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Volume 33
Main Index

Issue 1


Histamine H3 ligands: just pharmacological tools or potential therapeutic agents?
Hendrik Timmerman
pp 4 - 11; DOI:
10.1021/jm00163a001
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.alpha.-Diketone and .alpha.-keto ester derivatives of N-protected amino acids and peptides as novel inhibitors of cysteine and serine proteinases
Michael R. Angelastro, Shujaath Mehdi, Joseph P. Burkhart, Norton P. Peet, and Philippe Bey
pp 11 - 13; DOI:
10.1021/jm00163a002
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Aromatic thiazole derivatives: structurally novel and selective serotonin-3 receptor antagonists
Arthur A. Nagel, Terry Rosen, James Rizzi, June Daffeh, Karen Guarino, Jolanta Nowakowski, Lawrence A. Vincent, James Heym, Stafford McLean, and et al.
pp 13 - 16; DOI:
10.1021/jm00163a003
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Synthesis and anti-HIV activity of carbocyclic 2',3'-didehydro-2',3'-dideoxy 2,6-disubstituted purine nucleosides
Robert Vince and Mei Hua
pp 17 - 21; DOI:
10.1021/jm00163a004
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Inhibitors of cholesterol biosynthesis. 1. trans-6-(2-Pyrrol-1-ylethyl)-4-hydroxypyran-2-ones, a novel series of HMG-CoA reductase inhibitors. 1. Effects of structural modifications at the 2- and 5-positions of the pyrrole nucleus
Bruce D. Roth, D. F. Ortwine, M. L. Hoefle, C. D. Stratton, D. R. Sliskovic, M. W. Wilson, and R. S. Newton
pp 21 - 31; DOI:
10.1021/jm00163a005
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Inhibitors of cholesterol biosynthesis. 2. 1,3,5-Trisubstituted [2-(tetrahydro-4-hydroxy-2-oxopyran-6-yl)ethyl]pyrazoles
D. R. Sliskovic, B. D. Roth, M. W. Wilson, M. L. Hoefle, and R. S. Newton
pp 31 - 38; DOI:
10.1021/jm00163a006
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Synthesis and structural requirements of N-substituted norapomorphines for affinity and activity at dopamine D-1, D-2, and agonist receptor sites in rat brain
Yigong Gao, Vishnu J. Ram, Alexander Campbell, Nora S. Kula, Ross J. Baldessarini, and John L. Neumeyer
pp 39 - 44; DOI:
10.1021/jm00163a007
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Synthesis, structure, and antiparasitic activity of sulfamoyl derivatives of ribavirin
Ganesh D. Kini, Elizabeth M. Henry, Roland K. Robins, Steven B. Larson, J. Joseph Marr, Randolph L. Berens, Cyrus J. Bacchi, Henry C. Nathan, and Jan S. Keithly
pp 44 - 48; DOI:
10.1021/jm00163a008
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5-[(Aminoalkyl)amino]imidazo[4,5,1-de]acridin-6-ones as a novel class of antineoplastic agents. Synthesis and biological activity
Wieslaw M. Cholody, Sante Martelli, Jolanta Paradziej-Lukowicz, and Jerzy Konopa
pp 49 - 52; DOI:
10.1021/jm00163a009
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Synthesis and biological activity of new HMG-CoA reductase inhibitors. 1. Lactones of pyridine- and pyrimidine-substituted 3,5-dihydroxy-6-heptenoic (-heptanoic) acids
G. Beck, K. Kesseler, E. Baader, W. Bartmann, A. Bergmann, E. Granzer, H. Jendralla, B. Von Kerekjarto, R. Krause, and et al.
pp 52 - 60; DOI:
10.1021/jm00163a010
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Synthesis and biological activity of new HMG-CoA reductase inhibitors. 2. Derivatives of 7-(1H-pyrrol-3-yl)-substituted-3,5-dihydroxyhept-6(E)-enoic (-heptanoic) acids
H. Jendralla, E. Baader, W. Bartmann, G. Beck, A. Bergmann, E. Granzer, B. Von Kerekjarto, K. Kesseler, R. Krause, and et al.
pp 61 - 70; DOI:
10.1021/jm00163a011
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GABA agonists and uptake inhibitors. Synthesis, absolute stereochemistry, and enantioselectivity of (R)-(-)- and (S)-(+)-homo-.beta.-proline
Lone Nielsen, Lotte Brehm, and Povl Krogsgaard-Larsen
pp 71 - 77; DOI:
10.1021/jm00163a012
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Cephalosporin 3'-quinolone esters with a dual mode of action
Harry A. Albrecht, George Beskid, Ka Kong Chan, James G. Christenson, Roy Cleeland, Kenneth H. Deitcher, Nafsika H. Georgopapadakou, Dennis D. Keith, David L. Pruess, and et al.
pp 77 - 86; DOI:
10.1021/jm00163a013
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New leupeptin analogs: synthesis and inhibition data
Rose M. McConnell, George E. Barnes, Charles F. Hoyng, and J. Martin Gunn
pp 86 - 93; DOI:
10.1021/jm00163a014
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DNA intercalating properties of tetrahydro-9-aminoacridines. Synthesis and sodium-23 NMR spin-lattice relaxation time measurements
Joergen Dinesen, Jens Peter Jacobsen, Frede P. Hansen, Erik B. Pedersen, and Hanne Eggert
pp 93 - 97; DOI:
10.1021/jm00163a015
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Cyclization-activated prodrugs. Basic carbamates of 4-hydroxyanisole
Walfred S. Saari, John E. Schwering, Paulette A. Lyle, Steven J. Smith, and Edward L. Engelhardt
pp 97 - 101; DOI:
10.1021/jm00163a016
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Synthesis and biochemical studies of 7-substituted 4,6-androstadiene-3,17-diones as aromatase inhibitors
Pui Kai Li and Robert W. Brueggemeier
pp 101 - 105; DOI:
10.1021/jm00163a017
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cis-Diamineplatinum(II) complexes containing phosphono carboxylate ligands as antitumor agents
L. Steven Hollis, Arthur V. Miller, Alan R. Amundsen, John E. Schurig, and Eric W. Stern
pp 105 - 111; DOI:
10.1021/jm00163a018
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Hypoxia-selective antitumor agents. 3. Relationships between structure and cytotoxicity against cultured tumor cells for substituted N,N-bis(2-chloroethyl)anilines
Brian D. Palmer, William R. Wilson, Susan M. Pullen, and William A. Denny
pp 112 - 121; DOI:
10.1021/jm00163a019
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Synthesis and in vivo antitumor activity of 2-amino-9H-purine-6-sulfenamide, -sulfinamide, and -sulfonamide and related purine ribonucleosides
Ganapathi R. Revankar, Naeem B. Hanna, Nobutaka Imamura, Arthur F. Lewis, Steven B. Larson, Rick A. Finch, Thomas L. Avery, and Roland K. Robins
pp 121 - 128; DOI:
10.1021/jm00163a020
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A novel, nonsteroidal inhibitor of androgen binding to the rat androgen binding protein: diethyl [[[3-(2,6-dimethyl-4-pyridinyl)-4-fluorophenyl]amino]methylene]propanedioate
Richard C. Winneker, Margaret M. Wagner, and Baldev Singh
pp 129 - 132; DOI:
10.1021/jm00163a021
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Anticandidal properties of N3-(4-methoxyfumaroyl)-L-2,3-diaminopropanoic acid oligopeptides
Ryszard Andruszkiewicz, Slawomir Milewski, Teresa Zieniawa, and Edward Borowski
pp 132 - 135; DOI:
10.1021/jm00163a022
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Structure-activity relationships of antifilarial antimycin analogs: a multivariate pattern recognition study
David L. Selwood, David J. Livingstone, John C. W. Comley, Alan B. O'Dowd, Alan T. Hudson, Peter Jackson, Karamjit S. Jandu, Valerie S. Rose, and Jeremy N. Stables
pp 136 - 142; DOI:
10.1021/jm00163a023
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Synthesis and structure-activity relationships of new 7-[3-(fluoromethyl)piperazinyl]- and -(fluorohomopiperazinyl)quinolone antibacterials
Carl B. Ziegler, P. Bitha, N. A. Kuck, T. J. Fenton, P. J. Petersen, and Y. I. Lin
pp 142 - 146; DOI:
10.1021/jm00163a024
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Inhibition of monoamine oxidases A and B by simple isoquinoline alkaloids: racemic and optically active 1,2,3,4-tetrahydro-, 3,4-dihydro-, and fully aromatic isoquinolines
Michael E. Bembenek, Creed W. Abell, Linda A. Chrisey, Maria D. Rozwadowska, Wieslaw Gessner, and Arnold Brossi
pp 147 - 152; DOI:
10.1021/jm00163a025
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Indolo[2,1-a]isoquinolines. Syntheses, steroid hormone receptor binding affinities, and cytostatic activity
Reinhard Ambros, Martin R. Schneider, and Silvia Von Angerer
pp 153 - 160; DOI:
10.1021/jm00163a026
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Synthesis and anticonvulsant activity of some new 2-substituted 3-aryl-4(3H)-quinazolinones
James F. Wolfe, Terry L. Rathman, Mark C. Sleevi, James A. Campbell, and Thomas D. Greenwood
pp 161 - 166; DOI:
10.1021/jm00163a027
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Structure-activity relationship of anthracyclines in vitro
D. Hoffmann, H. G. Berscheid, D. Boettger, P. Hermentin, H. H. Sedlacek, and H. P. Kraemer
pp 166 - 171; DOI:
10.1021/jm00163a028
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Synthesis and characterization of iodobenzamide analogs: potential D-2 dopamine receptor imaging agents
Raymond A. Murphy, Hank F. Kung, Mei Ping Kung, and Jeffrey Billings
pp 171 - 178; DOI:
10.1021/jm00163a029
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Fluoro carbocyclic nucleosides: synthesis and antiviral activity of 2'- and 6'-fluoro carbocyclic pyrimidine nucleosides including carbocyclic 1-(2-deoxy-2-fluoro-.beta.-D-arabinofuranosyl)-5-methyluracil and carbocyclic 1-(2-deoxy-2-fluoro-.beta.-D-arabinofuranosyl)-5-iodouracil
Alan D. Borthwick, Derek N. Evans, Barrie E. Kirk, Keith Biggadike, Anne M. Exall, Peter Youds, Stanley M. Roberts, David J. Knight, and Jonathan A. V. Coates
pp 179 - 186; DOI:
10.1021/jm00163a030
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Synthesis and antiviral activity of 9-alkoxypurines. 1. 9-(3-Hydroxypropoxy)- and 9-[3-hydroxy-2-(hydroxymethyl)propoxy]purines
Michael R. Harnden, Paul G. Wyatt, Malcolm R. Boyd, and David Sutton
pp 187 - 196; DOI:
10.1021/jm00163a031
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Benzodiazepine receptor binding activity of 8-substituted-9-(3-substituted-benzyl)-6-(dimethylamino)-9H-purines
James L. Kelley, Ed W. McLean, James A. Linn, Mark P. Krochmal, Robert M. Ferris, and James L. Howard
pp 196 - 202; DOI:
10.1021/jm00163a032
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Structure-activity relationships of N2-substituted guanines as inhibitors of HSV1 and HSV2 thymidine kinases
Catherine Hildebrand, Daniele Sandoli, Federico Focher, Joseph Gambino, Giovanni Ciarrocchi, Silvio Spadari, and George Wright
pp 203 - 206; DOI:
10.1021/jm00163a033
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Synthesis and structure-activity relationships of dynorphin A-(1-8) amide analogs
Hiroshi Yoshino, Takahiro Nakazawa, Yoshihiro Arakawa, Takeru Kaneko, Yutaka Tsuchiya, Manabu Matsunaga, Shin Araki, Masuhiro Ikeda, Kiyomi Yamatsu, and Shinro Tachibana
pp 206 - 212; DOI:
10.1021/jm00163a034
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Synthesis and antifolate properties of 9-alkyl-10-deazaminopterins
Joseph I. DeGraw, Pamela H. Christie, Roy L. Kisliuk, Yvette Gaumont, and Francis M. Sirotnak
pp 212 - 215; DOI:
10.1021/jm00163a035
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Synthesis and .beta.-adrenergic antagonist activity of stereoisomeric practolol and propranolol derivatives
Katerina Leftheris and Murray Goodman
pp 216 - 223; DOI:
10.1021/jm00163a036
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Antihypertensive dihydropyridines with 1,4,4-trisubstitution
Michael J. Kukla, Henry J. Breslin, and Alan Gill
pp 223 - 228; DOI:
10.1021/jm00163a037
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Synthesis of thromboxane receptor antagonists with bicyclo[3.1.0]hexane ring systems
Susumu Kamata, Nobuhiro Haga, Tatsuo Tsuri, Kiyohisa Uchida, Hisato Kakushi, Hitoshi Arita, and Kohji Hanasaki
pp 229 - 239; DOI:
10.1021/jm00163a038
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N-[(Arylmethoxy)phenyl] carboxylic acids, hydroxamic acids, tetrazoles, and sulfonyl carboxamides. Potent orally active leukotriene D4 antagonists of novel structure
John H. Musser, Anthony F. Kreft, Reinhold H. W. Bender, Dennis M. Kubrak, David Grimes, Richard P. Carlson, James M. Hand, and Joseph Chang
pp 240 - 245; DOI:
10.1021/jm00163a039
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Assessment of the in vivo and in vitro opioid activity of bridged hexahydroaporphine and isoquinoline molecules
Victoria F. Roche, Edward B. Roche, Paul K. Lemcke, William S. Wire, and Thomas F. Burks
pp 245 - 248; DOI:
10.1021/jm00163a040
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[Cyclic] [D-Pen2,D-Pen5]enkephalin analogs with increased affinity and selectivity for .delta.-opioid receptors
Geza Toth, Thomas H. Kramer, Richard Knapp, George Lui, Peg Davis, Thomas F. Burks, Henry I. Yamamura, and Victor J. Hruby
pp 249 - 253; DOI:
10.1021/jm00163a041
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Alkylation of DNA by C-10 of 2,7-diaminomitosene
Bhashyam S. Iyengar, Robert T. Dorr, Nancy G. Shipp, and William A. Remers
pp 253 - 257; DOI:
10.1021/jm00163a042
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Synthesis and in vitro evaluation of some modified 4-thiopyrimidine nucleosides for prevention or reversal of AIDS - associated neurological disorders
Eduardo Palomino, Bernard R. Meltsner, David Kessel, and Jerome P. Horwitz
pp 258 - 263; DOI:
10.1021/jm00163a043
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Phosphoramidate peptide inhibitors of human skin fibroblast collagenase
Zbigniew P. Kortylewicz and Richard E. Galardy
pp 263 - 273; DOI:
10.1021/jm00163a044
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1-(Substituted-benzyl)imidazole-2(3H)thione inhibitors of dopamine .beta.-hydroxylase
Benjamin J. Burke and A. J. Hopfinger
pp 274 - 281; DOI:
10.1021/jm00163a045
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Tertiary (2-haloethyl)amine derivatives of the muscarinic agent McN-A-343, [4-[[N-(3-chlorophenyl)carbamoyl]oxy]-2-butynyl]trimethylammonium chloride
Bjoern Ringdahl, Charlotta Mellin, Frederick J. Ehlert, Margareth Roch, Kathleen M. Rice, and Donald J. Jenden
pp 281 - 286; DOI:
10.1021/jm00163a046
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Highly selective .kappa.-opioid analgesics. 3. Synthesis and structure-activity relationships of novel N-[2-(1-pyrrolidinyl)-4- or -5-substituted cyclohexyl]arylacetamide derivatives
Paul R. Halfpenny, David C. Horwell, John Hughes, John C. Hunter, and David C. Rees
pp 286 - 291; DOI:
10.1021/jm00163a047
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Cephalosporins to carbapenems: 1-oxygenated carbapenems and carbapenams
Robert L. Rosati, Leilani V. Kapili, Peter Morrissey, and James A. Retsema
pp 291 - 297; DOI:
10.1021/jm00163a048
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Cationic antiprotozoal drugs. Trypanocidal activity of 2-(4'-formylphenyl)imidazo[1,2-a]pyridinium guanylhydrazones and related derivatives of quaternary heteroaromatic compounds
Richard J. Sundberg, Daniel J. Dahlhausen, G. Manikumar, B. Mavunkel, A. Biswas, V. Srinivasan, H. A. Musallam, Willis A. Reid, and Arba L. Ager
pp 298 - 307; DOI:
10.1021/jm00163a049
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Synthesis of some 3-(1-azabicyclo[2.2.2]octyl) 3-amino-2-hydroxy-2-phenylpropionates: profile of antimuscarinic efficacy and selectivity
Vicki H. Audia, Daniel W. McPherson, Moshe Weitzberg, W. Janusz Rzeszotarski, Bonnie Sturm, James F. Kachur, Mary Abreu, and Carl Kaiser
pp 307 - 310; DOI:
10.1021/jm00163a050
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4-(1,2,5,6-Tetrahydro-1-alkyl-3-pyridinyl)-2-thiazolamines: a novel class of compounds with central dopamine agonist properties
Juan C. Jaen, Lawrence D. Wise, Bradley W. Caprathe, Haile Tecle, Stephen Bergmeier, Christine C. Humblet, Thomas G. Heffner, Leonard T. Meltzer, and Thomas A. Pugsley
pp 311 - 317; DOI:
10.1021/jm00163a051
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Synthesis and cardiotonic activity of novel biimidazoles
Donald P. Matthews, James R. McCarthy, Jeffrey P. Whitten, Philip R. Kastner, Charlotte L. Barney, Franklin N. Marshall, Marcia A. Ertel, Therese Burkhard, Philip J. Shea, and Takashi Kariya
pp 317 - 327; DOI:
10.1021/jm00163a052
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N-Phenyl-2-pyridinecarbothioamides as gastric mucosal protectants
William A. Kinney, Nancy E. Lee, Robert M. Blank, Christopher A. Demerson, Carol S. Sarnella, Noreen T. Scherer, G. Nabi Mir, Luis E. Borella, John F. DiJoseph, and Cheryl Wells
pp 327 - 336; DOI:
10.1021/jm00163a053
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Growth inhibition and induction of cellular differentiation of human myeloid leukemia cells in culture by carbamoyl congeners of ribavirin
Yogesh S. Sanghvi, Birendra K. Bhattacharya, Ganesh D. Kini, Steven S. Matsumoto, Steven B. Larson, Weldon B. Jolley, Roland K. Robins, and Ganapathi R. Revankar
pp 336 - 344; DOI:
10.1021/jm00163a054
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Orally effective acid prodrugs of the .beta.-lactamase inhibitor sulbactam
Arthur R. English, Dennis Girard, V. John Jasys, Robert J. Martingano, and Michael S. Kellogg
pp 344 - 347; DOI:
10.1021/jm00163a055
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Atrial natriuretic peptide receptor modulators: effects of disubstituted quinazolines on receptor binding and in vitro biological activity
Melvin J. Yu, Jefferson R. McCowan, Mitchell I. Steinberg, Sally A. Wiest, Virginia L. Wyss, and Jong Sin Horng
pp 348 - 353; DOI:
10.1021/jm00163a056
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Thymosin-like peptides as potential immunostimulants. Synthesis via the polymeric-reagent method
Michael Mokotoff, Ming Zhao, Steven M. Roth, Jean A. Shelley, Joseph N. Slavoski, and Nicola M. Kouttab
pp 354 - 360; DOI:
10.1021/jm00163a057
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2-Substituted-1-naphthols as potent 5-lipoxygenase inhibitors with topical antiinflammatory activity
Douglas G. Batt, George D. Maynard, Joseph J. Petraitis, Joan E. Shaw, William Galbraith, and Richard R. Harris
pp 360 - 370; DOI:
10.1021/jm00163a058
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Renin inhibitors based on dipeptide analogs. Incorporation of the hydroxyethylene isostere at the P2/P3 sites
Dale Kempf, Ed De Lara, Herman H. Stein, Jerome Cohen, David A. Egan, and Jacob J. Plattner
pp 371 - 374; DOI:
10.1021/jm00163a059
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Relationship between structure, conformational flexibility, and biological activity of agonists and antagonists at the N-methyl-D-aspartic acid subtype of excitatory amino acid receptors
Ulf Madsen, Lotte Brehm, Kjeld Schaumburg, Flemming S. Joergensen, and Povl Krogsgaard-Larsen
pp 374 - 380; DOI:
10.1021/jm00163a060
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6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents
Donald W. Combs, Marianne S. Rampulla, Stanley C. Bell, Dieter H. Klaubert, Alfonso J. Tobia, Robert Falotico, Barbara Haertlein, Constance Lakas-Weiss, and John B. Moore
pp 380 - 386; DOI:
10.1021/jm00163a061
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Synthesis and serotonin binding site studies of some conformationally restricted indolylethylamine analogs based on 2-amino-3-(3'-indolyl)bicyclo[2.2.2]octane
M. F. Schlecht, D. Tsarouhtsis, M. N. Lipovac, and E. A. Debler
pp 386 - 394; DOI:
10.1021/jm00163a062
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Synthesis of peptidyl fluoromethyl ketones and peptidyl .alpha.-keto esters as inhibitors of porcine pancreatic elastase, human neutrophil elastase, and rat and human neutrophil cathepsin G
Norton P. Peet, Joseph P. Burkhart, Michael R. Angelastro, Eugene L. Giroux, Shujaath Mehdi, Philippe Bey, Michael Kolb, Bernhard Neises, and Daniel Schirlin
pp 394 - 407; DOI:
10.1021/jm00163a063
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Thiazolo[4,5-d]pyrimidine nucleosides. The synthesis of certain 3-.beta.-D-ribofuranosylthiazolo[4,5-d]pyrimidines as potential immunotherapeutic agents
Katsuhiko Nagahara, Jack D. Anderson, Ganesh D. Kini, N. Kent Dalley, Steven B. Larson, Donald F. Smee, Ai Jin, Brahma S. Sharma, Weldon B. Jolley, and et al.
pp 407 - 415; DOI:
10.1021/jm00163a064
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Estrogen synthetase inhibitors. 2. Comparison of the in vitro aromatase inhibitory activity for a variety of nitrogen heterocycles substituted with diarylmethane or diarylmethanol groups
C. David Jones, Mark A. Winter, Kenneth S. Hirsch, Nancy Stamm, Harold M. Taylor, Howard E. Holden, James D. Davenport, Eriks V. Krumkalns, and Robert G. Suhr
pp 416 - 429; DOI:
10.1021/jm00163a065
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Synthesis and structure-affinity of a series of 7.alpha.-undecylestradiol derivatives: a potential vector for therapy and imaging of estrogen-receptor-positive cancers
Jean N. DaSilva and Johan E. Van Lier
pp 430 - 434; DOI:
10.1021/jm00163a066
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Antifolate and antibacterial activities of 5-substituted 2,4-diaminoquinazolines
Neil V. Harris, Christopher Smith, and Keith Bowden
pp 434 - 444; DOI:
10.1021/jm00163a067
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Synthesis and dopamine agonist properties of (+)-trans-3,4,4a,10b-tetrahydro-4-propyl-2H,5H-[1]benzopyrano[4,3-b]-1,4-oxazin-9-ol and its enantiomers
Horace A. DeWald, Thomas G. Heffner, Juan C. Jaen, David M. Lustgarten, Andrew T. McPhail, Leonard T. Meltzer, Thomas A. Pugsley, and Lawrence D. Wise
pp 445 - 450; DOI:
10.1021/jm00163a068
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Cholecystokinin-A receptor ligands based on the .kappa.-opioid agonist tifluadom
Mark G. Bock, Robert M. DiPardo, Ben E. Evans, Kenneth E. Rittle, Willie L. Whitter, Daniel F. Veber, Roger M. Freidinger, Raymond S. L. Chang, T. B. Chen, and Victor J. Lotti
pp 450 - 455; DOI:
10.1021/jm00163a069
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Editorial - Ethical Guidelines to Publication of Chemical Research
Philip S. Portoghese
pp 1 - 3; DOI:
10.1021/jm00163a600
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Book Reviews

pp 456 - 460; DOI:
10.1021/jm00163a601
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Issue 2


N5-Acetyl-N5-hydroxy-L-ornithine-derived siderophore-carbacephalosporin .beta.-lactam conjugates: iron transport mediated drug delivery
E. Kurt Dolence, Albert A. Minnick, and Marvin J. Miller
pp 461 - 464; DOI:
10.1021/jm00164a001
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Design and synthesis of 4H-3,1-benzoxazin-4-ones as potent alternate substrate inhibitors of human leukocyte elastase
Allen Krantz, Robin W. Spencer, Tim F. Tam, Teng Jiam Liak, Leslie J. Copp, Everton M. Thomas, and Steven P. Rafferty
pp 464 - 479; DOI:
10.1021/jm00164a002
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Synthesis and biological activity of novel vitamin D analogs: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1.alpha.,25-dihydroxy-26,27-dimethylvitamin D3
Harpal S. Gill, James M. Londowski, Robert A. Corradino, Alan R. Zinsmeister, and Rajiv Kumar
pp 480 - 490; DOI:
10.1021/jm00164a003
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Antitumor properties of tetrahydrobenz(a)anthraquinone derivatives
Charles E. Morreal, Ralph J. Bernacki, Marilyn Hillman, Alice Atwood, and Donna Cartonia
pp 490 - 492; DOI:
10.1021/jm00164a004
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Synthesis and antihypertensive activity of 4-(1,2-dihydro-2-oxo-1-pyridyl)-2H-1-benzopyrans and related compounds, new potassium channel activators
Rolf Bergmann and Rolf Gericke
pp 492 - 504; DOI:
10.1021/jm00164a005
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Synthesis and antiinflammatory activity of cis- and trans-6,6a,7,8,9,10,10a,11-octahydro-11-oxodibenzo[b,e]thiepinacetic and -oxepinacetic acids
Mikio Kurokawa, Hitoshi Uno, Hideo Nakamura, Fuminori Sato, and Shunsuke Naruto
pp 504 - 509; DOI:
10.1021/jm00164a006
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Aldosterone antagonists. 3. Synthesis and activities of steroidal 7.alpha.-(alkoxycarbonyl)-15,16-methylene spirolactones
Klaus Nickisch, Dieter Bittler, Henry Laurent, Wolfgang Losert, Yukishige Nishino, Ekkehard Schillinger, and Rudolf Wiechert
pp 509 - 513; DOI:
10.1021/jm00164a007
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Conformation-activity relationship of sweet molecules. Comparison of aspartame and naphthimidazolesulfonic acids
M. A. Castiglione-Morelli, F. Lelj, F. Naider, M. Tallon, T. Tancredi, and P. A. Temussi
pp 514 - 520; DOI:
10.1021/jm00164a008
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Development of a high affinity and stereoselective photoaffinity label for the D-1 dopamine receptor: synthesis and resolution of 7-[125I]iodo-8-hydroxy-3-methyl-1-(4'-azidophenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine
John L. Neumeyer, Nandkishore Baindur, Jun Yuan, Gillian Booth, Phillip Seeman, and Hyman B. Niznik
pp 521 - 526; DOI:
10.1021/jm00164a009
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Reversible inhibitors of the gastric (H+/K+)-ATPase. 1. 1-Aryl-4-methylpyrrolo[3,2-c]quinolines as conformationally restrained analogs of 4-(arylamino)quinolines
Thomas H. Brown, Robert J. Ife, David J. Keeling, Shiona M. Laing, Colin A. Leach, Michael E. Parsons, Carolyn A. Price, David R. Reavill, and Kenneth J. Wiggall
pp 527 - 533; DOI:
10.1021/jm00164a010
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New inhibitors of renin that contain novel phosphostatine Leu-Val replacements
Joseph F. Dellaria, Robert G. Maki, Herman H. Stein, Jerome Cohen, David Whittern, Kennan Marsh, Daniel J. Hoffman, Jacob J. Plattner, and Thomas J. Perun
pp 534 - 542; DOI:
10.1021/jm00164a011
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Antiulcer agents. 4-Substituted 2-guanidinothiazoles: reversible, competitive, and selective inhibitors of gastric H+,K+-ATPase
John L. LaMattina, Peter A. McCarthy, Lawrence A. Reiter, William F. Holt, and Li An Yeh
pp 543 - 552; DOI:
10.1021/jm00164a012
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Hypolipidemic activity of rifamycin derivatives
Peter Traxler, Wilhelm Kump, Klaus Mueller, and Werner Tosch
pp 552 - 560; DOI:
10.1021/jm00164a013
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Synthesis and biological activity of an acyclic analog of 5,6,7,8-tetrahydrofolic acid, N-[4-[[3-(2,4-diamino-1,6-dihydro-6-oxo-5-pyrimidinyl)propyl]amino]benzoyl]-L-glutamic acid
James L. Kelley, Ed W. McLean, Naomi K. Cohn, Mark P. Edelstein, David S. Duch, Gary K. Smith, Mary H. Hanlon, and Robert Ferone
pp 561 - 567; DOI:
10.1021/jm00164a014
PDF
Antitubulin effects of derivatives of 3-demethylthiocolchicine, methylthio ethers of natural colchicinoids, and thioketones derived from thiocolchicine. Comparison with colchicinoids
Anjum Muzaffar, Arnold Brossi, Chii M. Lin, and Ernest Hamel
pp 567 - 571; DOI:
10.1021/jm00164a015
PDF
1,2,4-Diazaphosphole nucleosides. Synthesis, structure, and antitumor activity of nucleosides with a .lambda.3 phosphorus atom
Timothy A. Riley, Steven B. Larson, Thomas L. Avery, Rick A. Finch, and Roland K. Robins
pp 572 - 576; DOI:
10.1021/jm00164a016
PDF
Hemicholinium-3 congeners as potential antagonists to organophosphate-induced toxicity
Joseph G. Cannon, M. Fethi Sahin, John Paul Long, Jan R. Flynn, and Ranbir K. Bhatnagar
pp 577 - 579; DOI:
10.1021/jm00164a017
PDF
.beta.-Lactam analogs of oxotremorine. 3- and 4-Methyl-substituted 2-azetidinones
Bjoern M. Nilsson, Bjorn Ringdahl, and Uli Hacksell
pp 580 - 584; DOI:
10.1021/jm00164a018
PDF
Long-acting dihydropyridine calcium antagonists. 4. Synthesis and structure-activity relationships for a series of basic and nonbasic derivatives of 2[(2-aminoethoxy)methyl]-1,4-dihydropyridine calcium antagonists
David Alker, Simon F. Campbell, Peter E. Cross, Roger A. Burges, Anthony J. Carter, and Donald G. Gardiner
pp 585 - 591; DOI:
10.1021/jm00164a019
PDF
Novel glutamic acid-derived cholecystokinin receptor ligands
R. M. Freidinger, W. L. Whitter, N. P. Gould, M. K. Holloway, R. S. L. Chang, and V. J. Lotti
pp 591 - 595; DOI:
10.1021/jm00164a020
PDF
Affinity of 2-(tetrahydroisoquinolin-2-ylmethyl)- and 2-(isoindolin-2-ylmethyl)imidazolines for .alpha.-adrenoceptors. Differential affinity of imidazolines for the [3H]idazoxan-labeled .alpha.2-adrenoceptor vs the [3H]yohimbine-labeled site
Robin D. Clark, Jacob Berger, Pushkal Garg, Klaus K. Weinhardt, Michael Spedding, Andrew T. Kilpatrick, Christine M. Brown, and Alison C. MacKinnon
pp 596 - 600; DOI:
10.1021/jm00164a021
PDF
Aporphines as antagonists of dopamine D-1 receptors
John M. Schaus, Robert D. Titus, Mark M. Foreman, Norman R. Mason, and Lewis L. Truex
pp 600 - 607; DOI:
10.1021/jm00164a022
PDF
Design, synthesis, testing, and quantitative structure-activity relationship analysis of substituted salicylaldehyde Schiff bases of 1-amino-3-hydroxyguanidine tosylate as new antiviral agents against coronavirus
Pou Hsiung Wang, James G. Keck, Eric J. Lien, and Michael M. C. Lai
pp 608 - 614; DOI:
10.1021/jm00164a023
PDF
Potential antisecretory antidiarrheals. 2. .alpha.2-Adrenergic 2-[(aryloxy)alkyl]imidazolines
Alan E. Moormann, Barnett S. Pitzele, P. H. Jones, Gary W. Gullikson, David Albin, Stella S. Yu, Robert G. Bianchi, Elizabeth L. Sanguinetti, Barbara Rubin, and et al.
pp 614 - 626; DOI:
10.1021/jm00164a024
PDF
Synthesis and cardiac electrophysiological activity of aryl-substituted derivatives of the class III antiarrhythmic agent sematilide. Potential class I/III agents
Gary B. Phillips, Thomas K. Morgan, Klaus Nickisch, Joan M. Lind, Robert P. Gomez, Ronald A. Wohl, Thomas M. Argentieri, and Mark E. Sullivan
pp 627 - 633; DOI:
10.1021/jm00164a025
PDF
1,9-Alkano-bridged 2,3,4,5-tetrahydro-1H-3-benzazepines with affinity for the .alpha.2-adrenoceptor and the 5-HT1A receptor
Robin D. Clark, Klaus K. Weinhardt, Jacob Berger, Lawrence E. Fisher, Christine M. Brown, Alison C. MacKinnon, Andrew T. Kilpatrick, and Michael Spedding
pp 633 - 641; DOI:
10.1021/jm00164a026
PDF
Total synthesis of the four stereoisomers of dihexadecanoyl phosphatidylinositol and the substrate stereospecificity of human erythrocyte membrane phosphatidylinositol 4-kinase
Rodney C. Young, C. Peter Downes, Drake S. Eggleston, Martin Jones, Colin H. Macphee, Kishore K. Rana, and John G. Ward
pp 641 - 646; DOI:
10.1021/jm00164a027
PDF
Design of an antithrombotic-antihypertensive agent (Wy 27569). Synthesis and evaluation of a series of 2-heteroaryl substituted dihydropyridines
John L. Archibald, Gerald Bradley, Albert Opalko, Terence J. Ward, Janet C. White, Christine Ennis, and Nicholas B. Shepperson
pp 646 - 652; DOI:
10.1021/jm00164a028
PDF
(8.beta.)-6-Methylergoline amide derivatives as serotonin antagonists: N1-substituent effects on vascular 5HT2 receptor activity
Jerry W. Misner, William L. Garbrecht, Gifford Marzoni, Kathleen R. Whitten, and Marlene L. Cohen
pp 652 - 656; DOI:
10.1021/jm00164a029
PDF
Antimitotic agents. Synthesis of imidazo[4,5-c]pyridin-6-ylcarbamates and imidazo[4,5-b]pyridin-5-ylcarbamates
Carroll Temple
pp 656 - 661; DOI:
10.1021/jm00164a030
PDF
Synthesis and biological activity of atrial natriuretic factor analogs: effect of modifications to the disulfide bridge
John DiMaio, Jorge Jaramillo, Dominik Wernic, Louis Grenier, Ewald Welchner, and Julian Adams
pp 661 - 667; DOI:
10.1021/jm00164a031
PDF
Autoxidation of the serotonergic neurotoxin 5,7-dihydroxytryptamine
Tahereh Tabatabaie, Monika Z. Wrona, and Glenn Dryhurst
pp 667 - 672; DOI:
10.1021/jm00164a032
PDF
Synthesis and antifolate properties of 10-alkyl-5,10-dideaza analogs of methotrexate and tetrahydrofolic acid
Joseph I. DeGraw, Pamela H. Christie, Roy L. Kisliuk, Yvette Gaumont, and Francis M. Sirotnak
pp 673 - 677; DOI:
10.1021/jm00164a033
PDF
Novel prodrugs which are activated to cytotoxic alkylating agents by carboxypeptidase G2
Caroline J. Springer, Pari Antoniw, Bagshawe, Frances Searle, Graham M. F. Bisset, and Michael Jarman
pp 677 - 681; DOI:
10.1021/jm00164a034
PDF
The preparation of 2'-deoxy-2'-fluoro-1',2'-seconucleosides as potential antiviral agents
Purushotham Vemishetti, Racha Saibaba, Raymond P. Panzica, and Elie Abushanab
pp 681 - 686; DOI:
10.1021/jm00164a035
PDF
Structure-activity correlations for psychotomimetics. 1. Phenylalkylamines: electronic, volume, and hydrophobicity parameters
Brian W. Clare
pp 687 - 702; DOI:
10.1021/jm00164a036
PDF
Nonneurotoxic tetralin and indan analogs of 3,4-(methylenedioxy)amphetamine (MDA)
David E. Nichols, William K. Brewster, Michael P. Johnson, Robert Oberlender, and Robert M. Riggs
pp 703 - 710; DOI:
10.1021/jm00164a037
PDF
Folate analogs. 33. Synthesis of folate and antifolate poly-.gamma.-glutamates by [(9-fluorenylmethoxy)oxy]carbonyl chemistry and biological evaluation of certain methotrexate polyglutamate polylysine conjugates as inhibitors of the growth of H35 hepatoma cells
Ann Abraham, M. G. Nair, R. L. Kisliuk, J. Galivan, and Y. Gaumont
pp 711 - 717; DOI:
10.1021/jm00164a038
PDF
Synthesis and antiviral and cytotoxic activity of iodohydrin and iodomethoxy derivatives of 5-vinyl-2'-deoxyuridines, 2'-fluoro-2'-deoxyuridine, and uridine
Rakesh Kumar, Lihua Xu, Edward E. Knaus, Leonard I. Wiebe, Dorothy R. Tovell, D. Lorne Tyrrell, and Theresa M. Allen
pp 717 - 723; DOI:
10.1021/jm00164a039
PDF
Synthesis and inhibitory potency of peptides corresponding to the subunit 2 C-terminal region of herpes virus ribonucleotide reductases
Pierrette Gaudreau, Helene Paradis, Yves Langelier, and Paul Brazeau
pp 723 - 730; DOI:
10.1021/jm00164a040
PDF
Methylating agents as trypanocides
Philip G. Penketh, Krishnamurthy Shyam, Alan A. Divo, Curtis L. Patton, and Alan C. Sartorelli
pp 730 - 732; DOI:
10.1021/jm00164a041
PDF
Synthesis, brain uptake, and pharmacological properties of a glyceryl lipid containing GABA and the GABA-T inhibitor .gamma.-vinyl-GABA
James N. Jacob, Gary W. Hesse, and Victor E. Shashoua
pp 733 - 736; DOI:
10.1021/jm00164a042
PDF
Conjugate addition ligands of opioid antagonists. Methacrylate esters and ethers of 6.alpha.- and 6.beta.-naltrexol
Leslie D. Olsen, Peter Klein, Wendel L. Nelson, Yi He Yao, and Eric J. Simon
pp 737 - 741; DOI:
10.1021/jm00164a043
PDF
Functionalized congener approach for the design of novel muscarinic agents. Synthesis and pharmacological evaluation of N-methyl-N-[4-(1-pyrrolidinyl)-2-butynyl] amides
Barton J. Bradbury, Jesse Baumgold, and Kenneth A. Jacobson
pp 741 - 748; DOI:
10.1021/jm00164a044
PDF
Topically active carbonic anhydrase inhibitors. 3. Benzofuran- and indole-2-sulfonamides
Samuel L. Graham, Jacob M. Hoffman, Pierre Gautheron, Stuart R. Michelson, Thomas H. Scholz, Harvey Schwam, Kenneth L. Shepard, Anthony M. Smith, Robert L. Smith, and et al.
pp 749 - 754; DOI:
10.1021/jm00164a045
PDF
5-HT1 and 5-HT2 binding profiles of the serotonergic agents .alpha.-methylserotonin and 2-methylserotonin
Abd M. Ismaiel, Milt Titeler, Keith J. Miller, Thomas S. Smith, and Richard A. Glennon
pp 755 - 758; DOI:
10.1021/jm00164a046
PDF
3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 6. trans-6-[2-(Substituted-1-naphthyl)ethyl(or ethenyl)]-3,4,5,6-tetrahydro-4-hydroxy-2H-pyran-2-ones
John D. Prugh, Alfred W. Alberts, Albert A. Deana, James L. Gilfillian, Jesse W. Huff, Robert L. Smith, and J. Mark Wiggins
pp 758 - 765; DOI:
10.1021/jm00164a047
PDF
Lipophilic 1,3-xylyl-21-crown-6 macrocyclic polyether 2-carboxylic acids as biological mimics of the ionophore antibiotics
Frank J. Urban, Larry R. Chappel, Arthur E. Girard, Banavara L. Mylari, and Ian J. Pimblett
pp 765 - 771; DOI:
10.1021/jm00164a048
PDF
Voronoi binding site model of a polycyclic aromatic hydrocarbon binding protein
Laurent G. Boulu, Gordon M. Crippen, Hugh A. Barton, Hoonjeong Kwon, and Michael A. Marletta
pp 771 - 775; DOI:
10.1021/jm00164a049
PDF
1,4-Dihydronaphthoquinones, hydroindoloquinones, benzofurans, and benzothiophenes as inhibitors of 5-lipoxygenase. Synthesis and structure-activity studies
Ayako Yamashita, Robert G. Schaub, Michael K. Bach, Gordon J. White, Arthur Toy, Nabil B. Ghazal, Michael D. Burdick, John R. Brashler, and Marilyn S. Holm
pp 775 - 781; DOI:
10.1021/jm00164a050
PDF
Some benzyl-substituted imidazoles, triazoles, tetrazoles, pyridinethiones, and structural relatives as multisubstrate inhibitors of dopamine .beta.-hydroxylase. 4. Structure-activity relationships at the copper binding site
Lawrence I. Kruse, Carl Kaiser, Walter E. DeWolf, Joseph A. Finkelstein, James S. Frazee, Eileen L. Hilbert, Stephen T. Ross, Kathryn E. Flaim, and John L. Sawyer
pp 781 - 789; DOI:
10.1021/jm00164a051
PDF
Synthesis and pharmacological evaluation of a series of dibenzo[a,d]cycloalkenimines as N-methyl-D-aspartate antagonists
Wayne J. Thompson, Paul S. Anderson, Susan F. Britcher, Terry A. Lyle, J. Eric Thies, Catherine A. Magill, Sandor L. Varga, John E. Schwering, Paulette A. Lyle, and et al.
pp 789 - 808; DOI:
10.1021/jm00164a052
PDF
Chloro-substituted, sterically hindered 5,11-dicarbo analogs of clozapine as potential chiral antipsychotic agents
Daniel A. Davis, Tomas De Paulis, Aaron Janowsky, and Howard E. Smith
pp 809 - 814; DOI:
10.1021/jm00164a053
PDF
Potential antitumor agents. 59. Structure-activity relationships for 2-phenylbenzimidazole-4-carboxamides, a new class of minimal DNA-intercalating agents which may not act via topoisomerase II
William A. Denny, Gordon W. Rewcastle, and Bruce C. Baguley
pp 814 - 819; DOI:
10.1021/jm00164a054
PDF
Analogs of carbamyl aspartate as inhibitors of dihydroorotase: preparation of boronic acid transition-state analogs and a zinc chelator carbamylhomocysteine
David H. Kinder, Sandra K. Frank, and Matthew M. Ames
pp 819 - 823; DOI:
10.1021/jm00164a055
PDF
An approach to trapping .gamma.-glutamyl radical intermediates proposed for vitamin K dependent carboxylase: .alpha.,.beta.-methyleneglutamic acid
James T. Slama, Rajiv K. Satsangi, Anne Simmons, Vincent Lynch, Randall E. Bolger, and John Suttie
pp 824 - 832; DOI:
10.1021/jm00164a056
PDF
Synthesis and immunosuppressive activity of some side-chain variants of mycophenolic acid
Peter H. Nelson, Elsie Eugui, Ching C. Wang, and Anthony C. Allison
pp 833 - 838; DOI:
10.1021/jm00164a057
PDF
Renin inhibitors containing isosteric replacements of the amide bond connecting the P3 and P2 sites
James S. Kaltenbronn, J. P. Hudspeth, E. A. Lunney, B. M. Michniewicz, E. D. Nicolaides, J. T. Repine, W. H. Roark, M. A. Stier, F. J. Tinney, and et al.
pp 838 - 845; DOI:
10.1021/jm00164a058
PDF
Synthesis, antiretrovirus effects and phosphorylation kinetics of 3'-isocyano-3'-deoxythymidine and 3'-isocyano-2',3'-dideoxyuridine
Johann Hiebl, Erich Zbiral, Jan Balzarini, and Erik De Clercq
pp 845 - 848; DOI:
10.1021/jm00164a059
PDF
New quinolone antibacterial agents. Synthesis and biological activity of 7-(3,3- or 3,4-disubstituted-1-pyrrolidinyl)quinoline-3-carboxylic acids
Susan E. Hagen, John M. Domagala, Carl L. Heifetz, Joseph P. Sanchez, and Marjorie Solomon
pp 849 - 854; DOI:
10.1021/jm00164a060
PDF
N-Phenyl-N'-pyridinylureas as anticonvulsant agents
Michael R. Pavia, Sandra J. Lobbestael, Charles P. Taylor, Fred M. Hershenson, and David L. Miskell
pp 854 - 861; DOI:
10.1021/jm00164a061
PDF
Glycolipids as host resistance stimulators
Mitree M. Ponpipom, William K. Hagmann, Laura A. O'Grady, Jesse J. Jackson, David D. Wood, and Hans J. Zweerink
pp 861 - 867; DOI:
10.1021/jm00164a062
PDF
Synthesis and antiviral activity of 3'-heterocyclic substituted 3'-deoxythymidines
Piet Wigerinck, Arthur Van Aerschot, Gerard Janssen, Paul Claes, Jan Balzarini, Erik De Clercq, and Piet Herdewijn
pp 868 - 873; DOI:
10.1021/jm00164a063
PDF
Studies on Ca2+ channel antagonists. A 2-diazo-3,3,3-trifluoropropionamide derivative related to verapamil as a potential photoaffinity probe
Louis J. Theodore, Wendel L. Nelson, Bharti Dave, and John C. Giacomini
pp 873 - 877; DOI:
10.1021/jm00164a064
PDF
Design and synthesis of 14.alpha.-methyl-15-aza-D-homosterols as novel antimycotics
Roland E. Dolle, H. S. Allaudeen, and Lawrence I. Kruse
pp 877 - 880; DOI:
10.1021/jm00164a065
PDF
Improved delivery through biological membranes. 39. Brain-specific chemical delivery systems for 26-lactam antibiotics. In vitro and in vivo studies of some dihydropyridine and dihydroisoquinoline derivatives of benzylpenicillin in rats [Erratum to document cited in CA111(8):63813y]
Whei Mei Wu, Emil Pop, Efraim Shek, and Nicholas Bodor
pp 880 - 880; DOI:
10.1021/jm00164a066
PDF
Book Reviews

pp 880 - 882; DOI:
10.1021/jm00164a600
PDF

Issue 3


Molecular modeling software and methods for medicinal chemistry
N. Claude Cohen, Jeffrey M. Blaney, Christine Humblet, Peter Gund, and David C. Barry
pp 883 - 894; DOI:
10.1021/jm00165a001
PDF
Selective opioid receptor agonists and antagonists: research tools and potential therapeutic agents
Dennis M. Zimmerman and J. David Leander
pp 895 - 902; DOI:
10.1021/jm00165a002
PDF
4'-[(4-Piperidyl)carbonyl]methanesulfonanilides as potent, selective, bioavailable class III antiarrhythmic agents
Hitoshi Oinuma, Kazutoshi Miyake, Motosuke Yamanaka, Kenichi Nomoto, Hiroshi Katoh, Kohei Sawada, Mitsumasa Shino, and Sachiyuki Hamano
pp 903 - 905; DOI:
10.1021/jm00165a003
PDF
Neural networks applied to structure-activity relationships
Tomoo Aoyama, Yuji Suzuki, and Hiroshi Ichikawa
pp 905 - 908; DOI:
10.1021/jm00165a004
PDF
Antioxidant-based inhibitors of leukotriene biosynthesis. The discovery of 6-[1-[2-(hydroxymethyl)phenyl]-1-propen-3-yl]-2,3-dihydro-5-benzofuranol, a potent topical antiinflammatory agent
Milton L. Hammond, Robert A. Zambias, Michael N. Chang, Norman P. Jensen, John McDonald, Kathryn Thompson, David A. Boulton, Ihor E. Kopka, Karen M. Hand, and et al.
pp 908 - 918; DOI:
10.1021/jm00165a005
PDF
Preparation and anticonvulsant activity of a series of functionalized .alpha.-aromatic and .alpha.-heteroaromatic amino acids
Harold Kohn, Kailash N. Sawhney, Philippe LeGall, Judith D. Conley, David W. Robertson, and J. David Leander
pp 919 - 926; DOI:
10.1021/jm00165a006
PDF
Synthesis and anticonvulsant activity of 2-benzylglutarimides
R. Richard Goehring, Thomas D. Greenwood, Godson C. Nwokogu, Jyothi S. Pisipati, Tommie G. Rogers, and James F. Wolfe
pp 926 - 931; DOI:
10.1021/jm00165a007
PDF
Selective inhibition of .gamma.-aminobutyric acid aminotransferase by (3R,4R), (3S,4S)- and (3R,4S), (3S,4R)-4-amino-5-fluoro-3-phenylpentanoic acids
Richard B. Silverman and Shrenik M. Nanavati
pp 931 - 936; DOI:
10.1021/jm00165a008
PDF
Steroidal A ring aryl carboxylic acids: a new class of steroid 5.alpha.-reductase inhibitors
Dennis A. Holt, Mark A. Levy, David L. Ladd, Hye Ja Oh, Jill M. Erb, Julie I. Heaslip, Martin Brandt, and Brian W. Metcalf
pp 937 - 942; DOI:
10.1021/jm00165a009
PDF
Inhibition of steroid 5.alpha.-reductase by unsaturated 3-carboxy steroids
Dennis A. Holt, Mark A. Levy, Hye Ja Oh, Jill M. Erb, Julie I. Heaslip, Martin Brandt, Hsuan Yin Lan-Hargest, and Brian W. Metcalf
pp 943 - 950; DOI:
10.1021/jm00165a010
PDF
Novel [(diazomethyl)carbonyl]-1,2,3,4-tetrahydronaphthalene derivatives as potential photoaffinity ligands for the 5-HT1A receptor
Toni B. Kline, David L. Nelson, and Krishnan Namboodiri
pp 950 - 955; DOI:
10.1021/jm00165a011
PDF
Neuronal mapping of the heart with 6-[18F]fluorometaraminol
Donald M. Wieland, Karen C. Rosenspire, Gary D. Hutchins, Marcian Van Dort, Jill M. Rothley, Suresh G. Mislankar, Helen T. Lee, Christopher C. Massin, David L. Gildersleeve, and et al.
pp 956 - 964; DOI:
10.1021/jm00165a012
PDF
Small peptide inhibitors of smooth muscle myosin light chain kinase
Federico C. A. Gaeta, Laura S. Lehman de Gaeta, Timothy P. Kogan, Yat Sun Or, Carolyn Foster, and Michael Czarniecki
pp 964 - 972; DOI:
10.1021/jm00165a013
PDF
Plant antitumor agents. 29. Synthesis and biological activity of ring D and ring E modified analogs of camptothecin
Allan W. Nicholas, Mansukh C. Wani, Govindarajan Manikumar, Monroe E. Wall, Kurt W. Kohn, and Yves Pommier
pp 972 - 978; DOI:
10.1021/jm00165a014
PDF
Acid-stable 2'-fluoro purine dideoxynucleosides as active agents against HIV
Victor E. Marquez, Christopher K. H. Tseng, Hiroaki Mitsuya, Shizuko Aoki, James A. Kelley, Harry Ford, Jeri S. Roth, Samuel Broder, David G. Johns, and John S. Driscoll
pp 978 - 985; DOI:
10.1021/jm00165a015
PDF
Synthesis and biological activity of novel quaternary ammonium derivatives of alkylglycerols as potent inhibitors of protein kinase C
Canio J. Marasco, Claude Piantadosi, Karen L. Meyer, Susan Morris-Natschke, Khalid S. Ishaq, George W. Small, and Larry W. Daniel
pp 985 - 992; DOI:
10.1021/jm00165a016
PDF
Hydroxamic acid inhibitors of 5-lipoxygenase: quantitative structure-activity relationships
James B. Summers, Ki H. Kim, Hormoz Mazdiyasni, James H. Holms, James D. Ratajczyk, Andrew O. Stewart, Richard D. Dyer, and George W. Carter
pp 992 - 998; DOI:
10.1021/jm00165a017
PDF
Synthesis, conformation, and immunosuppressive activities of three analogs of cyclosporin A modified in the 1-position
Johannes D. Aebi, Donald T. Deyo, Chong Qing Sun, Dominique Guillaume, Brian Dunlap, and Daniel H. Rich
pp 999 - 1009; DOI:
10.1021/jm00165a018
PDF
NMR studies of the conjugation of mechlorethamine with glutathione
Michael P. Gamcsik, Terence G. Hamill, and Michael Colvin
pp 1009 - 1014; DOI:
10.1021/jm00165a019
PDF
Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model
Tommy Liljefors, Klaus P. Boegesoe, John Hyttel, Haakan Wikstroem, Kjell Svensson, and Arvid Carlsson
pp 1015 - 1022; DOI:
10.1021/jm00165a020
PDF
Synthesis of N-[N-(4-deoxy-4-amino-10-methylpteroyl)-4-fluoroglutamyl]-.gamma.-glutamate, an unusual substrate for folylpoly-.gamma.-glutamate synthetase and .gamma.-glutamyl hydrolase
Nicholas J. Licato, James K. Coward, Zenia Nimec, John Galivan, Wanda E. Bolanowska, and John J. McGuire
pp 1022 - 1027; DOI:
10.1021/jm00165a021
PDF
Synthesis and in vitro activity of stereoisomers of a novel thromboxane receptor antagonist, (.+-.)-(5Z)-7-[(3-endo-[(phenylsulfonyl)amino]bicyclo[2.2.1]hept-2-exo-yl]heptenoic acid
Mitsuaki Ohtani and Masayuki Narisada
pp 1027 - 1031; DOI:
10.1021/jm00165a022
PDF
A structure-affinity study of the binding of 4-substituted analogs of 1-(2,5-dimethoxyphenyl)-2-aminopropane at 5-HT2 serotonin receptors
Mark R. Seggel, M. Y. Yousif, Robert A. Lyon, Milt Titeler, Bryan L. Roth, Eva A. Suba, and Richard A. Glennon
pp 1032 - 1036; DOI:
10.1021/jm00165a023
PDF
Cannabimimetic activity of novel enantiomeric, benzofuran cannabinoids
Raphael Mechoulam, Aviva Breuer, Tobjorn U. C. Jaerbe, Arto J. Hiltunen, and Robert Glaser
pp 1037 - 1043; DOI:
10.1021/jm00165a024
PDF
Binding of cis-(1,2-diaminocyclohexane)platinum(II) and its derivatives to duplex DNA
Kenneth J. Miller, Sharon L. McCarthy, and Morris Krauss
pp 1043 - 1046; DOI:
10.1021/jm00165a025
PDF
Structure and activity of hydrogenated derivatives of (+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine (MK-801)
Terry A. Lyle, Catherine A. Magill, Susan F. Britcher, George H. Denny, Wayne J. Thompson, Joan S. Murphy, Antony R. Knight, John A. Kemp, George R. Marshall, and et al.
pp 1047 - 1052; DOI:
10.1021/jm00165a026
PDF
High potency dipeptide sweeteners. 1. L-Aspartyl-D-phenylglycine esters
J. M. Janusz, J. M. Gardlik, P. A. Young, R. V. Burkes, S. J. Stoll, A. F. Estelle, and C. M. Riley
pp 1052 - 1061; DOI:
10.1021/jm00165a027
PDF
Structural requirements for agonist actions at the benzodiazepine receptor: studies with analogs of 6-(benzyloxy)-4-(methoxymethyl)-.beta.-carboline-3-carboxylic acid ethyl ester
Sean P. Hollinshead, Mark L. Trudell, Phil Skolnick, and James M. Cook
pp 1062 - 1069; DOI:
10.1021/jm00165a028
PDF
Synthesis and structure-activity relationship of C5-substituted analogs of (.+-.)-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5, 10-imine [(.+-.)-desmethyl-MK801]: ligands for the NMDA receptor-coupled phencyclidine binding site
James A. Monn, Andrew Thurkauf, Mariena V. Mattson, Arthur E. Jacobson, and Kenner C. Rice
pp 1069 - 1076; DOI:
10.1021/jm00165a029
PDF
A unified approach to systematic isosteric substitution for acidic groups and application to NMDA antagonists related to 2-amino-7-phosphonoheptanoate
B. L. Chenard, C. A. Lipinski, B. W. Dominy, E. E. Mena, R. T. Ronau, G. C. Butterfield, L. C. Marinovic, M. Pagnozzi, T. W. Butler, and T. Tsang
pp 1077 - 1083; DOI:
10.1021/jm00165a030
PDF
Book Reviews

pp 1083 - 1084; DOI:
10.1021/jm00165a600
PDF

Issue 4


Inhibitors of human leukocyte proteinase-3
W. C. Groutas, J. R. Hoidal, M. J. Brubaker, M. A. Stanga, R. Venkataraman, B. H. Gray, and N. V. Rao
pp 1085 - 1087; DOI:
10.1021/jm00166a001
PDF
Synthesis and pharmacological studies of N-[4-[2-hydroxy-3-[[2-[4-(1H-imidazol-1-yl)phenoxy]ethyl]amino]propoxy]phenyl]methanesulfonamide, a novel antiarrhythmic agent with class II and class III activities
Thomas K. Morgan Jr., Randall Lis, William C. Lumma Jr., Ronald A. Wohl, Klaus Nickisch, Gary B. Phillips, Joan M. Lind, John W. Lampe, Susan V. Di Meo, and et al.
pp 1087 - 1090; DOI:
10.1021/jm00166a002
PDF
Synthesis and cardiac electrophysiological activity of N-substituted-4-(1H-imidazol-1-yl)benzamides - new selective class III agents
Thomas K. Morgan Jr., Randall Lis, William C. Lumma Jr., Klaus Nickisch, Ronald A. Wohl, Gary B. Phillips, Robert P. Gomez, John W. Lampe, Susan V. Di Meo, and et al.
pp 1091 - 1097; DOI:
10.1021/jm00166a003
PDF
Conformational analysis of cyproheptadine hydrochloride
Maruse Sadek, David J. Craik, Jon G. Hall, and Peter R. Andrews
pp 1098 - 1107; DOI:
10.1021/jm00166a004
PDF
Chalcogenapyrylium dyes as photochemotherapeutic agents. 2. Tumor uptake, mitochondrial targeting, and singlet-oxygen-induced inhibition of cytochrome c oxidase
Michael R. Detty, Paul B. Merkel, Russell Hilf, Scott L. Gibson, and Stephen K. Powers
pp 1108 - 1116; DOI:
10.1021/jm00166a005
PDF
Computer-aided molecular modeling of a thromboxane receptor antagonist S-145 and its related compounds
Kiyoshi Ezumi, Masumi Yamakawa, and Masayuki Narisada
pp 1117 - 1122; DOI:
10.1021/jm00166a006
PDF
Dehydrogenase binding by tiazofurin anabolites
Barry M. Goldstein, J. Ellis Bell, and Victor E. Marquez
pp 1123 - 1127; DOI:
10.1021/jm00166a007
PDF
Novel quinuclidine-based ligands for the muscarinic cholinergic receptor
John Saunders, Mark Cassidy, Stephen B. Freedman, Elizabeth A. Harley, Leslie L. Iversen, Clare Kneen, Angus M. MacLeod, Kevin J. Merchant, Roger J. Snow, and Raymond Baker
pp 1128 - 1138; DOI:
10.1021/jm00166a008
PDF
Synthesis and .alpha.2-adrenoceptor effects of substituted catecholimidazoline and catecholimidazole analogs in human platelets
Duane D. Miller, Akihiko Hamada, Michael T. Clark, Adeboye Adejare, Popat N. Patil, Gamal Shams, Karl J. Romstedt, Sung U. Kim, Urusa Intrasuksri, and et al.
pp 1138 - 1144; DOI:
10.1021/jm00166a009
PDF
Novel 21-aminosteroids that inhibit iron-dependent lipid peroxidation and protect against central nervous system trauma
E. Jon Jacobsen, John M. McCall, Donald E. Ayer, Fred J. VanDoornik, John R. Palmer, Kenneth L. Belonga, J. Mark Braughler, Edward D. Hall, David J. Houser, and et al.
pp 1145 - 1151; DOI:
10.1021/jm00166a010
PDF
Selective class III antiarrhythmic agents. 1. Bis(arylalkyl)amines
Peter E. Cross, John E. Arrowsmith, Geoffrey N. Thomas, Michael Gwilt, Roger A. Burges, and Alan J. Higgins
pp 1151 - 1155; DOI:
10.1021/jm00166a011
PDF
Potential antipsychotic agents. 5. Synthesis and antidopaminergic properties of substituted 5,6-dimethoxysalicylamides and related compounds
Thomas Hoegberg, Stefan Bengtsson, Tomas De Paulis, Lars Johansson, Peter Stroem, Haakan Hall, and Sven Ove Oegren
pp 1155 - 1163; DOI:
10.1021/jm00166a012
PDF
Design, synthesis, and 5-lipoxygenase-inhibiting properties of 1-thio-substituted butadienes
Rudolf Hanko, Michael D. Hammond, Romanis Fruchtmann, Joerg Pfitzner, and Graham A. Place
pp 1163 - 1170; DOI:
10.1021/jm00166a013
PDF
Probes for narcotic receptor mediated phenomena. 17. Synthesis and evaluation of a series of trans-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzeneacetamide (U50,488) related isothiocyanate derivatives as opioid receptor affinity ligands
Brian R. De Costa, Richard B. Rothman, Victor Bykov, Linda Band, Agu Pert, Arthur E. Jacobson, and Kenner C. Rice
pp 1171 - 1176; DOI:
10.1021/jm00166a014
PDF
DNA-directed alkylating agents. 1. Structure-activity relationships for acridine-linked aniline mustards: consequences of varying the reactivity of the mustard
Trudi A. Gourdie, Kisione K. Valu, G. Lance Gravatt, Theodore J. Boritzki, Bruce C. Baguley, Laurence P. G. Wakelin, William R. Wilson, Paul D. Woodgate, and William A. Denny
pp 1177 - 1186; DOI:
10.1021/jm00166a015
PDF
Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 1. Initial structure-activity relationships
Raymond D. Youssefyeh, Ernest Magnien, Thomas D. Y. Lee, Wan Kit Chan, Clara J. Lin, Robert A. Galemmo Jr., William H. Johnson Jr., Jenny Tan, Henry F. Campbell, and et al.
pp 1186 - 1194; DOI:
10.1021/jm00166a016
PDF
Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene D4 receptor antagonists. 2. Effects of an additional phenyl ring on receptor affinity
Fu Chih Huang, Robert A. Galemmo Jr., William H. Johnson Jr., Gregory B. Poli, Matthew M. Morrissette, James J. Mencel, James D. Warus, Henry F. Campbell, George W. Nuss, and et al.
pp 1194 - 1200; DOI:
10.1021/jm00166a017
PDF
Synthesis and biological evaluation of 14-alkoxymorphinans. 3. Extensive study on cyprodime-related compounds
Helmut Schmidhammer, Colin F. C. Smith, Daniela Erlach, Martin Koch, Roland Krassnig, Wolfgang Schwetz, and Christine Wechner
pp 1200 - 1206; DOI:
10.1021/jm00166a018
PDF
Acyclic purine phosphonate analogs as antiviral agents. Synthesis and structure-activity relationships
Choung Un Kim, Bing Yu Luh, Peter F. Misco, Joanne J. Bronson, Michael J. M. Hitchcock, Ismail Ghazzouli, and John C. Martin
pp 1207 - 1213; DOI:
10.1021/jm00166a019
PDF
Synthesis and biological evaluation of carbocyclic analogs of lyxofuranosides of 2-amino-6-substituted purines and 2-amino-6-substituted-8-azapurines
Mark L. Peterson and Robert Vince
pp 1214 - 1219; DOI:
10.1021/jm00166a020
PDF
Synthesis and antitumor evaluation in mice of certain 7-deazapurine (pyrrolo[2,3-d]pyrimidine) and 3-deazapurine (imidazo[4,5-c]pyridine) nucleosides structurally related to sulfenosine, sulfinosine, and sulfonosine
Kandasamy Ramasamy, Nobutaka Imamura, Naeem B. Hanna, Rick A. Finch, Thomas L. Avery, Roland K. Robins, and Ganapathi R. Revankar
pp 1220 - 1225; DOI:
10.1021/jm00166a021
PDF
Properties of the nucleic acid photoaffinity labeling agent 3-azidoamsacrine
Tiee Leou Shieh, Patricia Hoyos, Eric Kolodziej, Joseph G. Stowell, William M. Baird, and Stephen R. Byrn
pp 1225 - 1230; DOI:
10.1021/jm00166a022
PDF
Preparation of triazolo[1,5-c]pyrimidines as potential antiasthma agents
Jeffrey B. Medwid, Rolf Paul, Jannie S. Baker, John A. Brockman, Mila T. Du, William A. Hallett, J. William Hanifin, Robert A. Hardy Jr., M. Ernestine Tarrant, and et al.
pp 1230 - 1241; DOI:
10.1021/jm00166a023
PDF
Intrinsic isotope effects suggest that the reaction coordinate symmetry for the cytochrome P-450-catalyzed hydroxylation of octane is isozyme independent
Jeffrey P. Jones, Allan E. Rettie, and William F. Trager
pp 1242 - 1246; DOI:
10.1021/jm00166a024
PDF
The synthesis and antibacterial activities of quinolones containing five- and six-membered heterocyclic substituents at the 7-position
Curt S. Cooper, Pamela L. Klock, Daniel T. W. Chu, and Prabhavathi B. Fernandes
pp 1246 - 1252; DOI:
10.1021/jm00166a025
PDF
Analogs of 1,5-bis(4-amidinophenoxy)pentane (pentamidine) in the treatment of experimental Pneumocystis carinii pneumonia
Richard R. Tidwell, Susan Kilgore Jones, J. Dieter Geratz, Kwasi A. Ohemeng, Michael Cory, and James Edwin Hall
pp 1252 - 1257; DOI:
10.1021/jm00166a026
PDF
Diels-Alder adducts of vinyl porphyrins: synthesis and in vivo photodynamic effect against a rat bladder tumor
Alan R. Morgan, Greta M. Garbo, Rick W. Keck, Robert A. Miller, Steven H. Selman, and Dimitris Skalkos
pp 1258 - 1262; DOI:
10.1021/jm00166a027
PDF
Synthesis of perfluoroalkylated xylitol ethers and esters: new surfactants for biomedical uses
Leila Zarif, Jacques Greiner, Simonne Pace, and Jean G. Riess
pp 1262 - 1269; DOI:
10.1021/jm00166a028
PDF
Design and synthesis and propranolol analogs as serotonergic agents [Erratum to document cited in CA110(19):172847n]
M. Edward Pierson, Robert A. Lyon, Milt Titeler, Steven B. Schulman, Paul Kowalski, and Richard A. Glennon
pp 1270 - 1270; DOI:
10.1021/jm00166a029
PDF
Synthesis and antiproliferative effects of novel 5'-fluorinated analogs of 5'-deoxy-5'-(methylthio)adenosine [Erratum to document cited in CA110(21):193314b]
Janice R. Sufrin, Arthur J. Spiess, Debora L. Kramer, Paul R. Libby, and Carl W. Porter
pp 1270 - 1270; DOI:
10.1021/jm00166a030
PDF
Synthesis of the 2-chloro analogs of 3'-deoxyadenosine, 2',3'-dideoxyadenosine, and 2',3'-didehydro-2',3'-dideoxyadenosine as potential antiviral agents [Erratum to document cited in CA110(21):193310x]
Andre Rosowsky, Vishnu C. Solan, Joseph G. Sodroski, and Ruth M. Ruprecht
pp 1270 - 1270; DOI:
10.1021/jm00166a031
PDF
Synthesis and biological properties of N63-carboxamides of teicoplanin antibiotics. Structure-activity relationships [Erratum to document cited in CA111(21):195401x]
Adriano Malabarba, Aldo Trani, Paolo Strazzolini, Giuseppe Cietto, Pietro Ferrari, Giorgio Tarzia, Rosa Pallanza, and Marisa Berti
pp 1270 - 1270; DOI:
10.1021/jm00166a032
PDF
Book Reviews

pp 1271 - 1274; DOI:
10.1021/jm00166a600
PDF

Issue 5


Receptor triggering and receptor regulation: structure-activity relationships from the receptor's point of view
Morley D. Hollenberg
pp 1275 - 1281; DOI:
10.1021/jm00167a001
PDF
Cyclobut-A and cyclobut-G: broad-spectrum antiviral agents with potential utility for the therapy of AIDS
Daniel W. Norbeck, Earl Kern, Seiji Hayashi, William Rosenbrook, Hing Sham, Thomas Herrin, Jacob J. Plattner, John Erickson, Jacob Clement, and et al.
pp 1281 - 1285; DOI:
10.1021/jm00167a002
PDF
Hydroxyethylamine analogs of the p17/p24 substrate cleavage site are tight-binding inhibitors of HIV protease
Daniel H. Rich, Jeremy Green, Mihaly V. Toth, Garland R. Marshall, and Stephen B. H. Kent
pp 1285 - 1288; DOI:
10.1021/jm00167a003
PDF
Hypoxia-selective antitumor agents. 4. Relationships between structure, physicochemical properties, and hypoxia-selective cytotoxicity for nitracrine analogs with varying side chains: the "iminoacridan hypothesis"
William A. Denny, Graham J. Atwell, Robert F. Anderson, and William R. Wilson
pp 1288 - 1295; DOI:
10.1021/jm00167a004
PDF
Role of hydrogen bonding in ligand interaction with the N-methyl-D-aspartate receptor ion channel
Paul D. Leeson, Robert W. Carling, Kim James, Julian D. Smith, Kevin W. Moore, Erik H. F. Wong, and Raymond Baker
pp 1296 - 1305; DOI:
10.1021/jm00167a005
PDF
A model for compounds active against human rhinovirus-14 based on x-ray crystallography data
Guy D. Diana, Adi M. Treasurywala, Thomas R. Bailey, Richard C. Oglesby, Daniel C. Pevear, and Frank J. Dutko
pp 1306 - 1311; DOI:
10.1021/jm00167a006
PDF
The discovery of potent nonpeptide angiotensin II receptor antagonists: a new class of potent antihypertensives
John V. Duncia, Andrew T. Chiu, David J. Carini, George B. Gregory, Alexander L. Johnson, William A. Price, Gregory J. Wells, Pancras C. Wong, Joseph C. Calabrese, and Pieter B. M. W. M. Timmermans
pp 1312 - 1329; DOI:
10.1021/jm00167a007
PDF
Part VI. Nonpeptide angiotensin II receptor antagonists: N-[(benzyloxy)benzyl]imidazoles and related compounds as potent antihypertensives
David J. Carini, John V. Duncia, Alexander L. Johnson, Andrew T. Chiu, William A. Price, Pancras C. Wong, and Pieter B. M. W. Timmermans
pp 1330 - 1336; DOI:
10.1021/jm00167a008
PDF
Renin inhibitory peptides. A .beta.-aspartyl residue as a replacement for the histidyl residue at the P-2 site
Suvit Thaisrivongs, Boryeu Mao, Donald T. Pals, Steve R. Turner, and Lisa T. Kroll
pp 1337 - 1343; DOI:
10.1021/jm00167a009
PDF
Fluoronaphthyridines and quinolones as antibacterial agents. 2. Synthesis and structure-activity relationships of new 1-tert-butyl 7-substituted derivatives
D. Bouzard, P. Di Cesare, M. Essiz, J. P. Jacquet, J. R. Kiechel, P. Remuzon, A. Weber, T. Oki, M. Masuyoshi, and et al.
pp 1344 - 1352; DOI:
10.1021/jm00167a010
PDF
Stereospecific synthesis and antiviral properties of different enantiomerically pure carbocyclic 2'-deoxyribonucleoside analogs derived from common chiral pools: (+)-(1R,5S)- and (-)-(1S,5R)-2-oxabicyclo[3.3.0]oct-6-en-3-one
J. Beres, G. Sagi, I. Tomoskozi, L. Gruber, E. Baitz-Gacs, L. Otvos, and E. De Clercq
pp 1353 - 1360; DOI:
10.1021/jm00167a011
PDF
Antirhinovirus activity of 6-anilino-9-benzyl-2-chloro-9H-purines
James L. Kelley, James A. Linn, and J. W. T. Selway
pp 1360 - 1363; DOI:
10.1021/jm00167a012
PDF
Antitumor agents. 111. New 4-hydroxylated and 4-halogenated anilino derivatives of 4'-demethylepipodophyllotoxin as potent inhibitors of human DNA topoisomerase II
Kuo Hsiung Lee, Scott A. Beers, Masami Mori, Zhe Qing Wang, Yao Haur Kuo, Li Li, Su Ying Liu, Jang Yang Chang, Fu Sheng Han, and Yung Chi Cheng
pp 1364 - 1368; DOI:
10.1021/jm00167a013
PDF
Polyamine analogs with antitumor activity
Michael L. Edwards, N. J. Prakash, D. M. Stemerick, S. P. Sunkara, A. J. Bitonti, G. F. Davis, J. A. Dumont, and P. Bey
pp 1369 - 1375; DOI:
10.1021/jm00167a014
PDF
Potential antitumor agents. 60. Relationships between structure and in vivo colon 38 activity for 5-substituted 9-oxoxanthene-4-acetic acids
Graham J. Atwell, Gordon W. Rewcastle, Bruce C. Baguley, and William A. Denny
pp 1375 - 1379; DOI:
10.1021/jm00167a015
PDF
Nucleoside conjugates. 11. Synthesis and antitumor activity of 1-.beta.-D-arabinofuranosylcytosine and cytidine conjugates of thioether lipids
Chung Il Hong, Alan J. Kirisits, Alexander Nechaev, David J. Buchheit, and Charles R. West
pp 1380 - 1386; DOI:
10.1021/jm00167a016
PDF
Cytotoxicity and antitumor activity of some tetrahedral bis(diphosphino)gold(I) chelates
Susan J. Berners-Price, Gerald R. Girard, David T. Hill, Blaine M. Sutton, Penelope S. Jarrett, Leo F. Faucette, Randall K. Johnson, Christopher K. Mirabelli, and Peter J. Sadler
pp 1386 - 1392; DOI:
10.1021/jm00167a017
PDF
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents
K. R. Horspool, M. F. G. Stevens, Christopher G. Newton, E. Lunt, R. J. A. Walsh, B. L. Pedgrift, G. U. Baig, F. Lavelle, and C. Fizames
pp 1393 - 1399; DOI:
10.1021/jm00167a018
PDF
Synthesis and biological properties of novel phosphotriesters: a new approach to the introduction of biologically active nucleotides into cells
Stuart N. Farrow, A. Stanley Jones, Ajit Kumar, Richard T. Walker, Jan Balzarini, and Erik De Clercq
pp 1400 - 1406; DOI:
10.1021/jm00167a019
PDF
Novel benzamides as selective and potent gastric prokinetic agents. 1. Synthesis and structure-activity relationships of N-[(2-morpholinyl)alkyl]benzamides
Shiro Kato, Toshiya Morie, Katsuhiko Hino, Tatsuya Kon, Shunsuke Naruto, Naoyuki Yoshida, Tadahiko Karasawa, and Junichi Matsumoto
pp 1406 - 1413; DOI:
10.1021/jm00167a020
PDF
Synthesis, pharmacological effects, and conformation of 4,4-disubstituted 1,4-dihydropyridines
Siegfried Goldmann, Liborius Born, Stanislav Kazda, Bernd Pittel, and Matthias Schramm
pp 1413 - 1418; DOI:
10.1021/jm00167a021
PDF
Synthesis and antihyperglycemic activity of novel 5-(naphthalenylsulfonyl)-2,4-thiazolidinediones
Arie Zask, Ivo Jirkovsky, James W. Nowicki, and Michael L. McCaleb
pp 1418 - 1423; DOI:
10.1021/jm00167a022
PDF
Molecular design, synthesis, and antiinflammatory activity of a series of .beta.-aminoxypropionic acids
Bruno Macchia, A. Balsamo, A. Lapucci, F. Macchia, A. Martinelli, S. Nencetti, E. Orlandini, M. Baldacci, G. Mengozzi, and et al.
pp 1423 - 1430; DOI:
10.1021/jm00167a023
PDF
Retinobenzoic acids. 5. Retinoidal activities of compounds having a trimethylsilyl or trimethylgermyl group(s) in human promyelocytic leukemia cells HL-60
Takeru Yamakawa, Hiroyuki Kagechika, Emiko Kawachi, Yuichi Hashimoto, and Koichi Shudo
pp 1430 - 1437; DOI:
10.1021/jm00167a024
PDF
Synthesis and pharmacological evaluation of amino, azido, and nitrogen mustard analogs of 10-substituted cannabidiol and 11- or 12-substituted .DELTA.8-tetrahydrocannabinol
David R. Compton, Patrick J. Little, Billy R. Martin, Jeffery W. Gilman, Jayanta K. Saha, Vaman S. Jorapur, Howard P. Sard, and Raj K. Razdan
pp 1437 - 1443; DOI:
10.1021/jm00167a025
PDF
Synthesis, conformation, and immunosuppressive activity of cyclosporines that contain .epsilon.-oxygen (4R)-4-[(E)-butenyl]-4,N-dimethyl-L-threonine analogs in the 1-position
Chong Qing Sun, Dominique Guillaume, Brian Dunlap, and Daniel H. Rich
pp 1443 - 1452; DOI:
10.1021/jm00167a026
PDF
Synthesis and anticonvulsant activity of 1-phenylcyclohexylamine analogs
Andrew Thurkauf, Brian De Costa, Shunichi Yamaguchi, Mariena V. Mattson, Arthur E. Jacobson, Kenner C. Rice, and Michael A. Rogawski
pp 1452 - 1458; DOI:
10.1021/jm00167a027
PDF
(Phosphinyloxy)acyl amino acid inhibitors of angiotensin converting enzyme. 2. Terminal amino acid analogs of (S)-1-[6-amino-2-[[hydroxy(4-phenylbutyl)phosphinyl]oxy]-1-oxohexyl]-L-proline
Donald S. Karanewsky, Michael C. Badia, David W. Cushman, Jack M. DeForrest, Tamara Dejneka, Ving G. Lee, Melanie J. Loots, and Edward W. Petrillo
pp 1459 - 1469; DOI:
10.1021/jm00167a028
PDF
Synthesis and biological activity of some derivatives of rifamycin P
B. Cavalleri, M. Turconi, G. Tamborini, E. Occelli, G. Cietto, R. Pallanza, R. Scotti, M. Berti, G. Romano, and F. Parenti
pp 1470 - 1476; DOI:
10.1021/jm00167a029
PDF
Structure-activity relationships for the carboxy-terminus-truncated analogs of angiotensin II, a new class of angiotensin II antagonists
Philippe R. Bovy, Joan M. O'Neal, Gillian M. Olins, Dennis R. Patton, Ellen G. McMahon, Maria Palomo, John P. Koepke, Khadijeh S. Salles, Angelo J. Trapani, and et al.
pp 1477 - 1482; DOI:
10.1021/jm00167a030
PDF
N-(3-[18F]Fluoropropyl)-N-nordiprenorphine: synthesis and characterization of a new agent for imaging opioid receptors with positron emission tomography
Paul L. Chesis, Dah Ren Hwang, and Michael J. Welch
pp 1482 - 1490; DOI:
10.1021/jm00167a031
PDF
Studies on hindered phenols and analogs. 2. 1,3-Benzoxathioles having SRS-A inhibiting activity
Yuichi Aizawa, Tsutomu Kanai, Kazuo Hasegawa, Takeshi Yamaguchi, Yoshio Iizuka, Teiki Iwaoka, and Takao Yoshioka
pp 1491 - 1496; DOI:
10.1021/jm00167a032
PDF
Specific bradycardic agents. 1. Chemistry, pharmacology, and structure-activity relationships of substituted benzazepinones, a new class of compounds exerting antiischemic properties
Manfred Reiffen, Wolfgang Eberlein, Peter Mueller, Manfred Psiorz, Klaus Noll, Joachim Heider, Christian Lillie, Walter Kobinger, and Peter Luger
pp 1496 - 1504; DOI:
10.1021/jm00167a033
PDF
Synthesis and biological evaluation of prodrugs of zidovudine
Sunil K. Aggarwal, Sudhir R. Gogu, S. R. S. Rangan, and Krishna C. Agrawal
pp 1505 - 1510; DOI:
10.1021/jm00167a034
PDF
Dihydropyrimidine calcium channel blockers: 2-heterosubstituted 4-aryl-1,4-dihydro-6-methyl-5-pyrimidinecarboxylic acid esters as potent mimics of dihydropyridines
Karnail S. Atwal, George C. Rovnyak, Joseph Schwartz, Suzanne Moreland, Anders Hedberg, Jack Z. Gougoutas, Mary F. Malley, and David M. Floyd
pp 1510 - 1515; DOI:
10.1021/jm00167a035
PDF
Synthesis and antimalarial activity of (+)-deoxoartemisinin
Mankil Jung, Xun Li, Daniel A. Bustos, Hala N. ElSohly, James D. McChesney, and Wilbur K. Milhous
pp 1516 - 1518; DOI:
10.1021/jm00167a036
PDF
Synthesis and antitumor activity of 1-[[(dialkylamino)alkyl]amino]-4-methyl-5H-pyrido[4,3-b]benzo[e]- and -benzo[g])indoles. A new class of antineoplastic agents
Nguyen Chi Hung, Jean Marc Lhoste, Francois Lavelle, Marie Christine Bissery, and Emile Bisagni
pp 1519 - 1528; DOI:
10.1021/jm00167a037
PDF
Book Reviews

pp 1528 - 1528; DOI:
10.1021/jm00167a600
PDF

Issue 6


Potassium channel modulators: scientific applications and therapeutic promise
David W. Robertson and Mitchell I. Steinberg
pp 1529 - 1541; DOI:
10.1021/jm00168a001
PDF
(S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin: a putative 5-HT1A-receptor antagonist
Sven Erik Hillver, Lena Bjoerk, Yi Lin Li, Bjoern Svensson, Svante Ross, Nils Erik Anden, and Uli Hacksell
pp 1541 - 1544; DOI:
10.1021/jm00168a002
PDF
Phenyl selenones: alkyl transfer by selenium-carbon bond cleavage
Sang Ihn Kang and Colin Paul Spears
pp 1544 - 1547; DOI:
10.1021/jm00168a003
PDF
Naltrindole-5'-isothiocyanate: a nonequilibrium, highly selective .delta.-opioid receptor antagonist
P. S. Portoghese, M. Sultana, and A. E. Takemori
pp 1547 - 1548; DOI:
10.1021/jm00168a004
PDF
DNA binding by antitumor anthracene derivatives
Timothy P. Wunz, Mary T. Craven, Michael D. Karol, G. Craig Hill, and William A. Remers
pp 1549 - 1553; DOI:
10.1021/jm00168a005
PDF
Synthesis and structure-activity relationships of 6-substituted 2',3'-dideoxypurine nucleosides as potential anti-human immunodeficiency virus agents
Chung K. Chu, Giliyar V. Ullas, Lak S. Jeong, Soon K. Ahn, Bogdan Doboszewski, Zhi X. Lin, J. Warren Beach, and Raymond F. Schinazi
pp 1553 - 1561; DOI:
10.1021/jm00168a006
PDF
Synthesis and bioactivity of a new class of rigid glutamate analogs. Modulators of the N-methyl-D-aspartate receptor
Alan P. Kozikowski, Werner Tuckmantel, Ian J. Reynolds, and Jarda T. Wroblewski
pp 1561 - 1571; DOI:
10.1021/jm00168a007
PDF
Synthesis, metabolism, and pharmacological activity of 3.alpha.-hydroxy steroids which potentiate GABA-receptor-mediated chloride ion uptake in rat cerebral cortical synaptoneurosomes
Robert H. Purdy, A. Leslie Morrow, James R. Blinn, and Steven M. Paul
pp 1572 - 1581; DOI:
10.1021/jm00168a008
PDF
Potent, low molecular weight renin inhibitors containing a C-terminal heterocycle: hydrogen bonding at the active site
Saul H. Rosenberg, Joseph F. Dellaria, Dale J. Kempf, Charles W. Hutchins, Keith W. Woods, Robert G. Maki, Ed De Lara, Kenneth P. Spina, Herman H. Stein, and et al.
pp 1582 - 1590; DOI:
10.1021/jm00168a009
PDF
Conformationally constrained congeners of 6-aryl-5-methyl-4,5-dihydro-3(2H)-pyridazinones active on the cardiovascular system: conformational studies by molecular mechanics calculations and proton NMR spectroscopy
Lucio Toma, Giorgio Cignarella, Daniela Barlocco, and Fiamma Ronchetti
pp 1591 - 1594; DOI:
10.1021/jm00168a010
PDF
Conformation-activity relationship study of 5-HT3 receptor antagonists and a definition of a model for this receptor site
Marcel F. Hibert, Remy Hoffmann, Robert C. Miller, and Albert A. Carr
pp 1594 - 1600; DOI:
10.1021/jm00168a011
PDF
Angiotensin converting enzyme inhibitors. 9. Novel [[N-(1-carboxyl-3-phenylpropyl)amino]acyl]glycine derivatives with diuretic activity
Jeffrey N. Barton, John J. Piwinski, Jerry W. Skiles, John R. Regan, Paul R. Menard, Rohit Desai, F. S. Golec, Laurence W. Reilly, Thomas Goetzen, and et al.
pp 1600 - 1606; DOI:
10.1021/jm00168a012
PDF
Angiotensin converting enzyme inhibitors. 10. Aryl sulfonamide substituted N-[1-carboxy-3-phenylpropyl]-L-alanyl-L-proline derivatives as novel antihypertensives
James J. Mencel, John R. Regan, Jeffrey Barton, Paul R. Menard, Joseph G. Bruno, Raul R. Calvo, Brian E. Kornberg, Alfred Schwab, Edward S. Neiss, and John T. Suh
pp 1606 - 1615; DOI:
10.1021/jm00168a013
PDF
Structural study of the N-terminal segment of neuropeptide tyrosine
Mylene Forest, Jean Claude Martel, Serge St-Pierre, Remi Quirion, and Alain Fournier
pp 1615 - 1619; DOI:
10.1021/jm00168a014
PDF
O'-(epoxyalkyl)tyrosines and (epoxyalkyl)phenylalanine as irreversible inactivators of serine proteases: synthesis and inhibition mechanism
Guillermo Tous, Andrew Bush, Ana Tous, and Frank Jordan
pp 1620 - 1634; DOI:
10.1021/jm00168a015
PDF
Structure-activity relationships of the lissoclinamides: cytotoxic cyclic peptides from the ascidian Lissoclinum patella
Clifford J. Hawkins, Martin F. Lavin, Karen A. Marshall, Anna L. Van den Brenk, and Diane J. Watters
pp 1634 - 1638; DOI:
10.1021/jm00168a016
PDF
Oligosaccharide mapping of low-molecular-weight heparins: structure and activity differences
Robert J. Linhardt, Duraikkannu Loganathan, Ali Al-Hakim, Hui Ming Wang, Jeanine M. Walenga, Debra Hoppensteadt, and Jawed Fareed
pp 1639 - 1645; DOI:
10.1021/jm00168a017
PDF
Pyridonecarboxylic acids as antibacterial agents. Part 14. Synthesis and structure-activity relationships of 5-substituted 6,8-difluoroquinolones, including sparfloxacin, a new quinolone antibacterial agent with improved potency
Teruyuki Miyamoto, Junichi Matsumoto, Katsumi Chiba, Hiroshi Egawa, Kohichiro Shibamori, Akira Minamida, Yoshiro Nishimura, Hidetsugu Okada, Masahiro Kataoka, and et al.
pp 1645 - 1656; DOI:
10.1021/jm00168a018
PDF
Comparative reactivity of 1-carba-1-dethiacephalosporins with cephalosporins
Larry C. Blaszczak, Raymond F. Brown, Gwendolyn K. Cook, William J. Hornback, Joseph M. Indelicato, Chris L. Jordan, Alan S. Katner, Michael D. Kinnick, John H. McDonald, III, and et al.
pp 1656 - 1662; DOI:
10.1021/jm00168a019
PDF
Nucleosides. 154. 2'-Azido-2',3'-dideoxypyrimidine nucleosides. Synthesis and antiviral activity against human immunodeficiency virus
James A. Warshaw and Kyoichi A. Watanabe
pp 1663 - 1666; DOI:
10.1021/jm00168a020
PDF
Vinylogous carbinolamine tumor inhibitors. 24. Synthesis, chemistry, and antineoplastic activity of .alpha.-halopyridinium salts: potential pyridone prodrugs of acylated vinylogous carbinolamine tumor inhibitors.
Wayne K. Anderson, Dennis C. Dean, and Toshiyasu Endo
pp 1667 - 1675; DOI:
10.1021/jm00168a021
PDF
High-potency dipeptide sweeteners. 2. L-Aspartylfuryl-, thienyl-, and imidazolylglycine esters
John M. Janusz, P. A. Young, R. B. Blum, and C. M. Riley
pp 1676 - 1682; DOI:
10.1021/jm00168a022
PDF
Synthesis and cytotoxicity of deoxyadenosine analogs: isomer distribution in the sodium salt glycosylation of 2,6-disubstituted purines
Zygmunt Kazimierczuk, Juhani Vilpo, Catherine Hildebrand, and George Wright
pp 1683 - 1687; DOI:
10.1021/jm00168a023
PDF
Cardiotonic agents. 6. Histamine analogs as potential cardiovascular selective H2 agonists
John W. Lampe, Reda G. Hanna, Thomas A. Piscitelli, Yuo Ling Chou, Paul W. Erhardt, William C. Lumma, Stanley S. Greenberg, William R. Ingebretsen, Dennis C. Marshall, and Jay Wiggins
pp 1688 - 1697; DOI:
10.1021/jm00168a024
PDF
Inhibition of vertebrate squalene epoxidase by extended and truncated analogs of trisnorsqualene alcohol
Stephanie E. Sen, Czeslaw Wawrzenczyk, and Glenn D. Prestwich
pp 1698 - 1701; DOI:
10.1021/jm00168a025
PDF
All atom molecular mechanics simulations on covalent complexes of anthramycin and neothramycin with deoxydecanucleotides
Shashidhar N. Rao and William A. Remers
pp 1701 - 1707; DOI:
10.1021/jm00168a026
PDF
A model for the antagonist binding site on the adenosine A1 receptor, based on steric, electrostatic, and hydrophobic properties
Philip J. M. Van Galen, Herman W. T. Van Vlijmen, Adriaan P. IJzerman, and Willem Soudijn
pp 1708 - 1713; DOI:
10.1021/jm00168a027
PDF
Design of peptidomimetic .delta. opioid receptor antagonists using the message-address concept
P. S. Portoghese, M. Sultana, and A. E. Takemori
pp 1714 - 1720; DOI:
10.1021/jm00168a028
PDF
Synthesis and biological evaluation of 2-styrylquinazolin-4(3H)-ones, a new class of antimitotic anticancer agents which inhibit tubulin polymerization
Jack B. Jiang, D. P. Hesson, B. A. Dusak, D. L. Dexter, G. J. Kang, and E. Hamel
pp 1721 - 1728; DOI:
10.1021/jm00168a029
PDF
Highly active and selective anticoagulants: D-Phe-Pro-Arg-H, a free tripeptide aldehyde prone to spontaneous inactivation, and its stable N-methyl derivative, D-MePhe-Pro-Arg-H
Sandor Bajusz, Erzsebet Szell, Daniel Bagdy, Eva Barabas, Gyula Horvath, Marianne Dioszegi, Zsuzsa Fittler, Gabriella Szabo, Attila Juhasz, and et al.
pp 1729 - 1735; DOI:
10.1021/jm00168a030
PDF
1,4-Bis(3-oxo-2,3-dihydropyridazin-6-yl)benzene analogs: potent phosphodiesterase inhibitors and inodilators
William J. Coates, H. Douglas Prain, Martin L. Reeves, and Brian H. Warrington
pp 1735 - 1741; DOI:
10.1021/jm00168a031
PDF
9,11-Epoxy-9-homoprosta-5-enoic acid analogs as thromboxane A2 receptor antagonists
Jagabandhu Das, Steven E. Hall, Masami Nakane, Martin F. Haslanger, Joyce A. Reid, Dianne Garber, Vu Chi Truc, Don N. Harris, Anders Hedberg, and Martin L. Ogletree
pp 1741 - 1748; DOI:
10.1021/jm00168a032
PDF
Novel 3-hydroxy-2(1H)-pyridinones. Synthesis, iron(III)-chelating properties and biological activity
Michael Streater, Paul D. Taylor, Robert C. Hider, and John Porter
pp 1749 - 1755; DOI:
10.1021/jm00168a033
PDF
Trans-10,11-dihydroxy-5,6,6a,7,8,12b-hexahydrobenzo[a]phenanthridine: a highly potent selective dopamine D1 full agonist
William K. Brewster, David E. Nichols, Robert M. Riggs, David M. Mottola, Timothy W. Lovenberg, Mark H. Lewis, and Richard B. Mailman
pp 1756 - 1764; DOI:
10.1021/jm00168a034
PDF
Structure-activity relationships for metal-labeled blood flow tracers: comparison of keto aldehyde bis(thiosemicarbazonato)copper(II) derivatives
Elizabeth K. John and Mark A. Green
pp 1764 - 1770; DOI:
10.1021/jm00168a035
PDF
Evolution of a series of peptidoleukotriene antagonists: synthesis and structure-activity relationships of 1,6-disubstituted indoles and indazoles
Frederick J. Brown, Ying K. Yee, Laura A. Cronk, Kevin C. Hebbel, Robert D. Krell, and David W. Snyder
pp 1771 - 1781; DOI:
10.1021/jm00168a036
PDF
Evolution of a series of peptidoleukotriene antagonists: synthesis and structure/activity relationships of 1,3,5-substituted indoles and indazoles
Victor G. Matassa, Thomas P. Maduskuie, Howard S. Shapiro, Barrie Hesp, David W. Snyder, David Aharony, Robert D. Krell, and Richard A. Keith
pp 1781 - 1790; DOI:
10.1021/jm00168a037
PDF
Substituted vitamin K epoxide analogs. New competitive inhibitors and substrates of vitamin K1 epoxide reductase
Robert P. Ryall, Dhirendra L. Nandi, and Richard B. Silverman
pp 1790 - 1797; DOI:
10.1021/jm00168a038
PDF
Synthesis and antiviral activity of (S)-9-[4-hydroxy-3-(phosphonomethoxy)butyl]guanine
Choung Un Kim, Bing Yu Luh, and John C. Martin
pp 1797 - 1800; DOI:
10.1021/jm00168a039
PDF
Synthesis and dopamine receptor affinities of enantiomers of 2-substituted apomorphines and their N-n-propyl analogs
Yigong Gao, Ross J. Baldessarini, Nora S. Kula, and John L. Neumeyer
pp 1800 - 1805; DOI:
10.1021/jm00168a040
PDF
Long-acting dihydropyridine calcium antagonists. 5. Synthesis and structure-activity relationships for a series of 2-[[(N-substituted-heterocyclyl)ethoxy]methyl]-1,4-dihydropyridine calcium antagonists
David Alker, Simon F. Campbell, Peter E. Cross, Roger A. Burges, Anthony J. Carter, and Donald G. Gardiner
pp 1805 - 1811; DOI:
10.1021/jm00168a041
PDF
Synthesis of quaternary amine ether lipids and evaluation of neoplastic cell growth inhibitory properties
Susan L. Morris-Natschke, Karen L. Meyer, Canio J. Marasco, Claude Piantadosi, Fiona Rossi, Patrick L. Godwin, and Edward J. Modest
pp 1812 - 1818; DOI:
10.1021/jm00168a042
PDF
Syntheses and platelet aggregation inhibitory and antithrombotic properties of [2-[(.omega.-Aminoalkoxy)phenyl]benzenes
Ryoji Kikumoto, Hiroto Hara, Kunihiro Ninomiya, Masanori Osakabe, Mamoru Sugano, Harukazu Fukami, and Yoshikuni Tamao
pp 1818 - 1823; DOI:
10.1021/jm00168a043
PDF
The synthesis and antiallergy activity of 1-(aryloxy)-4-(4-arylpiperazinyl)-2-butanol derivatives
David A. Walsh, Ying Ho Chen, Jerry B. Green, Joseph C. Nolan, and John M. Yanni
pp 1823 - 1827; DOI:
10.1021/jm00168a044
PDF
Synthesis and biological evaluation of analogs of Pro-Leu-Gly-NH2 modified at the leucyl residue
Rodney L. Johnson, Roger J. Bontems, Kaipeen E. Yang, and Ram K. Mishra
pp 1828 - 1832; DOI:
10.1021/jm00168a045
PDF
Synthesis and anti-HIV evaluation of 2',3'-dideoxyribo-5-chloropyrimidine analogs: reduced toxicity of 5-chlorinated 2',3'-dideoxynucleosides
Arthur Van Aerschot, Dirk Everaert, Jan Balzarini, Koen Augustyns, Liu Jie, Gerard Janssen, Oswald Peeters, Norbert Blaton, Camiel De Ranter, and et al.
pp 1833 - 1839; DOI:
10.1021/jm00168a046
PDF
Book Reviews

pp 1840 - 1842; DOI:
10.1021/jm00168a600
PDF

Issue 7


Cyclic hexapeptide oxytocin antagonists. Potency-, selectivity-, and solubility-enhancing modifications
Roger M. Freidinger, P. D. Williams, R. D. Tung, M. G. Bock, D. J. Pettibone, B. V. Clineschmidt, R. M. DiPardo, J. M. Erb, V. M. Garsky, and et al.
pp 1843 - 1845; DOI:
10.1021/jm00169a001
PDF
Vinblastine and vincristine are inhibitors of monoamine oxidase B
Jong Keun Son, John P. N. Rosazza, and Michael W. Duffel
pp 1845 - 1848; DOI:
10.1021/jm00169a002
PDF
Potent and highly selective neurokinin antagonists
P. Ward, G. B. Ewan, C. C. Jordan, S. J. Ireland, R. M. Hagan, and J. R. Brown
pp 1848 - 1851; DOI:
10.1021/jm00169a003
PDF
Synthesis and antiinflammatory activity of novel 12.beta.-substituted analogs of betamethasone
Mitchell A. Avery, George Detre, Dennis Yasuda, Wan Ru Chao, Masato Tanabe, David Crowe, Richard Peters, and Wesley K. M. Chong
pp 1852 - 1858; DOI:
10.1021/jm00169a004
PDF
Spiro hydantoin aldose reductase inhibitors derived from 8-aza-4-chromanones
Reinhard Sarges, Steven W. Goldstein, Willard M. Welch, Archie C. Swindell, Todd W. Siegel, and Thomas A. Beyer
pp 1859 - 1865; DOI:
10.1021/jm00169a005
PDF
1-(Thienylalkyl)imidazole-2(3H)-thiones as potent competitive inhibitors of dopamine .beta.-hydroxylase
James R. McCarthy, Donald P. Matthews, Robert J. Broersma, Roger D. McDermott, Philip R. Kastner, Jean Marie Hornsperger, David A. Demeter, Herschel J. R. Weintraub, and Jeffrey P. Whitten
pp 1866 - 1873; DOI:
10.1021/jm00169a006
PDF
Design and synthesis of highly potent and selective cyclic dynorphin A analogs
Andrew M. Kawasaki, Richard J. Knapp, Thomas H. Kramer, William S. Wire, Olga S. Vasquez, Henry I. Yamamura, Thomas F. Burks, and Victor J. Hruby
pp 1874 - 1879; DOI:
10.1021/jm00169a007
PDF
Novel piperidine derivatives. Synthesis and anti-acetylcholinesterase activity of 1-benzyl-4-[2-(N-benzoylamino)ethyl]piperidine derivatives
Hachiro Sugimoto, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizo Higurashi, Norio Karibe, Yoichi Iimura, Atsushi Sasaki, Yoshiyuki Kawakami, Takaharu Nakamura, and et al.
pp 1880 - 1887; DOI:
10.1021/jm00169a008
PDF
Synthesis of (3'R,5'S)-trans-3'-hydroxycotinine, a major metabolite of nicotine. Metabolic formation of 3'-hydroxycotinine in humans is highly stereoselective
Peyton Jacob, Alexander T. Shulgin, and Neal L. Benowitz
pp 1888 - 1891; DOI:
10.1021/jm00169a009
PDF
Effect of structure on potency and selectivity in 2,6-disubstituted-4-(2-arylethenyl)phenol lipoxygenase inhibitors
Edward S. Lazer, Hin Chor Wong, Craig D. Wegner, Anne G. Graham, and Peter R. Farina
pp 1892 - 1898; DOI:
10.1021/jm00169a010
PDF
Synthesis and calcium ion antagonistic activity of 2-[2-[(aminoalkyl)oxy]-5-methoxyphenyl]-3,4-dihydro-4-methyl-3-oxo-2H-1,4-benzothiazines
Masanobu Fujita, Susumu Ito, Atsutoshi Ota, Nobuharu Kato, Koji Yamamoto, Yoichi Kawashima, Hideyasu Yamauchi, and Junichi Iwao
pp 1898 - 1905; DOI:
10.1021/jm00169a011
PDF
Structure-activity relationships of 8-cycloalkyl-1,3-dipropylxanthines as antagonists of adenosine receptors
T. Katsushima, L. Nieves, and J. N. Wells
pp 1906 - 1910; DOI:
10.1021/jm00169a012
PDF
Benzodiazepine receptor-binding activity of 9-(1-phenylethyl)purines
James L. Kelley, Ed W. McLean, Robert M. Ferris, and James L. Howard
pp 1910 - 1914; DOI:
10.1021/jm00169a013
PDF
Structure-activity relationships of antineoplastic agents in multidrug resistance
Cynthia D. Selassie, Corwin Hansch, and Tasneem A. Khwaja
pp 1914 - 1919; DOI:
10.1021/jm00169a014
PDF
2-(Arylalkylamino)adenosin-5'-uronamides: a new class of highly selective adenosine A2 receptor ligands
Alan J. Hutchison, Michael Williams, Reynalda De Jesus, Rina Yokoyama, Howard H. Oei, Geetha R. Ghai, Randy L. Webb, Harry C. Zoganas, George A. Stone, and Michael F. Jarvis
pp 1919 - 1924; DOI:
10.1021/jm00169a015
PDF
5-Hydroxytryptamine (5-HT3) receptor antagonists. 1. Indazole and indolizine-3-carboxylic acid derivatives
Jose Bermudez, Charles S. Fake, Graham F. Joiner, Karen A. Joiner, Frank D. King, Wesley D. Miner, and Gareth J. Sanger
pp 1924 - 1929; DOI:
10.1021/jm00169a016
PDF
5-Hydroxytryptamine (5-HT3) receptor antagonists. 2. 1-Indolinecarboxamides
Jose Bermudez, Steven Dabbs, Karen A. Joiner, and Frank D. King
pp 1929 - 1932; DOI:
10.1021/jm00169a017
PDF
5-Hydroxytryptamine (5-HT3) receptor antagonists. 3. Ortho-substituted phenylureas
Jose Bermudez, Steven Dabbs, and Frank D. King
pp 1932 - 1935; DOI:
10.1021/jm00169a018
PDF
Conformational restriction of angiotensin II: cyclic analogs having high potency
Kerry L. Spear, Monica S. Brown, Emily J. Reinhard, Ellen G. McMahon, Gillian M. Olins, Maria A. Palomo, and Dennis R. Patton
pp 1935 - 1940; DOI:
10.1021/jm00169a019
PDF
Crystallographic studies of angiotensin converting enzyme inhibitors and analysis of preferred zinc coordination geometry
Roland J. Hausin and Penelope W. Codding
pp 1940 - 1947; DOI:
10.1021/jm00169a020
PDF
Chalcones: a new class of antimitotic agents
Michael L. Edwards, David M. Stemerick, and Prasad S. Sunkara
pp 1948 - 1954; DOI:
10.1021/jm00169a021
PDF
Analogs of growth hormone-releasing factor (1-29) amide containing the reduced peptide bond isostere in the N-terminal region
Simon J. Hocart, William A. Murphy, and David H. Coy
pp 1954 - 1958; DOI:
10.1021/jm00169a022
PDF
Cyclohexane diester analogs of phorbol ester as potential activators of protein kinase C
David E. Kerr, Lon F. Kissinger, and Mohammed Shoyab
pp 1958 - 1962; DOI:
10.1021/jm00169a023
PDF
Water-soluble renin inhibitors: design of a subnanomolar inhibitor with a prolonged duration of action
Saul H. Rosenberg, Keith W. Woods, Hing L. Sham, Hollis D. Kleinert, Donald L. Martin, Herman Stein, Jerome Cohen, David A. Egan, Barbara Bopp, and et al.
pp 1962 - 1969; DOI:
10.1021/jm00169a024
PDF
Inhibition of ornithine decarboxylase by the isomers of 1,4-dimethylputrescine
Nora Moyano, Judith Frydman, Graciela Buldain, Oscar Ruiz, and Rosalia B. Frydman
pp 1969 - 1974; DOI:
10.1021/jm00169a025
PDF
Synthesis and biological activities of novel 5-(2-acylethynyl)uracils
Nitya G. Kundu, Biswajit Das, C. Paul Spears, Anjali Majumdar, and San Ihn Kang
pp 1975 - 1979; DOI:
10.1021/jm00169a026
PDF
Synthesis and antiviral activity of some 7-[(2-hydroxyethoxy)methyl]pyrazolo[3,4-d]pyrimidine analogs of sangivamycin and toyocamycin
Naveen K. Saxena, Lisa A. Coleman, John C. Drach, and Leroy B. Townsend
pp 1980 - 1983; DOI:
10.1021/jm00169a027
PDF
Synthesis, antiproliferative, and antiviral activity of certain 4-substituted and 4,5-disubstituted 7-[(1,3-dihydroxy-2-propoxy)methyl]pyrrolo[2,3-d]pyrimidines
Jeffrey S. Pudlo, M. Reza Nassiri, Earl R. Kern, Linda L. Wotring, John C. Drach, and Leroy B. Townsend
pp 1984 - 1992; DOI:
10.1021/jm00169a028
PDF
Synthesis and antiviral activity of metabolites of rimantadine
Percy S. Manchand, Richard L. Cerruti, Joseph A. Martin, Christopher H. Hill, John H. Merrett, Elizabeth Keech, Robert B. Belshe, Edward V. Connell, and Iain S. Sim
pp 1992 - 1995; DOI:
10.1021/jm00169a029
PDF
Nucleosides. 153. Synthesis of 1-methyl-5-(3-azido-2,3-dideoxy-.beta.-D-erythro-pentofuranosyl)uracil and 1-methyl-5-(3-azido-2,3-dideoxy-2-fluoro-.beta.-D-arabinofuranosyl)uracil. The C-nucleoside isostere of 3'-azido-3'-deoxythymidine and its 2'-"up"-fluoro analog
Elzbieta Sochacka, Barbara Nawrot, Krzysztof W. Pankiewicz, and Kyoichi A. Watanabe
pp 1995 - 1999; DOI:
10.1021/jm00169a030
PDF
Monomethyl ether derivatives of 7,8-dihydroxy- and 8,9-dihydroxy-4-propyl-1,2,3,4,4a,5,6,10b-octahydrobenzo[f]quinolines as possible products of metabolism by catechol-O-methyltransferase
Joseph G. Cannon, Kathleen A. Walker, Antonio Montanari, John Paul Long, and Jan R. Flynn
pp 2000 - 2006; DOI:
10.1021/jm00169a031
PDF
Synthesis, antitumor activity, and antiviral activity of 3-substituted 3-deazacytidines and 3-substituted 3-deazauridines
Dennis J. McNamara, P. Dan Cook, Lois B. Allen, Mary Jo Kehoe, Carolyn S. Holland, and Annette G. Teepe
pp 2006 - 2011; DOI:
10.1021/jm00169a032
PDF
Synthesis and antibacterial activity of thiazolo-, oxazolo-, and imidazolo[3,2-a][1,8]naphthyridinecarboxylic acids
Hirosato Kondo, Masahiro Taguchi, Yoshimasa Inoue, Fumio Sakamoto, and Goro Tsukamoto
pp 2012 - 2015; DOI:
10.1021/jm00169a033
PDF
Synthesis of (R)-(-)- and (S)-(+)-4-fluorodeprenyl, (R)-(-)- and (S)-(+)-[N-11C-methyl]-4-fluorodeprenyl and PET studies in baboon brain
Alain Plenevaux, Stephen L. Dewey, Joanna S. Fowler, Marcel Guillaume, and Alfred P. Wolf
pp 2015 - 2019; DOI:
10.1021/jm00169a034
PDF
1,2-Dihydro-1-oxopyrrolo[3,2,1-kl]phenothiazine-2-carboxamides and congeners, dual cyclooxygenase/5-lipoxygenase inhibitors with anti-inflammatory activity
Banavara L. Mylari, Thomas J. Carty, Peter F. Moore, and William J. Zembrowski
pp 2019 - 2024; DOI:
10.1021/jm00169a035
PDF
Synthesis of 3-arylecgonine analogs as inhibitors of cocaine binding and dopamine uptake
Richard H. Kline, Jeremy Wright, Kristine M. Fox, and Mohyee E. Eldefrawi
pp 2024 - 2027; DOI:
10.1021/jm00169a036
PDF
Synthesis and antiallergy activity of N-[2-(dimethylamino)ethyl]-4-aryl-1-piperazinecarboxamide derivatives
David A. Walsh, Jerry B. Green, Stephen K. Franzyshen, Joseph C. Nolan, and John M. Yanni
pp 2028 - 2032; DOI:
10.1021/jm00169a037
PDF
Porphyrin dimers as photosensitizers in photodynamic therapy
Ravindra K. Pandey, Kevin M. Smith, and Thomas J. Dougherty
pp 2032 - 2038; DOI:
10.1021/jm00169a038
PDF
Kinetic and equilibrium binding studies of amsacrine-4-carboxamides: a class of asymmetrical DNA intercalating agents which bind by threading through the DNA helix
Laurence P. G. Wakelin, Pat Chetcuti, and William A. Denny
pp 2039 - 2044; DOI:
10.1021/jm00169a039
PDF
Potent inhibition of thymidylate synthase by two series of nonclassical quinazolines
Dennis J. McNamara, Ellen M. Berman, David W. Fry, and Leslie M. Werbel
pp 2045 - 2051; DOI:
10.1021/jm00169a040
PDF
Synthesis and muscarinic activities of 1,2,4-thiadiazoles
Angus M. MacLeod, Raymond Baker, Stephen B. Freedman, Shailendra Patel, Kevin J. Merchant, Michael Roe, and John Saunders
pp 2052 - 2059; DOI:
10.1021/jm00169a041
PDF
Book Reviews

pp 2059 - 2062; DOI:
10.1021/jm00169a600
PDF

Issue 8


Improved delivery through biological membranes. 36. Extension of a redox-based chemical-delivery system to .alpha.,.beta.-unsaturated ketones
Marcus E. Brewster, Margaret Deyrup, Klara Czako, and Nicholas Bodor
pp 2063 - 2065; DOI:
10.1021/jm00170a001
PDF
A radiotracer for mapping cholinergic neurons of the brain
Yong Woon Jung, Marcian E. Van Dort, David L. Gildersleeve, and Donald M. Wieland
pp 2065 - 2068; DOI:
10.1021/jm00170a002
PDF
Methylsulfamic acid esters. A new chemical class of oral antiarthritic agents
David A. Walsh, Young S. Lo, Dwight A. Shamblee, William J. Welstead, Joseph C. Nolan, and Gustav Graff
pp 2068 - 2070; DOI:
10.1021/jm00170a003
PDF
Nonsteroidal anti-inflammatory drug hydroxamic acids. Dual inhibitors of both cyclooxygenase and 5-lipoxygenase
Daniel L. Flynn, Thomas Capiris, W. J. Cetenko, David T. Connor, Richard D. Dyer, Catherine R. Kostlan, Donald E. Nies, Denis J. Schrier, and Jagadish C. Sircar
pp 2070 - 2072; DOI:
10.1021/jm00170a004
PDF
Purine derivatives as competitive inhibitors of human erythrocyte membrane phosphatidylinositol 4-kinase
Rodney C. Young, Martin Jones, Kevin J. Milliner, Kishore K. Rana, and John G. Ward
pp 2073 - 2080; DOI:
10.1021/jm00170a005
PDF
Thermodynamics of the interaction of inhibitors with the binding site of recombinant human renin
D. E. Epps, J. Cheney, H. Schostarez, T. K. Sawyer, M. Prairie, W. C. Krueger, and F. Mandel
pp 2080 - 2086; DOI:
10.1021/jm00170a006
PDF
3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1*) agonist and rotationally restricted phenolic analog of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole
John E. Macor, Carol A. Burkhart, James H. Heym, Jeffrey L. Ives, Lorraine A. Lebel, Michael E. Newman, Jann A. Nielsen, Kevin Ryan, David W. Schulz, and et al.
pp 2087 - 2093; DOI:
10.1021/jm00170a007
PDF
Antiandrogenic steroidal sulfonylpyrazoles
Robert G. Christiansen, Malcolm R. Bell, Thomas E. D'Ambra, John P. Mallamo, John L. Herrmann, James H. Ackerman, Chester J. Opalka, Rudolph K. Kullnig, Richard C. Winneker, and et al.
pp 2094 - 2100; DOI:
10.1021/jm00170a008
PDF
Synthesis of a new class of 2,3-dihydro-2-oxo-1H-benzimidazole-1-carboxylic acid derivatives as highly potent 5-HT3 receptor antagonists
Marco Turconi, Massimo Nicola, Myrna Gil Quintero, Luciano Maiocchi, Rosella Micheletti, Ettore Giraldo, and Arturo Donetti
pp 2101 - 2108; DOI:
10.1021/jm00170a009
PDF
Synthesis and biological evaluation of new antimuscarinic compounds with amidine basic centers. A useful bioisosteric replacement of classical cationic heads
Enzo Cereda, Antoine Ezhaya, Myrna Gil Quintero, Elio Bellora, Enrica Dubini, Rosella Micheletti, Antonio Schiavone, Alessandro Brambilla, Giovanni Battista Schiavi, and Arturo Donetti
pp 2108 - 2113; DOI:
10.1021/jm00170a010
PDF
Synthesis and biological evaluation of a series of parenteral 3'-quaternary ammonium cephalosporins
Raymond F. Brown, Michael D. Kinnick, John M. Morin Jr., Robert T. Vasileff, Fred T. Counter, Edward O. Davidson, Paul W. Ensminger, Judith A. Eudaly, Jeffrey S. Kasher, and et al.
pp 2114 - 2121; DOI:
10.1021/jm00170a011
PDF
Synthesis and activity of NAcSerAspLysPro analogs on cellular interactions between T-cell and erythrocytes in rosette formation
Josiane Thierry, Marie Pierre Papet, Nathalie Saez-Servent, Jacqueline Plissonneau-Haumont, Pierre Potier, and Maryse Lenfant
pp 2122 - 2127; DOI:
10.1021/jm00170a012
PDF
Synthesis and broad-spectrum antiviral activity of 7,8-dihydro-7-methyl-8-thioxoguanosine
Elizabeth M. Henry, Ganesh D. Kini, Steven B. Larson, Roland K. Robins, Hassan A. Alaghamandan, and Donald F. Smee
pp 2127 - 2130; DOI:
10.1021/jm00170a013
PDF
Synthesis and central nervous system actions of thyrotropin-releasing hormone analog containing a dihydroorotic acid moiety
Mamoru Suzuki, Hiroshi Sugano, Kazuo Matsumoto, Michio Yamamura, and Ryuichi Ishida
pp 2130 - 2137; DOI:
10.1021/jm00170a014
PDF
Synthesis and antiviral activity of monofluoro and difluoro analogs of pyrimidine deoxyribonucleosides against human immunodeficiency virus (HIV-1)
Joseph A. Martin, David J. Bushnell, Ian B. Duncan, Stephen J. Dunsdon, Michael J. Hall, Peter J. Machin, John H. Merrett, Kevin E. B. Parkes, Noel A. Roberts, and et al.
pp 2137 - 2145; DOI:
10.1021/jm00170a015
PDF
Synthesis and anti-HIV-1 activity of 2'-"up"-fluoro analogs of active anti-AIDS nucleosides 3'-azido-3'-deoxythymidine (AZT) and 2',3'-dideoxycytidine (DDC)
Kyoichi A. Watanabe, Kazuho Harada, Joanna Zeidler, Jasenka Matulic-Adamic, Kiyobumi Takahashi, Wu Yun Ren, Ling Chin Cheng, Jack J. Fox, Ting Chao Chou, and et al.
pp 2145 - 2150; DOI:
10.1021/jm00170a016
PDF
Synthesis and anti-HIV activity of several 2'-fluoro-containing pyrimidine nucleosides
Roman Z. Sterzycki, Ismail Ghazzouli, Vera Brankovan, John C. Martin, and Muzammil M. Mansuri
pp 2150 - 2157; DOI:
10.1021/jm00170a017
PDF
2-(4-Amino-4-carboxybutyl)aziridine-2-carboxylic acid. A potent irreversible inhibitor of diaminopimelic acid epimerase. Spontaneous formation from .alpha.-(halomethyl)diaminopimelic acids
Fritz Gerhart, William Higgins, Chantal Tardif, and Jean Bernard Ducep
pp 2157 - 2162; DOI:
10.1021/jm00170a018
PDF
Synthesis and antiviral activity of some acyclic and C-acyclic pyrrolo[2,3-d]pyrimidine nucleoside analogs
Sharon M. Bennett, Nguyen Ba Nghe, and Kelvin K. Ogilvie
pp 2162 - 2173; DOI:
10.1021/jm00170a019
PDF
Guanosine analogs. Synthesis of nucleosides of certain 3-substituted 6-aminopyrazolo[3,4-d]pyrimidin-4(5H)-ones as potential immunotherapeutic agents
Roger J. Bontems, Jack D. Anderson, Donald F. Smee, Ai Jin, Hassan A. Alaghamandan, Brahma S. Sharma, Weldon B. Jolley, Roland K. Robins, and Howard B. Cottam
pp 2174 - 2178; DOI:
10.1021/jm00170a020
PDF
Cytotoxicity and antitumor activity of bis(platinum) complexes. A novel class of platinum complexes active in cell lines resistant to both cisplatin and 1,2-diaminocyclohexane complexes
Nicholas Farrell, Yun Qu, and Miles P. Hacker
pp 2179 - 2184; DOI:
10.1021/jm00170a021
PDF
Antitumor and DNA-binding properties of a group of oligomeric complexes of platinum(II) and platinum(IV)
Adam Peritz, Salaam Al-Baker, Jean F. Vollano, James C. Dabrowiak, John E. Schurig, and William T. Bradner
pp 2184 - 2188; DOI:
10.1021/jm00170a022
PDF
Brain targeting of anti-HIV nucleosides: synthesis and in vitro and in vivo studies of dihydropyridine derivatives of 3'-azido-2',3'-dideoxyuridine and 3'-azido-3'-deoxythymidine
C. K. Chu, V. S. Bhadti, K. J. Doshi, J. T. Etse, J. M. Gallo, F. D. Boudinot, and R. F. Schinazi
pp 2188 - 2192; DOI:
10.1021/jm00170a023
PDF
Organic phosphorus compounds. 5. (4-Benzothiazol-2-ylbenzyl)amidophosphonate as potent calcium antagonistic vasodilators
Kohichiro Yoshino, Katsumi Goto, Kazuya Yoshiizumi, Tominori Morita, and Goro Tsukamoto
pp 2192 - 2196; DOI:
10.1021/jm00170a024
PDF
Conformational analysis and structure-activity relationships of selective dopamine D-1 receptor agonists and antagonists of the benzazepine series
Ingrid Pettersson, Tommy Liljefors, and Klaus Boegesoe
pp 2197 - 2204; DOI:
10.1021/jm00170a025
PDF
Synthesis and biological evaluation of 4-fluoro-, 7-fluoro-, and 4,7-difluoro-5,6-dihydroxytryptamines
Masami Kawase, Achintya K. Sinhababu, Eva M. McGhee, Terry Milby, and Ronald T. Borchardt
pp 2204 - 2211; DOI:
10.1021/jm00170a026
PDF
Synthesis, phencyclidine-like pharmacology, and antiischemic potential of meta-substituted 1-(1-phenylcyclohexyl)-1,2,3,6-tetrahydropyridines
Andrew Thurkauf, Brian De Costa, Mariena V. Mattson, Charles P. France, Madelon T. Price, John W. Olney, James H. Woods, A. E. Jacobson, and Kenner C. Rice
pp 2211 - 2215; DOI:
10.1021/jm00170a027
PDF
Improved delivery through biological membranes. 50. Antihypertensive activity of redox derivatives of tryptophan
Emil Pop, Wesley Anderson, Katalin Prokai-Tatrai, Marcus E. Brewster, Melvin Fregly, and Nicholas Bodor
pp 2216 - 2221; DOI:
10.1021/jm00170a028
PDF
In vivo intracerebral microdialysis studies in rats of MPP+ (1-methyl-4-phenylpyridinium) analogs and related charged species
Hans Rollema, E. Anne Johnson, Raymond G. Booth, Patricia Caldera, Peter Lampen, Stephen K. Youngster, Anthony J. Trevor, Noreen Naiman, and Neal Castagnoli
pp 2221 - 2230; DOI:
10.1021/jm00170a029
PDF
Inotropic 'A' ring substituted sulmazole and isomazole analogs
Paul Barraclough, James W. Black, David Cambridge, David Collard, David Firmin, V. Paul Gerskowitch, Robert C. Glen, Heather Giles, Alan P. Hill, and et al.
pp 2231 - 2239; DOI:
10.1021/jm00170a030
PDF
4-Amino[1,2,4]triazolo[4,3-a]quinoxalines. A novel class of potent adenosine receptor antagonists and potential rapid-onset antidepressants
Reinhard Sarges, Harry R. Howard, Ronald G. Browne, Lorraine A. Lebel, Patricia A. Seymour, and B. Kenneth Koe
pp 2240 - 2254; DOI:
10.1021/jm00170a031
PDF
4-Isoxazolyl-1,4-dihydropyridines: biological, theoretical, and structural studies
N. R. Natale, David J. Triggle, Robert B. Palmer, Barbara J. Lefler, and W. Daniel Edwards
pp 2255 - 2259; DOI:
10.1021/jm00170a032
PDF
Synthesis and evaluation of 1,2,2-tris(sulfonyl)hydrazines as antineoplastic and trypanocidal agents
Krishnamurthy Shyam, Philip G. Penketh, Alan A. Divo, Regina H. Loomis, Curtis L. Patton, and Alan C. Sartorelli
pp 2259 - 2264; DOI:
10.1021/jm00170a033
PDF
Monophosphoric acid diesters of 7.beta.-hydroxycholesterol and of pyrimidine nucleosides as potential antitumor agents: synthesis and preliminary evaluation of antitumor activity
Yu Hua Ji, Christiane Moog, Gaby Schmitt, Pierre Bischoff, and Bang Luu
pp 2264 - 2270; DOI:
10.1021/jm00170a034
PDF
Quinolone antibacterial agents substituted at the 7-position with spiroamines. Synthesis and structure-activity relationships
Townley P. Culbertson, Joseph P. Sanchez, Laura Gambino, and Josephine A. Sesnie
pp 2270 - 2275; DOI:
10.1021/jm00170a035
PDF
Potent renin inhibitory peptides containing hydrophilic end groups
Gordon L. Bundy, Donald T. Pals, Judy A. Lawson, Sally J. Couch, Michael F. Lipton, and Michael A. Mauragis
pp 2276 - 2283; DOI:
10.1021/jm00170a036
PDF
Resolution, absolute stereochemistry, and enantioselectivity of 2-methyl-4-phenyl-1,2,3,4-tetrahydroisoquinolin-4-ol
Masaru Kihara, Minoru Kashimoto, Shigeru Kobayashi, Yukio Ishida, Hideki Moritoki, and Zenei Taira
pp 2283 - 2286; DOI:
10.1021/jm00170a037
PDF
Electrophilic .alpha.-methylene-.gamma.-lactone and isothiocyanate opioid ligands related to etorphine
Peter Klein, Wendel L. Nelson, Yi He Yao, and Eric J. Simon
pp 2286 - 2296; DOI:
10.1021/jm00170a038
PDF
Antiinflammatory agents. 4. Syntheses and biological evaluation of potential pro-drugs of 2-amino-3-benzoylbenzeneacetic acid and 2-amino-3-(4-chlorobenzoyl)benzeneacetic acid
David A. Walsh, H. Wayne Moran, Dwight A. Shamblee, William J. Welstead, Joseph C. Nolan, Lawrence F. Sancilio, and Gustav Graff
pp 2296 - 2304; DOI:
10.1021/jm00170a039
PDF
Potential antipsychotic agents. 7. Synthesis and antidopaminergic properties of the atypical highly potent (S)-5-bromo-2,3-dimethoxy-N-[(1-ethyl-2-pyrrolidinyl)methyl]benzamide and related compounds. A comparative study
Thomas Hoegberg, Tomas De Paulis, Lars Johansson, Yatendra Kumar, Haakan Hall, and Sven Ove Oegren
pp 2305 - 2309; DOI:
10.1021/jm00170a040
PDF
Book Reviews

pp 2310 - 2310; DOI:
10.1021/jm00170a600
PDF

Issue 9


Bioactive alkaloids. 4. Results of recent investigations with colchicine and physostigmine
Arnold Brossi
pp 2311 - 2319; DOI:
10.1021/jm00171a001
PDF
Trifluoromethylacetylenic alcohols as affinity labels: inactivation of estradiol dehydrogenase by a trifluoromethylacetylenic secoestradiol
Saurabh S. Lawate and Douglas F. Covey
pp 2319 - 2321; DOI:
10.1021/jm00171a002
PDF
Receptor ligands which bind the oxytocin receptor with selectivity and high affinity. Chemical modification of a Streptomyces silvensis derived cyclic hexapeptide
Mark G. Bock, R. M. DiPardo, P. D. Williams, D. J. Pettibone, B. V. Clineschmidt, R. G. Ball, D. F. Veber, and R. M. Freidinger
pp 2321 - 2323; DOI:
10.1021/jm00171a003
PDF
Azulene derivatives: new non-prostanoid thromboxane A2 receptor antagonists
Tsuyoshi Tomiyama, Shuichi Wakabayashi, Kazuhiro Kosakai, and Masayuki Yokota
pp 2323 - 2326; DOI:
10.1021/jm00171a004
PDF
1,2,4-Triazolo[4,3-a]pyrazine derivatives with human renin inhibitory activity. 1. Synthesis and biological properties of alkyl alcohol and statine derivatives
David A. Roberts, Robert H. Bradbury, David Brown, Alan Faull, David Griffiths, John S. Major, Alec A. Oldham, Robert J. Pearce, Arnold H. Ratcliffe, and et al.
pp 2326 - 2334; DOI:
10.1021/jm00171a005
PDF
1,2,4-Triazolo[4,3-a]pyrazine derivatives with human renin inhibitory activity. 2. Synthesis, biological properties and molecular modeling of hydroxyethylene isostere derivatives
Robert H. Bradbury, John S. Major, Alec A. Oldham, Janet E. Rivett, David A. Roberts, Anthony M. Slater, David Timms, and David Waterson
pp 2335 - 2342; DOI:
10.1021/jm00171a006
PDF
Synthetic and computer-assisted analyses of the pharmacophore for the benzodiazepine receptor inverse agonist site
Michael S. Allen, Yun C. Tan, Mark L. Trudell, Kris Narayanan, Liesl R. Schindler, Michael J. Martin, Christopher Schultz, Timothy J. Hagen, Konrad F. Koehler, and et al.
pp 2343 - 2357; DOI:
10.1021/jm00171a007
PDF
Synthesis and quantitative structure-activity relationships of diclofenac analogs
Peter Moser, Alfred Sallmann, and Irmgard Wiesenberg
pp 2358 - 2368; DOI:
10.1021/jm00171a008
PDF
Synthesis and biological evaluation of some cyclic phosphoramidate nucleoside derivatives
A. Kumar, P. L. Coe, A. S. Jones, R. T. Walker, J. Balzarini, and Eric De Clercq
pp 2368 - 2375; DOI:
10.1021/jm00171a009
PDF
Synthesis and antitumor activity of novel 4-demethoxyanthracyclines
Nigel Adams, Colin Blake, Michael J. Broadhurst, David J. Bushnell, Cedric H. Hassall, Hans R. Hartmann, Elizabeth Keech, Alan R. Stratton, and Gareth J. Thomas
pp 2375 - 2379; DOI:
10.1021/jm00171a010
PDF
Synthesis and antitumor activity of 9-[(carbamoyloxy)alkyl]anthracyclines a novel class of anthracycline derivatives
Nigel Adams, Colin Blake, Michael J. Broadhurst, David J. Bushnell, Cedric H. Hassall, Hans R. Hartmann, Elizabeth Keech, Alan R. Stratton, and Gareth J. Thomas
pp 2380 - 2384; DOI:
10.1021/jm00171a011
PDF
[(1-Pyrenylmethyl)amino] alcohols, a new class of antitumor DNA intercalators. Discovery and initial amine side chain structure-activity studies
Kenneth W. Bair, Richard L. Tuttle, Vincent C. Knick, Michael Cory, and David D. McKee
pp 2385 - 2393; DOI:
10.1021/jm00171a012
PDF
Novel agents effective against solid tumors: the diarylsulfonylureas. Synthesis, activities, and analysis of quantitative structure-activity relationships
J. Jeffry Howbert, C. Sue Grossman, Thomas A. Crowell, Brent J. Rieder, Richard W. Harper, Kenneth E. Kramer, Eddie V. Tao, James Aikins, Gerald A. Poore, and et al.
pp 2393 - 2407; DOI:
10.1021/jm00171a013
PDF
Synthesis and dopamine receptor affinities of 2-(4-fluoro-3-hydroxyphenyl)ethylamine and N-substituted derivatives
Francesco Claudi, Mario Cardellini, Gian Mario Cingolani, Alessandro Piergentili, Guidubaldo Peruzzi, and Walter Balduini
pp 2408 - 2412; DOI:
10.1021/jm00171a014
PDF
Synthesis of substituted 7,12-dihydropyrido[3,2-b:5,4-b']diindoles: rigid planar benzodiazepine receptor ligands with inverse agonist/antagonist properties
Mark L. Trudell, Sherry L. Lifer, Yun Chou Tan, Michael J. Martin, Li Deng, Phil Skolnick, and James M. Cook
pp 2412 - 2420; DOI:
10.1021/jm00171a015
PDF
Synthesis and structure-activity relationships of N,N'-di-o-tolylguanidine analogs, high-affinity ligands for the haloperidol-sensitive .sigma. receptor
Michael W. Scherz, Michelle Fialeix, James B. Fischer, N. Laxma Reddy, Alfred C. Server, Mark S. Sonders, Barbara C. Tester, Eckard Weber, Scott T. Wong, and John F. W. Keana
pp 2421 - 2429; DOI:
10.1021/jm00171a016
PDF
N-Fluoroalkylated and N-alkylated analogs of the dopaminergic D-2 receptor antagonist raclopride
G. S. Lannoye, Stephen M. Moerlein, D. Parkinson, and M. J. Welch
pp 2430 - 2437; DOI:
10.1021/jm00171a017
PDF
A novel series of selective leukotriene antagonists: exploration and optimization of the acidic region in 1,6-disubstituted indoles and indazoles
Ying K. Yee, Peter R. Bernstein, Edward J. Adams, Frederick J. Brown, Laura A. Cronk, Kevin C. Hebbel, Edward P. Vacek, Robert D. Krell, and David W. Snyder
pp 2437 - 2451; DOI:
10.1021/jm00171a018
PDF
Hydroxyperfluoroazobenzenes: novel inhibitors of enzymes of androgen biosynthesis
Michael Jarman, S. Elaine Barrie, John J. Deadman, John Houghton, Raymond McCague, and Martin G. Rowlands
pp 2452 - 2455; DOI:
10.1021/jm00171a019
PDF
Photoactivatable opiate derivatives as irreversible probes of the .mu.-opioid receptor
Jean Luc Galzi, Annick Mejean, Brigitte Ilien, Catherine Mollereau, Jean Claude Meunier, Maurice Goeldner, and Christian Hirth
pp 2456 - 2464; DOI:
10.1021/jm00171a020
PDF
7-Oxabicyclo[2.2.1]heptyl carboxylic acids as thromboxane A2 antagonists: aza .omega.-chain analogs
Masami Nakane, Joyce A. Reid, Wen Ching Han, Jagabandhu Das, Vu Chi Truc, Martin F. Haslanger, Dianne Garber, Don N. Harris, Anders Hedberg, and et al.
pp 2465 - 2476; DOI:
10.1021/jm00171a021
PDF
Synthesis of new (.+-.)-3,5-dihydroxypentyl nucleoside analogs from 1-amino-5-(benzyloxy)pentan-3-ol and their antiviral evaluation
Michel Legraverend, Hassane Boumchita, Aurelio Zerial, Christiane Huel, Marc Lemaitre, and Emile Bisagni
pp 2476 - 2480; DOI:
10.1021/jm00171a022
PDF
5'-O-Phosphonomethyl-2',3'-dideoxynucleosides: synthesis and anti-HIV activity
Liu Jie, Arthur Van Aerschot, Jan Balzarini, Gerard Janssen, Roger Busson, Jos Hoogmartens, Erik De Clercq, and Piet Herdewijn
pp 2481 - 2487; DOI:
10.1021/jm00171a023
PDF
Synthesis and antiviral activity of some 3'-C-difluoromethyl- and 3'-deoxy-3'-C-fluoromethyl nucleosides
Mark J. Bamford, Paul L. Coe, and Richard T. Walker
pp 2488 - 2494; DOI:
10.1021/jm00171a024
PDF
Synthesis and antiviral activity of 3'-deoxy-3'-C-hydroxymethyl nucleosides
Mark J. Bamford, Paul L. Coe, and Richard T. Walker
pp 2494 - 2501; DOI:
10.1021/jm00171a025
PDF
S-[2-[(2'-carbamoylethyl)amino]ethyl] phosphorothioate and related compounds as potential antiradiation agents
F. Ivy Carroll, M. B. Gopinathan, and Abraham Philip
pp 2501 - 2508; DOI:
10.1021/jm00171a026
PDF
Synthesis and evaluation of novel electrophilic nitrofuran carboxamides and carboxylates as radiosensitizers and bioreductively activated cytotoxins
Matthew A. Naylor, Miriam A. Stephens, Shirley Cole, Michael D. Threadgill, Ian J. Stratford, Peter O'Neill, E. Martin Fielden, and Gerald E. Adams
pp 2508 - 2513; DOI:
10.1021/jm00171a027
PDF
Inhibition of human leukocyte elastase. 1. Inhibition by C-7-substituted cephalosporin tert-butyl esters
James B. Doherty, Bonnie M. Ashe, Peter L. Barker, Thomas J. Blacklock, John W. Butcher, Gilbert O. Chandler, M. Ellen Dahlgren, Philip Davies, Conrad P. Dorn Jr., and et al.
pp 2513 - 2521; DOI:
10.1021/jm00171a028
PDF
Inhibition of human leukocyte elastase. 2. Inhibition by substituted cephalosporin esters and amides
Paul E. Finke, Bonnie M. Ashe, Wilson B. Knight, Alan L. Maycock, Manuel A. Navia, Shrenik K. Shah, Kevan R. Thompson, Dennis J. Underwood, Hazel Weston, and et al.
pp 2522 - 2528; DOI:
10.1021/jm00171a029
PDF
Inhibition of human leukocyte elastase. 3. Synthesis and activity of 3'-substituted cephalosporins
Shrenik K. Shah, Karen A. Brause, Gilbert O. Chandler, Paul E. Finke, Bonnie M. Ashe, Hazel Weston, Wilson B. Knight, Alan L. Maycock, and James B. Doherty
pp 2529 - 2535; DOI:
10.1021/jm00171a030
PDF
Aqua[1-(2,6-dichloro-4-hydroxyphenyl)-2-phenylethylenediamine](sulfato)platinum(II) complexes with variable substituents in the 2-phenyl ring. 1. Synthesis and antitumor and estrogenic properties
Ronald Gust, Thomas Burgemeister, Albrecht Mannschreck, and Helmut Schoenenberger
pp 2535 - 2544; DOI:
10.1021/jm00171a031
PDF
Approaches to isozyme-specific inhibitors. 17. Attachment of a selectivity-inducing substituent to a multisubstrate adduct. Implications for facilitated design of potent, isozyme-selective inhibitors
Francis Kappler and Alexander Hampton
pp 2545 - 2551; DOI:
10.1021/jm00171a032
PDF
Novel inhibitors of human renin. Cyclic peptides based on the tetrapeptide sequence Glu-D-Phe-Lys-D-Trp
Anand S. Dutta, James J. Gormley, Peter F. McLachlan, and John S. Major
pp 2552 - 2560; DOI:
10.1021/jm00171a033
PDF
Inhibitors of human renin. Cyclic peptide analogs containing a D-Phe-Lys-D-Trp sequence
Anand S. Dutta, James J. Gormley, Peter F. McLachlan, and John S. Major
pp 2560 - 2568; DOI:
10.1021/jm00171a034
PDF
Antibacterials. Synthesis and structure-activity studies of 3-aryl-2-oxooxazolidines. 2. The "A" group
Walter A. Gregory, David R. Brittelli, C. L. J. Wang, Hollis S. Kezar, III, Randall K. Carlson, Chung Ho Park, Peter F. Corless, Steven J. Miller, P. Rajagopalan, and et al.
pp 2569 - 2578; DOI:
10.1021/jm00171a035
PDF
1,3-Dialkyl-3-acyltriazenes, a novel class of antineoplastic alkylating agents
R. H. Smith, D. A. Scudiero, and Christopher J. Michejda
pp 2579 - 2583; DOI:
10.1021/jm00171a036
PDF
Neural networks applied to pharmaceutical problems. III. Neural networks applied to quantitative structure-activity relationship (QSAR) analysis
Tomoo Aoyama, Yuji Suzuki, and Hiroshi Ichikawa
pp 2583 - 2590; DOI:
10.1021/jm00171a037
PDF
Cyclization-activated prodrugs. Basic esters of 5-bromo-2'-deoxyuridine
Walfred S. Saari, John E. Schwering, Paulette A. Lyle, Steven J. Smith, and Edward L. Engelhardt
pp 2590 - 2595; DOI:
10.1021/jm00171a038
PDF
Synthesis of new nucleoside phosphoraziridines as potential site-directed antineoplastic agents
Robert G. Breiner, William C. Rose, Joseph A. Dunn, Joan E. MacDiarmid, and Thomas J. Bardos
pp 2596 - 2602; DOI:
10.1021/jm00171a039
PDF
Synthesis and evaluation of .alpha.-[[(2-haloethyl)amino]methyl]-2-nitro-1H-imidazole-1-ethanols as prodrugs of .alpha.-[(1-aziridinyl)methyl]-2-nitro-1H-imidazole-1-ethanol (RSU-1069) and its analogs which are radiosensitizers and bioreductively activated cytotoxins
Terence C. Jenkins, Matthew A. Naylor, Peter O'Neill, Michael D. Threadgill, Shirley Cole, Ian J. Stratford, Gerald E. Adams, E. Martin Fielden, Mark J. Suto, and Michael A. Stier
pp 2603 - 2610; DOI:
10.1021/jm00171a040
PDF
Antimalarial activity of new water-soluble dihydroartemisinin derivatives. 3. Aromatic amine analogs
Ai J. Lin, Liang Quan Li, Daniel L. Klayman, Clifford F. George, and Judith L. Flippen-Anderson
pp 2610 - 2614; DOI:
10.1021/jm00171a041
PDF
Synthesis and antineoplastic properties of ether-linked thioglycolipids
Pedro N. Guivisdalsky, Robert Bittman, Zigrida Smith, Merle L. Blank, Fred Snyder, Sandra Howard, and Hassan Salari
pp 2614 - 2621; DOI:
10.1021/jm00171a042
PDF
Synthesis and in vitro LTD4 antagonist activity of bicyclic and monocyclic cyclopentylurethane and cyclopentylacetamide N-arylsulfonyl amides
Victor G. Matassa, Frederick J. Brown, Peter R. Bernstein, Howard S. Shapiro, Thomas P. Maduskuie Jr., Laura A. Cronk, Edward P. Vacek, Ying K. Yee, David W. Snyder, and et al.
pp 2621 - 2629; DOI:
10.1021/jm00171a043
PDF
Dihydropyrimidine calcium channel blockers. II. 3-Substituted-4-aryl-1,4-dihydro-6-methyl-5-pyrimidinecarboxylic acid esters as potent mimics of dihydropyridines
Karnail S. Atwal, George C. Rovnyak, S. David Kimball, David M. Floyd, Suzanne Moreland, Brian N. Swanson, Jack Z. Gougoutas, Joseph Schwartz, Kaye M. Smillie, and Mary F. Malley
pp 2629 - 2635; DOI:
10.1021/jm00171a044
PDF
1-(Aminoalkyl)-2-phenylindoles as novel pure estrogen antagonists
Erwin Von Angerer, Norbert Knebel, Mario Kager, and Bernhard Ganss
pp 2635 - 2640; DOI:
10.1021/jm00171a045
PDF
Synthesis and evaluation of a series of aryl[e]fused pyrazolo[4,3-c]pyridines with potential anxiolytic activity
Ian T. Forbes, Christopher N. Johnson, Graham E. Jones, Julia Loudon, Jane M. Nicholass, Mervyn Thompson, and Neil Upton
pp 2640 - 2645; DOI:
10.1021/jm00171a046
PDF
Tricyclic heteroaromatic systems. [1]benzopyranopyrrol-4-ones and [1]benzopyrano-1,2,3-triazol-4-ones as benzodiazepine receptor ligands. Synthesis and structure-activity relationships
Vittoria Colotta, Lucia Cecchi, Fabrizio Melani, Guido Filacchioni, Claudia Martini, Gino Giannaccini, and Antonio Lucacchini
pp 2646 - 2651; DOI:
10.1021/jm00171a047
PDF
Heterosubstituted anthracene-9,10-dione analogs. The synthesis and antitumor evaluation of 5,8-bis[(aminoalkyl)amino]naphtho[2,3-b]thiophene-4,9-diones
A. Paul Krapcho, Mary E. Petry, and Miles P. Hacker
pp 2651 - 2655; DOI:
10.1021/jm00171a048
PDF
NMR studies of configuration and tautomeric equilibria in nitroacridine antitumor agents
Maruta Boyd and William A. Denny
pp 2656 - 2659; DOI:
10.1021/jm00171a049
PDF
Antitumor agents. 113. New 4.beta.-arylamino derivatives of 4'-O-demethylepipodophyllotoxin and related compounds as potent inhibitors of human DNA topoisomerase II
Zhe Qing Wang, Yao Haur Kuo, Dora Schnur, J. Phillip Bowen, Su Ying Liu, Fu Sheng Han, Jang Yang Chang, Yung Chi Cheng, and Kuo Hsiung Lee
pp 2660 - 2666; DOI:
10.1021/jm00171a050
PDF
Synthesis and antihypertensive activity of 4-(substituted-carbonylamino)-2H-1-benzopyrans
Valerie A. Ashwood, Frederick Cassidy, Martin C. Coldwell, John M. Evans, Thomas C. Hamilton, David R. Howlett, Duncan M. Smith, and Geoffrey Stemp
pp 2667 - 2672; DOI:
10.1021/jm00171a051
PDF
Crystallographic and molecular modeling studies on 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione and its butyl analog, inhibitors of mammalian aromatase. Comparison with natural substrates: prediction of enantioselectivity for N-alkyl derivatives
Charles A. Laughton, Robert McKenna, Stephen Neidle, Michael Jarman, Ray McCague, and Martin G. Rowlands
pp 2673 - 2679; DOI:
10.1021/jm00171a052
PDF
Affinity of 2-(tetrahydroisoquinolin-2-ylmethyl)- and 2-(isoindolin-2-ylmethyl)imidazolines for .alpha.-adrenoceptors. Differential affinity of imidazolines for the [3H]idazoxan-labeled .alpha.2-adrenoceptor vs. the [3H]yohimbime-labeled site [Erratum to document cited in CA112(7):55713w
Robin D. Clark, Jacob Berger, Pushkal Garg, Klaus K. Weinhardt, Michael Spedding, Andrew T. Kilpatrick, Christine M. Brown, and Alison C. MacKinnon
pp 2679 - 2679; DOI:
10.1021/jm00171a053
PDF
Cholecystokinin-A receptor ligands based on the .kappa.-opioid agonist tifluadom [Erratum to document cited in CA112(5):30228d]
Mark G. Bock, Robert M. DiPardo, Ben E. Evans, Kenneth E. Rittle, Willie L. Whitter, Daniel F. Veber, Roger M. Freidinger, Raymond S. L. Chang, T. B. Chen, and Victor J. Lotti
pp 2679 - 2679; DOI:
10.1021/jm00171a054
PDF
Estrogen synthetase inhibitors. 2. Comparison of the in vitro aromatase inhibitory activity for a variety of nitrogen heterocycles substituted with diarylmethane or diarylmethanol groups [Erratum to document cited in CA112(5):35753f]
C. Jones, Winter David, A Mark, Kenneth S. Hirsch, Nancy Stamm, Harold M. Taylor, Howard E. Holden, James D. Davenport, Eriks V. Krumkalns, and Robert G. Suhr
pp 2679 - 2679; DOI:
10.1021/jm00171a055
PDF
Book Reviews

pp 2680 - 2684; DOI:
10.1021/jm00171a600
PDF

Issue 10


Antiatherosclerotic agents. A structurally novel bivalent inhibitor of AcylCoA:cholesterol O-acyltransferase with systemic activity
Ronald B. Gammill, Frank P. Bell, Larry T. Bell, Sharon N. Bisaha, and Grace J. Wilson
pp 2685 - 2687; DOI:
10.1021/jm00172a001
PDF
Structure-based, C2 symmetric inhibitors of HIV protease
Dale J. Kempf, Daniel W. Norbeck, LynnMarie Codacovi, Xiu Chun Wang, William E. Kohlbrenner, Norman E. Wideburg, Deborah A. Paul, Mark F. Knigge, Sudthida Vasavanonda, and et al.
pp 2687 - 2689; DOI:
10.1021/jm00172a002
PDF
Synthesis and biological activity of 1,2,4-oxadiazole derivatives: highly potent and efficacious agonists for cortical muscarinic receptors
Leslie J. Street, Raymond Baker, Tracey Book, Clare O. Kneen, Angus M. MacLeod, Kevin J. Merchant, Graham A. Showell, John Saunders, Richard H. Herbert, and et al.
pp 2690 - 2697; DOI:
10.1021/jm00172a003
PDF
Substituted 1,3-dihydro-2H-pyrrolo[2,3-b]pyridin-2-ones as potential antiinflammatory agents
Pauline C. Ting, James J. Kaminski, Margaret H. Sherlock, Wing C. Tom, Joe F. Lee, Robert W. Bryant, Arthur S. Watnick, and Andrew T. McPhail
pp 2697 - 2706; DOI:
10.1021/jm00172a004
PDF
Orally potent human renin inhibitors derived from angiotensinogen transition state: design, synthesis, and mode of interaction
Kinji Iizuka, Tetsuhide Kamijo, Hiromu Harada, Kenji Akahane, Tetsuhiro Kubota, Hideaki Umeyama, Toshimasa Ishida, and Yoshiaki Kiso
pp 2707 - 2714; DOI:
10.1021/jm00172a005
PDF
Thiazole as a carbonyl bioisostere. A novel class of highly potent and selective 5-HT3 receptor antagonists
Terry Rosen, Arthur A. Nagel, James P. Rizzi, Jeffrey L. Ives, June B. Daffeh, Alan H. Ganong, Karen Guarino, James Heym, Stafford McLean, and et al.
pp 2715 - 2720; DOI:
10.1021/jm00172a006
PDF
An initial three-component pharmacophore for specific serotonin-3 receptor ligands
James P. Rizzi, Arthur A. Nagel, Terry Rosen, Stafford McLean, and Thomas Seeger
pp 2721 - 2725; DOI:
10.1021/jm00172a007
PDF
Torsionally and hydrophobically modified 2,3-diarylindenes as estrogen-receptor ligands
Gregory M. Anstead, Chad S. Peterson, Kevin G. Pinney, Scott R. Wilson, and John A. Katzenellenbogen
pp 2726 - 2734; DOI:
10.1021/jm00172a008
PDF
Synthesis of acyclic and dehydroaspartic acid analogs of Ac-Asp-Glu-OH and their inhibition of rat brain N-acetylated .alpha.-linked acidic dipeptidase (NAALA dipeptidase)
Nalin Subasinghe, Marvin Schulte, Michael Y. M. Chan, Robert J. Roon, James F. Koerner, and Rodney L. Johnson
pp 2734 - 2744; DOI:
10.1021/jm00172a009
PDF
Penta- and hexadienoic acid derivatives: a novel series of 5-lipoxygenase inhibitors
J. L. Malleron, G. Roussel, G. Gueremy, G. Ponsinet, J. L. Robin, B. Terlain, and J. M. Tissieres
pp 2744 - 2749; DOI:
10.1021/jm00172a010
PDF
Direct C-glycosylation of guanine analogs: the synthesis and antiviral activity of certain 7- and 9-deazaguanine C-nucleosides
Nabih S. Girgis, Maged A. Michael, Donald F. Smee, Hassan A. Alaghamandan, Roland K. Robins, and Howard B. Cottam
pp 2750 - 2755; DOI:
10.1021/jm00172a011
PDF
Antimicrobial properties of N3-(iodoacetyl)-L-2,3-diaminopropanoic acid-peptide conjugates
Ryszard Andruszkiewicz, Henryk Chmara, Slawomir Milewski, Teresa Zieniawa, and Edward Borowski
pp 2755 - 2759; DOI:
10.1021/jm00172a012
PDF
4-Heterocyclyloxy-2H-1-benzopyran potassium channel activators
Rolf Bergmann, Volker Eiermann, and Rolf Gericke
pp 2759 - 2767; DOI:
10.1021/jm00172a013
PDF
Anti-HIV-1 activity, toxicity, and stability studies of representative structural families of polyoxometalates
Craig L. Hill, Mark S. Weeks, and Raymond F. Schinazi
pp 2767 - 2772; DOI:
10.1021/jm00172a014
PDF
2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents
John M. Kane, Bruce M. Baron, Mark W. Dudley, Stephen M. Sorensen, Michael A. Staeger, and Francis P. Miller
pp 2772 - 2777; DOI:
10.1021/jm00172a015
PDF
Binding of indolylalkylamines at 5-HT2 serotonin receptors: examination of a hydrophobic binding region
Richard A. Glennon, Chandra Chaurasia, and Milt Titeler
pp 2777 - 2784; DOI:
10.1021/jm00172a016
PDF
Chemistry and structure-activity relationships of C-17 unsaturated 18-cycloalkyl and cycloalkenyl analogs of enisoprost. Identification of a promising new antiulcer prostaglandin
P. W. Collins, A. F. Gasiecki, W. E. Perkins, G. W. Gullikson, R. G. Bianchi, S. W. Kramer, J. S. Ng, E. E. Yonan, L. Swenton, and et al.
pp 2784 - 2793; DOI:
10.1021/jm00172a017
PDF
Pyrroloisoquinoline antidepressants. 3. A focus on serotonin
Bruce E. Maryanoff, Jeffry L. Vaught, Richard P. Shank, David F. McComsey, Michael J. Costanzo, and Samuel O. Nortey
pp 2793 - 2797; DOI:
10.1021/jm00172a018
PDF
Benzophenone dicarboxylic acid antagonists of leukotriene B4. 1. Structure-activity relationships of the benzophenone nucleus
D. Mark Gapinski, Barbara E. Mallett, Larry L. Froelich, and William T. Jackson
pp 2798 - 2807; DOI:
10.1021/jm00172a019
PDF
Benzophenone dicarboxylic acid antagonists of leukotriene B4. 2. Structure-activity relationships of the lipophilic side chain
D. Mark Gapinski, Barbara E. Mallett, Larry L. Froelich, and William T. Jackson
pp 2807 - 2813; DOI:
10.1021/jm00172a020
PDF
A Free-Wilson/Fujita-Ban analysis and prediction of the analgesic potency of some 3-hydroxy- and 3-methoxy-N-alkylmorphinan-6-one opioids
Zurisaddai Hernandez-Gallegos and Pedro A. Lehmann
pp 2813 - 2817; DOI:
10.1021/jm00172a021
PDF
Imidazodiazepinediones: a new class of adenosine receptor antagonists
John W. Daly, Izumi Hide, and Peter K. Bridson
pp 2818 - 2821; DOI:
10.1021/jm00172a022
PDF
7-Deaza-2-phenyladenines: structure-activity relationships of potent A1 selective adenosine receptor antagonists
Christa E. Mueller, Izumi Hide, John W. Daly, Klaus Rothenhaeusler, and Kurt Eger
pp 2822 - 2828; DOI:
10.1021/jm00172a023
PDF
The development of a novel series of (quinolin-2-ylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 3. Structural variation of the acidic side chain to give antagonists of enhanced potency
Robert A. Galemmo Jr., William H. Johnson Jr., Keith S. Learn, Thomas D. Y. Lee, Fu Chih Huang, Henry F. Campbell, Raymond Youssefyeh, Susan V. O'Rourke, Glenn Schuessler, and et al.
pp 2828 - 2841; DOI:
10.1021/jm00172a024
PDF
Stereospecific synthesis, assignment of absolute configuration, and biological activity of the enantiomers of 3-[[[3-[2-(7-chloroquinolin-2-yl)-(E)-ethenyl]phenyl][[3-(dimethylamino)-3-oxopropyl]thio]methyl]thio]propionic acid, a potent and specific leukotriene D4 receptor antagonist
J. Y. Gauthier, T. Jones, E. Champion, L. Charette, R. Dehaven, A. W. Ford-Hutchinson, K. Hoogsteen, A. Lord, P. Masson, and et al.
pp 2841 - 2845; DOI:
10.1021/jm00172a025
PDF
Synthesis and antimicrobial and cytotoxic activities of pyrrole-containing analogs of trichostatin A
S. Massa, Marino Artico, F. Corelli, A. Mai, R. Di Santo, S. Cortes, M. E. Marongiu, A. Pani, and P. La Colla
pp 2845 - 2849; DOI:
10.1021/jm00172a026
PDF
Synthesis and antitumor activity of 2-.beta.-D-ribofuranosyloxazole-4-carboxamide (oxazofurin)
Palmarisa Franchetti, Gloria Cristalli, Mario Grifantini, Loredana Cappellacci, Sauro Vittori, and Giuseppe Nocentini
pp 2849 - 2852; DOI:
10.1021/jm00172a027
PDF
8-Substituted 5-[(aminoalkyl)amino]-6H-v-triazolo[4,5,1-de]acridin-6-ones as potential antineoplastic agents. Synthesis and biological activity
Wieslaw M. Cholody, Sante Martelli, and Jerzy Konopa
pp 2852 - 2856; DOI:
10.1021/jm00172a028
PDF
Propenyl carboxamide derivatives as antagonists of platelet-activating factor
Robert W. Guthrie, Gerald L. Kaplan, Francis A. Mennona, Jefferson W. Tilley, Richard W. Kierstead, Margaret O'Donnell, Herman Crowley, Bohdan Yaremko, and Ann F. Welton
pp 2856 - 2864; DOI:
10.1021/jm00172a029
PDF
Synthesis and anticonvulsant and sedative-hypnotic activity of 4-(alkylimino)-2,3-dihydro-4H-1-benzopyrans and benzothiopyrans
Anna Arnoldi, Alberto Bonsignori, Piero Melloni, Lucio Merlini, Maria Luisa Quadri, Alessandro C. Rossi, and Mariella Valsecchi
pp 2865 - 2869; DOI:
10.1021/jm00172a030
PDF
Nonsteroidal cardiotonics. 3. New 4,5-dihydro-6-(1H-indol-5-yl)pyridazin-3(2H)-ones and related compounds with positive inotropic activities
Alfred Mertens, Walter Gunar Friebe, Bernd Mueller-Beckmann, Wolfgang Kampe, Lothar Kling, and Wolfgang Von der Saal
pp 2870 - 2875; DOI:
10.1021/jm00172a031
PDF
Synthesis and pharmacological evaluation of a series of new 1,4-disubstituted 3-methyl-piperidine analgesics
Nhora Lalinde, John Moliterni, Denny Wright, H. Kenneth Spencer, Michael H. Ossipov, Theodore C. Spaulding, and Frieda G. Rudo
pp 2876 - 2882; DOI:
10.1021/jm00172a032
PDF
Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity
Randall Lis, Thomas K. Morgan, Anthony J. Marisca, Robert P. Gomez, Joan M. Lind, David D. Davey, Gary B. Phillips, and Mark E. Sullivan
pp 2883 - 2891; DOI:
10.1021/jm00172a033
PDF
(Pyrimidinyloxy)acetic acids and pyrimidineacetic acids as a novel class of aldose reductase inhibitors
John Ellingboe, Thomas Alessi, Jane Millen, Janet Sredy, Andrew King, Candace Prusiewicz, Frieda Guzzo, Donna VanEngen, and Jehan Bagli
pp 2892 - 2899; DOI:
10.1021/jm00172a034
PDF
2-Phenyl-2-(1-hydroxycycloalkyl)ethylamine derivatives: synthesis and antidepressant activity
John P. Yardley, G. E. Morris Husbands, Gary Stack, Jacqueline Butch, James Bicksler, John A. Moyer, Eric A. Muth, Terrance Andree, Horace Fletcher, III, and et al.
pp 2899 - 2905; DOI:
10.1021/jm00172a035
PDF
Synthesis and activity of a potent N-methyl-D-aspartic acid agonist, trans-1-aminocyclobutane-1,3-dicarboxylic acid, and related phosphonic and carboxylic acids
Robin D. Allan, Jane R. Hanrahan, Trevor W. Hambley, Graham A. R. Johnston, Kenneth N. Mewett, and Ann D. Mitrovic
pp 2905 - 2915; DOI:
10.1021/jm00172a036
PDF
New and versatile approaches to the synthesis of CPP-related competitive NMDA antagonists. Preliminary structure activity relationships and pharmacological evaluation
Sheryl J. Hays, Christopher F. Bigge, Perry M. Novak, James T. Drummond, Thomas P. Bobovski, Michael J. Rice, Graham Johnson, Laura J. Brahce, and Linda L. Coughenour
pp 2916 - 2924; DOI:
10.1021/jm00172a037
PDF
Synthesis and pharmacology of the enantiomers of cis-7-hydroxy-3-methyl-2-(dipropylamino)tetralin
Anette M. Johansson, Karin Fredriksson, Uli Hacksell, Cor J. Grol, Kjell Svensson, Arvid Carlsson, and Staffan Sundell
pp 2925 - 2929; DOI:
10.1021/jm00172a038
PDF
Synthesis of antimicrobial agents. 3. Syntheses and antibacterial activities of 7-(4-hydroxypiperazin-1-yl)quinolones
Toshio Uno, Hirosato Kondo, Yoshimasa Inoue, Yoshihiro Kawahata, Mikio Sotomura, Koji Iuchi, and Goro Tsukamoto
pp 2929 - 2932; DOI:
10.1021/jm00172a039
PDF

Issue 11


Mechanism and inhibition of cytochrome P-450 aromatase
Philip A. Cole and Cecil H. Robinson
pp 2933 - 2942; DOI:
10.1021/jm00173a001
PDF
Benzotriazinones as virtual-ring mimics of o-methoxybenzamides: novel and potent 5-HT3 receptor antagonists
Frank D. King, Steven Dabbs, Jose Bermudez, and Gareth J. Sanger
pp 2942 - 2944; DOI:
10.1021/jm00173a002
PDF
3-(2-Carboxyindol-3-yl)propionic acid derivatives: antagonists of the strychnine-insensitive glycine receptor associated with the N-methyl-D-aspartate receptor complex
Francesco G. Salituro, Boyd L. Harrison, Bruce M. Baron, Philip L. Nyce, Kenneth T. Stewart, and Ian A. McDonald
pp 2944 - 2946; DOI:
10.1021/jm00173a003
PDF
Structure-activity relationships in 1,4-benzodioxan related compounds. 3. 3-Phenyl analogs of 2-[[[2-(2,6-dimethoxyphenoxy)ethyl]amino]methyl]-1,4-benzodioxan (WB 4101) as highly selective .alpha.1-adrenoreceptor antagonists
Wilma Quaglia, Maria Pigini, Mario Giannella, and Carlo Melchiorre
pp 2946 - 2948; DOI:
10.1021/jm00173a004
PDF
(1R,3S)-1-(Aminomethyl)-3,4-dihydro-5,6-dihydroxy-3-phenyl-1H-2-benzopyran: a potent and selective D1 agonist
Michael P. DeNinno, Robert Schoenleber, Karen E. Asin, Robert MacKenzie, and John W. Kebabian
pp 2948 - 2950; DOI:
10.1021/jm00173a005
PDF
Development of CCK-tetrapeptide analogs as potent and selective CCK-A receptor agonists
Kazumi Shiosaki, Chun Wel Lin, Hana Kopecka, Richard Craig, Frank L. Wagenaar, Bruce Bianchi, Thomas Miller, David Witte, and Alex M. Nadzan
pp 2950 - 2952; DOI:
10.1021/jm00173a006
PDF
Phosphorus-containing inhibitors of HMG-CoA reductase. I. 4-[(2-Arylethyl)hydroxyphosphinyl]-3-hydroxybutanoic acids: a new class of cell selective inhibitors of cholesterol biosynthesis
Donald S. Karanewsky, Michael C. Badia, Carl P. Ciosek, Jeffrey A. Robl, Michael J. Sofia, Ligaya M. Simpkins, Barbara DeLange, Thomas W. Harrity, Scott A. Biller, and Eric M. Gordon
pp 2952 - 2956; DOI:
10.1021/jm00173a007
PDF
Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses
Heechung Yang, Jack Henkin, Ki H. Kim, and Jonathan Greer
pp 2956 - 2961; DOI:
10.1021/jm00173a008
PDF
(R)-4-Oxo-5-phosphononorvaline: a new competitive glutamate antagonist at the NMDA receptor complex
Jeffrey P. Whitten, Bruce M. Baron, Daniel Muench, Francis Miller, H. Steven White, and Ian A. McDonald
pp 2961 - 2963; DOI:
10.1021/jm00173a009
PDF
Antiarthritic and supressor cell inducing activity of azaspiranes: structure-function relationships of a novel class of immunomodulatory agents
Alison M. Badger, David A. Schwartz, Donald H. Picker, James W. Dorman, Fontaine C. Bradley, Elaine N. Cheeseman, Michael J. DiMartino, Nabil Hanna, and Christopher K. Mirabelli
pp 2963 - 2970; DOI:
10.1021/jm00173a010
PDF
Synthesis, biological evaluation, and quantitative structure-activity relationship analysis of [.beta.-(aroylamino)ethyl]piperazines and -piperidines and [2-[(arylamino)carbonyl]ethyl]piperazines, -piperidines, -pyrazinopyridoindoles, and -pyrazinoisoquinolines. A new class of potent H1 antagonists
Mridula Saxena, Shiv K. Agarwal, G. K. Patnaik, and Anil K. Saxena
pp 2970 - 2976; DOI:
10.1021/jm00173a011
PDF
Chemistry and pharmacology of the non-benzodiazepine anxiolytic enciprazine and related compounds
Juergen Engel, Ilona Fleischhauer, Vladimir Jakovlev, Axel Kleemann, Bernhard Kutscher, Bernd Nickel, Horst Rauer, Ulrich Werner, Istvan Szelenyi, and et al.
pp 2976 - 2981; DOI:
10.1021/jm00173a012
PDF
Synthesis, biological profile, and quantitative structure-activity relationship of a series of novel 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors
S. Y. Sit, R. A. Parker, I. Motoc, W. Han, N. Balasubramanian, J. D. Catt, P. J. Brown, W. E. Harte, M. D. Thompson, and J. J. Wright
pp 2982 - 2999; DOI:
10.1021/jm00173a013
PDF
Structural, conformational, and theoretical binding studies of antitumor antibiotic porfiromycin (N-methylmitomycin C), a covalent binder of DNA, by x-ray, NMR, and molecular mechanics
S. K. Arora, M. B. Cox, and P. Arjunan
pp 3000 - 3008; DOI:
10.1021/jm00173a014
PDF
DNA-directed alkylating agents. 2. Synthesis and biological activity of platinum complexes linked to 9-anilinoacridine
Brian D. Palmer, Ho H. Lee, Paul Johnson, Bruce C. Baguley, Geoffrey Wickham, Laurence P. G. Wakelin, W. David McFadyen, and William A. Denny
pp 3008 - 3014; DOI:
10.1021/jm00173a015
PDF
DNA-directed alkylating agents. 3. Structure-activity relationships for acridine-linked aniline mustards: consequences of varying the length of the linker chain
Kisione K. Valu, Trudi A. Gourdie, Theodore J. Boritzki, G. Lance Gravatt, Bruce C. Baguley, William R. Wilson, Laurence P. G. Wakelin, Paul D. Woodgate, and William A. Denny
pp 3014 - 3019; DOI:
10.1021/jm00173a016
PDF
Synthesis, in vitro binding profile, and CNS penetrability of the highly potent 5-HT3 receptor antagonist [3H]-4-(2-methoxyphenyl)-2-[4(5)-methyl-5(4)-imidazolylmethyl]thiazole
Terry Rosen, Thomas F. Seeger, Stafford McLean, Arthur A. Nagel, Jefferey L. Ives, Karen J. Guarino, Dianne Bryce, Jerome Furman, Robert W. Roth, and et al.
pp 3020 - 3023; DOI:
10.1021/jm00173a017
PDF
Variation in the aromatic ring of cromakalim: antihypertensive activity of pyranopyridines and 6-alkyl-2H-1-benzopyrans
Gordon Burrell, Frederick Cassidy, John M. Evans, Diane Lightowler, and Geoffrey Stemp
pp 3023 - 3027; DOI:
10.1021/jm00173a018
PDF
Relaxant activity of 4-amido-3,4-dihydro-2H-1-benzopyran-3-ols and 4-amido-2H-1-benzopyrans on guinea pig isolated trachealis
Derek R. Buckle, Jonathon R. S. Arch, Ashley E. Fenwick, Catherine S. V. Houge-Frydrych, Ivan L. Pinto, David G. Smith, Stephen G. Taylor, and John M. Tedder
pp 3028 - 3034; DOI:
10.1021/jm00173a019
PDF
Further insights into the oxidation chemistry and biochemistry of the serotonergic neurotoxin 5,6-dihydroxytryptamine
Satendra Singh and Glenn Dryhurst
pp 3035 - 3044; DOI:
10.1021/jm00173a020
PDF
Potential antimitotic agents. Synthesis of some ethyl benzopyrazin-7-ylcarbamates, ethyl pyrido[3,4-b]pyrazin-7-ylcarbamates, and ethyl pyrido[3,4-e]-as-triazin-7-ylcarbamates
Carroll Temple and Gregory A. Rener
pp 3044 - 3050; DOI:
10.1021/jm00173a021
PDF
Inhibition of enzymes of estrogen and androgen biosynthesis by esters of 4-pyridylacetic acid
Raymond McCague, Martin G. Rowlands, S. Elaine Barrie, and John Houghton
pp 3050 - 3055; DOI:
10.1021/jm00173a022
PDF
Inhibitors of the P450 enzymes aromatase and lyase. Crystallographic and molecular modeling studies suggest structural features of pyridylacetic acid derivatives responsible for differences in enzyme inhibitory activity
Charles A. Laughton and Stephen Neidle
pp 3055 - 3060; DOI:
10.1021/jm00173a023
PDF
Quinazoline antifolate thymidylate synthase inhibitors: alkyl, substituted alkyl, and aryl substituents in the C-2 position
Leslie R. Hughes, Ann L. Jackman, John Oldfield, Rodney C. Smith, Kenneth D. Burrows, Peter R. Marsham, Joel A. M. Bishop, Terence R. Jones, Brigid M. O'Connor, and A. Hilary Calvert
pp 3060 - 3067; DOI:
10.1021/jm00173a024
PDF
Quinazoline antifolate thymidylate synthase inhibitors: 2'-Fluoro-N10-propargyl-5,8,-dideazafolic acid and derivatives with modifications in the C-2 position
Ann L. Jackman, Peter R. Marsham, Timothy J. Thornton, Joel A. M. Bishop, Brigid M. O'Connor, Leslie R. Hughes, A. Hilary Calvert, and Terence R. Jones
pp 3067 - 3071; DOI:
10.1021/jm00173a025
PDF
Quinazoline-antifolate thymidylate synthase inhibitors: benzoyl ring modifications in the C2-methyl series
Peter R. Marsham, Ann L. Jackman, John Oldfield, Leslie R. Hughes, Timothy J. Thornton, Graham M. F. Bisset, Brigid M. O'Connor, Joel A. M. Bishop, and A. Hilary Calvert
pp 3072 - 3078; DOI:
10.1021/jm00173a026
PDF
Design of potent and selective linear antagonists of vasopressor (V1-receptor) responses to vasopressin
Maurice Manning, Stoytcho Stoev, Aleksander Kolodziejczyk, Wieslaw A. Klis, Marian Kruszynski, Aleksandra Misicka, Aleksandra Olma, Nga Ching Wo, and Wilbur H. Sawyer
pp 3079 - 3086; DOI:
10.1021/jm00173a027
PDF
Synthesis and structure-activity relationships of new 9-N-alkyl derivatives of 9(S)-erythromycylamine
Herbert A. Kirst, Julie A. Wind, James P. Leeds, Kevin E. Willard, Manuel Debono, Rosanne Bonjouklian, James M. Greene, Kevin A. Sullivan, Jonathan W. Paschal, and et al.
pp 3086 - 3094; DOI:
10.1021/jm00173a028
PDF
Synthesis and antiarrhythmic activity of 5,11-dihydro[1]benzoxepino[3,4-b]pyridines
Toshiaki Kumazawa, Hiroyuki Harakawa, Hiroyuki Obase, Yoshimasa Oiji, Masaaki Nito, Kazuhiro Kubo, Akio Ishii, Shinji Tomioka, and Yoshiyuki Yamada
pp 3095 - 3100; DOI:
10.1021/jm00173a029
PDF
Synthesis and evaluation of N-substituted cis-N-methyl-2-(1-pyrrolidinyl)cyclohexylamines as high affinity .sigma. receptor ligands. Identification of a new class of highly potent and selective .sigma. receptor probes
Brian R. De Costa, Wayne D. Bowen, Andrew Thurkauf, Daniel T. Finn, Sondra Vazirani, Richard B. Rothman, Linda Band, Patricia C. Contreras, Nancy M. Gray, and et al.
pp 3100 - 3110; DOI:
10.1021/jm00173a030
PDF
Potent anticonflict activity and lessening of memory impairment with a series of novel [1]benzothieno[2,3-c]pyridines and 1,2,3,4-tetrahydro[1]benzothieno[2,3-c]pyridines
Hiromu Kawakubo, Katuya Okazaki, Tadasi Nagatani, Katuyuki Takao, Shinichi Hasimoto, and Taisuke Sugihara
pp 3110 - 3116; DOI:
10.1021/jm00173a031
PDF
Synthesis and biological activity of an acyclic analog of 5,6,7,8-tetrahydrofolic acid, N-[4-[[3-(2,4-diamino-1,6-dihydro-6-oxo-5-pyrimidinyl)propyl]amino]benzoyl]-L-glutamic acid [Erratum to document cited in CA112(7):56616d]
James L. Kelley, Ed W. McLean, Naomi K. Cohn, Mark P. Edelstein, David S. Duch, Gary K. Smith, Mary H. Hanlon, and Robert Ferone
pp 3116 - 3116; DOI:
10.1021/jm00173a032
PDF
Book Reviews

pp 3117 - 3118; DOI:
10.1021/jm00173a600
PDF

Issue 12


Evidence for nitroxyl in the catalase-mediated bioactivation of the alcohol deterrent agent cyanamide
H. T. Nagasawa, E. G. DeMaster, B. Redfern, F. N. Shirota, and D. J. W. Goon
pp 3120 - 3122; DOI:
10.1021/jm00174a001
PDF
Synthesis and dopamine receptor affinity of (R)-(-)-2-fluoro-N-n-propylnorapomorphine: a highly potent and selective dopamine D2 agonist
John L. Neumeyer, Yigong Gao, Nora S. Kula, and Ross J. Baldessarini
pp 3122 - 3124; DOI:
10.1021/jm00174a002
PDF
Expedient synthesis and biochemical properties of an [125I]-labeled analogue of glyburide, a radioligand for ATP-inhibited potassium channels
David W. Robertson, Douglas A. Schober, Joseph H. Krushinski, Dale E. Mais, Dennis C. Thompson, and Donald R. Gehlert
pp 3124 - 3126; DOI:
10.1021/jm00174a003
PDF
A novel synthesis of xanthines: support for a new binding mode for xanthines with respect to adenosine at adenosine receptors
Norton P. Peet, Nelsen L. Lentz, Elaine C. Meng, Mark W. Dudley, Ann Marie L. Ogden, David A. Demeter, Herschel J. R. Weintraub, and Philippe Bey
pp 3127 - 3130; DOI:
10.1021/jm00174a004
PDF
4-[(Carboxymethyl)oxy]- and 4-[(carboxymethyl)amino]-5,7-dichloroquinoline-2-carboxylic acid: new antagonists of the strychnine-insensitive glycine binding site on the N-methyl-D-aspartate (NMDA) receptor complex
Boyd L. Harrison, Bruce M. Baron, Diane M. Cousino, and Ian A. McDonald
pp 3130 - 3132; DOI:
10.1021/jm00174a005
PDF
Chiral modifications of dolastatin 10: the potent cytostatic peptide (19aR)-isodolastatin 10
George R. Pettit, Sheo Bux Singh, Fiona Hogan, and Douglas D. Burkett
pp 3132 - 3133; DOI:
10.1021/jm00174a006
PDF
Flexible N-methyl-4-phenyl-1,2,3,6-tetrahydropyridine analog: synthesis and monoamine oxidase catalyzed bioactivation
S. Mbera Ngale Efange, R. H. Michelson, R. P. Remmel, R. J. Boudreau, A. K. Dutta, and A. Freshler
pp 3133 - 3138; DOI:
10.1021/jm00174a007
PDF
Hemoglobin S antigelation agents based on 5-bromotryptophan with potential for sickle cell anemia
Philomen Z. De Croos, Puckprink Sangdee, Brenda L. Stockwell, Leela Kar, Emmanuel B. Thompson, Michael E. Johnson, and Bruce L. Currie
pp 3138 - 3142; DOI:
10.1021/jm00174a008
PDF
11.beta.-Methoxy-, 11.beta.-ethyl, and 17.alpha.-ethynyl-substituted 16.alpha.-fluoroestradiols: receptor-based imaging agents with enhanced uptake efficiency and selectivity
Martin G. Pomper, Henry VanBrocklin, Andrea M. Thieme, Ralph D. Thomas, Dale O. Kiesewetter, Kathryn E. Carlson, Carla J. Mathias, Michael J. Welch, and John A. Katzenellenbogen
pp 3143 - 3155; DOI:
10.1021/jm00174a009
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Synthesis and estrogen receptor binding of novel 11.beta.-substituted estra-1,3,5(10)-triene-3,17.beta.-diols
Robert N. Hanson, Elio Napolitano, Rita Fiaschi, and Kay D. Onan
pp 3155 - 3160; DOI:
10.1021/jm00174a010
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Arabinofuranosylpyrrolo[2,3-d]pyrimidines as potential agents for human cytomegalovirus infections
Steven H. Krawczyk, Martha Bernier-Rodriguez, M. Reza Nassiri, Earl R. Kern, Linda L. Wotring, John C. Drach, and Leroy B. Townsend
pp 3160 - 3169; DOI:
10.1021/jm00174a011
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Synthesis and cytotoxicity studies of 8-amino-6-methyl-2-.beta.-D-ribofuranosyl-1,2,3,5,6,7-hexaazaacenaphthylene (7-Aza-TCN) and the corresponding 2'-deoxy- and arabinonucleoside analogues
Andrew M. Kawasaki, Linda L. Wotring, and Leroy B. Townsend
pp 3170 - 3176; DOI:
10.1021/jm00174a012
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Synthesis and biochemical evaluation of tritium-labeled 1-methyl-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-1H-indazole-3-carboxamide, a useful radioligand for 5HT3 receptors
David W. Robertson, William Bloomquist, Marlene L. Cohen, Leroy R. Reid, Kathryn Schenck, and David T. Wong
pp 3176 - 3181; DOI:
10.1021/jm00174a013
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Resolved pyrrolidine, piperidine, and perhydroazepine analogs of the muscarinic agent N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide
J. R. Michael Lundkvist, Hugo M. Vargas, Patrizia Caldirola, Bjoern Ringdahl, and Uli Hacksell
pp 3182 - 3189; DOI:
10.1021/jm00174a014
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Chemical and biochemical studies of 2-propynylpyrrolidine derivatives. Restricted-rotation analogs of N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide (BM-5)
Eugene J. Trybulski, Richard H. Kramss, Richard M. Mangano, and Andrew Rusinko
pp 3190 - 3198; DOI:
10.1021/jm00174a015
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Boc-Trp-Orn(Z)-Asp-NH2 and derivatives: a new family of CCK antagonists
R. Gonzalez-Muniz, F. Bergeron, I. Marseigne, C. Durieux, and Bernard P. Roques
pp 3199 - 3204; DOI:
10.1021/jm00174a016
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4-Alkyl-1,4-dihydropyridine derivatives as specific PAF-acether antagonists
Carlos E. Sunkel, Miguel Fau de Casa-Juana, Luis Santos, M. Mar Gomez, Mercedes Villarroya, M. Antonia Gonzalez-Morales, Jaime G. Priego, and M. Pilar Ortega
pp 3205 - 3210; DOI:
10.1021/jm00174a017
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Structure-activity relationship of antiestrogens. Studies on 2,3-diaryl-1-benzopyrans
Ashraf Saeed, Arun P. Sharma, Neelam Durani, Raka Jain, Susheel Durani, and Randhir S. Kapil
pp 3210 - 3216; DOI:
10.1021/jm00174a018
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Structure-activity relationship of antiestrogens. Effect of the side chain and its position on activity of 2,3-diaryl-2H-1-benzopyrans
Arun P. Sharma, Ashraf Saeed, Susheel Durani, and Randhir S. Kapil
pp 3216 - 3222; DOI:
10.1021/jm00174a019
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Structure-activity relationship of antiestrogens. Phenolic analogs of 2,3-diaryl-2H-1-benzopyrans
Arun P. Sharma, Ashraf Saeed, Susheel Durani, and Randhir S. Kapil
pp 3222 - 3229; DOI:
10.1021/jm00174a020
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Design of peptidomimetic .delta. opioid receptor antagonists using the message-address concept [Erratum to document cited in CA112(25):235659s]
P. S. Portoghese, M. Sultana, and A. E. Takemori
pp 3229 - 3229; DOI:
10.1021/jm00174a021
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Specific bradycardic agents. 1. