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Synthesis and pharmacological evaluation of conformationally restricted phenothiazine analogues Cor J. Grol, Durk Dijkstra, Wim Schunselaar, Ben H. C. Westerink, and Arnold R. Martin pp 5 - 9; DOI: 10.1021/jm00343a001 |
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Stereochemical studies on medicinal agents. 25. Absolute configuration and analgetic potency of .beta.-1,2-dimethyl-4-phenyl-4-(propionyloxy)piperidine enantiomers David S. Fries, Richard P. Dodge, Hakon Hope, and Philip S. Portoghese pp 9 - 12; DOI: 10.1021/jm00343a002 |
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Isoxicam and related 4-hydroxy-N-isoxazolyl-2H-1,2-benzothiazine-3-carboxamide, 1,1-dioxides. Potent nonsteroidal antiinflammatory agents Harold Zinnes, Jagadish C. Sircar, Neil Lindo, Martin L. Schwartz, Arthur C. Fabian, John Shavel, Charles F. Kasulanis, Jerome D. Genzer, Charles Lutomski, and G. DiPasquale pp 12 - 18; DOI: 10.1021/jm00343a003 |
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Enhanced antitumor properties of 3'-(4-morpholinyl) and 3'-(4-methoxy-1-piperidinyl) derivatives of 3'-deaminodaunorubicin Carol W. Mosher, Helen Y. Wu, Allan N. Fujiwara, and Edward M. Acton pp 18 - 24; DOI: 10.1021/jm00343a004 |
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Adriamycin analogs. 1. Preparation and antitumor evaluation of 7-O-(.beta.-D-glucosaminyl)daunomycinone and 7-O-(.beta.-D-glucosaminyl)adriamycinone and their N-trifluoroacetyl derivatives Mervyn Israel and Robert J. Murray pp 24 - 28; DOI: 10.1021/jm00343a005 |
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Adriamycin analogs. 2. Novel anomeric ribofuranoside analogs of daunorubicin Mervyn Israel, John E. Airey, Robert J. Murray, and John W. Gillard pp 28 - 31; DOI: 10.1021/jm00343a006 |
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Pyrazolo[3,4-d]pyrimidine ribonucleosides as anticoccidials. 1. Synthesis and activity of some nucleosides of purines and 4-(alkylthio)pyrazolo[3,4-d]pyrimidines Thomas A. Krenitsky, Janet L. Rideout, George W. Koszalka, Rosetta B. Inmon, Esther Y. Chao, Gertrude B. Elion, Victoria S. Latter, and Raymond B. Williams pp 32 - 35; DOI: 10.1021/jm00343a007 |
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[(3-Aryl-1,2-benzisoxazol-6-yl)oxy]acetic acids. A new diuretic series Gregory M. Shutske, Linda L. Setescak, Richard C. Allen, Larry Davis, Richard C. Effland, Karen Ranbom, Jan M. Kitzen, Jeffrey C. Wilker, and William J. Novick pp 36 - 44; DOI: 10.1021/jm00343a008 |
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Design of more potent antagonists of the antidiuretic responses to arginine-vasopressin Maurice Manning, Aleksandra Olma, Wieslaw A. Klis, Aleksander M. Kolodziejczyk, Janny Seto, and Wilbur H. Sawyer pp 45 - 50; DOI: 10.1021/jm00343a009 |
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Structure-anti-Parkinson activity relationships in the aminoadamantanes. Influence of bridgehead substitution James G. Henkel, Jeffrey T. Hane, and Gerald Gianutsos pp 51 - 56; DOI: 10.1021/jm00343a010 |
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4-Hydroxyquinoline-3-carboxylic acids as inhibitors of cell respiration. 2. Quantitative structure-activity relationship of dehydrogenase enzyme and Ehrlich ascites tumor cell inhibitions Eugene A. Coats, Kishorkant J. Shah, Stanley R. Milstein, Clara S. Genther, Dilip M. Nene, Jeffrey Roesener, James Schmidt, Michael Pleiss, Ellen Wagner, and John K. Baker pp 57 - 63; DOI: 10.1021/jm00343a011 |
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Synthesis of peptides by the solid-phase method. 7. Substance P and analogs A. Fournier, R. Couture, D. Regoli, M. Gendreau, and S. St-Pierre pp 64 - 68; DOI: 10.1021/jm00343a012 |
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2,3-Dihydro and carbocyclic analogs of tryptamines: interaction with serotonin receptors Richard A. Glennon, John M. Jacyno, and John J. Salley pp 68 - 70; DOI: 10.1021/jm00343a013 |
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Fluorinated retinoic acids and their analogs. 3. Synthesis and biological activity of aromatic 6-fluoro analogs Allen J. Lovey and Beverly A. Pawson pp 71 - 75; DOI: 10.1021/jm00343a014 |
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1-(Alkylamino)isochromans: hypotensives with peripheral and central activities J. M. McCall, R. B. McCall, R. E. TenBrink, B. V. Kamdar, S. J. Humphrey, V. H. Sethy, D. W. Harris, and C. Daenzer pp 75 - 81; DOI: 10.1021/jm00343a015 |
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Syntheses and activities of antioxidant derivatives of retinoic acid Steven C. Welch, John M. Gruber, and A. S. C. Prakasa Rao pp 81 - 84; DOI: 10.1021/jm00343a016 |
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Vinylogous carbinolamine tumor inhibitors. 11. Synthesis and antileukemic activity of fluorinated analogs of 2,3-dihydro-5-phenyl-6,7-bis(hydroxymethyl)-1H-pyrrolizine biscarbamate Wayne K. Anderson and Howard L. McPherson pp 84 - 86; DOI: 10.1021/jm00343a017 |
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Apyrogenic, adjuvant-active N-acetylmuramyl-dipeptides Pierre Lefrancier, Marcel Derrien, Xavier Jamet, Jean Choay, Edgar Lederer, Francoise Audibert, Monique Parant, Francine Parant, and Louis Chedid pp 87 - 90; DOI: 10.1021/jm00343a018 |
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Hypocholesterolemic and antiaggregatory properties of 2-hydroxytetronic acid redox analogs and their relationship to clofibric acid Donald T. Witiak, Satish S. Kokrady, Suman T. Patel, Huzoor Akbar, Dennis R. Feller, and Howard A. I. Newman pp 90 - 93; DOI: 10.1021/jm00343a019 |
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L-[4-11C]aspartic acid: enzymic synthesis, myocardial uptake, and metabolism Jorge R. Barrio, James E. Egbert, Eberhard Henze, Heinrich R. Schelbert, and Fritz J. Baumgartner pp 93 - 96; DOI: 10.1021/jm00343a020 |
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1-.beta.-D-arabinofuranosyl-1H-imidazo[4,5-c] pyridine (ara-3-deazaadenine) J. A. Montgomery, S. J. Clayton, and P. K. Chiang pp 96 - 98; DOI: 10.1021/jm00343a021 |
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Syntheses and diuretic activity of 1,2-dihydro-2-(3-pyridyl)-3H-pyrido[2,3-d]pyrimidin-4-one and related compounds Harlie A. Parish, Richard D. Gilliom, William P. Purcell, Ronald K. Browne, Roy F. Spirk, and Harold D. White pp 98 - 102; DOI: 10.1021/jm00343a022 |
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Fourth Smissman Award Address The Long Search for Valid Structure-Action Relationships in Drugs Adrien Albert pp 1 - 5; DOI: 10.1021/jm00343a600 |
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Book Reviews pp 103 - 104; DOI: 10.1021/jm00343a601 |
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A new stable prostacyclin mimic, 7-oxo-PGI2 G. Kovacs, V. Simonidesz, I. Tomoskozi, P. Kormoczy, I. Szekely, A. Papp-Behr, I. Stadler, L. Szekeres, and G. Papp pp 105 - 107; DOI: 10.1021/jm00344a001 |
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2-.beta.-D-ribofuranosylthiazole-4-carboxamide, a novel potential antitumor agent for lung tumors and metastases R. K. Robins, P. C. Srivastava, V. L. Narayanan, J. Plowman, and K. D. Paull pp 107 - 108; DOI: 10.1021/jm00344a002 |
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Synthesis and hypoglycemic activity of phenylalkyloxiranecarboxylic acid derivatives Klaus Eistetter and Horst P. O. Wolf pp 109 - 113; DOI: 10.1021/jm00344a003 |
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Aminomethyl-1,2,4-benzothiadiazines as potential analogs of .gamma.-aminobutyric acid. Unexpected discovery of a taurine antagonist Yves Girard, Joseph G. Atkinson, Dean R. Haubrich, Michael Williams, and George G. Yarbrough pp 113 - 116; DOI: 10.1021/jm00344a004 |
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Common anionic receptor site hypothesis: its relevance to the antagonist action of naloxone Ryszard J. Kobylecki, Robert W. Carling, John A. H. Lord, Colin F. C. Smith, and Anthony C. Lane pp 116 - 120; DOI: 10.1021/jm00344a005 |
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Darmstoff analogs. 2. Ring and side chain effects on smooth muscle contraction Robert A. Wiley, Wayne T. Harris, Catherine Brungardt, and Michael Marx pp 121 - 125; DOI: 10.1021/jm00344a006 |
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Crystal structures and pharmacological activity of calcium channel antagonists: 2,6-dimethyl-3,5-dicarbomethoxy-4-(unsubstituted, 3-methyl-, 4-methyl-, 3-nitro-, 4-nitro-, and 2,4-dinitrophenyl)-1,4-dihydropyridine Rune Fossheim, Knut Svarteng, Arvid Mostad, Christian Roemming, Eli Shefter, and David J. Triggle pp 126 - 131; DOI: 10.1021/jm00344a007 |
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Preparation and antiinflammatory activity of 2- and 4-pyridones James Benjamin Pierce, Zaven S. Ariyan, and Gaye Stuart Ovenden pp 131 - 136; DOI: 10.1021/jm00344a008 |
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.alpha.-Adrenergic agents. 2. Synthesis and .alpha.1-agonist activity of 2-aminotetralins R. M. DeMarinis, D. H. Shah, R. F. Hall, J. P. Hieble, and R. G. Pendleton pp 136 - 141; DOI: 10.1021/jm00344a009 |
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Mammary tumor inhibiting effect of 3,3'-diacetoxy-.alpha.,.beta.-dialkylstilbenes and of related stilbene oxides Martin R. Schneider, Helmut Schoenenberger, Ralf T. Michel, and H. P. Fortmeyer pp 141 - 145; DOI: 10.1021/jm00344a010 |
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Quantitative structure-activity relationships of aromatic esters of 1-methyl-4-piperidinol as analgesic Chen Yu Cheng, Einar Brochmann-Hanssen, and James A. Waters pp 145 - 152; DOI: 10.1021/jm00344a011 |
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Comparison of quantitative structure-activity relationships of the inhibition of leukemia cells in culture with the inhibition of dihydrofolate reductase from leukemia cells and other cell types Tasneem A. Khwaja, Stephanie Pentecost, Cynthia Dias Selassie, Zong Ru Guo, and Corwin Hansch pp 153 - 156; DOI: 10.1021/jm00344a012 |
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A comparison of the inhibition of growth of methotrexate-resistant and -sensitive leukemia cells in culture by triazines. Evidence for a new mechanism of cell resistance to methotrexate Cynthia Dias Selassie, Zong Ru Guo, Corwin Hansch, Tasneem A. Khwaja, and Stephanie Pentecost pp 157 - 161; DOI: 10.1021/jm00344a013 |
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Synthesis of pseudocofactor analogs as potential inhibitors of the folate enzymes Carroll Temple, L. Lee Bennett, Jerry D. Rose, Robert D. Elliott, and John H. Montgomery pp 161 - 166; DOI: 10.1021/jm00344a014 |
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Antiestrogen basicity-activity relationships: a comparison of the estrogen receptor binding and antiuterotrophic potencies of several analogs of (Z)-1,2-diphenyl-1-[4-[2-(dimethylamino)ethoxy]phenyl]-1-butene (Tamoxifen, Nolvadex) having altered basicity David W. Robertson, John A. Katzenellenbogen, James R. Hayes, and Benita S. Katzenellenbogen pp 167 - 171; DOI: 10.1021/jm00344a015 |
