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Stereoselective syntheses of the trans-decahydroquinoline-5-carboxylic acid epimers. Diastereomeric zwitterionic probes of .gamma.-aminobutyric acid-related biological properties in vitro and in vivo Donald T. Witiak, Raymond J. Patch, S. J. Enna, and Yiu K. Fung pp 1 - 8; DOI: 10.1021/jm00151a001 |
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Neuroleptic activity of chiral trans-hexahydro-.gamma.-carbolines Reinhard Sarges, Harry R. Howard, Kathy M. Donahue, Williard M. Welch, Beryl W. Dominy, Albert Weissman, B. Kenneth Koe, and Jon Bordner pp 8 - 19; DOI: 10.1021/jm00151a002 |
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Synthesis and antihypertensive activity of a series of 4-amino-6,7-dimethoxyquinazoline derivatives Philippe M. Manoury, Jean L. Binet, Andre P. Dumas, Francoise Lefevre-Borg, and Icilio Cavero pp 19 - 25; DOI: 10.1021/jm00151a003 |
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5-(Alkylsulfonyl)salicylanilides as potential dental antiplaque agents Michael T. Clark, Robert A. Coburn, Richard T. Evans, and Robert J. Genco pp 25 - 29; DOI: 10.1021/jm00151a004 |
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Synthesis and structure-activity relationships of antibacterial phosphonopeptides incorporating (1-aminoethyl)phosphonic acid and (aminomethyl)phosphonic acid Frank R. Atherton, Cedric H. Hassall, and Robert W. Lambert pp 29 - 40; DOI: 10.1021/jm00151a005 |
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Quantitative structure-activity relationship of the mutagenicity of substituted N-nitroso-N-benzylmethylamines: possible implications for carcinogenicity George M. Singer, A. W. Andrews, and Shu Mei Guo pp 40 - 44; DOI: 10.1021/jm00151a006 |
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Dipole moment in relation to hydrogen receptor histamine antagonist activity for cimetidine analogs Rodney C. Young, Graham J. Durant, John C. Emmett, C. Robin Ganellin, Michael J. Graham, Robert C. Mitchell, H. Douglas Prain, and Michael L. Roantree pp 44 - 49; DOI: 10.1021/jm00151a007 |
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Cycloheximide analogs as potential anticonvulsants David M. Piatak, Puifun Louisa Tang, and Cheng Chuan Yen pp 50 - 54; DOI: 10.1021/jm00151a008 |
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Correspondence analysis applied to steroid receptor binding Jean Christophe Dore, Jacques Gilbert, Tiiu Ojasoo, and Jean Pierre Raynaud pp 54 - 60; DOI: 10.1021/jm00151a009 |
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Potential neuroleptic agents. 4. Chemistry, behavioral pharmacology, and inhibition of [3H]spiperone binding of 3,5-disubstituted N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxysalicylamides Tomas De Paulis, Yatendra Kumar, Lars Johansson, Sten Raemsby, Haakan Hall, Maria Saellemark, Kristina Aengeby-Moeller, and Sven Ove Oegren pp 61 - 69; DOI: 10.1021/jm00151a010 |
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Potential antitumor agents. 45. Synthesis, DNA-binding interaction, and biological activity of triacridine derivatives Graham J. Atwell, Bruce C. Baguley, Dorota Wilmanska, and William A. Denny pp 69 - 74; DOI: 10.1021/jm00151a011 |
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2-Phenylindenes. Development of a new mammary tumor-inhibiting antiestrogen by combination of estrogenic side effect-lowering structural elements Martin R. Schneider and Hartwig Ball pp 75 - 79; DOI: 10.1021/jm00151a012 |
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Synthesis and antiviral activity of the carbocyclic analogs of 5-ethyl-2'-deoxyuridine and of 5-ethynyl-2'-deoxyuridine Y. Fulmer Shealy, C. Allen O'Dell, Gussie Arnett, and William M. Shannon pp 79 - 84; DOI: 10.1021/jm00151a013 |
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(o- and p-Nitrobenzyloxycarbonyl)-5-fluorouracil derivatives as potential conjugated bioreductive alkylating agents Tai Shun Lin, Lin Wang, Ippolito Antonini, Lucille A. Cosby, David A. Shiba, D. Lynn Kirkpatrick, and Alan C. Sartorelli pp 84 - 89; DOI: 10.1021/jm00151a014 |
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Peptides of 2-aminopimelic acid: antibacterial agents that inhibit diaminopimelic acid biosynthesis David A. Berges, Walter E. DeWolf, George L. Dunn, Sarah F. Grappel, David J. Newman, John J. Taggart, and Charles Gilvarg pp 89 - 95; DOI: 10.1021/jm00151a015 |
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Arginine-vasopressin analogs with high antidiuretic/vasopressor selectivity. Synthesis, biological activity and receptor binding affinity of arginine-vasopressin analogs with substitutions in positions 1, 2, 4, 7, and 8 Zbigniew Grzonka, Franciszek Kasprzykowski, Elzbieta Kojro, Krzysztof Darlak, Per Melin, Falk Fahrenholz, Peter Crause, and Rainer Boer pp 96 - 99; DOI: 10.1021/jm00151a016 |
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[p-(Thienylcarboxamido)phenoxy]propanolamine derivatives as diuretic and .beta.-adrenergic receptor blocking agents Etienne Bouley, Jean Marie Teulon, Michele Cazes, Alix Cloarec, and Romano Deghenghi pp 100 - 103; DOI: 10.1021/jm00151a017 |
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Carboxyl-modified amino acids and peptides as protease inhibitors Stewart A. Thompson, Peter R. Andrews, and Robert P. Hanzlik pp 104 - 111; DOI: 10.1021/jm00151a018 |
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Synthesis and structure-activity relationships of naftifine-related allylamine antimycotics Anton Stuetz, Apostolos Georgopoulos, Waltraud Granitzer, Gabor Petranyi, and Daniel Berney pp 112 - 125; DOI: 10.1021/jm00151a019 |
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Synthesis of alkyl-substituted arecoline derivatives as .gamma.-aminobutyric acid uptake inhibitors Christian Mueller-Uri, Ernst A. Singer, and Wilhelm Fleischhacker pp 125 - 132; DOI: 10.1021/jm00151a020 |
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7-(Trifluoromethyl)-4-aminoquinoline hypotensives: novel peripheral sympatholytics John M. McCall, R. E. TenBrink, Bharat V. Kamdar, Louis L. Skaletzky, Salvatore C. Perricone, Richard C. Piper, and Patrick J. Delehanty pp 133 - 137; DOI: 10.1021/jm00151a021 |
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Imidazo[4,5-c]pyridines (3-deazapurines) and their nucleosides as immunosuppressive and antiinflammatory agents Thomas A. Krenitsky, Janet L. Rideout, Esther Y. Chao, George W. Koszalka, Fred Gurney, Ronald C. Crouch, Naomi K. Cohn, Gerald Wolberg, and Ralph Vinegar pp 138 - 143; DOI: 10.1021/jm00151a022 |
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Metal complexes of mitomycins Bhashyam S. Iyengar, Takeo Takahashi, William A. Remers, and William T. Bradner pp 144 - 147; DOI: 10.1021/jm00151a023 |
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(.beta.-Chloro-.alpha.-aminoethyl)phosphonic acids as inhibitors of alanine racemase and D-alanine-D-alanine ligase Vo Quang Yen, Denis Carniato, Liliane Vo Quang, Anne Marie Lacoste, Eugene Neuzil, and Francois Le Goffic pp 148 - 151; DOI: 10.1021/jm00151a024 |
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Nucleosides. 136. Synthesis and antiviral effects of several 1-(2-deoxy-2-fluoro-.beta.-D-arabinofuranosyl)-5-alkyluracils. Some structure-activity relationships Tsann Long Su, Kyoichi A. Watanabe, Raymond F. Schinazi, and Jack J. Fox pp 151 - 154; DOI: 10.1021/jm00151a025 |
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Crystal structure of quinespar, a quinazoline analog of methotrexate Donald Mastropaolo, H. Warren Smith, Arthur Camerman, and Norman Camerman pp 155 - 158; DOI: 10.1021/jm00151a026 |
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3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 2. Structural modification of 7-(substituted aryl)-3,5-dihydroxy-6-heptenoic acids and their lactone derivatives William F. Hoffman, A. W. Alberts, E. J. Cragoe Jr., A. A. Deana, B. E. Evans, J. L. Gilfillan, N. P. Gould, J. W. Huff, F. C. Novello, and et al. pp 159 - 169; DOI: 10.1021/jm00152a001 |
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3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 3. 7-(3,5-Disubstituted-[1,1'-biphenyl]-2-yl)-3,5-dihydroxy-6-heptenoic acids and their lactone derivatives G. E. Stokker, A. W. Alberts, P. S. Anderson, E. J. Cragoe Jr., A. A. Deana, J. L. Gilfillan, J. Hirshfield, W. J. Holtz, W. F. Hoffman, and et al. pp 170 - 181; DOI: 10.1021/jm00152a002 |
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Synthesis and investigation of the .alpha.-adrenoceptor agonist and platelet antiaggregatory properties of 1,7,8-trisubstituted 2,3,4,5-tetrahydro-1H-2-benzazepine analogs of trimetoquinol Michael T. Clark, Jane Chang, Stephen S. Navran, Huzoor Akbar, Asoke Mukhopadhyay, Hebatalla Amin, Dennis R. Feller, and Duane D. Miller pp 181 - 185; DOI: 10.1021/jm00152a003 |
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Troponoids. 7. Chemistry and dopamine agaonist activity of ciladopa and related aralkyltroponylpiperazines Jehan Bagli, T. Bogri, Katherine Voith, and D. Lee pp 186 - 193; DOI: 10.1021/jm00152a004 |
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5-HT1 and 5-HT2 binding characteristics of 1-(2,5-dimethoxy-4-bromophenyl)-2-aminopropane analogs Richard A. Glennon, J. D. McKenney, Robert A. Lyon, and Milt Titeler pp 194 - 199; DOI: 10.1021/jm00152a005 |
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Synthesis, structure, and antitumor activity of N-salicyloyl-N'-(2-furylthiocarbonyl)hydrazine and its copper(II) complex Seema Agrawal, Nand K. Singh, Ram C. Aggarwal, Ajit Sodhi, and Priti Tandon pp 199 - 202; DOI: 10.1021/jm00152a006 |
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Systematic synthesis and biological evaluation of .alpha.- and .beta.-D-xylofuranosyl nucleosides of the five naturally occurring bases in nucleic acids and related analogs Gilles Gosselin, Marie Christine Bergogne, Jean De Rudder, Erik De Clercq, and Jean Louis Imbach pp 203 - 213; DOI: 10.1021/jm00152a007 |
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Synthesis and antiviral activity of (E)-5-(2-bromovinyl)uracil and (E)-5-(2-bromovinyl)uridine Erik De Clercq, Claude Desgranges, Piet Herdewijn, Iain S. Sim, A. Stanley Jones, Michael J. McLean, and Richard T. Walker pp 213 - 217; DOI: 10.1021/jm00152a008 |
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Correlation of the in vitro cytotoxic and in vivo antitumor activities of gold(I) coordination complexes Christopher K. Mirabell, Randall K. Johnson, David T. Hill, Leo F. Faucette, Gerald R. Girard, George Y. Kuo, Chiu Mei Sung, and Stanley T. Crooke pp 218 - 223; DOI: 10.1021/jm00152a009 |
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Glycine antagonists. Synthesis, structure, and biological effects of some bicyclic 5-isoxazolol zwitterions Lotte Brehm, Povl Krogsgaard-Larsen, Kjeld Schaumburg, Joergen S. Johansen, Erik Falch, and David R. Curtis pp 224 - 229; DOI: 10.1021/jm00152a010 |
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Enol lactone inhibitors of serine proteases. The effect of regiochemistry on the inactivation behavior of phenyl-substituted (halomethylene)tetra- and dihydrofuranones and tetrahydropyranones toward .alpha.-chymotrypsin: stable acyl enzyme intermediate Michael J. Sofia and John A. Katzenellenbogen pp 230 - 238; DOI: 10.1021/jm00152a011 |
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Digitoxigenin 3-O-.beta.-D-furanosides Ernest J. Prisbe, Julien P. H. Verheyden, Wayne W. Montgomery, and Arthur M. Strosberg pp 239 - 244; DOI: 10.1021/jm00152a012 |
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Antiarrhythmic activity of 17.beta.-aminoestratrienes. Comparison of 3-ols and 3-acetates with the corresponding 3-(3-amino-2-hydroxypropyl) ethers J. K. Campbell, R. T. Logan, R. J. Marshall, G. McGarry, T. Sleigh, and E. Winslow pp 244 - 250; DOI: 10.1021/jm00152a013 |
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Conformationally restricted inhibitors of angiotensin-converting enzyme. Synthesis and computations Eugene D. Thorsett, Elbert E. Harris, Susan D. Aster, Elwood R. Peterson, James P. Snyder, James P. Springer, Jordan Hirshfield, Edward W. Tristram, Arthur A. Patchett, and et al. pp 251 - 260; DOI: 10.1021/jm00152a014 |
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Cardiotonic agents. 3. Synthesis and biological activity of novel 6-(substituted 1H-imidazol-4(5)-yl)-3(2H)-pyridazinones Ila Sircar, George Bobowski, James A. Bristol, Ronald E. Weishaar, and Dale B. Evans pp 261 - 267; DOI: 10.1021/jm00152a015 |
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Synthesis and biological activity of certain nucleoside and nucleotide derivatives of pyrazofurin Charles R. Petrie, Ganapathi R. Revankar, N. Kent Dalley, Rose D. George, Patricia A. McKernan, Robert L. Hamill, and Roland K. Robins pp 268 - 278; DOI: 10.1021/jm00152a016 |
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Mapping the turkey erythrocyte .beta.-receptor: a distance geometry approach Marcel R. Linschoten, Teake Bultsma, Ad P. Ijzerman, and Hendrik Timmerman pp 278 - 286; DOI: 10.1021/jm00152a017 |
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Saturated analogs of poison ivy allergens. Synthesis of trans,trans- and cis,trans-3-alkyl-1,2-cyclohexanediols and sensitizing properties in allergic contact dermatitis Jean Pierre Lepoittevin and Claude Benezra pp 287 - 291; DOI: 10.1021/jm00152a018 |
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Pyrazolo[4,5-c]quinolines. Synthesis and specific inhibition of benzodiazepine receptor binding Fabrizio Melani, Lucia Cecchi, Giovanna Palazzino, Guido Filacchioni, Claudia Martini, Emanuela Pennacchi, and Antonio Lucacchini pp 291 - 295; DOI: 10.1021/jm00152a019 |
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Ketomethylene pseudopeptide analogs of substance P: synthesis and biological activity Ariel Ewenson, Ralph Laufer, Michael Chorev, Zvi Selinger, and Chaim Gilon pp 295 - 299; DOI: 10.1021/jm00152a020 |
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Resolution of flecainide acetate, N-(2-piperidylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)benzamide acetate, and antiarrhythmic properties of the enantiomers Elden H. Banitt, Jack R. Schmid, and Richard A. Newmark pp 299 - 302; DOI: 10.1021/jm00152a021 |
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Synthesis and evaluation of 2,3-dihydrobenzofuran analogs of the hallucinogen 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane: drug discrimination studies in rats David E. Nichols, Andrew J. Hoffman, Robert A. Oberlender, and Robert M. Riggs pp 302 - 304; DOI: 10.1021/jm00152a022 |
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Crystal structure of the dihydropyridine calcium antagonist felodipine. Dihydropyridine binding prerequisites assessed from crystallographic data Rune Fossheim pp 305 - 307; DOI: 10.1021/jm00152a023 |
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Book Reviews pp 308 - 312; DOI: 10.1021/jm00152a600 |
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Prostaglandin analogs. Part 9. Synthesis of a new chemically and metabolically stable prostacyclin analog with high and long-lasting oral activity W. Skuballa, E. Schillinger, C. S. Stuerzebecher, and H. Vorbrueggen pp 313 - 315; DOI: 10.1021/jm00153a001 |
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Unsaturated heterocyclic amines as potent time-dependent inhibitors of dopamine .beta.-hydroxylase Thomas M. Bargar, Robert J. Broersma, Lawrence C. Creemer, James R. McCarthy, Jean Marie Hornsperger, Michael G. Palfreyman, Joseph Wagner, and Michel J. Jung pp 315 - 317; DOI: 10.1021/jm00153a002 |
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Isozyme-specific enzyme inhibitors. 10. Adenosine 5'-triphosphate derivatives as substrates or inhibitors of methionine adenosyltransferases of rat normal and hepatoma tissues Francis Kappler, Ton T. Hai, and Alexander Hampton pp 318 - 322; DOI: 10.1021/jm00153a003 |
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Influence of alkyl-chain fluorination on the action of mammary tumor inhibiting 2,3-bis(hydroxyphenyl)butanes and 2,3-bis(hydroxyphenyl)but-2-enes Rolf W. Hartmann, Alexander Heindl, Martin R. Schneider, and Helmut Schoenenberger pp 322 - 328; DOI: 10.1021/jm00153a004 |
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Analogs of platelet activating factor. 4. Some modifications of the phosphocholine moiety A. Wissner, R. E. Schaub, P. E. Sum, C. A. Kohler, and B. M. Goldstein pp 328 - 333; DOI: 10.1021/jm00153a005 |
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Synthesis of amino acids and related compounds. 29. Synthesis and hypolipidemic activities of 5-thienyl-4-oxazoleacetic acid derivatives Tamon Moriya, Seiichi Takabe, Sadao Maeda, and Kazuo Matsumoto pp 333 - 341; DOI: 10.1021/jm00153a006 |
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Selective thromboxane synthetase inhibitors. 2. 3-(1H-Imidazol-1-ylmethyl)-2-methyl-1H-indole-1-propanoic acid and analogs. Peter E. Cross, Roger P. Dickinson, M. John Parry, and Michael J. Randall pp 342 - 346; DOI: 10.1021/jm00153a007 |
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Ribose-modified adenosine analogs as adenosine receptor agonists Michael D. Taylor, Walter H. Moos, Harriet W. Hamilton, Deedee S. Szotek, William C. Patt, Edward W. Badger, James A. Bristol, Robert F. Bruns, Thomas G. Heffner, and Thomas E. Mertz pp 346 - 353; DOI: 10.1021/jm00153a008 |
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Thiopurine methyltransferase: structure-activity relationships for benzoic acid inhibitors and thiophenol substrates Matthew M. Ames, Cynthia Dias Selassie, Lee C. Woodson, Jon A. Van Loon, Corwin Hansch, and Richard M. Weinshilboum pp 354 - 358; DOI: 10.1021/jm00153a009 |
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Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents Joseph P. Yevich, James S. New, David W. Smith, Walter G. Lobeck, John D. Catt, Joseph L. Minielli, Michael S. Eison, Duncan P. Taylor, Leslie A. Riblet, and Davis L. Temple pp 359 - 369; DOI: 10.1021/jm00153a010 |
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Synthesis and activity of 6-aryl-3-(hydroxypolymethyleneamino)pyridazines in animal models of epilepsy Andre Hallot, Roger Brodin, Josiane Merlier, Joelle Brochard, Jean Pierre Chambon, and Kathleen Biziere pp 369 - 375; DOI: 10.1021/jm00153a011 |
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Neurochemistry of aging. 1. Toxins for an animal mode of Alzheimer's disease J. S. Mistry, D. J. Abraham, and I. Hanin pp 376 - 380; DOI: 10.1021/jm00153a012 |
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Benzo[a]carbazole derivatives. Synthesis, estrogen receptor binding affinities, and mammary tumor inhibiting activity Erwin Von Angerer and Jelica Prekajac pp 380 - 386; DOI: 10.1021/jm00153a013 |
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Imidazo[2,1-b]benzothiazoles. 2. New immunosuppressive agents Toshiyasu Mase, Hideki Arima, Kenichi Tomioka, Toshimitsu Yamada, and Kiyoshi Murase pp 386 - 394; DOI: 10.1021/jm00153a014 |
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New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay John M. Domagala, Lori Doyle Hanna, Carl L. Heifetz, Marland P. Hutt, Thomas F. Mich, Joseph P. Sanchez, and Marjorie Solomon pp 394 - 404; DOI: 10.1021/jm00153a015 |
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N-Imidazolyl-4-chromanones, N-imidazolyl-1-tetralones, and their alcohols as hypolipemic agents raising high-density lipoproteins Paolo Cozzi, Umberto Branzoli, Pier Paolo Lovisolo, Gaetano Orsini, Germano Carganico, Antonio Pillan, and Augusto Chiari pp 404 - 410; DOI: 10.1021/jm00153a016 |
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Angiotensin converting enzyme inhibitors as antihypertensive agents: 1-[(2-mercaptocycloalkyl)carbonyl]-L-prolines Romeo Ciabatti, Giovanna Padova, Elvio Bellasio, Giorgio Tarzia, Adele Depaoli, Franco Battaglia, Mario Cellentani, Domenico Barone, and Emiliana Baldoli pp 411 - 417; DOI: 10.1021/jm00153a017 |
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Synthesis and antiviral activity of sulfonamidobenzophenone oximes and sulfonamidobenzamides Masaru Ogata, Hiroshi Matsumoto, Sumio Shimizu, Shiro Kida, Toru Wada, Motoo Shiro, and Kosaburo Sato pp 417 - 423; DOI: 10.1021/jm00153a018 |
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Synthesis and toxicity toward nigrostriatal dopamine neurons of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) analogs David S. Fries, Jan De Vries, Bernard Hazelhoff, and Alan S. Horn pp 424 - 427; DOI: 10.1021/jm00153a019 |
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Antipicornavirus activity of substituted phenoxybenzenes and phenoxypyridines Lowell D. Markley, Yulan C. Tong, Jacqueline K. Dulworth, David L. Steward, Christopher T. Goralski, Howard Johnston, Steven G. Wood, Anna P. Vinogradoff, and Thomas M. Bargar pp 427 - 433; DOI: 10.1021/jm00153a020 |
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Book Reviews pp 433 - 436; DOI: 10.1021/jm00153a600 |
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Development and therapeutic role of synthetic prostaglandins in peptic ulcer disease Paul W. Collins pp 437 - 443; DOI: 10.1021/jm00154a001 |
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Interaction of monoamine oxidase B with analogs of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine derived from prodine-type analgesics Arnold Brossi, Wieslaw P. Gessner, Richard R. Fritz, Michael E. Bembenek, and Creed W. Abell pp 444 - 445; DOI: 10.1021/jm00154a002 |
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1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid. New quinolone antibacterial with potent gram-positive activity John M. Domagala, Carl L. Heifetz, Thomas F. Mich, and Jeffrey B. Nichols pp 445 - 448; DOI: 10.1021/jm00154a003 |
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Tranexamic acid derivatives with enhanced absorption Carl M. Svahn, Ferenc Merenyi, and Lennart Karlson pp 448 - 453; DOI: 10.1021/jm00154a004 |
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A common structural model for central nervous system drugs and their receptors Edward J. Lloyd and Peter R. Andrews pp 453 - 462; DOI: 10.1021/jm00154a005 |
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Conformationally defined adrenergic agents. 2. Catechol imidazoline derivatives: biological effects at .alpha.1 and .alpha.2 adrenergic receptors John F. DeBernardis, John J. Kyncl, Fatima Z. Basha, David L. Arendsen, Yvonne C. Martin, Martin Winn, and Daniel J. Kerkman pp 463 - 467; DOI: 10.1021/jm00154a006 |
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Quinazoline antifolates inhibiting thymidylate synthase: benzoyl ring modifications Terence R. Jones, Michael J. Smithers, Michael A. Taylor, Ann L. Jackman, A. Hilary Calvert, Stephen J. Harland, and Kenneth R. Harrap pp 468 - 472; DOI: 10.1021/jm00154a007 |
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Potential antitumor agents. 46. Structure-activity relationships for acridine monosubstituted derivatives of the antitumor agent N-[2-(dimethylamino)ethyl]-9-aminoacridine-4-carboxamide Gordon W. Rewcastle, Graham J. Atwell, David Chambers, Bruce C. Baguley, and William A. Denny pp 472 - 477; DOI: 10.1021/jm00154a008 |
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Kinetics and mechanism of interaction of 10-propargyl-5,8-dideazafolate with thymidylate synthase Alfonso L. Pogolotti, Peter V. Danenberg, and Daniel V. Santi pp 478 - 482; DOI: 10.1021/jm00154a009 |
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Carbocyclic analogs of 5'-amino-5'deoxy- and 3'-amino-3'-deoxythymidines Y. Fulmer Shealy, C. Allen O'Dell, William M. Shannon, and Gussie Arnett pp 483 - 488; DOI: 10.1021/jm00154a010 |
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Synthesis, structure, and antitumor and antiviral activities of a series of 5-halouridine cyclic 3',5'-monophosphates Jozsef Beres, Wesley G. Bentrude, Alajos Kalman, Laszlo Parkanyi, Jan Balzarini, and Erik De Clercq pp 488 - 493; DOI: 10.1021/jm00154a011 |
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Synthesis and antitumor and antiviral properties of 5-alkyl-2'-deoxyuridines 3',5'-cyclic monophosphates, and neutral cyclic triesters Jozsef Beres, Wesley G. Bentrude, Jan Balzarini, Erik De Clercq, and Laszlo Otvos pp 494 - 499; DOI: 10.1021/jm00154a012 |
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Oxidation of 5-hydroxytryptamine and 5,7-dihydroxytryptamine. A new oxidation pathway and formation of a novel neurotoxin Monika Z. Wrona, Daniel Lemordant, L. Lin, C. LeRoy Blank, and Glenn Dryhurst pp 499 - 505; DOI: 10.1021/jm00154a013 |
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On the significance of clusters in the graphical display of structure-activity data James W. McFarland and Daniel J. Gans pp 505 - 514; DOI: 10.1021/jm00154a014 |
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Synthesis and inhibition of human acrosin and trypsin and acute toxicity of aryl 4-guanidinobenzoates J. M. Kaminski, L. Bauer, S. R. Mack, R. A. Anderson, D. P. Waller, and L. J. D. Zaneveld pp 514 - 519; DOI: 10.1021/jm00154a015 |
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Synthesis and biochemical evaluation of analogs of aminoglutethimide based on phenylpyrrolidine-2,5-dione Michael J. Daly, Gareth W. Jones, Paul J. Nicholls, H. John Smith, Martin G. Rowlands, and Michael A. Bunnett pp 520 - 523; DOI: 10.1021/jm00154a016 |
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Thromboxane synthetase inhibitors and antihypertensive agents. 1. N-[(1H-imidazol-1-yl)alkyl]aryl amides and N-[(1H-1,2,4-triazol-1-yl)alkyl]aryl amides William B. Wright, Jeffery B. Press, Peter S. Chan, Joseph W. Marsico, Margie F. Haug, Judy Lucas, Jess Tauber, and Andrew S. Tomcufcik pp 523 - 530; DOI: 10.1021/jm00154a017 |
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N-Substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines Alice Cheng, Edward Uyeno, Willma Polgar, Lawrence Toll, John A. Lawson, Joseph I. DeGraw, Gilda Loew, Arthur Camerman, and Norman Camerman pp 531 - 537; DOI: 10.1021/jm00154a018 |
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Synthesis and quantitative structure-activity relationships of antiallergic 2-hydroxy-N-(1H-tetrazol-5-yl)benzamides and N-(2-hydroxyphenyl)-1H-tetrazole-5-carboxamides Roger E. Ford, Phillip Knowles, Edward Lunt, Stuart M. Marshall, Audrey J. Penrose, Christopher A. Ramsden, Anthony J. H. Summers, Joyce L. Walker, and Derek E. Wright pp 538 - 549; DOI: 10.1021/jm00154a019 |
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Quantitative evaluation of the .beta.2-adrenoceptor intrinsic activity of N-tert-butylphenylethanolamines Adriaan P. Ijzerman, Teake Bultsma, and Hendrik Timmerman pp 549 - 554; DOI: 10.1021/jm00154a020 |
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Relationship between lipophilic character and urinary excretion of nitroimidazoles and nitrothiazoles in rats Giorgio Cantelli Forti, Maria Clelia Guerra, Anna Maria Barbaro, Patrizia Hrelia, Gian Luigi Biagi, and Pier Andrea Borea pp 555 - 561; DOI: 10.1021/jm00154a021 |
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Conformational analysis of clinically active anticonvulsant drugs M. G. Wong, J. A. Defina, and P. R. Andrews pp 562 - 572; DOI: 10.1021/jm00154a022 |
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Geometrical correspondence between phenazocine and the enkephalins Mark Froimowitz and Steven Matthysse pp 573 - 578; DOI: 10.1021/jm00154a023 |
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(1-Amino-2-propenyl)phosphonic acid, an inhibitor of alanine racemase and D-alanine:D-alanine ligase Vo Quang Yen, Denis Carniato, Liliane Vo Quang, Anne Marie Lacoste, Eugene Neuzil, and Francois Le Goffic pp 579 - 581; DOI: 10.1021/jm00154a024 |
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Synthesis and evaluation of 4-(substituted thio)-4-androstene-3,17-dione derivatives as potential aromatase inhibitors Yusuf J. Abul-Hajj pp 582 - 584; DOI: 10.1021/jm00154a025 |
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Substituted isatoic anhydrides: selective inactivators of trypsin-like serine proteases Michael H. Gelb and Robert H. Abeles pp 585 - 589; DOI: 10.1021/jm00154a026 |
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Absolute configuration of (-)-5-benzoyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid, the active enantiomer of ketorolac Angel Gusman, Francisco Yuste, Ruben A. Toscano, and John M. Young pp 589 - 591; DOI: 10.1021/jm00154a027 |
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Book Reviews pp 591 - 594; DOI: 10.1021/jm00154a600 |
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New .alpha.-methylene .gamma.-lactone derivatives of substituted nucleic acid bases as potential anticancer agents Utpal Sanyal, Saktimoyee Mitra, Prasun Pal, and S. K. Chakraborti pp 595 - 599; DOI: 10.1021/jm00155a001 |
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Molecular electrostatic potential of orthopramides: implications for their interaction with the D-2 dopamine receptor Han Van de Waterbeemd, Pierre Alain Carrupt, and Bernard Testa pp 600 - 606; DOI: 10.1021/jm00155a002 |
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Analogs of poison ivy urushiol. Synthesis and biological activity of disubstituted n-alkylbenzenes Mahmoud A. ElSohly, Prakash D. Adawadkar, Daniel A. Benigni, Edna S. Watson, and Thomas L. Little pp 606 - 611; DOI: 10.1021/jm00155a003 |
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Aminoglycoside antibiotics. 6. Chemical reactions of aminoglycosides with disodium carbenicillin Bhashyam S. Iyengar, Virendra Kumar, Timothy P. Wunz, and William A. Remers pp 611 - 614; DOI: 10.1021/jm00155a004 |
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A quantitative structure-activity relationship and molecular graphics analysis of hydrophobic effects in the interactions of inhibitors with alcohol dehydrogenase Corwin Hansch, Teri Klein, Judith McClarin, Robert Langridge, and Neal W. Cornell pp 615 - 620; DOI: 10.1021/jm00155a005 |
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Inhibition of chicken liver dihydrofolate reductase by 5-(substituted benzyl)-2,4-diaminopyrimidines. A QSAR and graphics analysis Cynthia Dias Selassie, Zhao Xia Fang, Ren Li Li, Corwin Hansch, Teri Klein, Robert Langridge, and Bernard T. Kaufman pp 621 - 626; DOI: 10.1021/jm00155a006 |
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Design and synthesis of 2-(arylamino)-4(3H)-quinazolinones as novel inhibitors of rat lens aldose reductase Jack DeRuiter, Abram N. Brubaker, Jane Millen, and Thomas N. Riley pp 627 - 629; DOI: 10.1021/jm00155a007 |
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Synthesis and evaluation of phenyl- and benzoylpiperazines as potential serotonergic agents Robert A. Lyon, Milt Titeler, J. D. McKenney, Philip S. Magee, and Richard A. Glennon pp 630 - 634; DOI: 10.1021/jm00155a008 |
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Bipyridine cardiotonics: the three-dimensional structures of amrinone and milrinone David W. Robertson, E. E. Beedle, John K. Swartzendruber, Noel D. Jones, T. K. Elzey, Raymond F. Kauffman, Harve Wilson, and J. Scott Hayes pp 635 - 640; DOI: 10.1021/jm00155a009 |
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Structurally specific binding of halogenated biphenyls to thyroxine transport protein Urs Rickenbacher, James D. McKinney, Stuart J. Oatley, and Colin C. F. Blake pp 641 - 648; DOI: 10.1021/jm00155a010 |
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Drug design via pharmacophore identification. Dopaminergic activity of 3H-benz[e]indol-8-amines and their mode of interaction with the dopamine receptor Andre A. Asselin, Leslie G. Humber, Katherine Voith, and Geoffrey Metcalf pp 648 - 654; DOI: 10.1021/jm00155a011 |
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Methotrexate analogs. 26. Inhibition of dihydrofolate reductase and folylpolyglutamate synthetase activity and in vitro tumor cell growth by methotrexate and aminopterin analogs containing a basic amino acid side chain Andre Rosowsky, James H. Freisheim, Richard G. Moran, Vishnu C. Solan, Henry Bader, Joel E. Wright, and Mary Radike-Smith pp 655 - 660; DOI: 10.1021/jm00155a012 |
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Synthesis of .DELTA.3-1-methylene-1-carbacephems Piet Herdewijn, Paul J. Claes, and Hubert Vanderhaeghe pp 661 - 664; DOI: 10.1021/jm00155a013 |
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Inhibitors of dihydropteroate synthase: substituent effects in the side-chain aromatic ring of 6-[[3-(aryloxy)propyl]amino]-5-nitrosoisocytosines and synthesis and inhibitory potency of bridged 5-nitrosoisocytosine-p-aminobenzoic acid analogs O. William Lever, Lawrence N. Bell, Clifton Hyman, H. Michael McGuire, and Robert Ferone pp 665 - 670; DOI: 10.1021/jm00155a014 |
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Synthesis and antiherpes virus activity of phosphate and phosphonate derivatives of 9-[(1,3-dihydroxy-2-propoxy)methyl]guanine Ernest J. Prisbe, John C. Martin, Danny P. C. McGee, Molly F. Barker, Donald F. Smee, Arit E. Duke, Thomas R. Matthews, and Julien P. H. Verheyden pp 671 - 675; DOI: 10.1021/jm00155a015 |
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Inhibitors of Bacillus subtilis DNA polymerase III. Influence of modifications in the pyrimidine ring of anilino- and (benzylamino)pyrimidines Debra J. Trantolo, George E. Wright, and Neal C. Brown pp 676 - 681; DOI: 10.1021/jm00155a016 |
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Synthesis and biological activity of several aminonucleoside-platinum(II) complexes Tai Shun Lin, Ren Xi Zhou, Kevin J. Scanlon, William F. Brubaker, Jung Ja Shim Lee, Kathleen Woods, Cynthia Humphreys, and William H. Prusoff pp 681 - 686; DOI: 10.1021/jm00155a017 |
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A lymphotropic prodrug of L-dopa: synthesis, pharmacological properties and pharmacokinetic behavior of 1,3-dihexadecanoyl-2-[(S)-2-amino-3-(3,4-dihydroxyphenyl)propanoyl]propane-1,2,3-triol Aaron Garzon-Aburbeh, Jacques H. Poupaert, Michel Claesen, and Pierre Dumont pp 687 - 691; DOI: 10.1021/jm00155a018 |
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In vitro inhibition of estrogen sulfoconjugation by some 2- and 4-substituted estra-1,3,5(10)-trien-17.beta.-ols Jerome P. Horwitz, Vaidyanathan K. Iyer, Harsha B. Vardhan, Jeanne Corombos, and Sam C. Brooks pp 692 - 698; DOI: 10.1021/jm00155a019 |
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Conformational energy calculations and electrostatic potentials of dihydrofolate reductase ligands: relevance to mode of binding and species specificity P. R. Andrews, M. Sadek, M. J. Spark, and D. A. Winkler pp 698 - 708; DOI: 10.1021/jm00155a020 |
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Synthesis and biological activities of 5-deaza analogs of aminopterin and folic acid Tsann Long Su, Jai Tung Huang, Joseph H. Burchenal, Kyoichi A. Watanabe, and Jack J. Fox pp 709 - 715; DOI: 10.1021/jm00155a021 |
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Synthesis and antitumor activity of cyclophosphamide analogs. 4. Preparation, kinetic studies, and anticancer screening of phenylketophosphamide and similar compounds related to the cyclophosphamide metabolite aldophosphamide Susan Marie Ludeman, Victoria Lee Boyd, Judith B. Regan, Kathleen A. Gallo, Gerald Zon, and Kiyoshi Ishii pp 716 - 727; DOI: 10.1021/jm00155a022 |
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Isohelical analysis of DNA groove-binding drugs David Goodsell and Richard E. Dickerson pp 727 - 733; DOI: 10.1021/jm00155a023 |
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Dopamine receptor agonists: 3-allyl-6-chloro-2,3,4,5-tetrahydro-1-(4-hydroxyphenyl)-1H-3-benzazepine-7,8-diol and a series of related 3-benzazepines Stephen T. Ross, Robert G. Franz, James W. Wilson, Martin Brenner, Robert M. DeMarinis, J. Paul Hieble, and Henry M. Sarau pp 733 - 740; DOI: 10.1021/jm00155a024 |
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Conformational effects on the activity of drugs. 11. Stereostructural models for the direct activation of the .alpha.- and .beta.-adrenergic receptor B. Macchia, A. Balsamo, E. Epifani, A. Lapucci, S. Nencetti, F. Macchia, M. C. Breschi, E. Martinotti, and R. Ceserani pp 740 - 747; DOI: 10.1021/jm00155a025 |
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Probes for narcotic receptor mediated phenomena. 9. Synthesis of (.+-.)-(3.alpha.,6a.alpha.,11a.beta.)-1,3,4,5,6,11a-hexahydro-2-methyl-2H-3,6a-methanobenzofuro[2,3-c]azocin-10-ol, and oxide-bridged 5-(m-hydroxyphenyl)morphan Terrence R. Burke, Arthur E. Jacobson, Kenner C. Rice, Ben Avi Weissman, Hsueh Cheng Huang, and J. V. Silverton pp 748 - 751; DOI: 10.1021/jm00155a026 |
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Proton NMR configurational correlation for retro-inverso dipeptides: application to the determination of the absolute configuration of "enkephalinase" inhibitors. Relationships between stereochemistry and enzyme recognition M. C. Fournie-Zaluski, E. Lucas-Soroca, J. Devin, and B. P. Roques pp 751 - 757; DOI: 10.1021/jm00155a027 |
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Preparation and evaluation of radioiodinated (iodophenyl)cholines and their morpholinium and piperidinium analogs as myocardial perfusion imaging agents Pamela L. Zabel, Yolanda Zea-Ponce, G. William Brown, Gary Morrissey, Duncan H. Hunter, Albert A. Driedger, and Michael J. Chamberlain pp 757 - 764; DOI: 10.1021/jm00155a028 |
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4-Amino-2-(substituted methyl)-2-butenoic acids: substrates and potent inhibitors of .gamma.-aminobutyric acid aminotransferase Richard B. Silverman, Susan C. Durkee, and Benedict J. Invergo pp 764 - 770; DOI: 10.1021/jm00155a029 |
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Improved glucose tolerance in rats treated with oxazolidinediones Rodney C. Schnur and Malcolm Morville pp 770 - 778; DOI: 10.1021/jm00155a030 |
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Crystal structures of .alpha.- and .beta.-funaltrexamine: conformational requirement of the fumaramate moiety in the irreversible blockage of .mu. opioid receptors Jane F. Griffin, Dennis L. Larson, and Philip S. Portoghese pp 778 - 783; DOI: 10.1021/jm00155a031 |
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Angiotensin-converting enzyme inhibitors: new orally active 1,4-thiazepine-2,5-diones, 1,4-thiazine-2,5-diones, and 1,4-benzothiazepine-2,5-diones possessing antihypertensive activity Jerry W. Skiles, John T. Suh, Bruce E. Williams, Paul R. Menard, Jeffrey N. Barton, Bernard Loev, Howard Jones, Edward S. Neiss, Alfred Schwab, and et al. pp 784 - 796; DOI: 10.1021/jm00155a032 |
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Zwitterionic 3'-O-acyl derivatives of thymidine 5'-phosphate as potential sources of intracellular thymidine 5'-phosphate in cells in culture Ram R. Chawla, Jerome J. Freed, Francis Kappler, and Alexander Hampton pp 797 - 802; DOI: 10.1021/jm00155a033 |
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Synthesis and biological properties of chitin synthetase inhibitors resistant to cellular peptidases Ponniah Shenbagamurthi, Herbert A. Smith, Jeffrey M. Becker, and Fred Naider pp 802 - 809; DOI: 10.1021/jm00155a034 |
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Synthesis and antiviral properties of 5-(2-substituted vinyl)-6-aza-2'-deoxyuridines William L. Mitchell, Paul Ravenscroft, Malcolm L. Hill, Lars J. S. Knutsen, Brian D. Judkins, Roger F. Newton, and David I. C. Scopes pp 809 - 816; DOI: 10.1021/jm00155a035 |
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Thromboxane synthetase inhibitors and antihypertensive agents. 2. N-[(1H-Imidazol-1-yl)alkyl]-1H-isoindole-1,3(2H)-diones and N-[(1H-1,2,4-triazol-1-yl)alkyl]-1H-isoindole-1,3(2H)-diones as unique antihypertensive agents Jeffery B. Press, William B. Wright, Peter S. Chan, Joseph W. Marsico, Margie F. Haug, Jess Tauber, and Andrew S. Tomcufcik pp 816 - 819; DOI: 10.1021/jm00155a036 |
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Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator Kohichiro Yoshino, Toshihiko Kohno, Toshio Uno, Tominori Morita, and Goro Tsukamoto pp 820 - 825; DOI: 10.1021/jm00155a037 |
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Agents for the treatment of brain edema. 2. [(2,3,9,9a-Tetrahydro-3-oxo-9a-substituted-1H-fluoren-7-yl)oxy]alkanoic acids and some of their analogs E. J. Cragoe Jr., O. W. Woltersdorf Jr., N. P. Gould, A. M. Pietruszkiewicz, C. Ziegler, Y. Sakurai, G. E. Stokker, P. S. Anderson, R. S. Bourke, and et al. pp 825 - 841; DOI: 10.1021/jm00155a038 |
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Enzymatic phosphorylation of the antiherpetic agent 9-[(2,3-dihydroxy-1-propoxy)methyl]guanine J. D. Karkas, W. T. Ashton, L. F. Canning, R. Liou, J. Germershausen, R. Bostedor, B. Arison, A. K. Field, and R. L. Tolman pp 842 - 848; DOI: 10.1021/jm00155a039 |
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3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 4. Side-chain ester derivatives of mevinolin W. F. Hoffman, A. W. Alberts, P. S. Anderson, J. S. Chen, R. L. Smith, and A. K. Willard pp 849 - 852; DOI: 10.1021/jm00155a040 |
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3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 5. 6-(Fluoren-9-yl)- and 6-(fluoren-9-ylidene)-3,5-dihydroxyhexanoic acids and their lactone derivatives G. E. Stokker, A. W. Alberts, J. L. Gilfillan, J. W. Huff, and R. L. Smith pp 852 - 855; DOI: 10.1021/jm00155a041 |
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5,5-Diaryl-2-thiohydantoins and 5,5-diaryl N3-substituted 2-thiohydantoins as potential hypolipidemic agents J. Ellsworth Tompkins pp 855 - 859; DOI: 10.1021/jm00155a042 |
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4-Aroyl-1,3-dihydro-2H-imidazol-2-ones: a new class of cardiotonic agents. 2. Effect of 4-pyridoyl substituents and related compounds Richard A. Schnettler, Richard C. Dage, and Frank P. Palopoli pp 860 - 862; DOI: 10.1021/jm00155a043 |
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Antineoplastic activity of 3'-(chloroethyl)nitrosourea analogs of 2'-deoxyuridine and 2'-deoxy-5-fluorouridine Tai Shun Lin, William F. Brubaker, Zi Hou Wang, Susanna Park, and William H. Prusoff pp 862 - 865; DOI: 10.1021/jm00155a044 |
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Synthesis and biological evaluation of cyclic analogs of l-carnitine as potential agents in the treatment of myocardial ischemia Patrick M. Woster and Wallace J. Murray pp 865 - 868; DOI: 10.1021/jm00155a045 |
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Allergenic .alpha.-methylene-.gamma.-butyrolactones. Study of the capacity of .beta.-acetoxy- and .beta.-hydroxy-.alpha.-methylene-.gamma.-butyrolactones to induce allergic contact dermatitis in guinea pigs Pierre Barbier and Claude Benezra pp 868 - 871; DOI: 10.1021/jm00155a046 |
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1,8-Diethyl-1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid: a potent antiinflammatory drug. Conformation and absolute configuration of its active enantiomer Leslie G. Humber, Christopher A. Demerson, and Panchanadam Swaminathan pp 871 - 874; DOI: 10.1021/jm00155a047 |
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Investigation of the structural requirements for the .kappa.-selective opioid receptor antagonist 6.beta.,6.beta.'-[ethylenebis(oxyethyleneimino)]bis[17-(cyclopropylmethyl)-4,5.alpha.-epoxymorphinan-3,14-diol](TENA) S. Botros, A. W. Lipkowski, A. E. Takemori, and P. S. Portoghese pp 874 - 876; DOI: 10.1021/jm00155a048 |
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Book Reviews pp 877 - 878; DOI: 10.1021/jm00155a600 |
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Additions and Corrections - Neuroleptic Activity of Chiral trans-Hexahrdro-γ-carbolines. Reinhard Sarges, Harry R. Howard, Kathy M. Donahue, Willard M. Welch, Beryl W. Dominy, Albert Weissman, B. Kenneth Koe, and Jon Bordner pp 876 - 876; DOI: 10.1021/jm00155a601 |
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Considerations for the design of nitrophenyl mustards as agents with selective toxicity for hypoxic tumor cells William A. Denny and William R. Wilson pp 879 - 887; DOI: 10.1021/jm00156a001 |
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Substituted 1-benzylimidazole-2-thiols as potent and orally active inhibitors of dopamine .beta.-hydroxylase Lawrence I. Kruse, Carl Kaiser, Walter E. DeWolf, James S. Frazee, Robert W. Erickson, Mildred Ezekiel, Eliot H. Ohlstein, Robert R. Ruffolo, and Barry A. Berkowitz pp 887 - 889; DOI: 10.1021/jm00156a002 |
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Synthesis and opioid activity of dermorphin tetrapeptides bearing D-methionine S-oxide at position 2 Severo Salvadori, Mauro Marastoni, Gianfranco Balboni, Gian Pietro Sarto, and Roberto Tomatis pp 889 - 894; DOI: 10.1021/jm00156a003 |
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7-Aroyl-2,3-dihydrobenzo[b]furan-3-carboxylic acids and 7-benzoyl-2,3-dihydrobenzo[b]thiophene-3-carboxylic acids as analgesic agents Elizabeth A. Boyle, Frank R. Mangan, Roger E. Markwell, Stephen A. Smith, Michael J. Thomson, Robert W. Ward, and Paul A. Wyman pp 894 - 898; DOI: 10.1021/jm00156a004 |
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The ensemble approach to distance geometry: application to the nicotinic pharmacophore Robert P. Sheridan, Ramaswamy Nilakantan, J. Scott Dixon, and R. Venkataraghavan pp 899 - 906; DOI: 10.1021/jm00156a005 |
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Structure-taste correlation of L-aspartyl dipeptides using the SIMCA method Yoshikatsu Miyashita, Yoshimasa Takahashi, Chiyozo Takayama, Kazuo Sumi, Kazuya Nakatsuka, Takehiko Ohkubo, Hidetsugu Abe, and Shinichi Sasaki pp 906 - 912; DOI: 10.1021/jm00156a006 |
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Structure-activity relationships of dopaminergic 5-hydroxy-2-aminotetralin derivatives with functionalized N-alkyl substituents Max P. Seiler, Andre P. Stoll, Annemarie Closse, Willy Frick, Annelise Jaton, and Jean Marie Vigouret pp 912 - 917; DOI: 10.1021/jm00156a007 |
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Conformational analysis of the dopamine-receptor agonist 5-hydroxy-2-(dipropylamino)tetralin and its C(2)-methyl-substituted derivative Anders Karlen, Anette M. Johansson, Lennart Kenne, Lars Erik Arvidsson, and Uli Hacksell pp 917 - 924; DOI: 10.1021/jm00156a008 |
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Antimalarial drugs. 60. Synthesis, antimalarial activity, and quantitative structure-activity relationships of tebuquine and a series of related 5-[(7-chloro-4-quinolinyl)amino]-3-[(alkylamino)methyl][1,1'-biphenyl]-2-ols and N.omega.-oxides Leslie M. Werbel, P. Dan Cook, Edward F. Elslager, Jocelyn H. Hung, Judith L. Johnson, Stephen J. Kesten, Dennis J. McNamara, Daniel F. Ortwine, and Donald F. Worth pp 924 - 939; DOI: 10.1021/jm00156a009 |
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Syntheses and in vitro evaluation of 4-(2-aminoethyl)-2(3H)-indolones and related compounds as peripheral prejunctional dopamine receptor agonists Robert M. DeMarinis, Ralph F. Hall, Robert G. Franz, Charles Webster, William F. Huffman, Mark S. Schwartz, Carl Kaiser, Stephen T. Ross, Gregory Gallagher Jr., and et al. pp 939 - 947; DOI: 10.1021/jm00156a010 |
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Synthesis, saludiuretic, and antihypertensive activity of 6,7-disubstituted 1(2H)- and 3,4-dihydro-1(2H)-phthalazinones S. Cherkez, J. Herzig, and H. Yellin pp 947 - 959; DOI: 10.1021/jm00156a011 |
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Modified di- and tripeptides of the C-terminal portion of oxytocin and vasopressin as possible cognition activation agents E. D. Nicolaides, F. J. Tinney, J. S. Kaltenbronn, J. T. Repine, D. A. DeJohn, E. A. Lunney, and W. H. Roark pp 959 - 971; DOI: 10.1021/jm00156a012 |
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Inhibition of cyclic nucleotide phosphodiesterases from pig coronary artery by benzo-separated analogs of 3-isobutyl-1-methylxanthine Stewart W. Schneller, Augusto C. Ibay, Elizabeth A. Martinson, and Jack N. Wells pp 972 - 978; DOI: 10.1021/jm00156a013 |
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Synthesis and antimitogenic activities of four analogs of cyclosporin A modified in the 1-position Daniel H. Rich, Madhup K. Dhaon, Brian Dunlap, and Stephen P. F. Miller pp 978 - 984; DOI: 10.1021/jm00156a014 |
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Potent vasopressin antagonists lacking the proline residue at position 7 Fadia El Fehail Ali, William Bryan, Hsin Lan Chang, William F. Huffman, Michael L. Moore, Grace Heckman, Lewis B. Kinter, Jeanne McDonald, Dulcie Schmidt, and et al. pp 984 - 988; DOI: 10.1021/jm00156a015 |
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Dog coronary artery adenosine receptor. Structure of the N6-aryl subregion Shozo Kusachi, Robert D. Thompson, Noboyuki Yamada, Daniel T. Daly, and R. A. Olsson pp 989 - 996; DOI: 10.1021/jm00156a016 |
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Cardiac glycosides. 6. Gitoxigenin C16 acetates, formates, methoxycarbonates, and digitoxosides. Synthesis and Na+,K+-ATPase inhibitory activities Toshihiro Hashimoto, Hargovind Rathore, Daisuke Satoh, Jane F. Griffin, Arthur H. L. From, Khalil Ahmed, Dwight S. Fullerton, and George Hong pp 997 - 1003; DOI: 10.1021/jm00156a017 |
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A novel class of conformationally restricted heterocyclic muscarinic agonists Per Sauerberg, Jens Jorgen Larsen, Erik Falch, and Povl Krogsgaard-Larsen pp 1004 - 1009; DOI: 10.1021/jm00156a018 |
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Indole-phenol-bioisosterism. Synthesis and antihypertensive activity of a pyrrolo analog of labetalol Andre A. Asselin, Leslie G. Humber, Danilo Crosilla, George Oshiro, Alexandra Wojdan, David Grimes, Richard J. Heaslip, Thomas J. Rimele, and Chia Cheng Shaw pp 1009 - 1015; DOI: 10.1021/jm00156a019 |
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Synthesis and biological activities of oligo(8-bromoadenylates) as analogs of 5'-O-triphosphoadenylyl(2'.fwdarw.5')adenylyl(2'.fwdarw.5')adenosine Krystyna Lesiak and Paul F. Torrance pp 1015 - 1022; DOI: 10.1021/jm00156a020 |
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The lysine pathway as a target for a new genera of synthetic antibacterial antibiotics? Jean Marc Girodeau, Constantin Agouridas, Maryse Masson, Roland Pineau, and Francois Le Goffic pp 1023 - 1030; DOI: 10.1021/jm00156a021 |
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Isozyme-specific enzyme inhibitors. 11. (L-homocysteine)-ATP S-C5' covalent adducts as inhibitors of rat methionine adenosyltransferases Francis Kappler, Ton T. Hai, Robert J. Cotter, Karen J. Hyver, and Alexander Hampton pp 1030 - 1038; DOI: 10.1021/jm00156a022 |
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Synthesis and .alpha.-D-glucosidase inhibitory activity of N-substituted valiolamine derivatives as potential oral antidiabetic agents Satoshi Horii, Hiroshi Fukase, Takao Matsuo, Yukihiko Kameda, Naoki Asano, and Katsuhiko Matsui pp 1038 - 1046; DOI: 10.1021/jm00156a023 |
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Structural studies on bioactive compounds. 4. A structure-antitumor activity study on analogs of N-methylformamide E. Nicholas Gate, Michael D. Threadgill, Malcolm F. G. Stevens, David Chubb, Lisa M. Vickers, Simon P. Langdon, John A. Hickman, and Andreas Gescher pp 1046 - 1052; DOI: 10.1021/jm00156a024 |
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Reactive 5'-substituted thymidine derivatives as potential inhibitors of nucleotide biosynthesis Robert D. Elliott, R. Wallace Brockman, and John A. Montgomery pp 1052 - 1056; DOI: 10.1021/jm00156a025 |
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Synthesis and biological activity of resolved carbon-10 diastereomers of 10-methyl- and 10-ethyl-10-deazaminopterin J. I. DeGraw, P. H. Christie, H. Tagawa, R. L. Kisliuk, Y. Gaumont, F. A. Schmid, and F. M. Sirotnak pp 1056 - 1061; DOI: 10.1021/jm00156a026 |
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Synthesis and dopaminergic activity of trans-6-methyl-7a,8,9,10,11,11a-hexahydro-7H-pyrrolo[3,2,1-gh]-4,7-phenanthroline and trans-1,2,3,4,4a,5,6,10b-octahydro-4,7-phenanthroline derivatives Francesco Claudi, Gloria Cristalli, Sante Martelli, and Vincenzo Perlini pp 1061 - 1065; DOI: 10.1021/jm00156a027 |
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.beta.1-Selective adrenoceptor antagonists: examples of the 2-[4-[3-(substituted amino)-2-hydroxypropoxy]phenyl]imidazole class. II John J. Baldwin, Marcia E. Christy, George H. Denny, Charles N. Habecker, Mark B. Freedman, Paulette A. Lyle, Gerald S. Ponticello, Sandor L. Varga, Dennis M. Gross, and Charles S. Sweet pp 1065 - 1080; DOI: 10.1021/jm00156a028 |
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Syntheses and antifolate activity of 5-methyl-5-deaza analogs of aminopterin, methotrexate, folic acid, and N10-methylfolic acid J. R. Piper, G. S. McCaleb, J. A. Montgomery, R. L. Kisliuk, Y. Gaumont, and F. M. Sirotnak pp 1080 - 1087; DOI: 10.1021/jm00156a029 |
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Probes for narcotic receptor mediated phenomena. 12. cis-(+)-3-Methylfentanyl isothiocyanate, a potent site-directed acylating agent for .delta. opioid receptors. Synthesis, absolute configuration, and receptor enantioselectivity Terrence R. Burke, Arthur E. Jacobson, Kenner C. Rice, J. V. Silverton, William F. Simonds, Richard A. Streaty, and Werner A. Klee pp 1087 - 1093; DOI: 10.1021/jm00156a030 |
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Synthesis and rat lens aldose reductase inhibitory activity of some benzopyran-2-ones Abram N. Brubaker, Jack De Ruiter, and William L. Whitmer pp 1094 - 1099; DOI: 10.1021/jm00156a031 |
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Antiinflammatory activity of substituted 6-hydroxypyrimido[2,1-f]purine-2,4,8(1H,3H,9H)-triones. Atypical nonsteroidal antiinflammatory agents David J. Blythin, James J. Kaminski, Martin S. Domalski, James Spitler, Daniel M. Solomon, David J. Conn, Shing Chun Wong, Laura Lehman Verbiar, Loretta A. Bober, and et al. pp 1099 - 1113; DOI: 10.1021/jm00156a032 |
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Quinazoline antifolates inhibiting thymidylate synthase. Variation of the amino acid Terence R. Jones, Michael J. Smithers, Richard F. Betteridge, Michael A. Taylor, Ann L. Jackman, A. Hilary Calvert, Lawrence C. Davies, and Kenneth R. Harrap pp 1114 - 1118; DOI: 10.1021/jm00156a033 |
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Indolo[2,1-c][1,4]benzodiazepines: a new class of antiallergic agents Chih Y. Ho, William E. Hageman, and Francis J. Persico pp 1118 - 1121; DOI: 10.1021/jm00156a034 |
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Structure-activity relationships for the competitive angiotensin antagonist [sarcosine1, O-methyltyrosine4]angiotensin II (sarmesin) Mahesh H. Goghari, Kevin J. Franklin, and Graham J. Moore pp 1121 - 1124; DOI: 10.1021/jm00156a035 |
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Drug development for senile cognitive decline Fred M. Hershenson and Walter H. Moos pp 1125 - 1130; DOI: 10.1021/jm00157a001 |
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Potential antiatherosclerotic agents. 5. An acyl-coenzyme A:cholesterol O-acyltransferase inhibitor with hypocholesterolemic activity Vern G. DeVries, Sheldon A. Schaffer, Elwood E. Largis, Minu D. Dutia, Ching Hua Wang, Jonathan D. Bloom, and Andrew S. Katocs pp 1131 - 1133; DOI: 10.1021/jm00157a002 |
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9-(2-Fluorobenzyl)-6-(methylamino)-9H-purine hydrochloride. Synthesis and anticonvulsant activity James L. Kelley and Francis E. Soroko pp 1133 - 1134; DOI: 10.1021/jm00157a003 |
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Novel 1,3-bis(aryloxy)propanes as leukotriene D4 antagonists Anthony F. Kreft, Dieter H. Klaubert, Stanley C. Bell, Thomas W. Pattison, John P. Yardley, Richard P. Carlson, James M. Hand, Joseph Y. Chang, and Alan J. Lewis pp 1134 - 1138; DOI: 10.1021/jm00157a004 |
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New antiarrhythmic agents. 2,2,5,5-Tetramethyl-3-pyrroline-3-carboxamides and 2,2,5,5-tetramethylpyrrolidine-3-carboxamides. Olga H. Hankovsky, Kalman Hideg, Ilona Bodi, and Laszlo Frank pp 1138 - 1152; DOI: 10.1021/jm00157a005 |
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Pepstatin analogs as novel renin inhibitors Remy Guegan, Joseph Diaz, Catherine Cazaubon, Michel Beaumont, Claude Carlet, Jacques Clement, Henri Demarne, Michel Mellet, Jean Paul Richaud, and et al. pp 1152 - 1159; DOI: 10.1021/jm00157a006 |
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Structure-activity study of 6-substituted 2-pyranones as inactivators of .alpha.-chymotrypsin William A. Boulanger and John A. Katzenellenbogen pp 1159 - 1163; DOI: 10.1021/jm00157a007 |
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Analogs of substance P. Peptides containing D-amino acid residues in various positions of substance P and displaying agonist or receptor selective antagonist effects Anand S. Dutta, James J. Gormley, Anthony S. Graham, Ian Briggs, James W. Growcott, and Alec Jamieson pp 1163 - 1171; DOI: 10.1021/jm00157a008 |
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Antagonists of substance P. Further modifications of SP antagonists obtained by replacing either positions 7, 9 or 7, 8 and 11 of SP with D-amino acid residues Anand S. Dutta, James J. Gormley, Anthony S. Graham, Ian Briggs, James W. Growcott, and Alec Jamieson pp 1171 - 1178; DOI: 10.1021/jm00157a009 |
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Synthesis of 2-(4-substituted-1-piperazinyl)benzimidazoles as H1-antihistaminic agents Ryuichi Iemura, Tsuneo Kawashima, Toshikazu Fukuda, Keizo Ito, and Goro Tsukamoto pp 1178 - 1183; DOI: 10.1021/jm00157a010 |
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Two stereoisomeric imidazoline derivatives. Synthesis, optical, and .alpha.2-adrenoceptor activities Juergen Biedermann, Alicia Leon-Lomeli, Harald O. Borbe, and Gerrit Prop pp 1183 - 1188; DOI: 10.1021/jm00157a011 |
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Synthesis and pharmacological evaluation of some new tetrahydroisoquinoline derivatives inhibiting dopamine uptake and/or possessing a dopaminomimetic property E. Zara-Kaczian, L. Gyorgy, Gyula Deak, A. Seregi, and M. Doda pp 1189 - 1195; DOI: 10.1021/jm00157a012 |
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Synthesis and gastric antisecretory properties of .alpha.-chain diene derivatives of misoprostol Paul W. Collins, Alan F. Gasiecki, Peter H. Jones, Raymond F. Bauer, Gary W. Gullikson, Emmett M. Woods, and Robert G. Bianchi pp 1195 - 1201; DOI: 10.1021/jm00157a013 |
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Synthesis and antitumor activity of tropolone derivatives. 3 Masatoshi Yamato, Kuniko Hashigaki, Nobuhiko Kokubu, Tazuko Tashiro, and Takashi Tsuruo pp 1202 - 1205; DOI: 10.1021/jm00157a014 |
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Phosphorus-31 nuclear magnetic resonance spectroscopic observation of the intracellular transformations of oncostatic cyclophosphamide metabolites Victoria L. Boyd, Joan D. Robbins, William Egan, and Susan M. Ludeman pp 1206 - 1210; DOI: 10.1021/jm00157a015 |
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Structure-activity relationship of novel oligopeptide antiviral and antitumor agents related to netropsin and distamycin J. William Lown, Krzysztof Krowicki, Jan Balzarini, and Erik De Clercq pp 1210 - 1214; DOI: 10.1021/jm00157a016 |
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7-Deoxydaunomycinone quinone methide reactivity with thiol nucleophiles K. Ramakrishnan and Jed Fisher pp 1215 - 1221; DOI: 10.1021/jm00157a017 |
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Peptides as receptor selectivity modulators of opiate pharmacophores A. W. Lipkowski, S. W. Tam, and P. S. Portoghese pp 1222 - 1225; DOI: 10.1021/jm00157a018 |
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New cyanomorpholinyl byproduct of doxorubicin reductive alkylation Edward M. Acton, George L. Tong, Dorris L. Taylor, Joyce A. Filppi, and Richard L. Wolgemuth pp 1225 - 1230; DOI: 10.1021/jm00157a019 |
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Esters and lactones of phenolic amino carboxylic acids. Prodrugs for iron chelation Colin G. Pitt, Y. Bao, J. Thompson, M. C. Wani, H. Rosenkrantz, and J. Metterville pp 1231 - 1237; DOI: 10.1021/jm00157a020 |
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Spin probes as mechanistic inhibitors and active site probes of thymidylate synthetase Prabhakar D. Devanesan and Albert M. Bobst pp 1237 - 1242; DOI: 10.1021/jm00157a021 |
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Synthesis and antitumor and antiviral properties of 5-halo- and 5-(trifluoromethyl)-2'-deoxyuridine 3',5'-cyclic monophosphates and neutral triesters Jozsef Beres, Gyula Sagi, Wesley G. Bentrude, Jan Balzarini, Erik De Clercq, and Laszlo Otvos pp 1243 - 1249; DOI: 10.1021/jm00157a022 |
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In the search for new anticancer drugs. 17. Linear and cyclic polyether analogs of N,N:N',N':N",N"-tri-1,2-ethanediylphosphoric triamide and N,N:N',N':N",N"-tri-1,2-ethanediylphosphorothioic triamide Geoge Sosnovsky, Jan Lukszo, and N. Uma Rao pp 1250 - 1256; DOI: 10.1021/jm00157a023 |
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Conformations of complexes between mitomycin and decanucleotides. 2. Application of the model to mitomycin C derivatives. Extension to covalent binding with adenine William A. Remers, Shashidhar N. Rao, U. Chandra Singh, and Peter A. Kollman pp 1256 - 1263; DOI: 10.1021/jm00157a024 |
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Adriamycin analogs. Preparation and biological evaluation of some thio ester analogues of adriamycin and N-(trifluoroacetyl)adriamycin 14-valerate Ramakrishnan Seshadri, John M. Idriss, and Mervyn Israel pp 1269 - 1273; DOI: 10.1021/jm00157a025 |
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Adriamycin analogues. Preparation and biological evaluation of some N-(trifluoroacetyl)-14-O-[N-acetylamino)acyl]adriamycin derivatives Mervyn Israel, David Taube, Ramakrishnan Seshadri, and John M. Idriss pp 1273 - 1276; DOI: 10.1021/jm00157a026 |
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Total chemical synthesis and antitumor evaluation of the 9-aza analog of N-(trifluoroacetyl)-4-demethoxydaunomycin Lester A. Mitscher, Harpal Gill, Joyce A. Filippi, and Richard L. Wolgemuth pp 1277 - 1281; DOI: 10.1021/jm00157a027 |
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Synthesis and biological activity of substance P C-terminal hexapeptide analogues: structure-activity studies Constantine Poulos, John R. Brown, and Christopher C. Jordan pp 1281 - 1284; DOI: 10.1021/jm00157a028 |
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[pGlu6, Pro9]SP6-11, a selective agonist for the substance P P-receptor subtype Ralph Laufer, Chaim Gilon, Michael Chorev, and Zvi Selinger pp 1284 - 1288; DOI: 10.1021/jm00157a029 |
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Hydrolysis of Pro-Ala dipeptides by lysosomal hydrolases. Models for the study of lysosomotropic amino acid prodrugs of penicillins C. Renard, A. Michael, and P. M. Tulkens pp 1291 - 1293; DOI: 10.1021/jm00157a030 |
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Synthesis and biological activity of 5-phenylselenenyl-substituted pyrimidine nucleosides Raymond F. Schinazi, Jack Arbiser, Jung Ja S. Lee, Thomas I. Kalman, and William H. Prusoff pp 1293 - 1295; DOI: 10.1021/jm00157a031 |
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Studies in potential filaricides. 18. Synthesis of 2,2'-disubstituted 5,5'-dibenzimidazolyl ketones and related compounds as potential anthelmintics Syed Abuzar, Satyavan Sharma, Nigar Fatma, S. Gupta, P. K. Murthy, J. C. Katiyar, R. K. Chatterjee, and A. B. Sen pp 1296 - 1299; DOI: 10.1021/jm00157a032 |
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Synthesis and evaluation of 2-substituted 1-methyl-1-(4-tolylsulfonyl)hydrazines as antineoplastic agents Robert T. Hrubiec, Krishnamurthy Shyam, Lucille A. Cosby, Ryosuke Furubayashi, and Alan C. Sartorelli pp 1299 - 1301; DOI: 10.1021/jm00157a033 |
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Inactivation of leukocyte elastase by aryl azolides and sulfonate salts. Structure-activity relationship studies W. C. Groutas, M. J. Brubaker, M. E. Zandler, V. Mazo-Gray, S. A. Rude, J. P. Crowley, J. C. Castrisos, D. A. Dunshee, and P. K. Giri pp 1302 - 1305; DOI: 10.1021/jm00157a034 |
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Analogs of caffeine and theophylline: effect of structural alterations on affinity at adenosine receptors J. W. Daly, W. L. Padgett, and M. T. Shamim pp 1305 - 1308; DOI: 10.1021/jm00157a035 |
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Muscarinic ganglionic stimulants: conformationally restrained analogs related to [4-[[N-(3-chlorophenyl)carbamoyl]oxy]-2-butynyl]trimethylammonium chloride Guenter Lambrecht, Ulrich Moser, Ernst Mutschler, Gerhard Walther, and Juergen Wess pp 1309 - 1311; DOI: 10.1021/jm00157a036 |
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Molecular basis for anticancer drug amplification. Interaction of phleomycin amplifiers with DNA L. Strekowski, S. Chandrasekaran, Yueh Hwa Wang, W. Daniel Edwards, and W. David Wilson pp 1311 - 1315; DOI: 10.1021/jm00157a037 |
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Analogs of platelet activating factor. 5. Multiple oxygen substitution of the alkoxy chain A. Wissner, C. A. Kohler, and B. M. Goldstein pp 1315 - 1319; DOI: 10.1021/jm00157a038 |
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Isolation, synthesis and antitumor evaluation of spirohydantoin aziridine, a mutagenic metabolite of spirohydantoin mustard Robert F. Struck, Marion C. Kirk, Louise S. Rice, and William J. Suling pp 1319 - 1321; DOI: 10.1021/jm00157a039 |
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Basically substituted ellipticine analogs as potential antitumor agents Leslie M. Werbel, Mario Angelo, David W. Fry, and Donald F. Worth pp 1321 - 1322; DOI: 10.1021/jm00157a040 |
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1,2-Bis(arylsulfonyl)hydrazines. 2. The influence of arenesulfonyl and aralkylsulfonyl substituents on antitumor and alkylating activity Krishnamurthy Shyam, Lucille A. Cosby, and Alan C. Sartorelli pp 1323 - 1325; DOI: 10.1021/jm00157a041 |
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Folate Analogues. 25. Synthesis and Biological Evaluation of N10-Propargylfolic Acid and Its Reduced Derivatives Maryam Ghazala, M.G. Nair, Tahereh R. Toghiyani, R.L. Kisliuk, Y. Gaumont, and T.I. Kalman pp 1263 - 1269; DOI: 10.1021/jm00157a600 |
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(S)-3-[(Benzyloxy)methyl]morpholine Hydrochloride: A Nonstimulant Appetite Suppressant without Conventional Neurotransmitter Releasing Properties George R. Brown, Alan J. Foubister, Gillian Forster, and Donald Stribling pp 1288 - 1290; DOI: 10.1021/jm00157a601 |
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Book Reviews pp 1325 - 1326; DOI: 10.1021/jm00157a602 |
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The mechanism of action of the antisecretory agent omeprazole Per Lindberg, Peter Nordberg, Tomas Alminger, Arne Braendstroem, and Bjoern Wallmark pp 1327 - 1329; DOI: 10.1021/jm00158a001 |
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Streptonigrin. 1. Structure-activity relationships among simple bicyclic analogs. Rate dependence of DNA degradation on quinone reduction potential Iftikhar A. Shaikh, Francis Johnson, and Arthur P. Grollman pp 1329 - 1340; DOI: 10.1021/jm00158a002 |
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Isomer-dependent cytostatic activity of bis(1-aziridinyl)cyclophosphazenes Adriaan A. Van der Huizen, Theo Wilting, Johan C. Van de Grampel, Peter Lelieveld, Aukje Van der Meer-Kalverkamp, Henk B. Lamberts, and Nanno H. Mulder pp 1341 - 1345; DOI: 10.1021/jm00158a003 |
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Sequentially labile water-soluble prodrugs of alprazolam Moo J. Cho, Vimala H. Sethy, and Lynn C. Haynes pp 1346 - 1350; DOI: 10.1021/jm00158a004 |
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Ribose as the preferential target for the oxidized form of elliptinium acetate in ribonucleos(T)ides. Biological activities of the resulting adducts Genevieve Pratviel, Jean Bernadou, Tam Ha, Gerard Meunier, Suzy Cros, Bernard Meunier, B. Gillet, and E. Guittet pp 1350 - 1355; DOI: 10.1021/jm00158a005 |
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Catechol estrogens of the 1,1,2-triphenyl-1-butene type. Relationship between structure, estradiol receptor affinity, estrogenic and antiestrogenic properties, and mammary tumor inhibiting activities Martin R. Schneider, Hartwig Ball, and Claus D. Schiller pp 1355 - 1362; DOI: 10.1021/jm00158a006 |
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Aromatase inhibitors. Synthesis and evaluation of mammary tumor inhibiting activity of 3-alkylated 3-(4-aminophenyl)piperidine-2,6-diones Rolf W. Hartmann and Christine Batzl pp 1362 - 1369; DOI: 10.1021/jm00158a007 |
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Synthesis and antitumor activities of unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones and related systems A. Paul Krapcho, John J. Landi, Kenneth J. Shaw, Donald G. Phinney, Miles P. Hacker, and John J. McCormack pp 1370 - 1373; DOI: 10.1021/jm00158a008 |
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Synthesis of pyrimidin-2-one nucleosides as acid-stable inhibitors of cytidine deaminase Chong Ho Kim, Victor E. Marquez, David T. Mao, David R. Haines, and John J. McCormack pp 1374 - 1380; DOI: 10.1021/jm00158a009 |
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One-electron reduction of 2- and 6-methyl-1,4-naphthoquinone bioreductive alkylating agents Ian Wilson, Peter Wardman, Tai Shun Lin, and Alan C. Sartorelli pp 1381 - 1384; DOI: 10.1021/jm00158a010 |
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Synthesis and anti-herpes virus activity of acyclic 2'-deoxyguanosine analogs related to 9-[(1,3-dihydroxy-2-propoxy)methyl]guanine John C. Martin, Danny P. C. McGee, Gary A. Jeffrey, Doug W. Hobbs, Donald F. Smee, Thomas R. Matthews, and Julian P. H. Verheyden pp 1384 - 1389; DOI: 10.1021/jm00158a011 |
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Synthesis and antiviral activity of certain nucleoside 5'-phosphonoformate derivatives Morteza M. Vaghefi, Patricia A. McKernan, and Roland K. Robins pp 1389 - 1393; DOI: 10.1021/jm00158a012 |
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4-Amino-6-chloro-2-piperazinopyrimidines with selective affinity for .alpha.2-adrenoceptors Claude Gueremy, Francois Audiau, Christian Renault, Jesus Benavides, Andre Uzan, and Gerard Le Fur pp 1394 - 1398; DOI: 10.1021/jm00158a013 |
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Synthesis and Class III antiarrhythmic activity of (phenyl-2-butenyl)ammonium salts. Effect of conformation on activity Thomas K. Morgan, Ronald A. Wohl, William C. Lumma, Chung Nan Wan, David D. Davey, Robert P. Gomez, Anthony J. Marisca, Martha Briggs, Mark E. Sullivan, and Samuel S. Wong pp 1398 - 1405; DOI: 10.1021/jm00158a014 |
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Selective monoamine oxidase inhibitors. 3. Cyclic compounds related to 4-aminophenethylamine. Preparation and neuron-selective action of some 5-(2-aminoethyl)-2,3-dihydroindoles Lennart Florvall, Yatendra Kumar, Anna Lena Ask, Ingrid Fagervall, Lucy Renyi, and Svante B. Ross pp 1406 - 1412; DOI: 10.1021/jm00158a015 |
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Conformationally defined adrenergic agents. 3. Modifications to the carbocyclic ring of 5,6-dihydroxy-1-(2-imidazolinyl)tetralin: improved separation of .alpha.1 and .alpha.2 adrenergic activities John F. DeBernardis, Martin Winn, David L. Arendsen, Daniel J. Kerkman, and John J. Kyncl pp 1413 - 1417; DOI: 10.1021/jm00158a016 |
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Dopaminergic pharmacophore of ergoline and its analogs. A molecular electrostatic potential study Darko Kocjan, Milan Hodoscek, and Dusan Hadzi pp 1418 - 1423; DOI: 10.1021/jm00158a017 |
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Detection of N-acetyl-p-benzoquinone imine produced during the hydrolysis of the model phenacetin metabolite N-(pivaloyloxy)phenacetin Michael Novak, Maria Pelecanou, and Joseph N. Zemis pp 1424 - 1429; DOI: 10.1021/jm00158a018 |
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Synthesis of [[(naphthalenylmethoxy)- and -(quinolinylmethoxy)phenyl]amino]oxoalkanoic acid esters. A novel series of leukotriene D4 antagonists and 5-lipoxygenase inhibitors John H. Musser, Dennis M. Kubrak, Joseph Chang, and Alan J. Lewis pp 1429 - 1435; DOI: 10.1021/jm00158a019 |
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Synthesis and antiinflammatory/analgesic activities of 11H-dibenzo[b,e]dioxepinacetic acids William K. Hagmann, Conrad P. Dorn, Robert A. Frankshun, Laura A. O'Grady, Philip J. Bailey, Anita Rackham, and Harry W. Dougherty pp 1436 - 1441; DOI: 10.1021/jm00158a020 |
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Synthesis and structure-activity relationship studies of a series of 5-aryl-4,6-dithianonanedioic acids and related compounds: a novel class of leukotriene antagonists Carl D. Perchonock, Irene Uzinskas, Mary E. McCarthy, Karl F. Erhard, John G. Gleason, Martin A. Wasserman, Roseanna M. Muccitelli, Jeris F. DeVan, Stephanie S. Tucker, and et al. pp 1442 - 1452; DOI: 10.1021/jm00158a021 |
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Ligand-receptor interactions via hydrogen-bond formation. Synthesis and pharmacological evaluation of pyrrolo and pyrido analogs of the cardiotonic agent 7-hydroxycyclindole Gervais Dionne, Leslie G. Humber, Andre Asselin, Juanita McQuillan, and Adi M. Treasurywala pp 1452 - 1457; DOI: 10.1021/jm00158a022 |
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Synthesis and analgesic evaluation of 4-(2-heptyloxy)-7-[(Z)-(3-hydroxycyclohexyl)]indole: a caveat on indole-phenol bioisosterism Richard M. Soll, Leslie G. Humber, David Deininger, Andre A. Asselin, Thuy T. Chau, and Barry M. Weichman pp 1457 - 1460; DOI: 10.1021/jm00158a023 |
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Thromboxane A2 synthase inhibitors. 5-(3-Pyridylmethyl)benzofuran-2-carboxylic acids Roy A. Johnson, Eldon G. Nidy, James W. Aiken, Norman J. Crittenden, and Robert R. Gorman pp 1461 - 1468; DOI: 10.1021/jm00158a024 |
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Peptidyl carbamates incorporating amino acid isosteres as novel elastase inhibitors George A. Digenis, Bushra J. Agha, Kiyoshi Tsuji, Masayuki Kato, and Masaki Shinogi pp 1468 - 1476; DOI: 10.1021/jm00158a025 |
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Buspirone analogs. 2. Structure-activity relationships of aromatic imide derivatives James S. New, Joseph P. Yevich, Michael S. Eison, Duncan P. Taylor, Arlene S. Eison, Leslie A. Riblet, Cam P. VanderMaelen, and Davis L. Temple pp 1476 - 1482; DOI: 10.1021/jm00158a026 |
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5-(Halomethyl)-2-pyranones as irreversible inhibitors of .alpha.-chymotrypsin William A. Boulanger and John A. Katzenellenbogen pp 1483 - 1487; DOI: 10.1021/jm00158a027 |
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N-Substituted sulfonamide carbonic anhydrase inhibitors with topical effects on intraocular pressure Michael W. Duffel, I. Silwai Ing, Tyrone M. Segarra, John A. Dixson, Charles F. Barfknecht, and Ronald D. Schoenwald pp 1488 - 1494; DOI: 10.1021/jm00158a028 |
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2-Alkyl-substituted 1,1-bis(4-acetoxyphenyl)-2-phenylethenes. Estrogen receptor affinity, estrogenic and antiestrogenic properties, and mammary tumor inhibiting activity Martin R. Schneider pp 1494 - 1498; DOI: 10.1021/jm00158a029 |
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Pyrimidinones. 3. N-Substituted 6-phenylpyrimidinones and pyrimidinediones with diuretic/hypotensive and antiinflammatory activity Harvey I. Skulnick, James H. Ludens, Michael G. Wendling, E. Myles Glenn, Norman A. Rohloff, Robert J. Smith, and Wendell Wierenga pp 1499 - 1504; DOI: 10.1021/jm00158a030 |
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Topical nonsteroidal antipsoriatic agents. 1. 1,2,3,4-Tetraoxygenated naphthalene derivatives Gordon H. Jones, Michael C. Venuti, John M. Young, D. V. Krishna Murthy, Brad E. Loe, Richard A. Simpson, Andrew H. Berks, Doreen A. Spires, Patrick J. Maloney, and et al. pp 1504 - 1511; DOI: 10.1021/jm00158a031 |
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Anticonvulsant activity of piperidinol and (dialkylamino)alkanol esters James A. Waters, Elizabeth B. Hollingsworth, John W. Daly, Gail Lewandowski, and Cyrus R. Creveling pp 1512 - 1516; DOI: 10.1021/jm00158a032 |
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Characterization of the neurotoxic potential of m-methoxy-MPTP and the use of its N-ethyl analog as a means of avoiding exposure to a possible Parkinson-causing agent Dennis M. Zimmerman, Buddy E. Cantrell, Jon K. Reel, Susan K. Hemrick-Luecke, and Ray W. Fuller pp 1517 - 1520; DOI: 10.1021/jm00158a033 |
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Analogs of 1,3-dipropyl-8-phenylxanthine: enhancement of selectivity at A1-adenosine receptors by aryl substituents J. W. Daly, W. L. Padgett, and M. T. Shamim pp 1520 - 1524; DOI: 10.1021/jm00158a034 |
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Synthesis and .beta.-adrenergic receptor blocking potency of 1-(substituted amino)-3-(4-indolyloxy)propan-2-ols Shanaz M. Tejani-Butt and David J. Brunswick pp 1524 - 1527; DOI: 10.1021/jm00158a035 |
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Synthesis and pharmacological evaluation of some 6-substituted 7-methyl-1,4-dioxa-7-azaspiro[4.5]decanes as potential dopamine agonists Abram N. Brubaker and Matt Colley pp 1528 - 1531; DOI: 10.1021/jm00158a036 |
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Synthesis and biological activity of benzothiazolo[3,2-a]quinolone antibacterial agents Daniel T. W. Chu, Prabhavathi B. Fernandes, and Andre G. Pernet pp 1531 - 1534; DOI: 10.1021/jm00158a037 |
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Anticonvulsant activity of 2- and 3-aminobenzanilides C. Randall Clark, Ching Ming Lin, and Ricky T. Sansom pp 1534 - 1537; DOI: 10.1021/jm00158a038 |
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3,17.beta.-dihydroxy-20,21-epoxy-19-norpregna-1,3,5(10)-trienes. Synthesis, rearrangement, cytotoxicity, and estrogen-receptor binding Julie C. Gill, Peter M. Lockey, Brian A. Marples, and John R. Traynor pp 1537 - 1540; DOI: 10.1021/jm00158a039 |
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Synthesis and biological activity of 3-amino-5-(3,5-diamino-6-chloropyrazin-2-yl)-1,2,4-oxadiazole. An amiloride prodrug Mark G. Bock, Robert L. Smith, Edward H. Blaine, and Edward J. Cragoe pp 1540 - 1544; DOI: 10.1021/jm00158a040 |
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Pyrazole derivatives. 5. Synthesis and antineoplastic activity of 3-(2-chloroethyl)-3,4-dihydro-4-oxopyrazolo[5,1-d]-1,2,3,5-tetrazine-8-carboxamide and related compounds C. C. Cheng, Edward F. Elslager, Leslie M. Werbel, and Wilbur R. Leopold pp 1544 - 1547; DOI: 10.1021/jm00158a041 |
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Antitumor agents. 78. Inhibition of human DNA topoisomerase II by podophyllotoxin and .alpha.-peltatin analogs Lee S. Thurston, Hiroshi Irie, Shohei Tani, Fu Sheng Han, Zong Chao Liu, Yung Chi Cheng, and Kuo Hsiung Lee pp 1547 - 1550; DOI: 10.1021/jm00158a042 |
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Activity of N-methyl-.alpha.- and -.beta.-funaltrexamine at opioid receptors M. S. Mohamed, D. L. Larson, A. E. Takemori, and P. S. Portoghese pp 1551 - 1553; DOI: 10.1021/jm00158a043 |
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Plant antitumor agents. 22. Isolation of 11-hydroxycamptothecin from Camptotheca acuminata decne: total synthesis and biological activity Monroe E. Wall, Mansukh C. Wani, Susan M. Natschke, and Allan W. Nicholas pp 1553 - 1555; DOI: 10.1021/jm00158a044 |
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Additions and Corrections - New α-Methylene γ-Lactone Derivatives of Substituted Nucleic Acid Bases as Potential Agents. Utpal Sanyal, Saktimoyee Mitra, Prasun Pal, and S. K .Chakraborti pp 1555 - 1555; DOI: 10.1021/jm00158a600 |
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Chemotherapeutic approaches to the treatment of the acquired immune deficiency syndrome (AIDS) Erik De Clercq pp 1561 - 1569; DOI: 10.1021/jm00159a001 |
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A stereochemical explanation of the dopamine agonist and antagonist activity of stereoisomeric pairs M. Froimowitz, J. L. Neumeyer, and R. J. Baldessarini pp 1570 - 1573; DOI: 10.1021/jm00159a002 |
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Design and synthesis of sodium (.beta.R*,.gamma.S*)-4-[[3-(4-acetyl-3-hydroxy-2-propylphenoxy)propyl]thio]-.gamma.-hydroxy-.beta.-methylbenzenebutanoate: a novel, selective, and orally active receptor antagonist of leukotriene D4 R. N. Young, P. Belanger, E. Champion, R. N. DeHaven, D. Denis, A. W. Ford-Hutchinson, R. Fortin, R. Frenette, J. Y. Gauthier, and et al. pp 1573 - 1576; DOI: 10.1021/jm00159a003 |
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Structure-activity relationships of (arylalkyl)imidazole anticonvulsants: comparison of the (fluorenylalkyl)imidazoles with nafimidone and denzimol David W. Robertson, Joseph H. Krushinski, E. E. Beedle, J. David Leander, David T. Wong, and R. C. Rathbun pp 1577 - 1586; DOI: 10.1021/jm00159a004 |
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Synthesis and renal vasodilator activity of 2-chlorodopamine and N-substituted derivatives James R. McCarthy, Jefferson McCowan, Mark B. Zimmerman, Marcia A. Wenger, and Lee W. Emmert pp 1586 - 1590; DOI: 10.1021/jm00159a005 |
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3,4-Dihydro-2-phenyl-2H-pyrano[2,3-b]pyridines with potent antirhinovirus activity Thomas M. Bargar, Jacqueline K. Dulworth, Michael T. Kenny, Renee Massad, John K. Daniel, Thomas Wilson, and Roger N. Sargent pp 1590 - 1595; DOI: 10.1021/jm00159a006 |
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Oxidation of 4-aryl- and 4-alkyl-substituted 2,6-dimethyl-3,5-bis(alkoxycarbonyl)-1,4-dihydropyridines by human liver microsomes and immunochemical evidence for the involvement of a form of cytochrome P-450 Ronald H. Boecker and F. Peter Guengerich pp 1596 - 1603; DOI: 10.1021/jm00159a007 |
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Syntheses and .beta.-adrenergic agonist and antiaggregatory properties of N-substituted trimetoquinol analogues Adeboye Adejare, Duane D. Miller, Joanne S. Fedyna, Chang Ho Ahn, and Dennis R. Feller pp 1603 - 1609; DOI: 10.1021/jm00159a008 |
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Molecular requirements of the recognition site of cholinergic receptors. 22. Resolution, absolute configuration, and cholinergic enantioselectivity of (+)- and (-)-cis-2-methyl-5-[(dimethylamino)methyl]-1,3-oxathiolane methiodide Elisabetta Teodori, Fulvio Gualtieri, Piero Angeli, Livio Brasili, Mario Giannella, and Maria Pigini pp 1610 - 1615; DOI: 10.1021/jm00159a009 |
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Synthesis and dopaminergic activity of some halogenated mono- and dihydroxylated 2-aminotetralins Joseph Weinstock, Dimitri Gaitanopoulos, Hye Ja Oh, Francis R. Pfeiffer, Carole B. Karash, Joseph W. Venslavsky, Henry M. Sarau, Kathryn E. Flaim, J. Paul Hieble, and Carl Kaiser pp 1615 - 1627; DOI: 10.1021/jm00159a010 |
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(5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones. A series of novel potential antipsychotic agents Lawrence D. Wise, Donald E. Butler, Horace A. DeWald, David Lustgarten, Linda L. Coughenour, David A. Downs, Thomas G. Heffner, and Thomas A. Pugsley pp 1628 - 1637; DOI: 10.1021/jm00159a011 |
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Selective thromboxane synthetase inhibitors. 3. 1H-Imidazol-1-yl-substituted benzo[b]furan-, benzo[b]thiophene- and indole-2- and 3-carboxylic acids Peter E. Cross, Roger P. Dickinson, M. John Parry, and Michael J. Randall pp 1637 - 1643; DOI: 10.1021/jm00159a012 |
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Selective thromboxane synthetase inhibitors. 4. 2-(1H-Imidazol-1-ylmethyl)benzo[b]furan-, -benzo[b]thiophene-, -indole- and -naphthalenecarboxylic acids Peter E. Cross, Roger P. Dickinson, M. John Parry, and Michael J. Randall pp 1643 - 1650; DOI: 10.1021/jm00159a013 |
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Synthesis and opioid antagonist potencies of naltrexamine bivalent ligands with conformationally restricted spacers P. S. Portoghese, G. Ronsisvalle, D. L. Larson, and A. E. Takemori pp 1650 - 1653; DOI: 10.1021/jm00159a014 |
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Synthesis of thyrotropin-releasing hormone analogs. 2. Tripeptides structurally greatly different from TRH with high central nervous system activity Tamas Szirtes, Lajos Kisfaludy, Eva Palosi, and Laszlo Szporny pp 1654 - 1658; DOI: 10.1021/jm00159a015 |
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Topological similarities between a cyclic enkephalin analog and a potent opiate alkaloid: a computer-modeling approach John DiMaio, Christopher I. Bayly, G. Villeneuve, and Andre Michel pp 1658 - 1663; DOI: 10.1021/jm00159a016 |
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In vitro labeling of serotonin-S2 receptors. Synthesis and binding characteristics of [3H]-7-aminoketanserin Walter Wouters, Cornelus G. M. Janssen, Jacky Van Dun, Jos B. A. Thijssen, and Pierre M. Laduron pp 1663 - 1668; DOI: 10.1021/jm00159a017 |
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Influence of alkyl chain ramification on estradiol receptor binding affinity and intrinsic activity of 1,2-dialkylated 1,2-bis(4- or 3-hydroxyphenyl)ethane estrogens and antiestrogens Rolf W. Hartmann pp 1668 - 1674; DOI: 10.1021/jm00159a018 |
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Potential tumor- or organ-imaging agents. 26. Polyiodinated 2-substituted triacylglycerols as hepatographic agents Jamey P. Weichert, Marc A. Longino, Susan W. Schwendner, and Raymond E. Counsell pp 1674 - 1682; DOI: 10.1021/jm00159a019 |
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N6-Substituted N-alkyladenosine-5'-uronamides: bifunctional ligands having recognition groups for A1 and A2 adenosine receptors R. A. Olsson, Shozo Kusachi, Robert D. Thompson, Dieter Ukena, William Padgett, and John W. Daly pp 1683 - 1689; DOI: 10.1021/jm00159a020 |
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Nonquaternary cholinesterase reactivators. 4. Dialkylaminoalkyl thioesters of .alpha.-keto thiohydroximic acids as reactivators of ethyl methylphosphonyl- and 1,2,2-trimethylpropyl methylphosphonyl-acetylcholinesterase in vitro Clifford D. Bedford, Michiko Miura, Jeffrey C. Bottaro, Robert A. Howd, and Harold W. Nolen pp 1689 - 1696; DOI: 10.1021/jm00159a021 |
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Long-acting dihydropyridine calcium antagonists. 1. 2-Alkoxymethyl derivatives incorporating basic substituents John E. Arrowsmith, Simon F. Campbell, Peter E. Cross, John K. Stubbs, Roger A. Burges, Donald G. Gardiner, and Kenneth J. Blackburn pp 1696 - 1702; DOI: 10.1021/jm00159a022 |
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Methotrexate analogs. 28. Synthesis and biological evaluation of new .gamma.-monoamides of aminopterin and methotrexate Andre Rosowsky, Henry Bader, Mary Radike-Smith, Carol A. Cucchi, Michael M. Wick, and James H. Freisheim pp 1703 - 1709; DOI: 10.1021/jm00159a023 |
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Synthesis of anthraquinonyl glucosaminosides and studies on the influence of aglycone hydroxyl substitution on superoxide generation, DNA binding, and antimicrobial properties Hanley N. Abramson, Jon W. Banning, Joseph P. Nachtman, Edward T. Roginski, Maniklal Sardessai, Henry C. Wormser, Jender Wu, Ziad Nagia, Ronald R. Schroeder, and Maria Margarida Bernardo pp 1709 - 1714; DOI: 10.1021/jm00159a024 |
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Thiol addition to quinones: model reactions for the inactivation of thymidylate synthase by 5-p-benzoquinonyl-2'-deoxyuridine 5'-phosphate Madhavi K. Vadnere, Linda Maggiora, and Mathias P. Mertes pp 1714 - 1720; DOI: 10.1021/jm00159a025 |
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Carbocyclic analogs of 5-halocytosine nucleosides Y. Fulmer Shealy, C. Allen O'Dell, Gussie Arnett, William M. Shannon, Martha C. Thorpe, James M. Riordan, and William C. Coburn pp 1720 - 1725; DOI: 10.1021/jm00159a026 |
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Thiazole-4-carboxamide adenine dinucleotide (TAD). Analogs stable to phosphodiesterase hydrolysis Victor E. Marquez, Christopher K. H. Tseng, Gulilat Gebeyehu, David A. Cooney, Gurpreet S. Ahluwalia, James A. Kelley, Maha Dalal, Richard W. Fuller, Yvonne A. Wilson, and David G. Johns pp 1726 - 1731; DOI: 10.1021/jm00159a027 |
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Synthesis of 11H-pyridocarbazoles and derivatives. Comparison of their DNA binding and antitumor activity with those of 6H- and 7H-pyridocarbazoles Elie Lescot, Gabriel Muzard, Judith Markovits, Joel Belleney, Bernard P. Roques, and Jean Bernard Le Pecq pp 1731 - 1737; DOI: 10.1021/jm00159a028 |
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Comparative toxicities and analgesic activities of three monomethylated analogs of acetaminophen Peter J. Harvison, Anthony J. Forte, and Sidney D. Nelson pp 1737 - 1743; DOI: 10.1021/jm00159a029 |
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Isozyme-specific enzyme inhibitors. 12. C- and N-methylmethionines as substrates and inhibitors of methionine adenosyltranferases of normal and hepatoma rat tissues Hong Lim, Francis Kappler, Ton T. Hai, and Alexander Hampton pp 1743 - 1748; DOI: 10.1021/jm00159a030 |
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Queuine analogs. Their synthesis and inhibition of growth of mouse L5178Y cells in vitro Hiroshi Akimoto, Hiroaki Nomura, Mitsuzi Yoshida, Nobuko Shindo-Okada, Akio Hoshi, and Susumu Nishimura pp 1749 - 1753; DOI: 10.1021/jm00159a031 |
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Folate analogs. 26. Syntheses and antifolate activity of 10-substituted derivatives of 5,8-dideazafolic acid and of the poly-.gamma.-glutamyl metabolites of N10-propargyl-5,8-dideazafolic acid (PDDF) M. G. Nair, Nitin T. Nanavati, Indira G. Nair, Roy L. Kisliuk, Y. Gaumont, M. C. Hsiao, and Thomas I. Kalman pp 1754 - 1760; DOI: 10.1021/jm00159a032 |
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Mitomycin C analogs with increased metal complexing ability Bhashyam S. Iyengar, Salah M. Sami, Takeo Takahashi, Elizabeth E. Sikorski, William A. Remers, and William T. Bradner pp 1760 - 1764; DOI: 10.1021/jm00159a033 |
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Carrier-linked primaquine in the chemotherapy of malaria Jan Hofsteenge, Anne Capuano, Rita Altszuler, and Stanford Moore pp 1765 - 1769; DOI: 10.1021/jm00159a034 |
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Potential antitumor agents. 47. 3'-Methylamino analogs of amsacrine with in vivo solid tumor activity Graham J. Atwell, Bruce C. Baguley, Graeme J. Finlay, Gordon W. Rewcastle, and William A. Denny pp 1769 - 1776; DOI: 10.1021/jm00159a035 |
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Synthesis and evaluation of 1-(arylsulfonyl)-2-[(methoxycarbonyl)sulfenyl]-1-methylhydrazines as antineoplastic agents Robert T. Hrubiec, Krishnamurthy Shyam, Lucille A. Cosby, and Alan C. Sartorelli pp 1777 - 1779; DOI: 10.1021/jm00159a036 |
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Effect of methoxy substitution on the adrenergic activity of three structurally related .alpha.2-adrenoreceptor antagonists Michael R. Stillings, C. David England, Anthony P. Welbourn, and Colin F. C. Smith pp 1780 - 1783; DOI: 10.1021/jm00159a037 |
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Analgesic actions of 3-substituted 6-tert-butyl-1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines Linda J. James and Robert T. Parfitt pp 1783 - 1785; DOI: 10.1021/jm00159a038 |
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Synthesis and antifolate properties of 5,10-methylenetetrahydro-8,10-dideazaminopterin J. I. DeGraw, W. T. Colwell, R. L. Kisliuk, Y. Gaumont, and F. M. Sirotnak pp 1786 - 1789; DOI: 10.1021/jm00159a039 |
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Studies on calcium(2+) channel antagonists. 5-[(3,4-Dimethoxyphenethyl)methylamino]-2-(3,4-dimethoxyphenyl)-2-isopropylpentyl isothiocyanate, a chemoaffinity ligand derived from verapamil Louis J. Theodore, Wendel L. Nelson, Ray H. Zobrist, Kathleen M. Giacomini, and John C. Giacomini pp 1789 - 1792; DOI: 10.1021/jm00159a040 |
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Amino-substituted p-benzoquinones Abraham E. Mathew, Robert K. Y. Zee-Cheng, and C. C. Cheng pp 1792 - 1795; DOI: 10.1021/jm00159a041 |
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4,5-Disubstituted primaquine analogues as potential antimalarial agents F. Ivy Carroll, Bertold D. Berrang, and Carl P. Linn pp 1796 - 1798; DOI: 10.1021/jm00159a042 |
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Biologically active derivatives of gossypol: synthesis and antimalarial activities of peri-acylated gossylic nitriles Robert E. Royer, Lorraine M. Deck, Naomi M. Campos, Lucy A. Hunsaker, and David L. Vander Jagt pp 1799 - 1801; DOI: 10.1021/jm00159a043 |
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Studies in antifertility agents. 50. Stereoselective binding of d- and l-centchromans to estrogen receptors and their antifertility activity M. Salman, Suprabhat Ray, Nitya Anand, A. K. Agarwal, M. M. Singh, S. S. Setty, and V. P. Kamboj pp 1801 - 1803; DOI: 10.1021/jm00159a044 |
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Inhibitors of human purine nucleoside phosphorylase. Synthesis, purine nucleoside phosphorylase inhibition, and T-cell cytotoxicity of 2,5-diaminothiazolo[5,4-d]pyrimidin-7(6H)-one and 2,5-diaminothiazolo[4,5-d]pyrimidin-7(6H)-one. Two thioisosteres of 8-aminoguanine Jagadish C. Sircar, Mark J. Suto, Mary E. Scott, Mi K. Dong, and Richard B. Gilbertsen pp 1804 - 1806; DOI: 10.1021/jm00159a045 |
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Book Reviews pp 1806 - 1808; DOI: 10.1021/jm00159a600 |
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Sustained brain-specific delivery of estradiol causes long-term suppression of luteinizing hormone secretion James W. Simpkins, Jill McCornack, Kerry S. Estes, Marcus E. Brewster, Efraim Shek, and Nicholas Bodor pp 1809 - 1812; DOI: 10.1021/jm00160a001 |
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Molecular design toward biologically significant compounds based on platelet activating factor: a highly selective agonist as a potential antihypertensive agent Masaji Ohno, Kagari Fujita, Masafumi Shiraiwa, Akihiro Izumi, Susumu Kobayashi, Hirotaka Yoshiwara, Ichiro Kudo, Keizo Inoue, and Shoshichi Nojima pp 1812 - 1814; DOI: 10.1021/jm00160a002 |
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Synthesis and inhibitory activity on carbonic anhydrase of some new sulpiride analogs studied by means of a new method Claudio Botre, Francesco Botre, Giancarlo Jommi, and Roberto Signorini pp 1814 - 1820; DOI: 10.1021/jm00160a003 |
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Functional cholesteryl binding agents: synthesis, characterization, and evaluation of antibody binding to modified phospholipid vesicles Timothy R. Carroll, Alan Davison, and Alun G. Jones pp 1821 - 1826; DOI: 10.1021/jm00160a004 |
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Structure-activity studies of 16-methoxy-16-methyl prostaglandins Umberto Guzzi, Romeo Ciabatti, Giovanna Padova, Franco Battaglia, Mario Cellentani, Adele Depaoli, Giulio Galliani, Pierfranco Schiatti, and Giuseppe Spina pp 1826 - 1832; DOI: 10.1021/jm00160a005 |
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Dihydropyridazinone cardiotonics. The discovery and inotropic activity of 1,3-dihydro-3,3-dimethyl-5-(1,4,5,6-tetrahydro-6-oxo-3-pyridazinyl)-2H-indol-2-one David W. Robertson, Joseph H. Krushinski, E. E. Beedle, V. Wyss, G. Don Pollock, Harve Wilson, Raymond F. Kauffman, and J. Scott Hayes pp 1832 - 1840; DOI: 10.1021/jm00160a006 |
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Inactivation of .gamma.-aminobutyric acid aminotransferase by (S,E)-4-amino-5-fluoropent-2-enoic acid and effect on the enzyme of (E)-3-(1-aminocyclopropyl)-2-propenoic acid Richard B. Silverman, Benedict J. Invergo, and Jacob Mathew pp 1840 - 1846; DOI: 10.1021/jm00160a007 |
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New effective gonadotropin releasing hormone antagonists with minimal potency for histamine release in vitro Jean E. Rivier, John Porter, Catherine L. Rivier, Marilyn Perrin, Anne Corrigan, William A. Hook, Reuben P. Siraganian, and Wylie W. Vale pp 1846 - 1851; DOI: 10.1021/jm00160a008 |
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Mechanism of action of the marine natural product stypoldione: evidence for reaction with sulfhydryl groups E. Timothy O'Brien, David J. Asai, Amiram Groweiss, Bruce H. Lipshutz, William Fenical, Robert S. Jacobs, and Leslie Wilson pp 1851 - 1855; DOI: 10.1021/jm00160a009 |
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Opioid agonist and antagonist bivalent ligands. The relationship between spacer length and selectivity at multiple opioid receptors P. S. Portoghese, D. L. Larson, L. M. Sayre, C. B. Yim, G. Ronsisvalle, S. W. Tam, and A. E. Takemori pp 1855 - 1861; DOI: 10.1021/jm00160a010 |
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Synthesis and biological activity of analogs of .beta.-chlornaltrexamine and .beta.-funaltrexamine at opioid receptors P. S. Portoghese, Michael D. Rein, and A. E. Takemori pp 1861 - 1864; DOI: 10.1021/jm00160a011 |
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Preparation and antitumor activity of 7-substituted 1,2-aziridinomitosenes Bhashyam S. Iyengar, William A. Remers, and William T. Bradner pp 1864 - 1868; DOI: 10.1021/jm00160a012 |
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Irreversible blockage of opioid receptor types by ester homologs of .beta.-funaltrexamine J. W. Schoenecker, A. E. Takemori, and P. S. Portoghese pp 1868 - 1871; DOI: 10.1021/jm00160a013 |
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Methotrexate analogs. 29. Effect of .gamma.-aminobutyric acid spacers between the pteroyl and glutamate moieties on enzyme binding and cell growth inhibition Andre Rosowsky, Ronald A. Forsch, James H. Freisheim, Peter V. Danenberg, Richard G. Moran, and Michael M. Wick pp 1872 - 1876; DOI: 10.1021/jm00160a014 |
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Tricyclic epines. Novel (E)- and (Z)-11H-dibenz[b,e]azepines as potential central nervous system agents. Variation of the basic side chain Gerd Steiner, Albrecht Franke, Erich Haedicke, Dieter Lenke, Hans Juergen Teschendorf, Hans Peter Hofmann, Horst Kreiskott, and Wolfgang Worstmann pp 1877 - 1888; DOI: 10.1021/jm00160a015 |
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Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics Hans Rollema, Dora Mastebroek, Haakan Wikstroem, Kjell Svensson, Arvid Carlsson, and Staffan Sundell pp 1889 - 1895; DOI: 10.1021/jm00160a016 |
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A molecular mechanics approach to the understanding of presynaptic selectivity for centrally acting dopamine receptor agonists of the phenylpiperidine series Tommy Liljefors and Haakan Wikstroem pp 1896 - 1904; DOI: 10.1021/jm00160a017 |
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Synthesis and dopaminergic binding of 2-aryldopamine analogs: phenethylamines, 3-benzazepines, and 9-(aminomethyl)fluorenes David L. Ladd, Joseph Weinstock, Margaret Wise, George W. Gessner, John L. Sawyer, and Kathryn E. Flaim pp 1904 - 1912; DOI: 10.1021/jm00160a018 |
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Synthesis and biological activities of dynorphin A analogues with opioid antagonist properties Jean E. Gairin, Honore Mazarguil, Paul Alvinerie, Serge Saint-Pierre, Jean Claude Meunier, and Jean Cros pp 1913 - 1917; DOI: 10.1021/jm00160a019 |
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Conformation and activity of tetrahydrofuran lignans and analogs as specific platelet-activating-factor antagonists Tesfaye Biftu, Nancy F. Gamble, Thomas Doebber, San Bao Hwang, Tsung Ying Shen, James Snyder, James P. Springer, and Robert Stevenson pp 1917 - 1921; DOI: 10.1021/jm00160a020 |
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Acyl, N-protected .alpha.-aminoacyl, and peptidyl derivatives as prodrug forms of the alcohol deterrent agent cyanamide Chul Hoon Kwon, Herbert T. Nagasawa, Eugene G. DeMaster, and Frances N. Shirota pp 1922 - 1929; DOI: 10.1021/jm00160a021 |
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Preparation and analgesic activity of (-)-11.alpha.-substituted 1,2,3,4,5,6-hexahydro-6.alpha.,7-(methyleneoxy)-2,6-methano-3-benzazocines Peter A. Cittern, Vijay K. Kapoor, and Robert T. Parfitt pp 1929 - 1933; DOI: 10.1021/jm00160a022 |
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Tissue distribution properties of technetium-99m-diamide-dimercaptide complexes and potential use as renal radiopharmaceuticals Sudhakar Kasina, Alan R. Fritzberg, Dennis L. Johnson, and Dennis Eshima pp 1933 - 1940; DOI: 10.1021/jm00160a023 |
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Cholecystokinin antagonists. Synthesis of asperlicin analogs with improved potency and water solubility Mark G. Bock, Robert M. DiPardo, Kenneth E. Rittle, Ben E. Evans, Roger M. Freidinger, Daniel F. Veber, Raymond S. L. Chang, Tsing Bau Chen, Maureen E. Keegan, and Victor J. Lotti pp 1941 - 1945; DOI: 10.1021/jm00160a024 |
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Cardiac glycosides. 7. Sugar stereochemistry and cardiac glycoside activity Hargovind Rathore, Arthur H. L. From, Khalil Ahmed, and Dwight S. Fullerton pp 1945 - 1952; DOI: 10.1021/jm00160a025 |
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Synthesis of novel angiotensin converting enzyme inhibitor quinapril and related compounds. A divergence of structure-activity relationships for non-sulfhydryl and sulfhydryl types Sylvester Klutchko, C. John Blankley, Robert W. Fleming, Jack M. Hinkley, Ann E. Werner, Ivan Nordin, Ann Holmes, Milton L. Hoefle, David M. Cohen, and et al. pp 1953 - 1961; DOI: 10.1021/jm00160a026 |
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Tuftsin analogs: synthesis, structure-function relationships, and implications for specificity of tuftsin's bioactivity Shlomo Dagan, Philip Gottlieb, Esther Tzehoval, Michael Feldman, Mati Fridkin, Koichi Yasumura, Kenji Okamoto, and Haruaki Yajima pp 1961 - 1968; DOI: 10.1021/jm00160a027 |
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Role of the C-terminal carboxylate in angiotensin II activity: alcohol, ketone, and ester analogs of angiotensin II Kun Hwa Hsieh and Garland R. Marshall pp 1968 - 1971; DOI: 10.1021/jm00160a028 |
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Conformationally defined adrenergic agents. 9. Binding requirements of phenolic phenylethylamines in the benzonorbornene skeleton at the active site of phenylethanolamine N-methyltransferase Gary L. Grunewald, William J. Bartlett, Thomas J. Reitz, Daniel J. Sall, and Hugh S. Arrington pp 1972 - 1982; DOI: 10.1021/jm00160a029 |
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Synthesis and adrenergic activity of ring-fluorinated phenylephrines Kenneth L. Kirk, Olarangbe Olubajo, Konstantin Buchhold, Gail A. Lewandowski, Fabian Gusovsky, David McCulloh, John W. Daly, and Cyrus R. Creveling pp 1982 - 1988; DOI: 10.1021/jm00160a030 |
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Cyclic analogs of 2-amino-4-phosphonobutanoic acid (APB) and their inhibition of hippocampal excitatory transmission and displacement of [3H]APB binding Stephen L. Crooks, Michael B. Robinson, James F. Koerner, and Rodney L. Johnson pp 1988 - 1995; DOI: 10.1021/jm00160a031 |
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Alkyl-substituted thiolo-, thiono-, and dithio-.gamma.-butyrolactones: new classes of convulsant and anticonvulsant agents Jeffrey A. Levine, James A. Ferrendelli, and Douglas F. Covey pp 1996 - 1999; DOI: 10.1021/jm00160a032 |
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.alpha.-Adrenoreceptor reagents. 4. Resolution of some potent selective prejunctional .alpha.2-adrenoreceptor antagonists Anthony P. Welbourn, Christopher B. Chapleo, Anthony C. Lane, Peter L. Myers, Alan G. Roach, Colin F. C. Smith, Michael R. Stillings, and Ian F. Tulloch pp 2000 - 2003; DOI: 10.1021/jm00160a033 |
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Chemical and stereochemical aspects of propranolol metabolism. Diastereomeric 1-(1-hydroxy-2-propylamino)-3-(1-naphthoxy)-2-propanols produced by rat liver microsomal .omega.-hydroxylation H. Umesha Shetty and Wendel L. Nelson pp 2004 - 2008; DOI: 10.1021/jm00160a034 |
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Derivatives of 1-(1,3-benzodioxol-5-yl)-2-butanamine: representatives of a novel therapeutic class David E. Nichols, Andrew J. Hoffman, Robert A. Oberlender, Peyton Jacob, and Alexander T. Shulgin pp 2009 - 2015; DOI: 10.1021/jm00160a035 |
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Assessment of a potential dopaminergic prodrug moiety in several ring systems Joseph G. Cannon, David C. Furlano, Russell G. Dushin, Yu An Chang, Stephen R. Baird, Laila N. Soliman, Jan R. Flynn, John Paul Long, and Ranbir K. Bhatnagar pp 2016 - 2020; DOI: 10.1021/jm00160a036 |
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Studies on prodrugs. 5. Synthesis and antimicrobial activity of N-(oxoalkyl)norfloxacin derivatives Hirosato Kondo, Fumio Sakamoto, Yasuo Kodera, and Goro Tsukamoto pp 2020 - 2024; DOI: 10.1021/jm00160a037 |
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Synthesis and aldose reductase inhibitory activity of substituted 2-oxoquinoline-1-acetic acid derivatives Jack DeRuiter, Abram N. Brubaker, William L. Whitmer, and James L. Stein pp 2024 - 2028; DOI: 10.1021/jm00160a038 |
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Stereochemical studies on medicinal agents. 30. Investigation of 4-(3-hydroxyphenyl)-4-methylpipecolic acid as a conformationally restricted mimic of the tyrosyl residue of leucine-enkephalinamide Elizabeth E. Sugg and Philip S. Portoghese pp 2028 - 2033; DOI: 10.1021/jm00160a039 |
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Synthesis of 8-amino-3-deazaguanine via imidazole precursors. Antitumor activity and inhibition of purine nucleoside phosphorylase David A. Berry, Richard B. Gilbertsen, and P. Dan Cook pp 2034 - 2037; DOI: 10.1021/jm00160a040 |
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Nucleoside conjugates. 7. Synthesis and antitumor activity of 1-.beta.-D-arabinofuranosylcytosine conjugates of ether lipids Chung Il Hong, Seung Ho An, David J. Buchheit, Alexander Nechaev, Alan J. Kirisits, Charles R. West, and Wolfgang E. Berdel pp 2038 - 2044; DOI: 10.1021/jm00160a041 |
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Chiral DNA gyrase inhibitors. 1. Synthesis and antimicrobial activity of the enantiomers of 6-fluoro-7-(1-piperazinyl)-1-(2-trans-phenylcyclopropyl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid Lester A. Mitscher, Padam N. Sharma, Daniel T. W. Chu, Linus L. Shen, and Andre G. Pernet pp 2044 - 2047; DOI: 10.1021/jm00160a042 |
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Nitrobenzyl derivatives as bioreductive alkylating agents: evidence for the reductive formation of a reactive intermediate D. L. Kirkpatrick, K. E. Johnson, and A. C. Sartorelli pp 2048 - 2052; DOI: 10.1021/jm00160a043 |
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Synthesis and estrogen receptor binding of 6,7-dihydro-8-phenyl-9-[4-[2-(dimethylamino)ethoxy]phenyl]-5H-benzocycloheptene, a nonisomerizable analog of tamoxifen. X-ray crystallographic studies Raymond McCague, Reiko Kuroda, Guy Leclercq, and Susanna Stoessel pp 2053 - 2059; DOI: 10.1021/jm00160a044 |
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Chloroalanyl antibiotic peptides: antagonism of their antimicrobial effects by L-alanine and L-alanyl peptides in gram-negative bacteria Kam Sing Cheung, William Boisvert, Stephen A. Lerner, and Michael Johnston pp 2060 - 2068; DOI: 10.1021/jm00160a045 |
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Synthesis and biochemical properties of 8-amino-6-fluoro-9-.beta.-D-ribofuranosyl-9H-purine John A. Secrist, L. Lee Bennett, Paula W. Allan, Lucy M. Rose, Chi Hsiung Chang, and John A. Montgomery pp 2069 - 2074; DOI: 10.1021/jm00160a046 |
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N-(Cyanomethyl)- and N-(2-methoxy-1-cyanoethyl)anthracyclines and related carboxyl derivatives Edward M. Acton, George L. Tong, Dorris L. Taylor, David G. Streeter, Joyce A. Filppi, and Richard L. Wolgemuth pp 2074 - 2079; DOI: 10.1021/jm00160a047 |
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Design and synthesis of potent and specific renin inhibitors containing difluorostatine, difluorostatone, and related analogs Suvit Thaisrivongs, Donald T. Pals, Warren M. Kati, Steve R. Turner, Lisa M. Thomasco, and William Watt pp 2080 - 2087; DOI: 10.1021/jm00160a048 |
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Design and synthesis of a potent and specific renin inhibitor with a prolonged duration of action in vivo Suvit Thaisrivongs, Donald T. Pals, Douglas W. Harris, Warren M. Kati, and Steve R. Turner pp 2088 - 2093; DOI: 10.1021/jm00160a049 |
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Neuroleptics from the 4a,9b-cis- and 4a,9b-trans-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole series. 2 Willard M. Welch, Charles A. Harbert, Albert Weissman, and B. Kenneth Koe pp 2093 - 2099; DOI: 10.1021/jm00160a050 |
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Dopamine receptor modulation by Pro-Leu-Gly-NH2 analogs possessing cyclic amino acid residues at the C-terminal position Rodney L. Johnson, G. Rajakumar, and Ram K. Mishra pp 2100 - 2104; DOI: 10.1021/jm00160a051 |
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Synthesis of Pro-Leu-Gly-NH2 analogs modified at the prolyl residue and evaluation of their effects on the receptor binding activity of the central dopamine receptor agonist, ADTN Rodney L. Johnson, G. Rajakumar, Kuo Long Yu, and Ram K. Mishra pp 2104 - 2107; DOI: 10.1021/jm00160a052 |
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Neuroleptics from the 4a,9b-trans-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole series. 3. Carboxamidoalkyl derivatives Willard M. Welch, Charles A. Harbert, Reinhard Sarges, Albert Weissman, and B. Kenneth Koe pp 2108 - 2111; DOI: 10.1021/jm00160a053 |
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3,7-Diazabicyclane. A new narcotic analgesic Paul S. Salva, Gilbert J. Hite, Richard A. Heyman, and Gerald Gianutsos pp 2111 - 2113; DOI: 10.1021/jm00160a054 |
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Synthesis of sulfur analogs of alkyl lysophospholipid and neoplastic cell growth inhibitory properties Susan Morris-Natschke, Jefferson R. Surles, Larry W. Daniel, Michael E. Berens, Edward J. Modest, and Claude Piantadosi pp 2114 - 2117; DOI: 10.1021/jm00160a055 |
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Synthesis of 10-acetyl-5,8-dideazafolic acid: a potent inhibitor of glycinamide ribonucleotide transformylase C. A. Caperelli and J. Conigliaro pp 2117 - 2119; DOI: 10.1021/jm00160a056 |
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N-(2-Hydroxyethyl)doxorubicin from hydrolysis of 3'-deamino-3'-(3-cyano-4-morpholinyl)doxorubicin Edward M. Acton, George L. Tong, Thomas H. Smith, Dorris L. Taylor, David G. Streeter, John H. Peters, G. Ross Gordon, Joyce A. Filppi, Richard L. Wolgemuth, and et al. pp 2120 - 2122; DOI: 10.1021/jm00160a057 |
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Book Reviews pp 2122 - 2124; DOI: 10.1021/jm00160a600 |
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Computer-aided studies of the structure-activity relationships between the structure of some steroids and their antiinflammatory activity Terry R. Stouch and Peter C. Jurs pp 2125 - 2136; DOI: 10.1021/jm00161a001 |
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Probes for narcotic receptor mediated phenomena. 13. Potential irreversible narcotic antagonist-based ligands derived from 6,14-endo-ethenotetrahydrooripavine with 7-(methoxyfumaroyl)amino, (bromoacetyl)amino, or isothiocyanate electrophiles: chemistry, biochemistry, and pharmacology Ralph A. Lessor, Balbir S. Bajwa, Kenner C. Rice, Arthur E. Jacobson, Richard A. Streaty, Werner A. Klee, Charles B. Smith, Mario D. Aceto, Everette L. May, and Louis S. Harris pp 2136 - 2141; DOI: 10.1021/jm00161a002 |
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Cardiotonic agents. 4. Synthesis and biological evaluation of N-substituted 2,4,4a,5-tetrahydro-3H-indeno[1,2-c]pyridazin-3-ones: rigid structures derived from CI-930 and analogs Ila Sircar, Bradley L. Duell, Michael H. Cain, Sandra E. Burke, and James A. Bristol pp 2142 - 2148; DOI: 10.1021/jm00161a003 |
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Docking flexible ligands to macromolecular receptors by molecular shape Renee L. DesJarlais, Robert P. Sheridan, J. Scott Dixon, Irwin D. Kuntz, and R. Venkataraghavan pp 2149 - 2153; DOI: 10.1021/jm00161a004 |
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Bioisosteric prototype design of biaryl imidazolyl and triazolyl competitive histamine H2-receptor antagonists Christopher A. Lipinski, John L. LaMattina, and P. J. Oates pp 2154 - 2163; DOI: 10.1021/jm00161a005 |
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Synthesis of congeners and prodrugs of the benzene maleimide photoadduct, mitindomide, as potential antitumor agents. 2 Howard M. Deutsch, Leslie T. Gelbaum, Mark McLaughlin, Thomas J. Fleischmann, Laurence L. Earnhart, Rudiger D. Haugwitz, and Leon H. Zalkow pp 2164 - 2170; DOI: 10.1021/jm00161a006 |
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Comparative antiaggregatory activity in human platelets of a benzopyranone aci-reductone, clofibric acid, and a 2,3-dihydrobenzofuran analog Donald T. Witiak, Sung K. Kim, Karl Romstedt, Howard A. I. Newman, and Dennis R. Feller pp 2170 - 2174; DOI: 10.1021/jm00161a007 |
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Nonquaternary cholinesterase reactivators. 3. 3(5)-Substituted 1,2,4-oxadiazol-5(3)-aldoximes and 1,2,4-oxadiazole-5(3)-thiocarbohydroximates as reactivators of organophosphonate-inhibited eel and human acetylcholinesterase in vitro Clifford D. Bedford, Robert A. Howd, Oliver D. Dailey, Alexi Miller, Harold W. Nolen, Richard A. Kenley, John R. Kern, and John S. Winterle pp 2174 - 2183; DOI: 10.1021/jm00161a008 |
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Alkylglycidic acids: potential new hypoglycemic agents Winston Ho, Gene F. Tutwiler, Sandra C. Cottrell, Dave J. Morgans, Okan Tarhan, and Richard J. Mohrbacher pp 2184 - 2190; DOI: 10.1021/jm00161a009 |
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Conformationally restricted congeners of hypotensive and platelet aggregation inhibitors: 6-aryl-5-methyl-4,5-dihydro-3(2H)-pyridazinones derived from 5H-indeno[1,2-c]pyridazine Giorgio Cignarella, Daniela Barlocco, Gerard A. Pinna, Mario Loriga, Odoardo Tofanetti, Mauro Germini, and Franca Sala pp 2191 - 2194; DOI: 10.1021/jm00161a010 |
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Synthesis and antihypertensive activity of 4-(cyclic amido)-2H-1-benzopyrans Valerie A. Ashwood, Robin E. Buckingham, Frederick Cassidy, John M. Evans, Erol A. Faruk, Thomas C. Hamilton, David J. Nash, Geoffrey Stemp, and Kenneth Willcocks pp 2194 - 2201; DOI: 10.1021/jm00161a011 |
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Phenethyl ester derivative analogs of the C-terminal tetrapeptide of gastrin as potent gastrin antagonists Jean Martinez, Marc Rodriguez, Jean Pierre Bali, and Jeanine Laur pp 2201 - 2206; DOI: 10.1021/jm00161a012 |
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A two-component approach to predicting antitumor activity from chemical structure in large-scale screening Louis Hodes pp 2207 - 2212; DOI: 10.1021/jm00161a013 |
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Antibacterial activity of phosphono dipeptides related to alafosfalin Barbara Lejczak, Pawel Kafarski, Helena Sztajer, and Przemyslaw Mastalerz pp 2212 - 2217; DOI: 10.1021/jm00161a014 |
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Synthesis and radioprotective activity of new cysteamine and cystamine derivatives J. Oiry, J. Y. Pue, J. L. Imbach, M. Fatome, H. Sentenac-Roumanou, and C. Lion pp 2217 - 2225; DOI: 10.1021/jm00161a015 |
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In the search for new anticancer drugs. 19. A predictive design of N,N:N',N':N",N"-tri-1,2-ethanediylphosphoric triamide (TEPA) analogues George Sosnovsky, N. Uma Maheswara Rao, and Shu Wen Li pp 2225 - 2230; DOI: 10.1021/jm00161a016 |
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Synthesis and antitumor activity of certain 3-.beta.-D-ribofuranosyl-1,2,4-triazolo[3,4-f]-1,2,4-triazines related to formycin prepared via ring closure of a 1,2,4-triazine precursor Kandasamy Ramasamy, Bheemarao G. Ugarkar, Patricia A. McKernan, Roland K. Robins, and Ganapathi R. Revankar pp 2231 - 2235; DOI: 10.1021/jm00161a017 |
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10-Acetyl-10-hydroxyxantho[2,3-f]tetralin 8-glycosides as angular chromophore analogs of anthracyclines: synthesis, redox properties, microsomal oxygen consumption, and antileukemic evaluation J. William Lown, Sham M. Sondhi, and James A. Plambeck pp 2235 - 2241; DOI: 10.1021/jm00161a018 |
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Vinylogous carbinolamine tumor inhibitors. 19. Synthesis and antineoplastic activity of bis[[[(alkylamino)carbonyl]oxy]methyl]-substituted 3-pyrrolines as prodrugs of tumor inhibitory pyrrolebis(carbamates) Wayne K. Anderson and Arnold S. Milowsky pp 2241 - 2249; DOI: 10.1021/jm00161a019 |
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Selective monoamine oxidase inhibitors. 4. 4-Aminophenethylamine derivatives with neuron-selective action Lennart Florvall, Ingrid Fagervall, Anna Lena Ask, and Svante B. Ross pp 2250 - 2256; DOI: 10.1021/jm00161a020 |
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Syntheses of 3',4'-dihydroxy-5,6,7- and 5,7,8-trioxygenated 3',4'-dihydroxy flavones having alkoxy groups and their inhibitory activities against arachidonate 5-lipoxygenase Tokunaru Horie, Masao Tsukayama, Hiroki Kourai, Chieko Yokoyama, Masayuki Furukawa, Tanihiro Yoshimoto, Shozo Yamamoto, Shigekatsu Watanabe-Kohno, and Katsuya Ohata pp 2256 - 2262; DOI: 10.1021/jm00161a021 |
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Studies on 1,2,3-triazoles. 13. (Piperazinylalkoxy)-[1]benzopyrano[2,3-d]-1,2,3-triazol-9(1H)-ones with combined H1-antihistamine and mast cell stabilizing properties Derek R. Buckle, Caroline J. M. Rockell, Harry Smith, and Barbara A. Spicer pp 2262 - 2267; DOI: 10.1021/jm00161a022 |
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Comparison of (-)-eseroline with (+)-eseroline and dihydroseco analogs in antinociceptive assays: confirmation of rubreserine structure by x-ray analysis Bernhard Schonenberger, Arthur E. Jacobson, Arnold Brossi, Richard Streaty, Werner A. Klee, Judith L. Flippen-Anderson, and Richard Gilardi pp 2268 - 2273; DOI: 10.1021/jm00161a023 |
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Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines Christopher B. Chapleo, Malcolm Myers, Peter L. Myers, John F. Saville, Alan C. B. Smith, Michael R. Stillings, Ian F. Tulloch, Donald S. Walter, and Anthony P. Welbourn pp 2273 - 2280; DOI: 10.1021/jm00161a024 |
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Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 2. Aminoalkyl derivatives Michael R. Stillings, Anthony P. Welbourn, and Donald S. Walter pp 2280 - 2284; DOI: 10.1021/jm00161a025 |
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Structure-activity studies of 4,6-disubstituted 2-(morpholinocarbonyl)furo[3,2-b]indole derivatives with analgesic and antiinflammatory activities Yutaka Kawashima, Fusao Amanuma, Masakazu Sato, Shigeru Okuyama, Yoshimoto Nakashima, Kaoru Sota, and Ikuo Moriguchi pp 2284 - 2290; DOI: 10.1021/jm00161a026 |
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Synthetic 1,4-disubstituted 1,4-dihydro-5H-tetrazol-5-one derivatives of fentanyl: Alfentanil (R 39209), a potent, extremely short-acting narcotic analgesic Frans Janssens, Joseph Torremans, and Paul A. J. Janssen pp 2290 - 2297; DOI: 10.1021/jm00161a027 |
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Azasteroids: structure-activity relationships for inhibition of 5.alpha.-reductase and of androgen receptor binding Gary H. Rasmusson, Glenn F. Reynolds, Nathan G. Steinberg, Edward Walton, Gool F. Patel, Tehming Liang, Margaret A. Cascieri, Anne H. Cheung, Jerry R. Brooks, and Charles Berman pp 2298 - 2315; DOI: 10.1021/jm00161a028 |
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Synthesis and renal vasodilator activity of some dopamine agonist 1-aryl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diols: halogen and methyl analogs of fenoldopam Joseph Weinstock, David L. Ladd, James W. Wilson, Charles K. Brush, Nelson C. F. Yim, Gregory Gallagher Jr., Mary E. McCarthy, Joanne Silvestri, Henry M. Sarau, and et al. pp 2315 - 2325; DOI: 10.1021/jm00161a029 |
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Analgetic and antiinflammatory 7-aroylbenzofuran-5-ylacetic acids and 7-aroylbenzothiophene-5-ylacetic acids James P. Dunn, Neil A. Ackerman, and Albert J. Tomolonis pp 2326 - 2329; DOI: 10.1021/jm00161a030 |
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Synthesis and antiallergic activity of a novel series of 5-lipoxygenase inhibitors Kenneth L. Kees, John H. Musser, Joseph Chang, Maureen Skowronek, and Alan J. Lewis pp 2329 - 2334; DOI: 10.1021/jm00161a031 |
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9,11-Epoxy-9-homo-14-oxaprosta-5-enoic acid derivatives. Novel inhibitors of fatty acid cyclooxygenase Steven E. Hall, Wen Ching Han, Martin F. Haslanger, Don N. Harris, and Martin L. Ogletree pp 2335 - 2347; DOI: 10.1021/jm00161a032 |
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Antiinflammatory and aldose reductase inhibitory activity of some tricyclic arylacetic acids Mary Jane Cerelli, Daniel L. Curtis, James P. Dunn, Peter H. Nelson, Tina M. Peak, and L. David Waterbury pp 2347 - 2351; DOI: 10.1021/jm00161a033 |
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Furanose-pyranose isomerization of reduced pyrimidine and cyclic urea ribosides James A. Kelley, John S. Driscoll, John J. McCormack, Jeri S. Roth, and Victor E. Marquez pp 2351 - 2358; DOI: 10.1021/jm00161a034 |
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Plant antitumor agents. 23. Synthesis and antileukemic activity of camptothecin analogs Mansukh C. Wani, Allan W. Nicholas, and Monroe E. Wall pp 2358 - 2363; DOI: 10.1021/jm00161a035 |
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Synthesis and structure-activity relationships of new arylfluoronaphthyridine antibacterial agents Daniel T. W. Chu, Prabhavathi B. Fernandes, Akiyo K. Claiborne, Eugene H. Gracey, and Andre G. Pernet pp 2363 - 2369; DOI: 10.1021/jm00161a036 |
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Design and synthesis of conformationally constrained somatostatin analogs with high potency and specificity for .mu. opioid receptors John T. Pelton, Wieslaw Kazmierski, Karoly Gulya, Henry I. Yamamura, and Victor J. Hruby pp 2370 - 2375; DOI: 10.1021/jm00161a037 |
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5-HT1 and 5-HT2: binding characteristics of some quipazine analogs Richard A. Glennon, R. M. Slusher, Robert A. Lyon, Milt Titeler, and J. D. McKenney pp 2375 - 2380; DOI: 10.1021/jm00161a038 |
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6,7-Dichloro-1-(3,4,5-trimethoxybenzyl)-1,2,3,4-tetrahydroisoquinoline. A structurally novel .beta.-adrenergic receptor blocking agent Carl Kaiser, Hye Ja Oh, Blanche J. Garcia-Slanga, Anthony C. Sulpizio, J. Paul Hieble, Joyce E. Wawro, and Lawrence I. Kruse pp 2381 - 2384; DOI: 10.1021/jm00161a039 |
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Synthesis and biological evaluation of irreversible inhibitors of aldose reductase Jeffrey J. Ares, Peter F. Kador, and Duane D. Miller pp 2384 - 2389; DOI: 10.1021/jm00161a040 |
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9-(2-Deoxy-2-fluoro-.beta.-D-arabinofuranosyl)guanine: a metabolically stable cytotoxic analogue of 2'-deoxyguanosine John A. Montgomery, Anita T. Shortnacy, Dennis A. Carson, and John A. Secrist pp 2389 - 2392; DOI: 10.1021/jm00161a041 |
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Vinylogous carbinolamine tumor inhibitors. 20. Comparison of the chemical reactivities and antineoplastic activities of .alpha.,.beta.-, .alpha.,.beta.'-, .beta.,.beta.'- and .alpha.,.alpha.'-bis[[[(2-propylamino)carbonyl]oxy]methyl] substituted pyrroles Wayne K. Anderson and Arvela R. Heider pp 2392 - 2395; DOI: 10.1021/jm00161a042 |
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Comparative pharmacology in the rat of ketamine and its two principal metabolites, norketamine and (Z)-6-hydroxynorketamine Louis Y. Leung and Thomas A. Baillie pp 2396 - 2399; DOI: 10.1021/jm00161a043 |
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Carbocyclic purmocyin: synthesis and inhibition of protein biosynthesis Robert Vince, Susan Daluge, and Jay Brownell pp 2400 - 2403; DOI: 10.1021/jm00161a044 |
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3-(1H-Tetrazol-5-yl)-4(3H)-quinazolinone sodium salt (MDL 427): a new antiallergic agent Norton P. Peet, Larry E. Baugh, Shyam Sunder, Jon E. Lewis, Emily H. Matthews, Edward L. Olberding, and Dhiren N. Shah pp 2403 - 2409; DOI: 10.1021/jm00161a045 |
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Structure and solution conformation of the cytostatic cyclic tetrapeptide WF-3161, cyclo[L-leucyl-L-pipecolyl-L-(2-amino-8-oxo-9,10-epoxydecanoyl)-D-phenylalanyl] Megumi Kawai, Richard S. Pottorf, and Daniel H. Rich pp 2409 - 2411; DOI: 10.1021/jm00161a046 |
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Molecular determinants for the agonist activity of 2-methylhistamine and 4-methylhistamine at H2-receptors Patricia Reggio, Sid Topiol, and Harel Weinstein pp 2412 - 2415; DOI: 10.1021/jm00161a047 |
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2,3-Dialkyl(dimethylamino)indoles: interaction with 5HT1, 5HT2, and rat stomach fundal serotonin receptors Pawel Fludzinski, Laura A. Wittenauer, Kathryn W. Schenck, and Marlene L. Cohen pp 2415 - 2418; DOI: 10.1021/jm00161a048 |
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Book Reviews pp 2418 - 2424; DOI: 10.1021/jm00161a600 |
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Potent antagonists of vasopressin antidiuretic activity that lack the .beta.,.beta.-cyclopentamethylene-.beta.-mercaptopropionic acid substitution at position 1 Nelson C. F. Yim, Michael L. Moore, William F. Huffman, Heidi G. Bryan, Hsin Lan Chang, Lewis B. Kinter, Richard Edwards, Frans L. Stassen, Dulcie Schmidt, and Grace Heckman pp 2425 - 2426; DOI: 10.1021/jm00162a001 |
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Cardiotonic agents. 1. Synthesis and structure-activity relationships in a new class of 3-, 4- and 5-pyridyl-2(1H)-quinolone derivatives Gerard Leclerc, Gilbert Marciniak, Nicole Decker, and Jean Schwartz pp 2427 - 2432; DOI: 10.1021/jm00162a002 |
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Cardiotonic agents. 2. Synthesis and structure-activity relationships in a new class of 6-, 7-, and 8-pyridyl-2(1H)-quinolone derivatives Gerard Leclerc, Gilbert Marciniak, Nicole Decker, and Jean Schwartz pp 2433 - 2438; DOI: 10.1021/jm00162a003 |
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Spin trapping of superoxide and hydroxyl radicals with substituted pyrroline 1-oxides Marvin J. Turner and Gerald M. Rosen pp 2439 - 2444; DOI: 10.1021/jm00162a004 |
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Synthesis and antiviral evaluation of 1,4-dioxane nucleoside analogs related to nucleoside dialdehydes Ernest J. Prisbe pp 2445 - 2450; DOI: 10.1021/jm00162a005 |
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Theoretical study of the binding of polychlorinated biphenyls (PCBs), dibenzodioxins and dibenzofuran to human plasma prealbumin L. G. Pedersen, T. A. Darden, S. J. Oatley, and J. D. McKinney pp 2451 - 2457; DOI: 10.1021/jm00162a006 |
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Potential tumor- or organ-imaging agents. 27. Polyiodinated 1,3-disubstituted and 1,2,3-trisubstituted triacylglycerols Jamey P. Weichert, Michael P. Groziak, Marc A. Longino, Susan W. Schwendner, and Raymond E. Counsell pp 2457 - 2465; DOI: 10.1021/jm00162a007 |
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Multisubstrate inhibitors of dopamine .beta.-hydroxylase. 1. Some 1-phenyl and 1-phenyl-bridged derivatives of imidazole-2-thione Lawrence I. Kruse, Carl Kaiser, Walter E. DeWolf, James S. Frazee, Eleanor Garvey, Eileen L. Hilbert, Wayne A. Faulkner, Kathryn E. Flaim, John L. Sawyer, and Barry A. Berkowitz pp 2465 - 2472; DOI: 10.1021/jm00162a008 |
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Antitumor activity of (2-alkoxyalkyl)- and (2-alkoxyalkenyl)phosphocolines Rosanne Bonjouklian, Michael L. Phillips, Kathy M. Kuhler, Gerlad B. Grindey, Gerald A. Poore, Richard M. Schultz, and Marilyn G. Altom pp 2472 - 2477; DOI: 10.1021/jm00162a009 |
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Chemically stable homocinnamyl analogs of the leukotrienes: synthesis and preliminary biological evaluation P. R. Bernstein, D. W. Snyder, E. J. Adams, R. D. Krell, E. P. Vacek, and A. K. Willard pp 2477 - 2483; DOI: 10.1021/jm00162a010 |
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Molecular mechanics simulations on covalent complexes between anthramycin and B DNA Shashidhar Rao, U. Chandra Singh, and Peter A. Kollman pp 2484 - 2492; DOI: 10.1021/jm00162a011 |
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Conformations of complexes between pyrrolo[1,4]benzodiazepines and DNA segments William A. Remers, Massimo Mabilia, and Anton J. Hopfinger pp 2492 - 2503; DOI: 10.1021/jm00162a012 |
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Stereoselectivity of a potent calcium antagonist, 1-benzyl-3-pyrrolidinyl methyl 2,6-dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate Kazuharu Tamazawa, Hideki Arima, Tadao Kojima, Yasuo Isomura, Minoru Okada, Shigeo Fujita, Toshio Furuya, Toichi Takenaka, Osamu Inagaki, and Michio Terai pp 2504 - 2511; DOI: 10.1021/jm00162a013 |
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Substituted-vinyl hydroxytriarylethylenes, 1-[4-[2-(diethylamino)ethoxy]phenyl]-1-(4-hydroxyphenyl)-2-phenylethylenes: synthesis and effects on MCF 7 breast cancer cell proliferation Peter C. Ruenitz, Jerome R. Bagley, Colin K. W. Watts, Rosemary E. Hall, and Robert L. Sutherland pp 2511 - 2519; DOI: 10.1021/jm00162a014 |
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Inhibition of cathepsin D by substrate analogs containing statine and by analogs of pepstatin Nirankar S. Agarwal and Daniel H. Rich pp 2519 - 2524; DOI: 10.1021/jm00162a015 |
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Synthesis and calcium channel antagonist activity of dialkyl 1,4-dihydro-2,6-dimethyl-4-(pyridinyl)-3,5-pyridinedicarboxylates Lina Dagnino, Moy Cheong Li-Kwong-Ken, Michael W. Wolowyk, Hla Wynn, Christopher R. Triggle, and Edward E. Knaus pp 2524 - 2529; DOI: 10.1021/jm00162a016 |
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P-Dimethoxy-substituted trans-octahydrobenzo[f]- and -[g]quinolines: synthesis and assessment of dopaminergic agonist effects Joseph G. Cannon, Victor E. D. Amoo, John Paul Long, Ranbir K. Bhatnagar, and Jan R. Flynn pp 2529 - 2534; DOI: 10.1021/jm00162a017 |
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Additions and Corrections - Structure-Activity Studies on Antidepressannt 2,2-Diarylethylamines. Bruce E. Maryanoff, Samuel O. Nortey, and Joseph F. Gardocki pp 2534 - 2534; DOI: 10.1021/jm00162a600 |
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Additions and Corrections - Computer-Assisted Drug Design A. J. Hopfinger pp 2534 - 2534; DOI: 10.1021/jm00162a601 |
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Additions and Corrections - 4-[2-(Di-n-propylamino)ethyl]-2(3H)-indolone: A Prejunctional Dopamine Receptor Agonist. Gregory Gallagher, Jr., Patricia G. Lavanchy, James W. Wilson, J. Paul Hieble, and Robert M. DeMarinis pp 2534 - 2534; DOI: 10.1021/jm00162a602 |
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Additions and Corrections - New Antiarrhythmic Agents. 2,2,5,5-Tetramethyl-3-pyrroline-3-carboxamides and 2,2,5,5-Tetramethylpyrrolidine-3-carboxamides. Olga H. Hankovsky, Kálmán Hideg, Ilona Bódi, and László Frank pp 2534 - 2534; DOI: 10.1021/jm00162a603 |
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Additions and Corrections - Topical Nonsteroidal Antipsoriatic Agents. 1. 1,2,3,4-Tetraoxygenated Naphthalene Derivatives. Gordon H. Jones, Michael C. Venuti, John M. Young, D. V. Krishna Murthy, Brad E. Loe, Richard A. Simpson, Andrew H. Berks, Doreen A. Spires, Patrick J. Maloney, Myriam Kruseman, Sussan Rouhafza, Karen C. Kappas, Colin C. Beard, Stefan H. Unger, and Paul S. Cheung pp 2534 - 2534; DOI: 10.1021/jm00162a604 |
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Book Reviews pp 2534 - 2534; DOI: 10.1021/jm00162a605 |