286; DOI: 10.1021/jm00111a051 |
A new class of acyclic phosphonate nucleotide analogs: Phosphonate isosteres of acyclovir and ganciclovir monophosphates as antiviral agents Choung Un Kim, Peter F. Misco, Bing Yu Luh, Michael J. M. Hitchcock, Ismail Ghazzouli, and John C. Martin pp 2286 - 2294; DOI: 10.1021/jm00111a052 |
3-Alkyl-4-aminobutyric acids: the first class of anticonvulsant agents that activates L-glutamic acid decarboxylase Richard B. Silverman, Ryszard Andruszkiewicz, Shrenik M. Nanavati, Charles P. Taylor, and Mark G. Vartanian pp 2295 - 2298; DOI: 10.1021/jm00111a053 |
New pepstatin analogs: synthesis and pepsin inhibition Rose M. McConnell, Donna Frizzell, Amanda Camp, Anissa Evans, Wanda Jones, and Cathy Cagle pp 2298 - 2300; DOI: 10.1021/jm00111a054 |
Potent inhibitory effect of a series of modified cyclodextrin sulfates on the replication of HIV-1 in vitro Tamon Moriya, Hironori Kurita, Kazuo Matsumoto, Toru Otake, Haruyo Mori, Motoko Morimoto, Noboru Ueba, and Nobuharu Kunita pp 2301 - 2304; DOI: 10.1021/jm00111a055 |
Rationally designed "dipeptoid" analogs of CCK. .alpha.-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties [Erratum to document cited in CA114(5):43545w] David C. Horwell, John Hughes, John C. Hunter, Martyn C. Pritchard, Reginald S. Richardson, Edward Roberts, and Geoffrey N. Woodruff pp 2304 - 2304; DOI: 10.1021/jm00111a056 |
HIV protease: a novel chemotherapeutic target for AIDS Joel R. Huff pp 2305 - 2314; DOI: 10.1021/jm00112a001 |
Cholinergic activity of acetylenic imidazoles and related compounds Malcolm W. Moon, Connie G. Chidester, Richard F. Heier, Jeanette K. Morris, R. James Collins, Roland R. Russell, Jonathan W. Francis, G. Patrick Sage, and Vimala H. Sethy pp 2314 - 2327; DOI: 10.1021/jm00112a002 |
Sulfonylbenzoyl-nitrostyrenes: Potential bisubstrate type inhibitors of the EGF-receptor tyrosine protein kinase Peter M. Traxler, Oskar Wacker, Ha L. Bach, Johanna F. Geissler, Wilhelm Kump, Thomas Meyer, Urs Regenass, Johannes L. Roesel, and Nicholas Lydon pp 2328 - 2337; DOI: 10.1021/jm00112a003 |
Comparative molecular field analysis of some clodronic acid esters J. P. Bjorkroth, T. A. Pakkanen, J. Lindroos, E. Pohjala, H. Hanhijarvi, L. Lauren, R. Hannuniemi, A. Juhakoski, K. Kippo, and T. Kleimola pp 2338 - 2343; DOI: 10.1021/jm00112a004 |
Inhibitors of the protease from human immunodeficiency virus: design and modeling of a compound containing a dihydroxyethylene isostere insert with high binding affinity and effective antiviral activity Suvit Thaisrivongs, Alfredo G. Tomasselli, Joseph B. Moon, John Hui, Thomas J. McQuade, Steve R. Turner, Joseph W. Strohbach, W. Jeffrey Howe, W. Gary Tarpley, and Robert L. Heinrikson pp 2344 - 2356; DOI: 10.1021/jm00112a005 |
2-Chloro-1-(2,4-dichlorophenyl)-3-(1H-imidazol-1-yl)-2-phenylpropan-1-one hydrochloride, a novel, nonmutagenic antibacterial with specific activity against anaerobic bacteria Jon P. Dickens, George J. Ellames, Nigel J. Hare, Kevin R. Lawson, William R. McKay, Anthony P. Metters, Peter L. Myers, Anthony M. S. Pope, and Roger M. Upton pp 2356 - 2360; DOI: 10.1021/jm00112a006 |
Synthesis and biological activity of 2'-deoxy-4'-thio pyrimidine nucleosides John A. Secrist, Kamal N. Tiwari, James M. Riordan, and John A. Montgomery pp 2361 - 2366; DOI: 10.1021/jm00112a007 |
Modeling study of the structure of the macromolecular antitumor antibiotic neocarzinostatin. Origin of the stabilization of the chromophore Masaji Ishiguro, Seiichi Imajo, and Masahiro Hirama pp 2366 - 2373; DOI: 10.1021/jm00112a008 |
Synthesis and antitumor evaluations of symmetrically and unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones and 1,4-bis[(aminoalkyl)amino]-5,8-dihydroxyanthracene-9,10-diones A. Paul Krapcho, Zelleka Getahun, Kenneth L. Avery, Kevin J. Vargas, Miles P. Hacker, Silvano Spinelli, Gabriella Pezzoni, and Carla Manzotti pp 2373 - 2380; DOI: 10.1021/jm00112a009 |
Synthesis and antiviral activity of 3-substituted derivatives of 3,9-dihydro-9-oxo-5H-imidazo[1,2-a]purines, tricyclic analogs of acyclovir and ganciclovir Jerzy Boryski, Bozenna Golankiewicz, and Erik De Clercq pp 2380 - 2383; DOI: 10.1021/jm00112a010 |
5-(5-Bromothien-2-yl)-2'-deoxyuridine and 5-(5-chlorothien-2-yl)-2'-deoxyuridine are equipotent to (E)-5-(2-bromovinyl)-2'-deoxyuridine in the inhibition of herpes simplex virus type I replication P. Wigerinck, C. Pannecouque, R. Snoeck, P. Claes, E. De Clercq, and P. Herdewijn pp 2383 - 2389; DOI: 10.1021/jm00112a011 |
Synthesis and binding of [125I2]philanthotoxin-343, [125I2]philanthotoxin-343-lysine, and [125I2]philanthotoxin-343-arginine to rat brain membranes R. A. Goodnow, R. Bukownik, K. Nakanishi, P. N. R. Usherwood, A. T. Eldefrawi, N. A. Anis, and M. E. Eldefrawi pp 2389 - 2394; DOI: 10.1021/jm00112a012 |
Novel gonadotropin-releasing hormone antagonists: peptides incorporating modified N.omega.-cyanoguanidino moieties Paula Theobald, John Porter, Catherine Rivier, Anne Corrigan, Marilyn Perrin, Wylie Vale, Jean Rivier, William Hook, and Reuben Siraganian pp 2395 - 2402; DOI: 10.1021/jm00112a013 |
Synthesis and biological activity of angiotensin II analog containing a Val-His replacement, Val.psi.[CH(CONH2)HN]His Raju Mohan, Yuo Ling Chou, Ron Bihovsky, William C. Lumma, Paul W. Erhardt, and Kenneth J. Shaw pp 2402 - 2410; DOI: 10.1021/jm00112a014 |
Conformationally restricted polysubstituted biphenyl derivatives with angiotensin II receptors antagonist properties P. R. Bovy, J. T. Collins, G. M. Olins, E. G. McMahon, and W. C. Hutton pp 2410 - 2414; DOI: 10.1021/jm00112a015 |
Synthesis and DNA-binding properties of polyamine analogs Michael L. Edwards, Ronald D. Snyder, and David M. Stemerick pp 2414 - 2420; DOI: 10.1021/jm00112a016 |
Synthesis of structural analogs of lyngbyatoxin A and their evaluation as activators of protein kinase C Alan P. Kozikowski, Patrick W. Shum, Alakananda Basu, and John S. Lazo pp 2420 - 2430; DOI: 10.1021/jm00112a017 |
Pseudopeptide analogs of substance P and leucine enkephalinamide containing the .psi.(methyleneoxy) modification: synthesis and biological activity Eli Roubini, Ralph Laufer, Chaim Gilon, Zvi Selinger, Bernard P. Roques, and Michael Chorev pp 2430 - 2438; DOI: 10.1021/jm00112a018 |
Electrophilic .gamma.-lactone .kappa.-opioid receptor probes. Analogs of 2'-hydroxy-2-(tetrahydrofurfuryl)-5,9-dimethyl-6,7-benzomorphan diastereomers Peter Klein and Wendel L. Nelson pp 2438 - 2444; DOI: 10.1021/jm00112a019 |
Preparation and anticonvulsant activity of a series of functionalized .alpha.-heteroatom-substituted amino acids Harold Kohn, Kailash N. Sawhney, Philippe LeGall, David W. Robertson, and J. David Leander pp 2444 - 2452; DOI: 10.1021/jm00112a020 |
Studies of vitamin D (calciferol) and its analogs. 39. Arocalciferols: synthesis and biological evaluation of aromatic side-chain analogs of 1.alpha.,25-dihydroxyvitamin D3 Bruno Figadere, Anthony W. Norman, Helen L. Henry, H. Phillip Koeffler, Jian Yuan Zhou, and William H. Okamura pp 2452 - 2463; DOI: 10.1021/jm00112a021 |
Aldosterone antagonists. 4. Synthesis and activities of steroidal 6,6-ethylene-15,16-methylene 17-spirolactones Klaus Nickisch, Sybille Beier, Dieter Bittler, Walter Elger, Henry Laurent, Wolfgang Losert, Yukishige Nishino, Ekkehard Schillinger, and Rudolf Wiechert pp 2464 - 2468; DOI: 10.1021/jm00112a022 |
Synthesis and evaluation of antiinflammatory activities of a series of corticosteroid 17.alpha.-esters containing a functional group Hiroaki Ueno, Akira Maruyama, Motoyoshi Miyake, Etsuko Nakao, Kenichiro Nakao, Kohei Umezu, and Issei Nitta pp 2468 - 2473; DOI: 10.1021/jm00112a023 |
3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 8. Side chain ether analogs of lovastatin Ta Jyh Lee, W. J. Holtz, R. L. Smith, A. W. Alberts, and J. L. Gilfillan pp 2474 - 2477; DOI: 10.1021/jm00112a024 |
Naphthosultam derivatives: a new class of potent and selective 5-HT2 antagonists Jean Luc Malleron, Marie Therese Comte, Claude Gueremy, Jean Francis Peyronel, Alain Truchon, Jean Charles Blanchard, Adam Doble, Odile Piot, Jean Luc Zundel, and et al. pp 2477 - 2483; DOI: 10.1021/jm00112a025 |
A new class of analog of the bifunctional radiosensitizer .alpha.-(1-aziridinylmethyl)-2-nitro-1H-imidazole-1-ethanol (RSU 1069): the cycloalkylaziridines Mark J. Suto, Michael A. Stier, Leslie M. Werbel, Carla M. Arundel-Suto, Wilbur R. Leopold, William E. Elliott, and Judith S. Sebolt-Leopold pp 2484 - 2488; DOI: 10.1021/jm00112a026 |
3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 7. Modification of the hexahydronaphthalene moiety of simvastatin: 5-oxygenated and 5-oxa derivatives Mark E. Duggan, Alfred W. Alberts, Rick Bostedor, Yu Sheng Chao, John I. Germershausen, James L. Gilfillan, Wasyl Halczenko, George D. Hartman, Vincent Hunt, and et al. pp 2489 - 2495; DOI: 10.1021/jm00112a027 |
Synthesis and biochemical studies of 16- or 19-substituted androst-4-enes as aromatase inhibitors Mitsuteru Numazawa, Ayako Mutsumi, Kumiko Hoshi, Mariko Oshibe, Etsushi Ishikawa, and Hiroki Kigawa pp 2496 - 2504; DOI: 10.1021/jm00112a028 |
Syntheses of tolrestat analogs containing additional substituents in the ring and their evaluation as aldose reductase inhibitors. Identification of potent, orally active 2-fluoro derivatives Jay Wrobel, Jane Millen, Janet Sredy, Arlene Dietrich, Beverly J. Gorham, Michael Malamas, Joseph M. Kelly, John G. Bauman, Maria C. Harrison, and et al. pp 2504 - 2520; DOI: 10.1021/jm00112a029 |
Active conformation of 1,4-dihydropyridine calcium entry blockers. Effect of size of 2-aryl substituent on rotameric equilibria and receptor binding George Rovnyak, Niels Andersen, Jack Gougoutas, Anders Hedberg, S. David Kimball, Mary Malley, Suzanne Moreland, Michael Porubcan, and Andrew Pudzianowski pp 2521 - 2524; DOI: 10.1021/jm00112a030 |
Nonpeptide angiotensin II receptor antagonists: the discovery of a series of N-(biphenylylmethyl)imidazoles as potent, orally active antihypertensives David J. Carini, John V. Duncia, Paul E. Aldrich, Andrew T. Chiu, Alexander L. Johnson, Michael E. Pierce, William A. Price, Joseph B. Santella, III, Gregory J. Wells, and et al. pp 2525 - 2547; DOI: 10.1021/jm00112a031 |
GABA-uptake inhibitors: construction of a general pharmacophore model and successful prediction of a new representative Victor N'Goka, Gilbert Schlewer, Jean Michel Linget, Jean Pierre Chambon, and Camille Georges Wermuth pp 2547 - 2557; DOI: 10.1021/jm00112a032 |
3-Thienyl- and 3-furylaminobutyric acids. Synthesis and binding GABAB receptor studies Pascal Berthelot, Claude Vaccher, Nathalie Flouquet, Michel Debaert, Michel Luyckx, and Claude Brunet pp 2557 - 2560; DOI: 10.1021/jm00112a033 |
Synthesis and dopaminergic activity of 3-substituted 1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-1H-2-benzopyrans: characterization of an auxiliary binding region in the D1 receptor Michael P. DeNinno, Robert Schoenleber, Richard J. Perner, Linda Lijewski, Karen E. Asin, Donald R. Britton, Robert MacKenzie, and John W. Kebabian pp 2561 - 2569; DOI: 10.1021/jm00112a034 |
Highly selective adenosine A2 receptor agonists in a series of N-alkylated 2-aminoadenosines John E. Francis, Randy L. Webb, Geetha R. Ghai, Alan J. Hutchison, Michael A. Moskal, Reynalda DeJesus, Rina Yokoyama, Stephen L. Rovinski, Nicolina Contardo, and et al. pp 2570 - 2579; DOI: 10.1021/jm00112a035 |
Synthesis and evaluation of stilbene and dihydrostilbene derivatives as potential anticancer agents that inhibit tubulin polymerization Mark Cushman, Dhanapalan Nagarathnam, D. Gopal, Asit K. Chakraborti, Chii M. Lin, and Ernest Hamel pp 2579 - 2588; DOI: 10.1021/jm00112a036 |
Relaxant activity of 6-cyano-2,2-dimethyl-2H-1-benzopyran-4-carboxamides and -thiocarboxamides and their analogs in guinea pig trachealis Jonathan R. S. Arch, Derek R. Buckle, Claire Carey, Hilary Parr-Dobrzanski, Andrew Faller, Keith A. Foster, Catherine S. V. Houge-Frydrych, Ivan L. Pinto, David G. Smith, and Stephen G. Taylor pp 2588 - 2594; DOI: 10.1021/jm00112a037 |
Solid-state and solution conformation of 3'-amino-3'-deoxythymidine, precursor to a noncompetitive inhibitor of HIV-1 reverse transcriptase Terez Kovacs, Laszlo Parkanyi, Istvan Pelczer, Francisco Cervantes-Lee, Keith H. Pannell, and Paul F. Torrence pp 2595 - 2600; DOI: 10.1021/jm00112a038 |
Targeting 5'-deoxy-5'-(methylthio)adenosine phosphorylase by 5'-haloalkyl analogs of 5'-deoxy-5'-(methylthio)adenosine Janice R. Sufrin, Arthur J. Spiess, Debora L. Kramer, Paul R. Libby, John T. Miller, Ralph J. Bernacki, Younha Lee, Ronald T. Borchardt, and Carl W. Porter pp 2600 - 2606; DOI: 10.1021/jm00112a039 |
Synthesis and anticancer and antiviral activities of various 2'- and 3'-methylidene-substituted nucleoside analogs and crystal structure of 2'-deoxy-2'-methylidenecytidine hydrochloride Tai Shun Lin, Mei Zhen Luo, Mao Chin Liu, Regina H. Clarke-Katzenburg, Yung Chi Cheng, William H. Prusoff, William R. Mancini, George I. Birnbaum, Eric J. Gabe, and Jerzy Giziewicz pp 2607 - 2615; DOI: 10.1021/jm00112a040 |
Synthesis, stereochemistry, and biological activity of the 1-(1-phenyl-2-methylcyclohexyl)piperidines and the 1-(1-phenyl-4-methylcyclohexyl)piperidines. Absolute configuration of the potent trans-(-)-1-(1-phenyl-2-methylcyclohexyl)piperidine Maria A. Iorio, Lamberto Tomassini, Mariena V. Mattson, Clifford George, and Arthur E. Jacobson pp 2615 - 2623; DOI: 10.1021/jm00112a041 |
(1S)-1-(Aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinoline and heterocycle-condensed tetrahydropyridine derivatives: members of a novel class of very potent .kappa. opioid analgesics Vittorio Vecchietti, Geoffrey D. Clarke, Roberto Colle, Giuseppe Giardina, Giuseppe Petrone, and Massimo Sbacchi pp 2624 - 2633; DOI: 10.1021/jm00112a042 |
Analogs of the 5-HT1A serotonin antagonist 1-(2-methoxyphenyl)-4-[4-(2-phthalimido)butyl]piperazine with reduced .alpha.1-adrenergic affinity Revathi K. Raghupathi, Laura Rydelek-Fitzgerald, Milt Teitler, and Richard A. Glennon pp 2633 - 2638; DOI: 10.1021/jm00112a043 |
Acyclic analogs of 2-(4-phenylpiperidino)cyclohexanol (vesamicol): conformationally mobile inhibitors of vesicular acetylcholine transport S. M. N. Efange, R. H. Michelson, A. K. Dutta, and S. M. Parsons pp 2638 - 2643; DOI: 10.1021/jm00112a044 |
Synthesis of 2-deoxy-2-[(2,2-difluoro-3-hydroxytetradecanoyl)amino]-3-O-[(R)-3-(tetradecanoyloxy)tetradecanoyl]-D-glucopyranose 4-phosphate Masao Shiozaki, Yoshiyuki Kobayashi, Masami Arai, Takashi Watanabe, Tetsuo Hiraoka, Masahiro Nishijima, Sayuri Kuge, Toshiaki Otsuka, and Yuzuru Akamatsu pp 2643 - 2646; DOI: 10.1021/jm00112a045 |
3-(5-Alkyl-4-hydroxy-3-methoxy-1-naphthalenyl)-2-methyl-2-propenoic acids as orally active inhibitors of IL-1 generation Masayuki Tanaka, Kenichi Chiba, Makoto Okita, Toshihiko Kaneko, Katsuya Tagami, Shigeki Hibi, Yasushi Okamoto, Hiroshi Shirota, Masaki Goto, and et al. pp 2647 - 2649; DOI: 10.1021/jm00112a046 |
Probing the bradykinin receptor: mapping the geometric topography using ethers of hydroxyproline in novel peptides Donald J. Kyle, Jennifer A. Martin, Ronald M. Burch, John P. Carter, Songfeng Lu, Sonya Meeker, Judith C. Prosser, James P. Sullivan, James Togo, and et al. pp 2649 - 2653; DOI: 10.1021/jm00112a047 |
Determination of the relative binding free energies of peptide inhibitors to the HIV-1 protease David M. Ferguson, Randall J. Radmer, and Peter A. Kollman pp 2654 - 2659; DOI: 10.1021/jm00112a048 |
Book Reviews pp 2660 - 2664; DOI: 10.1021/jm00112a600 |
My odyssey in drug discovery George DeStevens pp 2665 - 2670; DOI: 10.1021/jm00113a001 |
Novel compounds possessing potent cAMP and cGMP phosphodiesterase inhibitory activity. Synthesis and cardiovascular effects of a series of imidazo[1,2-a]quinoxalinones and imidazo[1,5-a]quinoxalinones and their aza analogs David D. Davey, P. W. Erhardt, E. H. Cantor, S. S. Greenberg, W. R. Ingebretsen, and J. Wiggins pp 2671 - 2677; DOI: 10.1021/jm00113a002 |
Spatial requirements of the sodium channel binding site for class I antiarrhythmics as derived from the crystal structures of 4-substituted 2,6-bis(1-pyrrolidinylmethyl)phenols Marek L. Glowka, Robin L. Dargie, and Penelope W. Codding pp 2678 - 2684; DOI: 10.1021/jm00113a003 |
New aromatase inhibitors. Synthesis and biological activity of pyridyl-substituted tetralone derivatives Herbert Bayer, Christine Batzl, Rolf W. Hartman, and Albrecht Mannschreck pp 2685 - 2691; DOI: 10.1021/jm00113a004 |
Design and synthesis of P2-P1'-linked macrocyclic human renin inhibitors Ann E. Weber, Thomas A. Halgren, John J. Doyle, Robert J. Lynch, Peter K. S. Siegl, William H. Parsons, William J. Greenlee, and Arthur A. Patchett pp 2692 - 2701; DOI: 10.1021/jm00113a005 |
Studies on uricosuric diuretics. 4. Three-dimensional structure-activity relationships and receptor mapping of (aryloxy)acetic acid diuretics Hiroshi Koga, Haruhiko Sato, Takashi Dan, and Bunya Aoki pp 2702 - 2708; DOI: 10.1021/jm00113a006 |
Crystallographic and molecular modeling studies on trypanosomal triosephosphate isomerase: a critical assessment of the predicted and observed structures of the complex with 2-phosphoglycerate Martin E. M. Noble, Christophe L. M. J. Verlinde, Hillie Groendijk, Kor H. Kalk, Rik K. Wierenga, and Wim G. J. Hol pp 2709 - 2718; DOI: 10.1021/jm00113a007 |
Synthesis, ligand binding, QSAR, and CoMFA study of 3.beta.-(p-substituted phenyl)tropane-2.beta.-carboxylic acid methyl esters F. Ivy Carroll, Yigong Gao, M. Abdur Rahman, Philip Abraham, Karol Parham, Anita H. Lewin, John W. Boja, and Michael J. Kuhar pp 2719 - 2725; DOI: 10.1021/jm00113a008 |
Comparison of azabicyclic esters and oxadiazoles as ligands for the muscarinic receptor Barry S. Orlek, Frank E. Blaney, Frank Brown, Michael S. G. Clark, Michael S. Hadley, John Hatcher, Graham J. Riley, Howard E. Rosenberg, Harry J. Wadsworth, and Paul Wyman pp 2726 - 2735; DOI: 10.1021/jm00113a009 |
Dopamine autoreceptor agonists as potential antipsychotics. 3. 6-Propyl-4,5,5a,6,7,8-hexahydrothiazolo[4,5-f]quinolin-2-amine Bradley W. Caprathe, Juan C. Jaen, Lawrence D. Wise, Thomas G. Heffner, Thomas A. Pugsley, Leonard T. Meltzer, and Masood Parvez pp 2736 - 2746; DOI: 10.1021/jm00113a010 |
Folate analogs. 35. Synthesis and biological evaluation of 1-deaza, 3-deaza, and bridge-elongated analogs of N10-propargyl-5,8-dideazafolic acid Shu Wen Li, M. G. Nair, Donna M. Edwards, R. L. Kisliuk, Y. Gaumont, I. K. Dev, D. S. Duch, J. Humphreys, G. K. Smith, and Robert Ferone pp 2746 - 2754; DOI: 10.1021/jm00113a011 |
Structure-activity relationships of estrogenic ligands: synthesis and evaluation of (17.alpha.,20E)- and (17.alpha.,20Z)-21-halo-19-norpregna-1,3,5(10),20-tetraene-3,17.beta.-diols Elio Napolitano, Rita Fiaschi, and Robert N. Hanson pp 2754 - 2759; DOI: 10.1021/jm00113a012 |
C-Glycosidic analogs of lipid A and lipid X: synthesis and biological activities Hermann Vyplel, Dieter Scholz, Ingolf Macher, Karl Schindlmaier, and Eberhard Schuetze pp 2759 - 2767; DOI: 10.1021/jm00113a013 |
(Phenylmethoxy)phenyl derivatives of w-oxo- and w-tetrazolylalkanoic acids and related tetrazoles. Synthesis and evaluation as leukotriene D4 receptor antagonists Robert D. Dillard, Richard A. Hahn, Doris McCullough, F. Patrick Carr, Lynn E. Rinkema, Carlos R. Roman, and Jerome H. Fleisch pp 2768 - 2778; DOI: 10.1021/jm00113a014 |
Pregnanes that bind to the digitalis receptor: synthesis of 14-hydroxy-5.beta.,14.beta.-pregnane glycosides from digitoxin and digitoxigenin John F. Templeton, Peter Setiloane, V. P. Sashi Kumar, Yulan Yan, Talal H. Zeglam, and Frank S. LaBella pp 2778 - 2782; DOI: 10.1021/jm00113a015 |
The synthesis and antiviral activity of some 4'-thio-2'-deoxy nucleoside analogs Michael R. Dyson, Paul L. Coe, and Richard T. Walker pp 2782 - 2786; DOI: 10.1021/jm00113a016 |
Synthesis and biological evaluation of 4-purinylpyrrolidine nucleosides Mark L. Peterson and Robert Vince pp 2787 - 2797; DOI: 10.1021/jm00113a017 |
Synthesis and biological activity of sinefungin analogs Pierre Blanchard, Nerina Dodic, Jean Louis Fourrery, Francoise Lawrence, Abdel Malek Mouna, and Malka Robert-Gero pp 2798 - 2803; DOI: 10.1021/jm00113a018 |
Phosphorus-containing inhibitors of HMG-CoA reductase. 2. Synthesis and biological activities of a series of substituted pyridines containing a hydroxyphosphinyl moiety Jeffrey A. Robl, Laurelee A. Duncan, Jelka Pluscec, Donald S. Karanewsky, Eric M. Gordon, Carl P. Ciosek Jr., Lois C. Rich, Viviane C. Dehmel, Dorothy A. Slusarchyk, and et al. pp 2804 - 2815; DOI: 10.1021/jm00113a019 |
Modification of the enkephalin "message" with an artificial polycationic C-terminus Alan R. Jacobson, S. William Tam, and Lawrence M. Sayre pp 2816 - 2821; DOI: 10.1021/jm00113a020 |
Monoterpenic fragment analogs of aplasmomycin as potential antimalarials N. Balu, Jacob V. Thomas, and Sujata V. Bhat pp 2821 - 2823; DOI: 10.1021/jm00113a021 |
Applications of neural networks in quantitative structure-activity relationships of dihydrofolate reductase inhibitors T. A. Andrea and Hooshmand Kalayeh pp 2824 - 2836; DOI: 10.1021/jm00113a022 |
Boc-CCK-4 derivatives containing side-chain ureas as potent and selective CCK-A receptor agonists Kazumi Shiosaki, Chun Wel Lin, Hana Kopecka, Michael D. Tufano, Bruce R. Bianchi, Thomas R. Miller, David G. Witte, and Alex M. Nadzan pp 2837 - 2842; DOI: 10.1021/jm00113a023 |
Benzylated 1,2,3-triazoles as anticoccidiostats Richard J. Bochis, John C. Chabala, Ellwood Harris, Louis H. Peterson, Louis Barash, Thomas Beattie, Jeannette E. Brown, Donald W. Graham, Frank S. Waksmunski, and et al. pp 2843 - 2852; DOI: 10.1021/jm00113a024 |
Design and synthesis of HIV protease inhibitors. Variations of the carboxyterminus of the HIV protease inhibitor L-682,679 S. Jane DeSolms, Elizabeth A. Giuliani, James P. Guare, Joseph P. Vacca, William M. Sanders, Samuel L. Graham, J. Mark Wiggins, Paul L. Darke, Irving S. Sigal, and et al. pp 2852 - 2857; DOI: 10.1021/jm00113a025 |
Dual-action cephalosporins: cephalosporin 3'-quinolone carbamates Harry A. Albrecht, George Beskid, Nafsika H. Georgopapadakou, Dennis D. Keith, Frederick M. Konzelmann, David L. Pruess, Pamela L. Rossman, Chung Chen Wei, and James G. Christenson pp 2857 - 2864; DOI: 10.1021/jm00113a026 |
Potential antitumor agents. 63. Structure-activity relationships for side-chain analogs of the colon 38 active agent 9-oxo-9H-xanthene-4-acetic acid Gordon W. Rewcastle, Graham J. Atwell, Bruce C. Baguley, Maruta Boyd, Lindy L. Thomsen, Li Zhuang, and William A. Denny pp 2864 - 2870; DOI: 10.1021/jm00113a027 |
Determination of the mechanism of demethylenation of (methylenedioxy)phenyl compounds by cytochrome P450 using deuterium isotope effects Jon M. Fukuto, Yoshito Kumagai, and Arthur K. Cho pp 2871 - 2876; DOI: 10.1021/jm00113a028 |
N6,9-Disubstituted adenines: potent, selective antagonists at the A1 adenosine receptor Robert D. Thompson, Sherrie Secunda, John W. Daly, and Ray A. Olsson pp 2877 - 2882; DOI: 10.1021/jm00113a029 |
Interphenylene 7-oxabicyclo[2.2.1]heptane thromboxane A2(TxA2)antagonists. Semicarbazone .omega.-chains Raj N. Misra, Baerbel R. Brown, Wen Ching Han, Don N. Harris, Anders Hedberg, Maria L. Webb, and Steven E. Hall pp 2882 - 2891; DOI: 10.1021/jm00113a030 |
Synthesis and adenosine receptor affinity of a series of pyrazolo[3,4-d]pyrimidine analogs of 1-methylisoguanosine Fiona A. Harden, Ronald J. Quinn, and Peter J. Scammells pp 2892 - 2898; DOI: 10.1021/jm00113a031 |
Anxiolytic properties of certain annelated [1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-ones John E. Francis, Debra A. Bennett, James L. Hyun, Stephen L. Rovinski, Caryl L. Amrick, Patricia S. Loo, Deborah Murphy, Robert F. Neale, and Douglas E. Wilson pp 2899 - 2906; DOI: 10.1021/jm00113a032 |
1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-ones - inhibitors of blood platelet cAMP phosphodiesterase and induced aggregation Nicholas A. Meanwell, Herbert R. Roth, Edward C. R. Smith, Donald L. Wedding, J. J. Kim Wright, J. Stuart Fleming, and Elizabeth Gillespie pp 2906 - 2916; DOI: 10.1021/jm00113a033 |
Nucleosides and nucleotides. 100. 2'-C-Cyano-2'-deoxy-1-.beta.-D-arabinofuranosylcytosine (CNDAC): design of a potential mechanism-based DNA-strand-breaking antineoplastic nucleoside Akira Matsuda, Yuki Nakajima, Atsushi Azuma, Motohiro Tanaka, and Takuma Sasaki pp 2917 - 2919; DOI: 10.1021/jm00113a034 |
Potent, orally active imidazo[4,5-b]pyridine-based angiotensin II receptor antagonists Nathan B. Mantlo, Prasun K. Chakravarty, Debra L. Ondeyka, Peter K. S. Siegl, Raymond S. Chang, Victor J. Lotti, Kristie A. Faust, Terry W. Schorn, Tsing Bau Chen, and et al. pp 2919 - 2922; DOI: 10.1021/jm00113a035 |
2-Pyridinone derivatives: a new class of nonnucleoside, HIV-1-specific reverse transcriptase inhibitors Walfred S. Saari, Jacob M. Hoffman, John S. Wai, Thorsten E. Fisher, Clarence S. Rooney, Anthony M. Smith, Craig M. Thomas, Mark E. Goldman, Julie A. O'Brien, and et al. pp 2922 - 2925; DOI: 10.1021/jm00113a036 |
NMR studies of an FK-506 analog [U-13C]ascomycin, bound to FKBP: conformation and regions of ascomycin involved in binding A. M. Petros, R. T. Gampe Jr., G. Gemmecker, P. Neri, T. F. Holzman, R. Edalji, J. Hochlowski, M. Jackson, J. McAlpine, and et al. pp 2925 - 2928; DOI: 10.1021/jm00113a037 |
Substituted 2-(aminomethyl)piperidines: a novel class of selective protein kinase C inhibitors Barry G. Shearer, James P. Sullivan, J. Paul Carter, Rose M. Mathew, Phillip Waid, Jane R. Connor, Raymond J. Patch, and Ronald M. Burch pp 2928 - 2931; DOI: 10.1021/jm00113a038 |
A selective, reversible, competitive inhibitor of monoamine oxidase A containing no nitrogen, with negligible potentiation of tyramine-induced blood pressure rise Morton Harfenist, Daniel P. C. McGee, and Helen L. White pp 2931 - 2933; DOI: 10.1021/jm00113a039 |
Nitroheterocycle reduction as a paradigm for intramolecular catalysis of drug delivery to hypoxic cells Albert Firestone, R. Timothy Mulcahy, and Richard F. Borch pp 2933 - 2935; DOI: 10.1021/jm00113a040 |
Book Reviews pp 2936 - 2936; DOI: 10.1021/jm00113a600 |
NMR studies of molecular complexes as a tool in drug design Stephen W. Fesik pp 2937 - 2945; DOI: 10.1021/jm00114a001 |
Synthesis and pharmacological evaluation of 1-(aminomethyl)-3,4-dihydro-5-hydroxy-1H-2-benzopyrans as dopamine D1 selective ligands Michael R. Michaelides, Robert Schoenleber, Sheela Thomas, Diane M. Yamamoto, Donald R. Britton, Robert MacKenzie, and John W. Kebabian pp 2946 - 2953; DOI: 10.1021/jm00114a002 |
Structure-activity studies of antitumor agents based on pyrrolo[1,2-a]benzimidazoles: new reductive alkylating DNA cleaving agents Imadul Islam, Edward B. Skibo, Robert T. Dorr, and David S. Alberts pp 2954 - 2961; DOI: 10.1021/jm00114a003 |
Synthesis and biological activity of new HMG-CoA reductase inhibitors. 3. Lactones of 6-phenoxy-3,5-dihydroxyhexanoic acids H. Jendralla, E. Granzer, B. Von Kerekjarto, R. Krause, U. Schacht, E. Baader, W. Bartmann, G. Beck, A. Bergmann, and et al. pp 2962 - 2983; DOI: 10.1021/jm00114a004 |
Muscarinic receptor binding profile of para-substituted caramiphen analogs Robert L. Hudkins, Diane L. DeHaven-Hudkins, and James F. Stubbins pp 2984 - 2989; DOI: 10.1021/jm00114a005 |
Synthesis and muscarinic cholinergic receptor affinities of 3-quinuclidinyl .alpha.-(alkoxyalkyl)-.alpha.-aryl-.alpha.-hydroxyacetates Victor I. Cohen, Raymond E. Gibson, Linda H. Fan, Rosanna De la Cruz, Miriam S. Gitler, Erin Hariman, and Richard C. Reba pp 2989 - 2993; DOI: 10.1021/jm00114a006 |
2-Phenyl-3H-imidazo[4,5-b]pyridine-3-acetamides as nonbenzodiazepine anticonvulsants and anxiolytics Bruce E. Tomczuk, C. R. Taylor, L. Meredith Moses, Deborah B. Sutherland, Young S. Lo, David N. Johnson, William B. Kinnier, and Brian F. Kilpatrick pp 2993 - 3006; DOI: 10.1021/jm00114a007 |
Synthesis and antiviral activity of certain guanosine analogs in the thiazolo[4,5-d]pyrimidine ring system Ganesh D. Kini, Jack D. Anderson, Yogesh S. Sanghvi, Arthur F. Lewis, Donald F. Smee, Ganapathi R. Revankar, Roland K. Robins, and Howard B. Cottam pp 3006 - 3010; DOI: 10.1021/jm00114a008 |
Synthesis, calcium-channel-blocking activity, and antihypertensive activity of 4-(diarylmethyl)-1-[3-(aryloxy)propyl]piperidines and structurally related compounds James R. Shanklin, Christopher P. Johnson, Anthony G. Proakis, and Richard J. Barrett pp 3011 - 3022; DOI: 10.1021/jm00114a009 |
New 5H-pyridazino[4,5-b]indole derivatives. Synthesis and studies as inhibitors of blood platelet aggregation and inotropics A. Monge, I. Aldana, T. Alvarez, M. Font, E. Santiago, J. A. Latre, M. J. Bermejillo, M. J. Lopez-Unzu, and E. Fernandez-Alvarez pp 3023 - 3029; DOI: 10.1021/jm00114a010 |
Peptide derivatives specific for a Plasmodium falciparum proteinase inhibit the human erythrocyte invasion by merozoites Roger Mayer, Isabelle Picard, Philippe Lawton, Philippe Grellier, Christine Barrault, Michel Monsigny, and Joseph Schrevel pp 3029 - 3035; DOI: 10.1021/jm00114a011 |
An investigation of angiotensin II agonist and antagonist analogs with 5,5-dimethylthiazolidine-4-carboxylic acid and other constrained amino acids J. Samanen, T. Cash, D. Narindray, E. Brandeis, W. Adams, H. Weideman, T. Yellin, and D. Regoli pp 3036 - 3043; DOI: 10.1021/jm00114a012 |
Synthesis and antitumor properties of activated cyclophosphamide analogs Richard F. Borch and Gregory W. Canute pp 3044 - 3052; DOI: 10.1021/jm00114a013 |
Synthesis, activation, and cytotoxicity of aldophosphamide analogs Richard F. Borch and Ronald R. Valente pp 3052 - 3058; DOI: 10.1021/jm00114a014 |
Synthesis and receptor binding of enantiomeric N-substituted cis-N-[2-(3,4-dichlorophenyl)ethyl]-2-(1-pyrrolidinyl)cyclohexylamines as high-affinity .sigma. receptor ligands Lilian Radesca, Wayne D. Bowen, Lisa Di Paolo, and Brian R. De Costa pp 3058 - 3065; DOI: 10.1021/jm00114a015 |
Analogs of oxybutynin. Synthesis and antimuscarinic and bladder activity of some substituted 7-amino-1-hydroxy-5-heptyn-2-ones and related compounds J. Paul Carter, Lalita Noronha-Blob, Vicki H. Audia, Andrea C. Dupont, Daniel W. McPherson, Kenneth J. Natalie, W. Janusz Rzeszotarski, Ciro J. Spagnuolo, Philip P. Waid, and Carl Kaiser pp 3065 - 3074; DOI: 10.1021/jm00114a016 |
3-Methyl-2H-1-benzopyran potassium channel activators Rolf Gericke, Juergen Harting, Inge Lues, and Christine Schittenhelm pp 3074 - 3085; DOI: 10.1021/jm00114a017 |
Separation of .alpha.1-adrenergic and N-methyl-D-aspartate antagonist activity in a series of ifenprodil compounds B. L. Chenard, I. A. Shalaby, B. K. Koe, R. T. Ronau, T. W. Butler, M. A. Prochniak, A. W. Schmidt, and C. B. Fox pp 3085 - 3090; DOI: 10.1021/jm00114a018 |
Enantioselective and diastereoselective hydroxylation of bufuralol. Absolute configuration of the 7-(1-hydroxyethyl)-2-[1-hydroxy-2-(tert-butylamino)ethyl]benzofurans, the benzylic hydroxylation metabolites S. Ananda Weerawarna, Stefan M. Geisshusler, Satya S. Murthy, and Wendel L. Nelson pp 3091 - 3097; DOI: 10.1021/jm00114a019 |
Topically active carbonic anhydrase inhibitors. 4. [(Hydroxyalkyl)sulfonyl]benzene and [(hydroxyalkyl)sulfonyl]thiophenesulfonamides Kenneth L. Shepard, Samuel L. Graham, Ronald J. Hudcosky, Stuart R. Michelson, Thomas H. Scholz, Harvey Schwam, Anthony M. Smith, John M. Sondey, Kim M. Strohmaier, and et al. pp 3098 - 3105; DOI: 10.1021/jm00114a020 |
Nonpeptidic angiotensin II antagonists: synthesis and in vitro activity of a series of novel naphthalene and tetrahydronaphthalene derivatives Peter Buehlmayer, Leoluca Criscione, Walter Fuhrer, Pascal Furet, Marc De Gasparo, Stefan Stutz, and Steven Whitebread pp 3105 - 3114; DOI: 10.1021/jm00114a021 |
Development of a small RGD peptide fibrinogen receptor antagonist with potent antiaggregatory activity in vitro J. Samanen, F. Ali, T. Romoff, R. Calvo, E. Sorenson, J. Vasko, B. Storer, D. Berry, D. Bennett, and et al. pp 3114 - 3125; DOI: 10.1021/jm00114a022 |
Conformational restriction of the phenylalanine residue in a cyclic opioid peptide analog: effects on receptor selectivity and stereospecificity Peter W. Schiller, Grazyna Weltrowska, Nguyen Thi Mai Dung, Carole Lemieux, Nga N. Chung, Brian J. Marsden, and Brian C. Wilkes pp 3125 - 3132; DOI: 10.1021/jm00114a023 |
Synthesis and evaluation of some nitrobenzenesulfonamides containing nitroisopropyl and (ureidooxy)methyl groups as novel hypoxic cell-selective cytotoxic agents Walfred S. Saari, John E. Schwering, Paulette A. Lyle, Edward L. Engelhardt, Alan C. Sartorelli, and Sara Rockwell pp 3132 - 3138; DOI: 10.1021/jm00114a024 |
Monovalent sialosides that bind tightly to influenza A virus Peter L. Toogood, Peter K. Galliker, Gary D. Glick, and Jeremy R. Knowles pp 3138 - 3140; DOI: 10.1021/jm00114a025 |
Peptide to glycopeptide: glycosylated oligopeptide renin inhibitors with attenuated in vivo clearance properties Jed F. Fisher, Allen W. Harrison, Gordon L. Bundy, Karen F. Wilkinson, Bob D. Rush, and Mary J. Ruwart pp 3140 - 3143; DOI: 10.1021/jm00114a026 |
[123I]-2.beta.-carbomethoxy-3.beta.-(4-iodophenyl)tropane: high-affinity SPECT (single photon emission computed tomography) radiotracer of monoamine reuptake sites in brain John L. Neumeyer, Shaoyin Wang, Richard A. Milius, Ronald M. Baldwin, Yolanda Zea-Ponce, Paul B. Hoffer, Elzbieta Sybirska, Mohammed Al-Tikriti, Dennis S. Charney, and et al. pp 3144 - 3146; DOI: 10.1021/jm00114a027 |
Book Reviews pp 3147 - 3148; DOI: 10.1021/jm00114a600 |
Structure activity studies related to 2-(3,4-dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted-ethyl]acetamides: a novel series of potent and selective .kappa.-opioid agonists Jeffrey J. Barlow, Thomas P. Blackburn, Gerard F. Costello, Roger James, David J. Le Count, Brian G. Main, Robert J. Pearce, Keith Russell, and John S. Shaw pp 3149 - 3158; DOI: 10.1021/jm00115a001 |
Novel 1-phenylcycloalkanecarboxylic acid derivatives as potential anticonvulsant agents Silvia N. Calderon, Amy Hauck Newman, and Frank C. Tortella pp 3159 - 3164; DOI: 10.1021/jm00115a002 |
Synthesis, molecular modeling studies, and muscarinic receptor activity of azaprophen analogs David J. Triggle, Yong Who Kwon, Philip Abraham, J. Bruce Pitner, S. Wayne Mascarella, and F. I. Carroll pp 3164 - 3171; DOI: 10.1021/jm00115a003 |
Geiparvarin analogs. 2. Synthesis and cytostatic activity of 5-(4-arylbutadienyl)-3(2H)-furanones and of N-substituted 3-(4-oxo-2-furanyl)-2-buten-2-yl carbamates Daniele Simoni, Stefano Manfredini, Mojgan Aghazadeh Tabrizi, Rita Bazzanini, Pier G. Baraldi, Jan Balzarini, and Erik De Clercq pp 3172 - 3176; DOI: 10.1021/jm00115a004 |
Antimitotic agents. Alterations at the 2,3-positions of ethyl (5-amino-1,2-dihydropyrido[3,4-b]pyrazin-7-yl)carbamates Carroll Temple, Gregory A. Rener, Robert N. Comber, and William R. Waud pp 3176 - 3181; DOI: 10.1021/jm00115a005 |
Synthesis and biological evaluation of hydroxamate-based iron chelators Raymond J. Bergeron, Jan Wiegand, James S. McManis, and P. Thirumalai Perumal pp 3182 - 3187; DOI: 10.1021/jm00115a006 |
Synthesis and anti-HIV-1 activity of 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one (TIBO) derivatives. 2 Michael J. Kukla, Henry J. Breslin, Craig J. Diamond, Philip P. Grous, Chih Y. Ho, Milton Miranda, James D. Rodgers, Ronald G. Sherrill, Erik De Clercq, and et al. pp 3187 - 3197; DOI: 10.1021/jm00115a007 |
Synthesis and ocular antihypertensive activity of new imidazolidine derivatives containing a .beta.-blocking side chain D. Huber, J. D. Ehrhardt, N. Decker, J. Himber, G. Andermann, and G. Leclerc pp 3197 - 3204; DOI: 10.1021/jm00115a008 |
(Aminoalkyl)carbamates of forskolin: intermediates for the synthesis of functionalized derivatives of forskolin with different specificities for adenylyl cyclase and the glucose transporter Joan D. Robbins, Antonio Laurenza, Raymond W. Kosley, Gerard J. O'Malley, Bettina Spahl, and Kenneth B. Seamon pp 3204 - 3212; DOI: 10.1021/jm00115a009 |
Synthesis and selective class III antiarrhythmic activity of novel N-heteroaralkyl-substituted 1-(aryloxy)-2-propanolamine and related propylamine derivatives John A. Butera, Walter Spinelli, Viji Anantharaman, Nicholas Marcopulos, Roderick W. Parsons, Issam F. Moubarak, Catherine Cullinan, and Jehan F. Bagli pp 3212 - 3228; DOI: 10.1021/jm00115a010 |
Spiro[fluoreneisothiazolidin]one dioxides: new aldose reductase and L-hexonate dehydrogenase inhibitors Mark T. DuPriest, Brenda W. Griffin, Daniel Kuzmich, and Loretta G. McNatt pp 3229 - 3234; DOI: 10.1021/jm00115a011 |
Fluorescent probes for dopamine receptors: synthesis and characterization of fluorescein and 7-nitrobenz-2-oxa-1,3-diazol-4-yl conjugates of D-1 and D-2 receptor ligands Venkatesalu Bakthavachalam, Nandkishore Baindur, Bertha K. Madras, and John L. Neumeyer pp 3235 - 3241; DOI: 10.1021/jm00115a012 |
Complexes of .NO with nucleophiles as agents for the controlled biological release of nitric oxide. Vasorelaxant effects Chris M. Maragos, Deborah Morley, David A. Wink, Tambra M. Dunams, Joseph E. Saavedra, Aaron Hoffman, Alfred A. Bove, Lawrence Isaac, Joseph A. Hrabie, and Larry K. Keefer pp 3242 - 3247; DOI: 10.1021/jm00115a013 |
Synthesis and structure-activity relationships of a novel series of non-peptide angiotensin II receptor binding inhibitors specific for the AT2 subtype C. John Blankley, John C. Hodges, Sylvester R. Klutchko, Richard J. Himmelsbach, Alexander Chucholowski, Cleo J. Connolly, Sandra J. Neergaard, Michael S. Van Nieuwenhze, Alan Sebastian, and et al. pp 3248 - 3260; DOI: 10.1021/jm00115a014 |
Synthesis and antihypertensive activity of pyran oxygen and amide nitrogen replacement analogs of the potassium channel activator cromakalim Valerie A. Ashwood, Frederick Cassidy, John M. Evans, Stefania Gagliardi, and Geoffrey Stemp pp 3261 - 3267; DOI: 10.1021/jm00115a015 |
Substrate analog renin inhibitors containing replacements of histidine in P2 or isosteres of the amide bond between P3 and P2 sites Peter Raddatz, Alfred Jonczyk, Klaus Otto Minck, Claus Jochen Schmitges, and Jan Sombroek pp 3267 - 3280; DOI: 10.1021/jm00115a016 |
Antitumor properties of 2(1H)-pyrimidinone riboside (zebularine) and its fluorinated analogs John S. Driscoll, Victor E. Marquez, Jacqueline Plowman, Paul S. Liu, James A. Kelley, and Joseph J. Barchi pp 3280 - 3284; DOI: 10.1021/jm00115a017 |
Synthesis, characterization and myocardial uptake of cationic bis(arene)technetium(I) complexes Dennis W. Wester, Joseph R. Coveney, Dennis L. Nosco, Mark S. Robbins, and Richard T. Dean pp 3284 - 3290; DOI: 10.1021/jm00115a018 |
Synthesis and evaluation of a series of 3,5-disubstituted benzisoxazole-4,7-diones. Potent radiosensitizers in vitro Mark J. Suto, Michael A. Stier, R. Thomas Winters, William R. Turner, Cheryl D. Pinter, William E. Elliott, and Judith S. Sebolt-Leopold pp 3290 - 3294; DOI: 10.1021/jm00115a019 |
Synthesis and biological activity of a series of diaryl-substituted .alpha.-cyano-.beta.-hydroxypropenamides, a new class of anthelmintic agents Eric B. Sjogren, Michael A. Rider, Peter H. Nelson, Stanford Bingham, Anthony L. Poulton, Mark A. Emanuel, and Richard Komuniecki pp 3295 - 3301; DOI: 10.1021/jm00115a020 |
Gossypol and derivatives: a new class of aldose reductase inhibitors Lorraine M. Deck, David L. Vander Jagt, and Robert E. Royer pp 3301 - 3305; DOI: 10.1021/jm00115a021 |
Activity of acyclic 6-(phenylselenenyl)pyrimidine nucleosides against human immunodeficiency viruses in primary lymphocytes Naganna M. Goudgaon and Raymond F. Schinazi pp 3305 - 3309; DOI: 10.1021/jm00115a022 |
Synthesis and pharmacological evaluation of ether and related analogs of .DELTA.8-, .DELTA.9-, and .DELTA.9,11-tetrahydrocannabinol David R. Compton, W. Roy Prescott, Billy R. Martin, Craig Siegel, Patrick M. Gordon, and Raj K. Razdan pp 3310 - 3316; DOI: 10.1021/jm00115a023 |
Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone Joseph A. Cipollina, Edward H. Ruediger, James S. New, Mary E. Wire, Timothy A. Shepherd, David W. Smith, and Joseph P. Yevich pp 3316 - 3328; DOI: 10.1021/jm00115a024 |
Design of potent linear PAF antagonists Javier Bartroli, Elena Carceller, Manuel Merlos, Marta Giral, Julian Garcia-Rafanell, and Javier Forn pp 3328 - 3334; DOI: 10.1021/jm00115a025 |
Fluorinated colchicinoids: antitubulin and cytotoxic properties Israel Ringel, Dena Jaffe, Sara Alerhand, Oliver Boye, Anjum Muzaffar, and Arnold Brossi pp 3334 - 3338; DOI: 10.1021/jm00115a026 |
Antineoplastic agents. 219. Isolation and structure of the cell growth inhibitory constituents from the western Pacific marine sponge Axinella sp George R. Pettit, Cherry L. Herald, Michael R. Boyd, John E. Leet, Claude Dufresne, Dennis L. Doubek, Jean M. Schmidt, Ronald L. Cerny, John N. A. Hooper, and Klaus C. Rutzler pp 3339 - 3340; DOI: 10.1021/jm00115a027 |
Novel binding mode of highly potent HIV-proteinase inhibitors incorporating the (R)-hydroxyethylamine isostere Antonin Krohn, Sally Redshaw, Jenny C. Ritchie, Bradford J. Graves, and Marcos H. Hatada pp 3340 - 3342; DOI: 10.1021/jm00115a028 |
Book Reviews pp 3343 - 3344; DOI: 10.1021/jm00115a600 |
Antitumor agents. 120. New 4-substituted benzylamine and benzyl ether derivatives of 4'-O-demethylepipodophyllotoxin as potent inhibitors of human DNA topoisomerase II Xiao Ming Zhou, Zhe Qing Wang, Jang Yang Chang, Hong Xing Chen, Yung Chi Cheng, and Kuo Hsiung Lee pp 3346 - 3350; DOI: 10.1021/jm00116a001 |
Cholecystokinin (CCK) antagonists: (R)-tryptophan-based hybrid antagonists of high affinity and selectivity for CCK-A receptors James F. Kerwin, Frank Wagenaar, Hana Kopecka, Chun Wel Lin, Thomas Miller, David Witte, Michael Stashko, and Alex M. Nadzan pp 3350 - 3359; DOI: 10.1021/jm00116a002 |
Novel 1-phenylpiperazine and 4-phenylpiperidine derivatives as high-affinity .sigma. ligands Richard A. Glennon, Mamoun Y. Yousif, Abd M. Ismaiel, Mahmoud B. El-Ashmawy, J. L. Herndon, James B. Fischer, Alfred C. Server, and Kathleen J. Burke Howie pp 3360 - 3365; DOI: 10.1021/jm00116a003 |
(.+-.)-3-Allyl-6-bromo-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine, a new high affinity D1 dopamine receptor ligand: synthesis and structure-activity relationship John L. Neumeyer, Nandkishore Baindur, Hyman B. Niznik, H. C. Guan, and Philip Seeman pp 3366 - 3371; DOI: 10.1021/jm00116a004 |
Immunostimulation by a partially modified retro-inverso-tuftsin analog containing Thr1.sum..psi.[NHCO](R,S)Lys2 modification Antonio S. Verdini, Sergio Silvestri, Cristina Becherucci, Maria G. Longobardi, Luca Parente, Samuele Peppoloni, Mauro Perretti, Piero Pileri, Massimo Pinori, and et al. pp 3372 - 3379; DOI: 10.1021/jm00116a005 |
Molecular mechanics simulations on covalent complexes of mitomycin C and its analogs with left-handed DNA duplexes Shashidhar N. Rao, Bhashyam S. Iyengar, Timothy P. Wunz, and William A. Remers pp 3380 - 3388; DOI: 10.1021/jm00116a006 |
Activity of N6-substituted 2-chloroadenosines at A1 and A2 adenosine receptors Robert D. Thompson, Sherrie Secunda, John W. Daly, and Ray A. Olsson pp 3388 - 3390; DOI: 10.1021/jm00116a007 |
Synthesis and antibacterial activities of C-21 functionalized derivatives of (9R)-9-amino-9-deoxoerythromycins A and B Paul A. Lartey, Shari L. DeNinno, Ramin Faghih, Dwight J. Hardy, Jacob J. Clement, Jacob J. Plattner, and Richard L. Stephens pp 3390 - 3395; DOI: 10.1021/jm00116a008 |
Examination of HIV-1 protease secondary structure specificity using conformationally constrained inhibitors Michael Kahn, Hiroshi Nakanishi, R. Alan Chrusciel, Dennis Fitzpatrick, and Michael E. Johnson pp 3395 - 3399; DOI: 10.1021/jm00116a009 |
Delineating the pharmacophoric elements of huperzine A: importance of the unsaturated three-carbon bridge to its AChE inhibitory activity Alan P. Kozikowski, Chris P. Miller, Fumio Yamada, Yuan Ping Pang, Jacqueline H. Miller, Michael McKinney, and Richard G. Ball pp 3399 - 3402; DOI: 10.1021/jm00116a010 |
Novel alkaloids from the tropical plant Ancistrocladus abbreviatus inhibit cell killing by HIV-1 and HIV-2 Kirk P. Manfredi, John W. Blunt, John H. Cardellina, James B. McMahon, Lewis L. Pannell, Gordon M. Cragg, and Michael R. Boyd pp 3402 - 3405; DOI: 10.1021/jm00116a011 |
1,3,8-Trisubstituted xanthines. Effects of substitution pattern upon adenosine receptor A1/A2 affinity [Erratum to document cited in CA114(19):185119j] Ronald H. Erickson, Roger N. Hiner, Scott W. Feeney, Paul R. Blake, Waclaw J. Rzeszotarski, Rickey P. Hicks, Diane G. Costello, and Mary E. Abreu pp 3405 - 3405; DOI: 10.1021/jm00116a012 |
Synthesis and resolution of (.+-.)-7-chloro-8-hydroxy-1-(3'-iodophenyl)-3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine (TISCH): a high affinity and selective iodinated ligand for CNS D1 dopamine receptor [Erratum to document cited in CA114(13):122017d] Sumalee Chumpradit, Mei Pung Kung, Jeffrey J. Billings, and Hank F. Kung pp 3405 - 3405; DOI: 10.1021/jm00116a013 |
Stereospecific synthesis of (R)- and (S)-S-adenosyl-1,8-diamino-3-thiooctane, a potent inhibitor of polyamine biosynthesis. Comparison of asymmetric induction vs enantiomeric synthesis [Erratum to document cited in CA115(5):50181y] Chin Liu and James K. Coward pp 3406 - 3408; DOI: 10.1021/jm00116a014 |
Editorial - The Journal of Medicinal Chemistry Becomes a Biweekly Publication in 1992 Philip S. Portoghese pp 3345 - 3345; DOI: 10.1021/jm00116a600 |
Book Reviews pp 3408 - 3410; DOI: 10.1021/jm00116a601 |