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Lipophilic 5'-alkyl phosphate esters of 1-.beta.-D-arabinofuranosylcytosine and its N4-acyl and 2,2'-anhydro-3'-O-acyl derivatives as potential prodrugs A. Rosowsky, S. H. Kim, J. Ross, and M. M. Wick pp 171 - 178; DOI: 10.1021/jm00344a016 |
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Activated N-nitrosocarbamates for regioselective synthesis of N-nitrosoureas Jean Martinez, Joel Oiry, Jean Louis Imbach, and Francois Winternitz pp 178 - 182; DOI: 10.1021/jm00344a017 |
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Syntheses of .alpha.- and .gamma.-substituted amides, peptides, and esters of methotrexate and their evaluation as inhibitors of folate metabolism J. R. Piper, J. A. Montgomery, F. M. Sirotnak, and P. L. Chello pp 182 - 187; DOI: 10.1021/jm00344a018 |
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Adriamycin analogs. Preparation and biological evaluation of some N-perfluoroacyl analogs of daunorubicin, adriamycin, and N-(trifluoroacetyl)adriamycin 14-valerate and their 9,10-anhydro derivatives Mervyn Israel and Gopalakrishnan Potti pp 187 - 191; DOI: 10.1021/jm00344a019 |
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Synthesis of N-(carbonylamino)-1,2,3,6-tetrahydropyridines with analgesic, antiinflammatory, and hyperglycemic activity Jupita M. Yeung, Linda A. Corleto, and Edward E. Knaus pp 191 - 195; DOI: 10.1021/jm00344a020 |
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Book Reviews pp 196 - 196; DOI: 10.1021/jm00344a600 |
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Adenosine receptors: targets for future drugs John W. Daly pp 197 - 207; DOI: 10.1021/jm00345a001 |
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Inhibitors of gastric acid secretion: 3,4-diamino-1,2,5-thiadiazole 1-oxides and 1,1-dioxides as urea equivalents in a series of histamine H2 receptor antagonists William C. Lumma Jr., Paul S. Anderson, John J. Baldwin, William A. Bolhofer, Susan F. Britcher, Bradley V. Clineschmidt, George H. Denny, Charles N. Habecker, Jordan M. Hirshfield, and et al. pp 207 - 210; DOI: 10.1021/jm00345a002 |
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1,2,5-Thiadizole 1-oxide and 1,1-dioxide derivatives. A new class of potent histamine H2-receptor antagonists Aldo A. Algieri, George M. Luke, Robert T. Standridge, Myron Brown, Richard A. Partyka, and R. R. Crenshaw pp 210 - 212; DOI: 10.1021/jm00345a003 |
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Rigid analogs of dopamine: synthesis and interaction of 6-exo- and 6-endo-(3',4'-dihydroxyphenyl)-2-azabicyclo[2.2.2]octanes with dopamine uptake sites and receptors Say Jong Law, J. Michael Morgan, Lawrence W. Masten, Ronald F. Borne, George W. Arana, Nora S. Kula, and Ross J. Baldessarini pp 213 - 216; DOI: 10.1021/jm00345a004 |
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Aminotetralins as narcotic antagonists. 2. Synthesis and opiate-related activity of 1-phenyl-3-aminotetralins David S. Fries and Dominick J. Bertelli pp 216 - 220; DOI: 10.1021/jm00345a005 |
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Ring-hydroxylated analogs of lucanthone as antitumor agents Sydney Archer, Kenneth J. Miller, Rabindra Rej, Cecily Periana, and Lloyd Fricker pp 220 - 227; DOI: 10.1021/jm00345a006 |
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Synthesis and peripheral cardiovascular action of cis- and trans-2-(3,4-dimethoxybenzyl)cyclopentylamine hydrochlorides Sonia R. Teller and Charles H. Jarboe pp 227 - 231; DOI: 10.1021/jm00345a007 |
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Synthesis and orexigenic activity of some 1-methyl-4-piperidylidene-substituted pyrrolo[2,1-b][3]benzazepine and dibenzocycloheptene derivatives David C. Remy, Susan F. Britcher, Paul S. Anderson, Patrice C. Belanger, Yves Girard, and B. V. Clineschmidt pp 231 - 234; DOI: 10.1021/jm00345a008 |
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Synthesis and enzymic activity of 6-carbethoxy- and 6-ethoxy-3,7-disubstituted pyrazolo[1,5-a]pyrimidines and related derivatives as adenosine cyclic 3',5'-phosphate phosphodiesterase inhibitors Robert H. Springer, M. B. Scholten, Darrell E. O'Brien, Thomas Novinson, Jon P. Miller, and Roland K. Robins pp 235 - 242; DOI: 10.1021/jm00345a009 |
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Synthesis and enzymic activity of various substituted pyrazolo[1,5-a]-1,3,5-triazines as adenosine cyclic 3',5'-phosphate phosphodiesterase inhibitors Keitaro Senga, Darrell E. O'Brien, Mieka B. Scholten, Thomas Novinson, Jon P. Miller, and Roland K. Robins pp 243 - 249; DOI: 10.1021/jm00345a010 |
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Angiotensin-converting enzyme inhibitors: importance of the amide carbonyl of mercaptoacyl amino acids for hydrogen bonding to the enzyme Michael E. Condon, Edward W. Petrillo Jr., Denis E. Ryono, Joyce A. Reid, Richard Neubeck, Mohindar Puar, James E. Heikes, Emily F. Sabo, Kathryn A. Losee, and et al. pp 250 - 258; DOI: 10.1021/jm00345a011 |
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Catechol O-methyltransferase. 10. 5-Substituted, 3-hydroxy-4-methoxybenzoic acids (isovanillic acids) and 5-substituted, 3-hydroxy-4-methoxybenzaldehydes (isovanillins) as potential inhibitors Ronald T. Borchardt, Joan H. Huber, and Michael Houston pp 258 - 263; DOI: 10.1021/jm00345a012 |
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Catechol O-methyltransferase. 12. Affinity labeling the active site with the oxidation products of 5,6-dihydroxyindole Ronald T. Borchardt and Pramila Bhatia pp 263 - 271; DOI: 10.1021/jm00345a013 |
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Novel dimeric derivatives of leucomycins and tylosin, sixteen-membered macrolides Satoshi Omura, Katsuji Miyano, Hajime Matsubara, and Akira Nakagawa pp 271 - 275; DOI: 10.1021/jm00345a014 |
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Potential antitumor agents. 36. Quantitative relationships between experimental antitumor activity, toxicity, and structure for the general class of 9-anilinoacridine antitumor agents William A. Denny, Bruce F. Cain, Graham J. Atwell, Corwin Hansch, Augustine Panthananickal, and A. Leo pp 276 - 315; DOI: 10.1021/jm00345a015 |
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Quantitative structure-inhibitory activity relationships of phenols and fatty acids for Bacillus subtilis spore germination Yoko Yasuda, Kunio Tochikubo, Yoetsu Hachisuka, Hisao Tomida, and Ken Ikeda pp 315 - 320; DOI: 10.1021/jm00345a016 |
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Catechol O-methyltransferase. 11. Inactivation by 5-hydroxy-3-mercapto-4-methoxybenzoic acid Ronald T. Borchardt and Joan H. Huber pp 321 - 323; DOI: 10.1021/jm00345a017 |
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Antiestrogenic properties of substituted benz[a]anthracene-3,9-diols Charles E. Morreal, Dilip K. Sinha, Sara L. Schneider, Robert E. Bronstein, and Jean Dawidzik pp 323 - 326; DOI: 10.1021/jm00345a018 |
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N-Aralkyl substitution of 2-amino-5,6- and -6,7-dihydroxy-1,2,3,4-tetrahydronaphthalenes. 2. Derivatives of a hypotensive-positive inotropic agent David M. Stout and Richard J. Gorczynski pp 326 - 328; DOI: 10.1021/jm00345a019 |
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Nitro and amino derivatives of lucanthone as antitumor agents Sydney Archer and Rabindra Rej pp 328 - 331; DOI: 10.1021/jm00345a020 |
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1-Acyltriazoles as antiinflammatory agents Peter C. Wade, B. Richard Vogt, Thomas P. Kissick, Ligaya M. Simpkins, Douglas M. Palmer, and Robert C. Millonig pp 331 - 333; DOI: 10.1021/jm00345a021 |
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Book Reviews pp 333 - 334; DOI: 10.1021/jm00345a601 |
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N2-(.gamma.-D-glutamyl)-meso-2-(L),2'(D)-diaminopimelic acid as the minimal prerequisite structure of FK-156: its acyl derivatives with potent immunostimulating activity Yoshihiko Kitaura, Osamu Nakaguchi, Hidekazu Takeno, Satoshi Okada, Satoshi Yonishi, Keiji Hemmi, Joh Mori, Hachiro Senoh, Yasuhiro Mine, and Masashi Hashimoto pp 335 - 337; DOI: 10.1021/jm00346a001 |
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2-Arylpyrazolo[4,3-c]quinolin-3-ones: a novel agonist, a partial agonist and an antagonist of benzodiazepines Naokata Yokoyama, Barry Ritter, and Alan D. Neubert pp 337 - 339; DOI: 10.1021/jm00346a002 |
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(.+-.)-4-Aryl-4,5-dihydro-3H-1,3-benzodiazepines. 1. Synthesis and evaluation of (.+-.)-4,5-dihydro-2,3-dimethyl-4-phenyl-3H-1,3-benzodiazepine and analogs as potential antidepressant agents Harry M. Geyer, Lawrence L. Martin, Charles A. Crichlow, Frederick W. Dekow, Daniel B. Ellis, Hansjoerg Kruse, Linda L. Setescak, and Manfred Worm pp 340 - 346; DOI: 10.1021/jm00346a003 |
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(.+-.)-4-Aryl-4,5-dihydro-3H-1,3-benzodiazepines. 2. Nuclear substituted analogs of (.+-.)-4,5-dihydro-2,3-dimethyl-4-phenyl-3H-1,3-benzodiazepine and (.+-.)-4,5-dihydro-2-ethyl-3-methyl-4-phenyl-3H-1,3-benzodiazepine as potential antidepressant agents Lawrence L. Martin, Linda L. Setescak, Manfred Worm, Charles A. Crichlow, Harry M. Geyer, and Jeffrey C. Wilker pp 346 - 351; DOI: 10.1021/jm00346a004 |
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Dopaminergic activity of substituted 6-chloro-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines Francis R. Pfeiffer, James W. Wilson, Joseph Weinstock, George Y. Kuo, Pamela A. Chambers, Kenneth G. Holden, Richard A. Hahn, Joseph R. Wardell Jr., J. Tobia Alfonso, and et al. pp 352 - 358; DOI: 10.1021/jm00346a005 |
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Chemistry and hypoglycemic activity of N-[[(dialkylamino)alkoxy]phenyl]benzamidines James R. Shroff, Bill Elpern, Sidney Kobrin, and Peter Cervoni pp 359 - 362; DOI: 10.1021/jm00346a006 |
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Synthesis and dopaminergic properties of some exo- and endo-2-aminobenzonorbornenes designed as rigid analogs of dopamine Peter Burn, Peter A. Crooks, Frank Heatley, Brenda Costall, Robert J. Naylor, and Virinder Nohria pp 363 - 368; DOI: 10.1021/jm00346a007 |
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Preparation and evaluation of 2-substituted anthraquinones based on the anthracyclines Stephen Bennett, Derek Sharples, and Jeffrey R. Brown pp 369 - 373; DOI: 10.1021/jm00346a008 |
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Use of adenine nucleotide derivatives to assess the potential of exo-active-site-directed reagents as species- or isozyme-specific enzyme inactivators. 3. Synthesis of adenosine 5'-triphosphate derivatives with N6- or 8-substituents bearing iodoacetyl groups Alexander Hampton, Arvind D. Patel, Mitsuaki Maeda, Ton T. Hai, Chi Due Chang, Jung Bu Kang, Francis Kappler, Masanobu Abo, and Robert K. Preston pp 373 - 381; DOI: 10.1021/jm00346a009 |
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Use of adenine nucleotide derivatives to assess the potential of exo-active-site-directed reagents as species- or isozyme-specific enzyme inactivators. 4. Interactions of adenosine 5'-triphosphate derivatives with adenylate kinases from Escherichia coli and rat tissues Alexander Hampton, Donald Picker, Kenneth A. Nealy, and Mitsuaki Maeda pp 382 - 386; DOI: 10.1021/jm00346a010 |
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Use of adenine nucleotide derivatives to assess the potential of exo-active-site-directed reagents as species- or isozyme-specific enzyme inactivators. 5. Interactions of adenosine 5'-triphosphate derivatives with rat pyruvate kinases, Escherichia coli thymidine kinase, and yeast and rat hexokinases Alexander Hampton, Arvind D. Patel, Ram R. Chawla, Francis Kappler, and Ton T. Hai pp 386 - 392; DOI: 10.1021/jm00346a011 |
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Serotonin receptor affinity of cathinone and related analogs Richard A. Glennon and Stephen M. Liebowitz pp 393 - 397; DOI: 10.1021/jm00346a012 |
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Peptide sweeteners. 5. Side chain homologs relating zwitterionic and trifluoroacetylated amino acid anilide and dipeptide sweeteners Masao Kawai, Rolf Nyfeler, Judd M. Berman, and Murray Goodman pp 397 - 402; DOI: 10.1021/jm00346a013 |
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Solution conformation of the thermolysin inhibitors carbobenzoxy-L-phenylalanine and .beta.-phenylpropionyl-L-phenylalanine and comparison of the solution conformation to the enzyme-bound conformation Tiee Leou Shieh and Stephen R. Byrn pp 403 - 408; DOI: 10.1021/jm00346a014 |
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Design of potent and selective antagonists of the vasopressor responses to arginine-vasopressin Maurice Manning, Bernard Lammek, Marian Kruszynski, Janny Seto, and Wilbur H. Sawyer pp 408 - 414; DOI: 10.1021/jm00346a015 |
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Design of more potent and selective antagonists of the antidiuretic responses to arginine-vasopressin devoid of antidiuretic agonism Maurice Manning, Wieslaw A. Klis, Aleksandra Olma, Janny Seto, and Wilbur H. Sawyer pp 414 - 419; DOI: 10.1021/jm00346a016 |
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2-(Alkylthio)-1,2,4-triazolo[1,5-a]pyrimidines as adenosine 3',5'-monophosphate phosphodiesterase inhibitors with potential as new cardiovascular agents Thomas Novinson, Robert Springer, D. E. O'Brien, Mieka B. Scholten, Jon P. Miller, and Roland K. Robins pp 420 - 426; DOI: 10.1021/jm00346a017 |
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Molecular structures of 2,4-diaminopyrimidine antifolates with antineoplastic activity Vivian Cody and Sigmund F. Zakrzewski pp 427 - 430; DOI: 10.1021/jm00346a018 |
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Chemical synthesis and molecular pharmacology of hydroxylated 1-(1-phenylcyclohexyl)piperidine derivatives J. M. Kamenka, B. Chiche, R. Goudal, P. Geneste, J. Vignon, J. P. Vincent, and M. Lazdunski pp 431 - 435; DOI: 10.1021/jm00346a019 |
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A comparison of the inhibitory action of 5-(substituted-benzyl)-2,4-diaminopyrimidines on dihydrofolate reductase from chicken liver with that from bovine liver Ren Li Li, Corwin Hansch, and Bernard T. Kaufman pp 435 - 440; DOI: 10.1021/jm00346a020 |
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A new class of nitrosoureas. 4. Synthesis and antitumor activity of disaccharide derivatives of 3,3-disubstituted 1-(2-chloroethyl)-1-nitrosoureas Kenji Tsujihara, Masakatsu Ozeki, Tamio Morikawa, Masatoshi Kawamori, Yukio Akaike, and Yoshihisa Arai pp 441 - 446; DOI: 10.1021/jm00346a021 |
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Antiinflammatory agents. 2. Syntheses and antiinflammatory activity of substituted 2-aminophenylacetic acid derivatives David A. Walsh, Dwight A. Shamblee, William J. Welstead, and Lawrence F. Sancilio pp 446 - 451; DOI: 10.1021/jm00346a022 |
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Synthesis and pharmacological evaluation of reduced diastereoisomeric and quaternary ammonium derivatives of calcium antagonistic (methylenedioxy)indenes on the isolated rat aorta Donald T. Witiak, Richard J. Brumbaugh, Richard J. Heaslip, and Ralf G. Rahwan pp 452 - 456; DOI: 10.1021/jm00346a023 |
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Quaternary heterocyclylamino .beta.-lactams: a generic alternative to the classical acylamino side chain John Hannah, Charles R. Johnson, Arthur F. Wagner, and Edward Walton pp 457 - 469; DOI: 10.1021/jm00346a024 |
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Synthesis and biological activities of photoaffinity labeling analogs of substance P E. Escher, R. Couture, G. Champagne, J. Mizrahi, and D. Regoli pp 470 - 475; DOI: 10.1021/jm00346a025 |
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Lysine and ornithine analogs of methotrexate as inhibitors of dihydrofolate reductase Robert J. Kempton, Angelique M. Black, Gregory M. Anstead, A. Ashok Kumar, Dale T. Blankenship, and James H. Freisheim pp 475 - 477; DOI: 10.1021/jm00346a026 |
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Adriamycin analogs. Preparation of 9,10-anhydrodaunorubicin, 9,10-anhydroadriamycin, and some related compounds Gopalakrishnan Potti and Mervyn Israel pp 478 - 481; DOI: 10.1021/jm00346a027 |
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Synthesis and in vitro antimicrobial activity of 6-substituted 2H-1,3,5-thiadiazine-2,4(3H)-diones Robert A. Coburn, Chuen Huei Ho, and Martha L. Bronstein pp 481 - 483; DOI: 10.1021/jm00346a028 |
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Book Reviews pp 484 - 488; DOI: 10.1021/jm00346a600 |
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Prodrugs of L-cysteine as liver-protective agents. 2(R,S)-methylthiazolidine-4(R)-carboxylic acid (MTCA), a latent cysteine Herbert T. Nagasawa, David J. D. Goon, Richard T. Zera, and Daniel L. Yuzon pp 489 - 491; DOI: 10.1021/jm00347a001 |
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Metabolic formation of iminium species: the metabolism of phencyclidine Dennis Ward, Asher Kalir, Anthony Trevor, James Adams, Thomas Baillie, and Neal Castagnoli pp 491 - 492; DOI: 10.1021/jm00347a002 |
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Prostaglandins and congeners. 29. (16RS)-(.+-.)-15-Deoxy-16-hydroxy-16-vinylprostaglandin E2, an orally and transdermally active hypotensive agent of prolonged duration Jay E. Birnbaum, Peter Cervoni, Peter S. Chan, Sow-Mei L. Chen, M. Brawner Floyd, Charles V. Grudzinskas, Martin J. Weiss, and Franz Dessy pp 492 - 494; DOI: 10.1021/jm00347a003 |
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Synthesis of prostanoids with bicyclo[2.2.1]heptane, bicyclo[3.1.1]heptane and bicyclo[2.2.2]octane ring systems. Activities of 15-hydroxy epimers on human platelets Norman H. Wilson, Venkateswarlu Peesapati, Robert L. Jones, and Kenneth Hamilton pp 495 - 500; DOI: 10.1021/jm00347a004 |
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Agents with potential specificity against melanotic melanoma Ai Jeng Lin, James A. Kelley, Theodore R. Breitman, and John S. Driscoll pp 501 - 505; DOI: 10.1021/jm00347a005 |
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Antitumor agents. II. Bis(guanylhydrazones) of anthracene-9,10-dicarboxaldehydes K. C. Murdock, R. G. Child, Yang I Lin, J. D. Warren, P. F. Fabio, Ving J. Lee, P. T. Izzo, S. A. Lang Jr., Robert B. Angier, and et al. pp 505 - 518; DOI: 10.1021/jm00347a006 |
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Inhibition by 5-(substituted-benzyl)-2,4-diaminopyrimidines of murine tumor (L5178Y) cell cultures sensitive to and resistant to methotrexate. Further evidence for the sensitivity of resistant cells to hydrophobic drugs Cynthia Dias Selassie, Renli Li, Corwin Hansch, Tasneem A. Khwaja, and Cecilia B. Dias pp 518 - 522; DOI: 10.1021/jm00347a007 |
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Synthesis and biological evaluation of novel pyrimidine nucleoside analogs of 1,4-oxathiane, 1,4-dithiane, and 1,4-dioxane Lucjan J. J. Hronowski and Walter A. Szarek pp 522 - 526; DOI: 10.1021/jm00347a008 |
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Isomeric cyclopropyl ring-methylated homologs of trans-2-(2,5-dimethoxy-4-methylphenyl)cyclopropylamine, an hallucinogen analog James N. Jacob and David E. Nichols pp 526 - 530; DOI: 10.1021/jm00347a009 |
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Effects of certain hallucinogenic amphetamine analogs on the release of [3H]-serotonin from rat brain synaptosomes David E. Nichols, David H. Lloyd, Andrew J. Hoffman, Maxine B. Nichols, and George Yim pp 530 - 535; DOI: 10.1021/jm00347a010 |
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A new, potent, conformationally-restricted analog of amphetamine: 2-amino-1,2-dihydronaphthalene Bruce A. Hathaway, David E. Nichols, Maxine B. Nichols, and George K. W. Yim pp 535 - 538; DOI: 10.1021/jm00347a011 |
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Lysosomotropic agents. 4. Carbobenzoxyglycylphenylalanyl, a new protease-sensitive masking group for introduction into cells Raymond A. Firestone, Judith M. Pisano, Philip J. Bailey, Anita Sturm, Robert J. Bonney, Paul Wightman, Richard Devlin, C. Shirley Lin, Doris L. Keller, and Patricia C. Tway pp 539 - 544; DOI: 10.1021/jm00347a012 |
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DL-Threo-.beta.-fluoroaspartate and LD-threo-.beta.-fluoroasparagine: selective cytotoxic agents for mammalian cells in culture Andrew M. Stern, Bruce M. Foxman, Armen H. Tashjian, and Robert H. Abeles pp 544 - 550; DOI: 10.1021/jm00347a013 |
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Synthesis and biochemical properties of chemically stable product analogs of the reaction catalyzed by S-adenosyl-L-methionine decarboxylase Michael Kolb, Charles Danzin, Jacqueline Barth, and Nicole Claverie pp 550 - 556; DOI: 10.1021/jm00347a014 |
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Synthesis and structure-activity relationship of nonyl 3-acyldithiocarbazates and related compounds for uncoupling activities Masayuki Uda, Kouhei Toyooka, Kisako Horie, Masayuki Shibuya, Seiju Kubota, and Hiroshi Terada pp 557 - 560; DOI: 10.1021/jm00347a015 |
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Structure-activity relationships of nogalamycin analogs Paul F. Wiley, David W. Elrod, David J. Houser, and Floyd A. Richard pp 560 - 567; DOI: 10.1021/jm00347a016 |
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Agents for the treatment of brain injury. 1. (Aryloxy)alkanoic acids E. J. Cragoe, N. P. Gould, O. W. Woltersdorf, C. Ziegler, R. S. Bourke, L. R. Nelson, H. K. Kimelberg, J. B. Waldman, A. J. Popp, and N. Sedransk pp 567 - 579; DOI: 10.1021/jm00347a017 |
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Structural modifications of anguidin and antitumor activities of its analogs T. Kaneko, H. Schmitz, J. M. Essery, W. Rose, H. G. Howell, F. A. O'Herron, S. Nachfolger, J. Huftalen, W. T. Bradner, and et al. pp 579 - 589; DOI: 10.1021/jm00347a018 |
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Synthesis and some pharmacological properties of Z-Tyr(SO3H)-Met-Gly-Trp-Met-Asp(Phe-NH2)-OH, a 32-.beta.-aspartyl analog of cholecystokinin (pancreozymin)-27-33 Jean Martinez, Francois Winternitz, Miklos Bodanszky, Jerry D. Gardner, Michael D. Walker, and Victor Mutt pp 589 - 593; DOI: 10.1021/jm00347a019 |
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Effect of 4'-halogen substitution on the mutagenicity of trans-4-acetamidostilbene and trans-4-(N-hydroxyacetamido)stilbene in the Salmonella typhimurium test system Frances N. Shirota and Patrick E. Hanna pp 593 - 595; DOI: 10.1021/jm00347a020 |
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Use of a potential rabbit model for structure-behavioral activity studies of cannabinoids Paul Consroe, Arnold R. Martin, and Barbara Schneiderman Fish pp 596 - 599; DOI: 10.1021/jm00347a021 |
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Irreversible enzyme inhibitors. 202. Candidate active-site-directed irreversible inhibitors of 5-fluoro-2'-deoxyuridine phosphorylase from Walker 256 rat tumor derived from 1-benzyl-5-(3-ethoxybenzyl)uracil James L. Kelley and B. R. Baker pp 600 - 603; DOI: 10.1021/jm00347a022 |
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Inhibitors of adenosine deaminase. Studies in combining high-affinity enzyme-binding structural units. Erythro-1,6-dihydro-6-(hydroxymethyl)-9-(2-hydroxy-3-nonyl)purine and erythro-9-(2-hydroxy-3-nonyl)purine Peter W. K. Woo and David C. Baker pp 603 - 605; DOI: 10.1021/jm00347a023 |
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Renin inhibitors. Substitution of the leucyl residues of Leu-Leu-Val-Phe-OCH3 with 3-amino-2-hydroxy-5-methylhexanoic acid Rodney L. Johnson pp 605 - 610; DOI: 10.1021/jm00347a024 |
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Book Reviews pp 610 - 612; DOI: 10.1021/jm00347a602 |
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Synthesis and biological evaluation of 17-[131I]iodo-9-telluraheptadecanoic acid, a potential myocardial imaging agent M. M. Goodman, F. F. Knapp, A. P. Callahan, and L. A. Ferren pp 613 - 618; DOI: 10.1021/jm00348a001 |
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Potential organ- or tumor-imaging agents. 22. Acyl-labeled cholesterol esters R. H. Seevers, S. W. Schwendner, S. L. Swayze, and R. E. Counsell pp 618 - 621; DOI: 10.1021/jm00348a002 |
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Inhibitors of hepatic mixed-function oxidases. 4. Effects of benzimidazole and related compounds on aryl hydrocarbon hydroxylase activity from phenobarbitone and 3-methylcholanthrene induced rats Peter J. Little and Adrian J. Ryan pp 622 - 626; DOI: 10.1021/jm00348a003 |
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Carbocyclic analog of 3-deazaadenosine: a novel antiviral agent using S-adenosylhomocysteine hydrolase as a pharmacological target John A. Montgomery, Sarah J. Clayton, H. Jeanette Thomas, William M. Shannon, Gussie Arnett, Anne J. Bodner, In Kyung Kion, Giulio L. Cantoni, and Peter K. Chiang pp 626 - 629; DOI: 10.1021/jm00348a004 |
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Arylhydroxamic acid N,O-acyltransferase substrates. Acetyl transfer and electrophile generating activity of N-hydroxy-N-(4-alkyl-, 4-alkenyl-, and 4-cyclohexylphenyl)acetamides Bonnie L. K. Mangold and Patrick E. Hanna pp 630 - 638; DOI: 10.1021/jm00348a005 |
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Species- or isozyme-specific enzyme inhibitors. 4. Design of a two-site inhibitor of adenylate kinase with isozyme selectivity Alexander Hampton, Francis Kappler, and Donald Picker pp 638 - 644; DOI: 10.1021/jm00348a006 |
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Species- or isozyme-specific enzyme inhibitors. 5. Differential effects of thymidine substituents on affinity for rat thymidine kinase isozymes Alexander Hampton, Ram R. Chawla, and Francis Kappler pp 644 - 649; DOI: 10.1021/jm00348a007 |
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Double-head haptens. Synthesis of and experimentally induced contact sensitivity to substances containing two unrelated haptens, pyrocatechol and .alpha.-methylene-.gamma.-butyrolactone, in the same molecule Bernard Marchand and Claude Benezra pp 650 - 653; DOI: 10.1021/jm00348a008 |
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Potential antitrypanosomal agents. 1,N2-Disubstituted 2-amino-5-hydroxy-4-methylnaphtho[1,2-d]thiazolium salts and related compounds Peter Ulrich and Anthony Cerami pp 654 - 657; DOI: 10.1021/jm00348a009 |
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Avermectin acyl derivatives with anthelmintic activity Helmut Mrozik, Philip Eskola, Michael H. Fisher, John R. Egerton, Sam Cifelli, and Dan A. Ostlind pp 658 - 663; DOI: 10.1021/jm00348a010 |
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Structure-activity correlations of cytochalasins. Novel halogenated and related cytochalasin C and D derivatives B. H. Patwardhan, Michael Flashner, Carl A. Miller, and S. W. Tanenbaum pp 663 - 666; DOI: 10.1021/jm00348a011 |
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Structure-activity relationships for 2-substituted imidazoles as .alpha.2-adrenoceptor antagonists Joan M. Caroon, Robin D. Clark, Arthur F. Kluge, Ronald Olah, David B. Repke, Stefan H. Unger, Anton D. Michel, and Roger L. Whiting pp 666 - 670; DOI: 10.1021/jm00348a012 |
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Arylethanolamines derived from salicylamide with .alpha.- and .beta.-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers and related salicylamides James E. Clifton, Ian Collins, Peter Hallett, David Hartley, Lawrence H. C. Lunts, and Philip D. Wicks pp 670 - 679; DOI: 10.1021/jm00348a013 |
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Syntheses and adrenergic agonist properties of ring-fluorinated isoproterenols Kenneth L. Kirk, Daniele Cantacuzene, Brian Collins, George T. Chen, Yuth Nimit, and Cyrus R. Creveling pp 680 - 684; DOI: 10.1021/jm00348a014 |
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Synthesis, x-ray crystallographic determination, and opioid activity of erythro-5-methylmethadone enantiomers. Evidence which suggests that .mu. and .delta. opioid receptors possess different stereochemical requirements P. S. Portoghese, J. H. Poupaert, D. L. Larson, W. C. Groutas, G. D. Meitzner, D. C. Swenson, G. D. Smith, and W. L. Duax pp 684 - 688; DOI: 10.1021/jm00348a015 |
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Conformation-activity study of methadone and related compounds Mark Froimowitz pp 689 - 696; DOI: 10.1021/jm00348a016 |
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Absolute stereochemistry and dopaminergic activity of enantiomers of 2,3,4,5-tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine Carl Kaiser, Penelope A. Dandridge, Eleanor Garvey, Richard A. Hahn, Henry M. Sarau, Paulette E. Setler, Lawrence S. Bass, and Jon Clardy pp 697 - 703; DOI: 10.1021/jm00348a017 |
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Synthesis of 2-(alkylamino)-5,6- and -6,7-dihydroxy-3,4-dihydroquinazolines and evaluation as potential dopamine agonists John A. Grosso, David E. Nichols, Jai D. Kohli, and Dana Glock pp 703 - 708; DOI: 10.1021/jm00348a018 |
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Synthesis and cardiovascular activity of a new series of cyclohexylaralkylamine derivatives related to perhexiline Gerard Leclerc, Nicole Decker, and Jean Schwartz pp 709 - 714; DOI: 10.1021/jm00348a019 |
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Inhibitors of blood platelet aggregation. Activity of some 1H-benz[de]isoquinolinecarboximidamides on the in vivo blood platelet aggregation induced by collagen Tom Beetz, Dick G. Meuleman, and Joop H. Wieringa pp 714 - 719; DOI: 10.1021/jm00348a020 |
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Synthesis of N-[[(substituted-phenyl)carbonyl]amino]-1,2,3,6-tetrahydropyridines with analgesic and hyperglycemic activity Jupita M. Yeung, Linda A. Corleto, and Edward E. Knaus pp 720 - 723; DOI: 10.1021/jm00348a021 |
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Tryptophan analogs. 1. Synthesis and antihypertensive activity of positional isomers Max E. Safdy, Elva Kurchacova, Robert N. Schut, Horacio Vidrio, and Enrique Hong pp 723 - 730; DOI: 10.1021/jm00348a022 |
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2- and 6-Methyl-1,4-naphthoquinone derivatives as potential bioreductive alkylating agents Ippolito Antonini, Tai Shun Lin, Lucille A. Cosby, Yao Ren Dai, and Alan C. Sartorelli pp 730 - 735; DOI: 10.1021/jm00348a023 |
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2-(Aminomethyl)phenols, a new class of saluretic agents. 4. Effects of oxygen and/or nitrogen substitution G. E. Stokker, A. A. Deana, S. J. DeSolms, E. M. Schultz, R. L. Smith, E. J. Cragoe, J. E. Baer, H. F. Russo, and L. S. Watson pp 735 - 742; DOI: 10.1021/jm00348a024 |
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Alkaline phosphatase inhibition by a series of pyrido[2,1-b]quinazolines: a possible relationship with cromolyn-like antiallergy activity Charles F. Schwender, Brooks R. Sunday, and Victoria L. Decker pp 742 - 745; DOI: 10.1021/jm00348a025 |
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Isoxazolidine-3,5-diones as lens aldose reductase inhibitors Allen B. Richon, Michael E. Maragoudakis, and James S. Wasvary pp 745 - 747; DOI: 10.1021/jm00348a026 |
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Relative affinity of 17α- and/or 21-esters and 17α,21-diesters of cortisol for a glucocorticoid receptor from rat thymocytes A. J. Solo, Kenneth M. Tramposch, Daniel W. Szeto, and Mark J. Suto pp 747 - 749; DOI: 10.1021/jm00348a027 |
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Book Reviews pp 749 - 752; DOI: 10.1021/jm00348a600 |
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Metabolic activation and drug toxicity Sidney D. Nelson pp 753 - 765; DOI: 10.1021/jm00349a001 |
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Computer-assisted studies of structure-activity relationships of N-nitroso compounds using pattern recognition Susan L. Rose and Peter C. Jurs pp 769 - 776; DOI: 10.1021/jm00349a002 |
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Comparison of the inhibition of Escherichia coli and Lactobacillus casei dihydrofolate reductase by 2,4-diamino-5-(substituted-benzyl)pyrimidines: quantitative structure-activity relationships, x-ray crystallography, and computer graphics in structure-activity analysis Corwin Hansch, Renli Li, Jeffrey M. Blaney, and Robert Langridge pp 777 - 784; DOI: 10.1021/jm00349a003 |
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Computer graphics in drug design: molecular modeling of thyroid hormone-prealbumin interactions Jeffrey M. Blaney, Eugene C. Jorgensen, Michael L. Connolly, Thomas E. Ferrin, Robert Langridge, Stuart J. Oatley, Jane M. Burridge, and Colin C. F. Blake pp 785 - 790; DOI: 10.1021/jm00349a004 |
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Synthesis of analogs of the carboxyl protease inhibitor pepstatin. Effect of structure in subsite P3 on inhibition of pepsin Daniel H. Rich and Michael S. Bernatowicz pp 791 - 795; DOI: 10.1021/jm00349a005 |
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Synthesis and biological activity of some very hydrophobic superagonist analogs of luteinizing hormone-releasing hormone John J. Nestor, Teresa L. Ho, Richard A. Simpson, Bonnie L. Horner, Gordon H. Jones, Georgia I. McRae, and Brian H. Vickery pp 795 - 801; DOI: 10.1021/jm00349a006 |
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Species- and isozyme-specific enzyme inhibitors. 6. Synthesis and evaluation of two-substrate condensation products as inhibitors of hexokinases and thymidine kinases Alexander Hampton, Ton T. Hai, Francis Kappler, and Ram R. Chawla pp 801 - 805; DOI: 10.1021/jm00349a007 |
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Species- or isozyme-specific enzyme inhibitors. 7. Selective effects in inhibitions of rat adenylate kinase isozymes by adenosine 5'-phosphate derivatives Ton T. Hai, Donald Picker, Masanobu Abo, and Alexander Hampton pp 806 - 812; DOI: 10.1021/jm00349a008 |
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Synthesis of pyridazine analogs of the naturally occurring nucleosides cytidine, uridine, deoxycytidine and deoxyuridine David J. Katz, Dean S. Wise, and Leroy B. Townsend pp 813 - 821; DOI: 10.1021/jm00349a009 |
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Synthesis of some potential antihypertensive phthalazinylguanidines and quinoxalinylguanidines Christopher B. Chapleo, John C. Doxey, and Peter L. Myers pp 821 - 824; DOI: 10.1021/jm00349a010 |
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Preparation of the .alpha. and .beta. anomers of 9-(3,5-dideoxy-D-glycero-pent-4-enofuranosyl)adenine and their activity with leukemia L1210 cells in vitro Leon M. Lerner pp 825 - 828; DOI: 10.1021/jm00349a011 |
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(2-Chloroethyl)nitrosourea congeners of amino acid amides Tetsuo Suami, k Tsuguhiro Kato, Hiroaki Takino, and Takashi Hisamatsu pp 829 - 832; DOI: 10.1021/jm00349a012 |
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N,N'-Dialkyl-1,2-bis(hydroxyphenyl)ethylenediamines and N,N'-dialkyl-4,5-bis(4-hydroxyphenyl)imidazolidines. Syntheses and evaluation of their mammary tumor inhibiting activity Erwin Von Angerer, Guenter Egginger, Gerhard Kranzfelder, Horst Bernhauer, and Helmut Schoenenberger pp 832 - 837; DOI: 10.1021/jm00349a013 |
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Novel orally active inhibitors of passive cutaneous anaphylaxis in rats: N-[2-(4-Pyridinyl)-4-pyrimidinyl] ureas and dialkyl [[[2-(4-pyridinyl)-4-pyrimidinyl]amino]methylene]malonates George Y. Lesher, Baldev Singh, and Zigurd Mielens pp 837 - 842; DOI: 10.1021/jm00349a014 |
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Arylhydroxamic acid bioactivation via acyl group transfer. Structural requirements for transacylating and electrophile-generating activity of N-(2-fluorenyl)hydroxamic acids and related compounds Heui Mei Yeh and Patrick E. Hanna pp 842 - 846; DOI: 10.1021/jm00349a015 |
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Narcotic antagonistic potency of bivalent ligands which contain .beta.-naltrexamine. Evidence for simultaneous occupation of proximal recognition sites M. Erez, A. E. Takemori, and P. S. Portoghese pp 847 - 849; DOI: 10.1021/jm00349a016 |
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Synthesis and dopamine receptor binding of exo- and endo-2-amino-6,7-dihydroxybenzonorbornene, rigid analogs of 2-amino-6,7-dihydroxytetrahydronaphthalene David I. Schuster, Haralambos E. Katerinopoulos, William L. Holden, Anubhav P. S. Narula, Richard B. Libes, and Randall B. Murphy pp 850 - 854; DOI: 10.1021/jm00349a017 |
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Affinity of 10-(4-methylpiperazino)dibenz[b,f]oxepins for clozapine and spiroperidol binding sites in rat brain Terry W. Harris, Howard E. Smith, Philip L. Mobley, D. Hal Manier, and Fridolin Sulser pp 855 - 858; DOI: 10.1021/jm00349a018 |
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2-Amino-4,7-dimethoxyindan derivatives: synthesis and assessment of dopaminergic and cardiovascular actions R. D. Sindelar, J. Mott, C. F. Barfknecht, S. P. Arneric, J. R. Flynn, J. P. Long, and R. K. Bhatnagar pp 858 - 864; DOI: 10.1021/jm00349a019 |
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Antiallergics: 3-(1H-tetrazol-5-yl)-4H-pyrimido[2,1-b]benzothiazol-4-ones J. P. Yevich, D. L. Temple, R. R. Covington, D. A. Owens, R. J. Seidehamel, and K. W. Dungan pp 864 - 868; DOI: 10.1021/jm00349a020 |
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Pyridoquinoxaline N-oxides. 1. A new class of antitrichomonal agents Edward A. Glazer and Larry R. Chappel pp 868 - 870; DOI: 10.1021/jm00349a021 |
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Synthesis and tissue distribution study of iodine-labeled benzyl- and xylylamines Kenneth M. Tramposch, Hank F. Kung, and Monte Blau pp 870 - 873; DOI: 10.1021/jm00349a022 |
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Hydrogen bonding and anesthetic potency Satoshi Yokono, Donald D. Shieh, Hiroshi Goto, and Kasumi Arakawa pp 873 - 876; DOI: 10.1021/jm00349a023 |
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10-Propargylaminopterin and alkyl homologs of methotrexate as inhibitors of folate metabolism J. R. Piper, G. S. McCaleb, J. A. Montgomery, Roy L. Kisliuk, Y. Gaumont, and F. M. Sirotnak pp 877 - 880; DOI: 10.1021/jm00349a024 |
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Ring contraction of oleandrose on the macrolide antibiotic oleandomycin with [(methoxycarbonyl)sulfamoyl]triethylammonium hydroxide inner salt Arthur A. Nagel, Joseph DiBrino, Lawrence A. Vincent, and James A. Retsema pp 881 - 884; DOI: 10.1021/jm00349a025 |
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Book Reviews pp 884 - 884; DOI: 10.1021/jm00349a601 |
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Pyridoquinoxaline N-Oxides. 1. A New Class of Antitrichomonal Agents Edward A. Glazer, and Larry R. Chappel pp 766 - 769; DOI: 10.1021/jm00349a603 |
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Synthesis, decomposition kinetics, and preliminary toxicological studies of pure N-acetyl-p-benzoquinone imine, a proposed toxic metabolite of acetaminophen David C. Dahlin and Sidney D. Nelson pp 885 - 886; DOI: 10.1021/jm00350a001 |
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Inhibition of rat hepatic microsomal aminopyrine N-demethylase activity by benzimidazole derivatives. Quantitative structure-activity relationships Michael Murray, Adrian J. Ryan, and Peter J. Little pp 887 - 892; DOI: 10.1021/jm00350a002 |
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Quantitative structure-activity relationship by distance geometry: quinazolines as dihydrofolate reductase inhibitors Arup K. Ghose and Gordon M. Crippen pp 892 - 899; DOI: 10.1021/jm00350a003 |
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Structure-antitumor activity relationships of 9-anilinoacridines using pattern recognition Douglas R. Henry, Peter C. Jurs, and William A. Denny pp 899 - 908; DOI: 10.1021/jm00350a004 |
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Structure-activity relationships in potentially hallucinogenic N,N-dialkyltryptamines substituted in the benzene moiety Toni B. Kline, Frederick Benington, Richard D. Morin, and John M. Beaton pp 908 - 913; DOI: 10.1021/jm00350a005 |
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Potential affinity labels for the opiate receptor based on fentanyl and related compounds Bruce E. Maryanoff, Eric J. Simon, Theresa Gioannini, and H. Gorissen pp 913 - 919; DOI: 10.1021/jm00350a006 |
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(.+-.)-2-Depentylperhydrohistrionicotoxin: a new probe for a regulatory site on the nicotinic acetylcholine receptor-channel Kimio Takahashi, Arthur E. Jacobson, Chin Pong Mak, Bernhard Witkop, Arnold Brossi, Edson X. Albuquerque, J. E. Warnick, M. A. Maleque, A. Bavoso, and J. V. Silverton pp 919 - 925; DOI: 10.1021/jm00350a007 |
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Monophenolic octahydrobenzo[f]quinolines: central dopamine- and serotonin-receptor stimulating activity Haakan Wikstroem, Domingo Sanchez, Per Lindberg, Lars-Erik Arvidsson, Uli Hacksell, Anette Johansson, J. Lars G. Nilsson, Stephan Hjorth, and Arvid Carlsson pp 925 - 931; DOI: 10.1021/jm00350a008 |
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Use of (S)-(trifloxymethyl)oxirane in the synthesis of a chiral .beta.-adrenoceptor antagonist, (R)- and (S)-9-[[3-(tert-butylamino)-2-hydroxypropyl]oximino]fluorene John J. Baldwin, David E. McClure, Dennis M. Gross, and Michael Williams pp 931 - 936; DOI: 10.1021/jm00350a009 |
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Conformational analysis of the ergot alkaloids ergotamine and ergotaminine L. Pierri, I. H. Pitman, I. D. Rae, D. A. Winkler, and P. R. Andrews pp 937 - 942; DOI: 10.1021/jm00350a010 |
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Allergenic .alpha.-methylene-.gamma.-butyrolactones. Stereospecific synthesis of (+)- and (-)-.gamma.-methyl-.alpha.-methylene-.gamma.-butyrolactones. A study of the specificity of (+) and (-) enantiomers in inducing allergic contact dermatitis Pierre Barbier and Claude Benezra pp 943 - 946; DOI: 10.1021/jm00350a011 |
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Imidodisulfamides. 1. A novel class of antagonists of slow-reacting substance of anaphylaxis Fadia El-Fehail Ali, Penelope A. Dandridge, John G. Gleason, Robert D. Krell, Carolyn H. Kruse, Patricia G. Lavanchy, and Kenneth M. Snader pp 947 - 952; DOI: 10.1021/jm00350a012 |
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Synthesis and antitumor activity of new platinum complexes David B. Brown, A. R. Khokhar, M. P. Hacker, L. Lokys, J. H. Burchenal, R. A. Newman, J. J. McCormack, and David Frost pp 952 - 956; DOI: 10.1021/jm00350a013 |
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Affinity therapeutics. 1. Selective incorporation of 2-thiouracil derivatives in murine melanomas. Cytostatic activity of 2-thiouracil arotinoids, 2-thiouracil retinoids, arotinoids, and retinoids Frank Waetjen, Ole Buchardt, and Eyvind Langvad pp 956 - 960; DOI: 10.1021/jm00350a014 |
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Methotrexate analogs. 15. A methotrexate analogue designed for active-site-directed irreversible inactivation of dihydrofolate reductase A. Rosowsky, J. E. Wright, C. Ginty, and J. Uren pp 960 - 964; DOI: 10.1021/jm00350a015 |
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Antimalarials. 13. 5-Alkoxy analogs of 4-methylprimaquine Maurice P. LaMontagne, Anica Markovac, and M. Sami Khan pp 964 - 968; DOI: 10.1021/jm00350a016 |
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Antiparasitic agents. 5. Synthesis and anthelmintic activities of novel 2-heteroaromatic-substituted isothiocyanatobenzoxazoles and -benzothiazoles R. D. Haugwitz, R. G. Angel, G. A. Jacobs, B. V. Maurer, V. L. Narayanan, L. R. Cruthers, and J. Szanto pp 969 - 974; DOI: 10.1021/jm00350a017 |
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Pyridazinones. 1. Synthesis, antisecretory, and antiulcer activities of thio amide derivatives Toshihiro Yamada, Youichi Nobuhara, Azuma Yamaguchi, and Masahiko Ohki pp 975 - 982; DOI: 10.1021/jm00350a018 |
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Novel opiates and antagonists. 4. 7-Alkanoylhydromorphone James Quick, Patricia Herlihy, Raj K. Razdan, and John F. Howes pp 983 - 986; DOI: 10.1021/jm00350a019 |
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Novel opiates and antagonists. 5. 7-Carbethoxy-N-(cycloalkylmethyl)-3-hydroxymorphinan-6-ones and -isomorphinan-6-ones Patricia Herlihy, Haldean C. Dalzell, John F. Howes, and Raj K. Razdan pp 986 - 990; DOI: 10.1021/jm00350a020 |
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Aporphines. 39. Synthesis, dopamine receptor binding, and pharmacological activity of (R)-(-)- and (S)-(+)-2-hydroxyapomorphine John L. Neumeyer, G. W. Arana, Vishnu J. Ram, Nora S. Kula, and Ross J. Baldessarini pp 990 - 992; DOI: 10.1021/jm00350a021 |
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Brain levels and metabolism of the dopaminergic agonist 2-amino-6,7-dihydroxytetrahydronaphthalene after administration of various prodrugs A. S. Horn, H. Griever-Kazemier, and D. Dijkstra pp 993 - 996; DOI: 10.1021/jm00350a022 |
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Angiotensin converting enzyme inhibitors: modifications of a tripeptide analog Robert F. Meyer, Arnold D. Essenburg, Ronald D. Smith, and Harvey R. Kaplan pp 996 - 999; DOI: 10.1021/jm00350a023 |
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Synthesis and biological activity of 5'-substituted 5-fluoropyrimidine nucleosides Sudhir Ajmera and Peter V. Danenberg pp 999 - 1002; DOI: 10.1021/jm00350a024 |
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Book Reviews pp 1003 - 1008; DOI: 10.1021/jm00350a600 |
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Substance P Bengt E. B. Sandberg and Leslie L. Iversen pp 1009 - 1015; DOI: 10.1021/jm00351a001 |
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Design, synthesis, and testing of potential antisickling agents. 1. Halogenated benzyloxy and phenoxy acids Donald J. Abraham, Ahmed S. Mehanna, and Franki L. Williams pp 1015 - 1017; DOI: 10.1021/jm00351a002 |
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Drug latentiation by .gamma.-glutamyl transpeptidase Sanne D. J. Magnan, Frances N. Shirota, and Herbert T. Nagasawa pp 1018 - 1021; DOI: 10.1021/jm00351a003 |
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Comparative biological activities of highly potent active-site analogs of .alpha.-melanotropin Tomi K. Sawyer, Victor J. Hruby, Brian C. Wilkes, Matthew T. Draelos, Mac E. Hadley, and Marvin Bergsneider pp 1022 - 1027; DOI: 10.1021/jm00351a004 |
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Synthesis and immunoadjuvant activities of 2-acetamido-5-O-acetyl-6-O-acyl-2-deoxy-3-O-[(R)-2-propionyl-L-alanyl-D-isoglutamine]-D-glucofuranoses as potential prodrug forms of 6-O-acyl derivatives of N-acetylmuramyl dipeptide Philippe L. Durette, Conrad P. Dorn, Arthur Friedman, and Abner Schlabach pp 1028 - 1033; DOI: 10.1021/jm00351a005 |
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Synthesis and in vivo antitumor activity of potential 5-fluorouracil prodrugs A. Rosowsky, S. H. Kim, D. Trites, and M. Wick pp 1034 - 1040; DOI: 10.1021/jm00351a006 |
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Pyrazolo[3,4-d]pyrimidine ribonucleosides as anticoccidials. 2. Synthesis and activity of some nucleosides of 4-(alkylamino)-1H-pyrazolo[3,4-d]pyrimidines Janet L. Rideout, Thomas A. Krenitsky, George W. Koszalka, Naomi K. Cohn, Esther Y. Chao, Gertrude B. Elion, Victoria S. Latter, and Raymond B. Williams pp 1040 - 1044; DOI: 10.1021/jm00351a007 |
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New anticancer agents: synthesis of 1,2-dihydropyrido[3,4-b]pyrazines (1-deaza-7,8-dihydropteridines) Carroll Temple, Glynn P. Wheeler, Robert D. Elliott, Jerry D. Rose, Conrad L. Kussner, Robert N. Comber, and John A. Montgomery pp 1045 - 1050; DOI: 10.1021/jm00351a008 |
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Quinazolines and 1,4-benzodiazepines. 91. Structure-activity relationship between substituted 2-amino-N-(2-benzoyl-4-chlorophenyl)acetamides and 1,4-benzodiazepinones R. Ian Fryer, Willy Leimgruber, and Eugene J. Trybulski pp 1050 - 1055; DOI: 10.1021/jm00351a009 |
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Estrogenic and antiestrogenic activity of monophenolic analogs of tamoxifen, [(Z)-2-[p-(1,2-diphenyl-1-butenyl)phenoxy]-N,N-dimethylethylamine] Peter C. Ruenitz, Jerome R. Bagley, and Corwin M. Mokler pp 1056 - 1060; DOI: 10.1021/jm00351a010 |
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Carboxyimamidate, a low-molecular-weight polyelectrolyte with antitumor properties and low toxicity Joseph E. Fields, Samuel S. Asculai, John H. Johnson, and Randall K. Johnson pp 1060 - 1064; DOI: 10.1021/jm00351a011 |
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Nonsteroidal antiinflammatory agents. 1. 10,11-Dihydro-11-oxodibenz[b,f]oxepinacetic acids and related compounds Yasutaka Nagai, Akira Irie, Hideo Nakamura, Katsuhiko Hino, Hitoshi Uno, and Haruki Nishimura pp 1065 - 1070; DOI: 10.1021/jm00351a012 |
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1,1,2-Triphenylbut-1-enes: relationship between structure, estradiol receptor affinity, and mammary tumor inhibiting properties Martin R. Schneider, Erwin Von Angerer, Helmut Schoenenberger, Ralf T. Michel, and H. P. Fortmeyer pp 1070 - 1077; DOI: 10.1021/jm00351a013 |
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Synthesis, 470-MHz proton NMR spectra, and activity of delactonized derivatives of the anticancer drug etoposide Ian Jardine, Robert J. Strife, and John Kozlowski pp 1077 - 1081; DOI: 10.1021/jm00351a014 |
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.beta.-Carbolines: synthesis and neurochemical and pharmacological actions on brain benzodiazepine receptors Michael Cain, Robert W. Weber, Fil Guzman, James M. Cook, Steven A. Barker, Kenner C. Rice, Jacqueline N. Crawley, Steven M. Paul, and Phil Skolnick pp 1081 - 1091; DOI: 10.1021/jm00351a015 |
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(.+-.)-cis-2-Acetoxycyclobutyltrimethylammonium iodide: a semirigid analog of acetylcholine Joseph G. Cannon, Dale M. Crockatt, John Paul Long, and William Maixner pp 1091 - 1094; DOI: 10.1021/jm00351a016 |
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Antimalarials. 14. 5-(Aryloxy)-4-methylprimaquine analogs. A highly effective series of blood and tissue schizonticidal agents Maurice P. LaMontagne, Peter Blumbergs, and Richard E. Strube pp 1094 - 1097; DOI: 10.1021/jm00351a017 |
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Modifications of primaquine as antimalarials. 3. 5-Phenoxy derivatives of primaquine Edward A. Nodiff, Keiichi Tanabe, Eugene H. Chen, and Andrew J. Saggiomo pp 1097 - 1101; DOI: 10.1021/jm00351a018 |
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Hypobetalipoproteinemic agents. 3. Variation of the polycyclic portion of 4-(1-adamantyloxy)aniline William E. Heyd, Larry T. Bell, James R. Heystek, Paul E. Schurr, and Charles E. Day pp 1101 - 1103; DOI: 10.1021/jm00351a019 |
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Analogs of 3-quinuclidinyl benzilate W. J. Rzeszotarski, R. E. Gibson, W. C. Eckelman, D. A. Simms, E. M. Jagoda, N. L. Ferreira, and R. C. Reba pp 1103 - 1106; DOI: 10.1021/jm00351a020 |
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Synthesis and study of a spin-labeled cyclophosphamide analog 3-(1-oxy-2,2,6,6-tetramethyl-4-piperidinyl)cyclophosphamide Fai Po Tsui, Frank A. Robey, Thomas W. Engle, Susan Marie Ludeman, and Gerald Zon pp 1106 - 1110; DOI: 10.1021/jm00351a021 |
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Antiinflammatory properties of 8-aryl-5-isopropyl-2H-1,3-dioxolo[4,5-g]quinazolin-6(5H)-ones and -thiones William J. Houlihan, George Cooke, Richard Van Bochoven, John Perrine, Edward I. Takesue, and E. Jukniewicz pp 1110 - 1113; DOI: 10.1021/jm00351a022 |
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Book Reviews pp 1113 - 1114; DOI: 10.1021/jm00351a601 |
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Lipoproteins as potential site-specific delivery systems for diagnostic and therapeutic agents Raymond E. Counsell and Raymond C. Pohland pp 1115 - 1120; DOI: 10.1021/jm00352a001 |
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Receptor-based design of dihydrofolate reductase inhibitors: comparison of crystallographically determined enzyme binding with enzyme affinity in a series of carboxy-substituted trimethoprim analogs Lee F. Kuyper, Barbara Roth, David P. Baccanari, Robert Ferone, Christopher R. Beddell, John N. Champness, David K. Stammers, John G. Dann, Frank E. A. Norrington, and et al. pp 1120 - 1122; DOI: 10.1021/jm00352a002 |
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Two clonidine-like compounds with substituents at the 2-, 3-, and 6-position of the phenyl ring possessing pronounced hypotensive potencies Pieter B. M. W. M. Timmermans, Adriaan De Jonge, Pieter A. Van Zwieten, Johannes J. J. De Boer, and Nico W. Speckamp pp 1122 - 1123; DOI: 10.1021/jm00352a003 |
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Sparsophenicol: a new synthetic hybrid antibiotic inhibiting ribosomal peptide synthesis Jiri Zemlicka and Aruna Bhuta pp 1123 - 1125; DOI: 10.1021/jm00352a004 |
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Benzeneacetamide amines: structurally novel non-m.mu. opioids Jacob Szmuszkovicz and Philip F. Von Voigtlander pp 1125 - 1126; DOI: 10.1021/jm00352a005 |
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Conformation activity study of 4-phenylpiperidine analgesics Mark Froimowitz pp 1127 - 1133; DOI: 10.1021/jm00352a006 |
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Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems Jiban K. Chakrabarti, Terrence M. Hotten, Sarah E. Morgan, Ian A. Pullar, David M. Rackham, Francesca C. Risius, Susan Wedley, Michael O. Chaney, and Noel D. Jones pp 1133 - 1140; DOI: 10.1021/jm00352a007 |
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Nitrogen bridgehead compounds. Part 18. New antiallergic 4H-pyrido[1,2-a]pyrimidin-4-ones. Part I Istvan Hermecz, Tibor Breining, Zoltan Meszaros, Agnes Horvath, Lelle Vasvari-Debreczy, Franz Dessy, Christine DeVos, and Ludovic Rodriquez pp 1140 - 1145; DOI: 10.1021/jm00352a008 |
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Antiallergy agents. 2. 2-Phenyl-5-(1H-tetrazol-5-yl)pyrimidin-4(3H)-ones Peter F. Juby, Thomas W. Hudyma, Myron Brown, John M. Essery, and Richard A. Partyka pp 1145 - 1150; DOI: 10.1021/jm00352a009 |
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Tricyclics with analgesic and antidepressant activity. 2. [[(Alkylamino)ethyl]thio]dibenzo[b,f]thiepins and 10,11-dihydro derivatives Helen H. Ong, James A. Profitt, V. B. Anderson, Theodore C. Spaulding, Jeffrey C. Wilker, and Harry M. Geyer pp 1150 - 1153; DOI: 10.1021/jm00352a010 |
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Hypolipidemic 4,5-dihydro-4-oxo-5,5-disubstituted-2-furancarboxylic acids Ivo Jirkovsky and Mitchell N. Cayen pp 1154 - 1156; DOI: 10.1021/jm00352a011 |
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Hydroxy- and amino-substituted piperidinecarboxylic acids as .gamma.-aminobutyric acid agonists and uptake inhibitors Poul Jacobsen, Ibrahim M. Labouta, Kjeld Schaumburg, Erik Falch, and Povl Krogsgaard-Larsen pp 1157 - 1162; DOI: 10.1021/jm00352a012 |
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Behavioral and serotonin receptor properties of 4-substituted derivatives of the hallucinogen 1-(2,5-dimethoxyphenyl)-2-aminopropane Richard A. Glennon, Richard Young, Fredrick Benington, and Richard D. Morin pp 1163 - 1168; DOI: 10.1021/jm00352a013 |
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Potential histamine H2-receptor antagonists. 4. Benzylhistamines John C. Emmett, Graham J. Durant, C. Robin Ganellin, Anthony M. Roe, and John L. Turner pp 1168 - 1174; DOI: 10.1021/jm00352a014 |
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Alkylation of the prosthetic heme in cytochrome P-450 during oxidative metabolism of the sedative-hypnotic ethchlorvynol Paul R. Ortiz de Montellano, Hal S. Beilan, and James M. Mathews pp 1174 - 1179; DOI: 10.1021/jm00352a015 |
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Species- or isozyme-selective enzyme inhibitors. 8. Synthesis of disubstituted two-substrate condensation products as inhibitors of rat adenylate kinases Francis Kappler, Ton T. Hai, Masanobu Abo, and Alexander Hampton pp 1179 - 1184; DOI: 10.1021/jm00352a016 |
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Species- or isozyme-specific enzyme inhibitors. 9. Selective effects in inhibitions of rat pyruvate kinase isozymes by adenosine 5'-diphosphate derivatives Ton T. Hai, Masanobu Abo, and Alexander Hampton pp 1184 - 1188; DOI: 10.1021/jm00352a017 |
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Synthesis and evaluation of N-(phenylalkyl)acetohydroxamic acids as potential substrates for N-arylhydroxamic acid N,O-acyltransferase Adnan A. Elfarra, Heui Mei Yeh, and Patrick E. Hanna pp 1189 - 1192; DOI: 10.1021/jm00352a018 |
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Pentasubstituted quercetin analogs as selective inhibitors of particulate 3',5'-cyclic-AMP phosphodiesterase from rat brain Madeleine Picq, Annie F. Prigent, Georges Nemoz, Annie C. Andre, and Henri Pacheco pp 1192 - 1198; DOI: 10.1021/jm00352a019 |
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Importance of the aromatic ring in adrenergic amines. 7. Comparison of the stereoselectivity of norepinephrine N-methyltransferase for aromatics. Nonaromatic substrates and inhibitors Michael F. Rafferty, David S. Wilson, James A. Monn, Polina Krass, Ronald T. Borchardt, and Gary L. Grunewald pp 1198 - 1204; DOI: 10.1021/jm00352a020 |
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Directional probes of the hydrophobic component of the aromatic ring binding site of norepinephrine N-methyltransferase Michael F. Rafferty, Ronald T. Borchardt, and Gary L. Grunewald pp 1204 - 1208; DOI: 10.1021/jm00352a021 |
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Tritiated peptides. 12. Synthesis and biological activity of [4-3H-Phe8]substance P Mark C. Allen, Derek E. Brundish, Roy Wade, Bengt E. B. Sandberg, Michael R. Hanley, and Leslie L. Iversen pp 1209 - 1213; DOI: 10.1021/jm00352a022 |
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Carbon-7 substituted actinomycin D analogs as improved antitumor agents: synthesis and DNA-binding and biological properties Sisir K. Sengupta, Jerome E. Anderson, and Christine Kelley pp 1214 - 1219; DOI: 10.1021/jm00352a023 |
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Studies on the synthesis of chemotherapeutics. 12. Synthesis and antitumor activity of N-phthalidyl-5-fluorouracil derivatives Tetsuji Kametani, Kazuo Kigasawa, Mineharu Hiiragi, Kikuo Wakisaka, Kikuo Nakazato, Keiko Ichikawa, Kazunaga Fukawa, Osamu Irino, Naoyuki Nishimura, and Taiji Okada pp 1219 - 1222; DOI: 10.1021/jm00352a024 |
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Cardenolide analogs. 14. Synthesis and biological activity of glucosides of 17.beta.-modified derivatives of digitoxigenin Phillipa Smith, Lindsay Brown, John Boutagy, and Richard Thomas pp 1222 - 1226; DOI: 10.1021/jm00352a025 |
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Synthesis and antitumor activity of 10-alkyl-10-deazaminopterins. A convenient synthesis of 10-deazaminopterin J. I. DeGraw, V. H. Brown, H. Tagawa, R. L. Kisliuk, Y. Gaumont, and F. M. Sirotnak pp 1227 - 1230; DOI: 10.1021/jm00352a026 |
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Potential antitumor agents. 37. Organophosphorus derivatives of 9-anilinoacridine Gordon W. Rewcastle, Bruce C. Baguley, and Bruce F. Cain pp 1231 - 1235; DOI: 10.1021/jm00352a027 |
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Imidodisulfamides. 2. Substituted 1,2,3,4-tetrahydroisoquinolinylsulfonic imides as antagonists of slow-reacting substance of anaphylaxis Fadia El-Fehail Ali, John G. Gleason, David T. Hill, Robert D. Krell, Carolyn H. Kruse, Patricia G. Lavanchy, and Beth W. Volpe pp 1235 - 1240; DOI: 10.1021/jm00352a028 |
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Synthesis and spasmolytic activities of 2-(1,2-benzisoxazol-3-yl)-3{[.omega.-(dialkylamino)alkoxy]phenyl}acrylonitriles Shunsuke Naruto, Hiroyuki Mizuta, Tadahiro Sawayama, Toyokichi Yoshida, Hitoshi Uno, Katsuyoshi Kawashima, Yukinobu Sohji, Toshiaki Kadokawa, and Haruki Nishimura pp 1240 - 1245; DOI: 10.1021/jm00352a029 |
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A consideration for structure-taste correlations of perillartines using pattern-recognition techniques Yoshimasa Takahashi, Yoshikatsu Miyashita, Yuichiro Tanaka, Hidetsugu Abe, and Shinichi Sasaki pp 1245 - 1248; DOI: 10.1021/jm00352a030 |
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Probes of the active site of norepinephrine N-methyltransferase: effect of hydrophobic and hydrophilic interactions on side-chain binding of amphetamine and .alpha.-methylbenzylamine Gary L. Grunewald, James Monn, Michael F. Rafferty, Ronald T. Borchardt, and Polina Krass pp 1248 - 1250; DOI: 10.1021/jm00352a031 |
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Importance of the aromatic ring in adrenergic amines. 8. 2-(Aminomethyl)-trans-2-decalols as inhibitors of norepinephrine N-methyltransferase Michael F. Rafferty, Polina Krass, Ronald T. Borchardt, and Gary L. Grunewald pp 1250 - 1252; DOI: 10.1021/jm00352a032 |
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Mechanism of action of 5-nitro-2'-deoxyuridine Wendy L. Washtien and Daniel V. Santi pp 1252 - 1255; DOI: 10.1021/jm00352a033 |
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Synthesis and biological evaluation of 6-ethynyluracil, a thiol-specific alkylating pyrimidine Alan C. Schroeder, Alexander Bloch, Jack L. Perman, and Miroslav Bobek pp 1255 - 1258; DOI: 10.1021/jm00352a034 |
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Synthesis of 4-amino-1-.beta.-D-ribofuranosyl-1H-pyrrolo[2,3-b]pyridine (1-deazatubercidin) as a potential antitumor agent Ippolito Antonini, Francesco Claudi, Gloria Cristalli, Palmarisa Franchetti, Mario Grifantini, and Sante Martelli pp 1258 - 1261; DOI: 10.1021/jm00352a035 |
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2-Acetylpyridine thiosemicarbazones. 4. Complexes with transition metals as antimalarial and antileukemic agents John P. Scovill, Daniel L. Klayman, and Charles F. Franchino pp 1261 - 1264; DOI: 10.1021/jm00352a036 |
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Synthesis and pharmacology of metabolically stable tert-butyl ethers of morphine and levorphanol Erno Mohacsi, Willy Leimgruber, and Herman Baruth pp 1264 - 1266; DOI: 10.1021/jm00352a037 |
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Book Reviews pp 1266 - 1268; DOI: 10.1021/jm00352a600 |
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Retinoids at the threshold: their biological significance and therapeutic potential Beverly A. Pawson, Carl W. Ehmann, Loretta M. Itri, and Michael I. Sherman pp 1269 - 1277; DOI: 10.1021/jm00353a001 |
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N-methylnalorphine: definition of N-allyl conformation for antagonism at the opiate receptor Ryszard J. Kobylecki, Anthony C. Lane, Colin F. C. Smith, Laurence P. G. Wakelin, William B. T. Cruse, Ernst Egert, and Olga Kennard pp 1278 - 1280; DOI: 10.1021/jm00353a002 |
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Potential neuroleptic agents. 2,6-Dialkoxybenzamide derivatives with potent dopamine receptor blocking activities Lennart Florvall and Sven Ove Oegren pp 1280 - 1286; DOI: 10.1021/jm00353a003 |
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.beta.-Adrenergic blocking agents. 22. 1-Phenoxy-3-[[(substituted-amido)alkyl]amino]-2-propanols M. S. Large and L. H. Smith pp 1286 - 1292; DOI: 10.1021/jm00353a004 |
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Derivatives of the potent angiotensin converting enzyme inhibitor 5(S)-benzamido-4-oxo-6-phenylhexanoyl-L-proline: effect of changes at postions 2 and 5 of the hexanoic acid portion Ronald G. Almquist, Jac Crase, Clive Jennings-White, Robert F. Meyer, Milton L. Hoefle, Ronald D. Smith, Arnold D. Essenburg, and Harvey R. Kaplan pp 1292 - 1299; DOI: 10.1021/jm00353a005 |
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Nonsteroidal estrogens: synthesis and estrogen receptor binding affinity of derivatives of (3R*,4S*)-3,4-bis(4-hydroxyphenyl)hexane (hexestrol) and (2R*,3S*)-2,3-bis(4-hydroxyphenyl)pentane (norhexestrol) functionalized on the side chain Scott W. Landvatter and J. A. Katzenellenbogen pp 1300 - 1307; DOI: 10.1021/jm00353a006 |
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(2R*,3S*)-1-[125I]Iodo-2,3-bis(4-hydroxyphenyl)pentane ([125I]iodonorhexestrol), and (2R*,3S*)-1-[77Br]bromo-2,3-bis(4-hydroxyphenyl)pentane ([77Br]bromonorhexestrol), two .gamma.-emitting estrogens that show receptor-mediated uptake by target tissues in vivo Scott W. Landvatter, John A. Katzenellenbogen, Karen D. McElvany, and Michael J. Welch pp 1307 - 1312; DOI: 10.1021/jm00353a007 |
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Synthesis and biological activities of substance P antagonists S. Caranikas, J. Mizrahi, E. Escher, and D. Regoli pp 1313 - 1316; DOI: 10.1021/jm00353a008 |
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Structure-activity studies on the C-terminal amide of substance P Emanuel Escher, Rejean Couture, Constantinos Poulos, Nikos Pinas, Jacques Mizrahi, Dimitrios Theodoropoulos, and Domenico Regoli pp 1317 - 1321; DOI: 10.1021/jm00353a009 |
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Phospholipid-nucleoside conjugates. 3. Syntheses and preliminary biological evaluation of 1-.beta.-D-arabinofuranosylcytosine 5'-monophosphate-L-1,2-dipalmitin and selected 1-.beta.-D-arabinofuranosylcytosine 5'-diphosphate-L-1,2-diacylglycerols Eung K. Ryu, Robert J. Ross, Tatsuo Matsushita, Malcolm MacCoss, Chung I. Hong, and Charles R. West pp 1322 - 1329; DOI: 10.1021/jm00353a010 |
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Synthesis and antiviral properties of some 2'-deoxy-5-(fluoroalkenyl)uridines Paul L. Coe, Michael R. Harnden, A. Stanley Jones, Stewart A. Noble, and Richard T. Walker pp 1329 - 1334; DOI: 10.1021/jm00353a011 |
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Synthesis and antiviral activity of certain carbamoylpyrrolopyrimidine and pyrazolopyrimidine nucleosides Richard J. Goebel, Alexander D. Adams, Patricia A. McKernan, Byron K. Murray, Roland K. Robins, Ganapathi R. Revankar, and Peter G. Canonico pp 1334 - 1338; DOI: 10.1021/jm00353a012 |
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Potential radiosensitizing agent. 4. 2-Nitroimidazole nucleosides Masakazu Sakaguchi, Matthew W. Webb, and Krishna C. Agrawal pp 1339 - 1342; DOI: 10.1021/jm00353a013 |
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Potential radiosensitizing agents. 5. 2-Substituted benzimidazole derivatives Rajender P. Gupta, Cynthia A. Larroquette, and Krishna C. Agrawal pp 1342 - 1346; DOI: 10.1021/jm00353a014 |
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Phosphorus-31 NMR kinetic studies of the intra- and intermolecular alkylation chemistry of phosphoramide mustard and cognate N-phosphorylated derivatives of N,N-bis(2-chloroethyl)amine Thomas W. Engle, Gerald Zon, and William Egan pp 1347 - 1357; DOI: 10.1021/jm00353a015 |
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Spasmolytic agents. 2. 1,2,3,4-Tetrahydro-2-naphthylamine derivatives Munefumi Kanao, Takeshi Hashizume, Yoshifumi Ichikawa, Kiyoshi Irie, and Sumiro Isoda pp 1358 - 1363; DOI: 10.1021/jm00353a016 |
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Synthesis and comparison of some cardiovascular properties of the stereoisomers of labetalol Elijah H. Gold, Wei Chang, Marvin Cohen, Thomas Baum, Stewart Ehrreich, Gordon Johnson, Nicholas Prioli, and Edmund J. Sybertz pp 1363 - 1370; DOI: 10.1021/jm00353a017 |
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Structure-activity relationships of some technetium-99m labeled [(thioethyl)amino] carboxylates E. Chiotellis, C. I. Stassinopoulou, A. Varvarigou, and H. Vavouraki pp 1370 - 1374; DOI: 10.1021/jm00353a018 |
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Effect of N,N'-diethyl-1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamines on the DMBA-induced mammary carcinoma of the rat Erwin Von Angerer pp 1374 - 1377; DOI: 10.1021/jm00353a019 |
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Synthesis and biological activity of benzothiazolo- and benzoxazolo[3,2-a]quinolinium salts Osvaldo Cox, Henry Jackson, Vanessa A. Vargas, Adriana Baez, Julio I. Colon, Blanca C. Gonzalez, and Marino De Leon pp 1378 - 1381; DOI: 10.1021/jm00353a020 |
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Structure-activity relationships for hallucinogenic N,N-dialkyltryptamines: photoelectron spectra and serotonin receptor affinities of methylthio and methylenedioxy derivatives Toni B. Kline, Frederick Benington, Richard D. Morin, John M. Beaton, Richard A. Glennon, L. N. Domelsmith, K. N. Houk, and Melvin D. Rozeboom pp 1381 - 1383; DOI: 10.1021/jm00353a021 |
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Book Reviews pp 1384 - 1388; DOI: 10.1021/jm00353a600 |
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.alpha.2 Adrenoceptors: classification, localization, mechanisms and targets for drugs Pieter B. M. W. M. Timmermans and Pieter A. Van Zwieten pp 1389 - 1401; DOI: 10.1021/jm00354a001 |
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Ultra-short-acting .beta.-adrenergic receptor blocking agents. 1. (Aryloxy)propanolamines containing esters in the nitrogen substituent Paul W. Erhardt, Chi M. Woo, Richard J. Gorczynski, and William G. Anderson pp 1402 - 1407; DOI: 10.1021/jm00354a002 |
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Ultra-short-acting .beta.-adrenergic receptor blocking agents. 2. (Aryloxy)propanolamines containing esters on the aryl function Paul W. Erhardt, Chi M. Woo, William G. Anderson, and Richard J. Gorczynski pp 1408 - 1412; DOI: 10.1021/jm00354a003 |
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Correlation between affinity toward adrenergic receptors and approximate electrostatic potentials of phenylethylamine derivatives. 1. Effects of the side chain Tomaz Solmajer, Istvan Lukovits, and Dusan Hadzi pp 1413 - 1417; DOI: 10.1021/jm00354a004 |
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.beta.-Adrenergic blocking agents. 24. Heterocyclic substituted 1-(aryloxy)-3-[[(amido)alkyl]amino]propan-2-ols M. S. Large and L. H. Smith pp 1417 - 1422; DOI: 10.1021/jm00354a005 |
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Synthesis and biological evaluation of a metazocine-containing enkephalinamide. Evidence for nonidentical roles of the tyramine moiety in opiates and opioid peptides K. Ramakrishnan and P. S. Portoghese pp 1423 - 1427; DOI: 10.1021/jm00354a006 |
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A QSAR study of the inhibitory action of a series of enkephalin-like peptides in the guinea pig ileum and mouse vas deferens bioassays Jean Luc Fauchere pp 1428 - 1431; DOI: 10.1021/jm00354a007 |
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Synthesis and pharmacological characterization in vitro of cyclic enkephalin analogs: effect of conformational constraints on opiate receptor selectivity John DiMaio, Thi M. D. Nguyen, Carole Lemieux, and Peter W. Schiller pp 1432 - 1438; DOI: 10.1021/jm00354a008 |
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Conformational requirements for norepinephrine uptake inhibition by phenethylamines in brain synaptosomes. Effects of .alpha.-alkyl substitution Adrie P. De Jong, Stephen W. Fesik, and Alexandros Makriyannis pp 1438 - 1441; DOI: 10.1021/jm00354a009 |
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Conformationally restricted congeners of dopamine derived from 2-aminoindan Joseph G. Cannon, Julio A. Perez, Ranbir K. Bhatnagar, John Paul Long, and Fouad M. Sharabi pp 1442 - 1446; DOI: 10.1021/jm00354a010 |
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3'-Hydroxy- and (.+-.)-3',11-dihydroxy-.DELTA.9-tetrahydrocannabinol: (THC) biologically active metabolites of .DELTA.9-tetrahydrocannabinol G. R. Handrick, R. P. Duffley, G. Lambert, J. G. Murphy, H. C. Dalzell, J. F. Howes, R. K. Razdan, B. R. Martin, L. S. Harris, and W. L. Dewey pp 1447 - 1450; DOI: 10.1021/jm00354a011 |
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Spiro oxazolidinedione aldose reductase inhibitors Rodney C. Schnur, Reinhard Sarges, and Michael J. Peterson pp 1451 - 1454; DOI: 10.1021/jm00354a012 |
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Methotrexate analogs. 16. Importance of the side-chain amide carbonyl group as a structural determinant of biological activity A. Rosowsky and R. Forsch pp 1454 - 1459; DOI: 10.1021/jm00354a013 |
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2-Amino-6-chloro-4-(N-methylpiperazino)pyrimidines, inhibitors of spiroperidol binding Claude Gueremy, Francois Audiau, Andre Uzan, Gerard Le Fur, Jean Michel Leger, and Alain Carpy pp 1459 - 1465; DOI: 10.1021/jm00354a014 |
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Amino acid amide derivatives of 2-[3-(aminomethyl)-4H-1,2,4-triazol-4-yl]benzophenones, a novel class of annulated peptidoaminobenzophenones Kentaro Hirai, Toshio Fujishita, Teruyuki Ishiba, Hirohiko Sugimoto, Shigeru Matsutani, Yuji Tsukinoki, and Katsumi Hirose pp 1466 - 1473; DOI: 10.1021/jm00354a015 |
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Synthesis and pharmacological activity of 6-aryl-2-azabicyclo[4.2.1]nonanes Paul H. Mazzocchiu and Chong Ho Kim pp 1473 - 1476; DOI: 10.1021/jm00354a016 |
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4-Aroyl-1,3-dihydro-2H-imidazol-2-ones, a new class of cardiotonic agents Richard A. Schnettler, Richard C. Dage, and J. Martin Grisar pp 1477 - 1481; DOI: 10.1021/jm00354a017 |
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Synthesis and antiinflammatory activity of hexahydrothiopyrano[4,3-c]pyrazoles and related analogs George C. Rovnyak, Robert C. Millonig, Joseph Schwartz, and Virginia Shu pp 1482 - 1488; DOI: 10.1021/jm00354a018 |
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Selenium labeling in nuclear medicine. 2. D ring substituted estrogens Samy A. Sadek, Wayne V. Kessler, Stanley M. Shaw, John N. Anderson, and Gordon C. Wolf pp 1488 - 1492; DOI: 10.1021/jm00354a019 |
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Synthesis and topical antiinflammatory activity of some steroidal [16.alpha.,17.alpha.-d]-isoxazolidines Michael J. Green, Robert L. Tiberi, Richard Friary, Barry N. Lutsky, Joseph Berkenkoph, Xiomara Fernandez, and Margaret Monahan pp 1492 - 1495; DOI: 10.1021/jm00354a020 |
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A specific inhibitor of IgE-antibody formation: n-pentyl .beta.-D-fructopyranoside Yasushi Haraguchi, Akira Yagi, Akihide Koda, Naoki Inagaki, Kanji Noda, and Itsuo Nishioka pp 1495 - 1499; DOI: 10.1021/jm00354a021 |
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Potential tumor- or organ-imaging agents. 23. Sterol esters of iopanoic acid R. H. Seevers, M. P. Groziak, J. P. Weichert, S. W. Schwendner, S. M. Szabo, M. A. Longino, and R. E. Counsell pp 1500 - 1503; DOI: 10.1021/jm00354a022 |
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Preliminary studies of mesoionic 3-(substituted-aryl)-.psi.-oxatriazoles as potential antihypertensive agents Mary Q. Lund, Lemont B. Kier, Richard A. Glennon, and John L. Egle pp 1503 - 1505; DOI: 10.1021/jm00354a023 |
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Ammonium 7H-purin-6-yl 1-thio-.beta.-D-glucopyranosiduronate, a latent, selective anticancer agent Angela Parker and Leo Fedor pp 1505 - 1507; DOI: 10.1021/jm00354a024 |
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Crystal structure and anti-herpes simplex virus activity of 2,2'-anhydro-1-.beta.-D-arabinofuranosylthymine David H. Harrison, Raymond F. Schinazi, and Byron H. Rubin pp 1507 - 1510; DOI: 10.1021/jm00354a025 |
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Additions and Corrections- 1-Aryl-3-azabicyclo-[3.1.0]hexanes, a New Series of Nonnarcotic Analgesic Agents Joseph W. Epstein, Herbert J. Brabander, William J. Fanshawe, Corris M. Hofmann, Thomas C. McKenzie, Sidney R. Safir, Arnold C. Osterberg, D.B. Cosulich, and F.M. Lovell pp 1510 - 1510; DOI: 10.1021/jm00354a600 |
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Additions and Corrections-Synthesis and Evalutaion of Some Stable Multisubstrate Adducts as Inhibitors of Cathechol O-Methyltransferase Gary L. Anderson, Donald L. Bussolotti, and James K. Coward pp 1510 - 1511; DOI: 10.1021/jm00354a601 |
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Additions and Corrections - Synthesis and Evaluation of Some Stable Multisubstrate Adducts as Specific Inhibitors of Spermidine Synthase. Kuo-Chang Tang, Roy Mariuzza, and James K. Coward pp 1511 - 1511; DOI: 10.1021/jm00354a602 |
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Additions and Corrections - Quantitative Structure-Inhibitory Activity Relationships of Phenols and Fatty Acids for Bacilus subtillis Spore Germination. Yoko Yasuda, Kunio Tochikubo, Yoetsu Hachisuka, Hisao Tomida, and Ken Ikeda pp 1511 - 1511; DOI: 10.1021/jm00354a603 |
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Additions and Corrections - Amino Acids, Peptides, and Proteins. Volume 11. Specialist Periodical Reports. pp 1511 - 1511; DOI: 10.1021/jm00354a604 |
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Book Reviews pp 1511 - 1518; DOI: 10.1021/jm00354a605 |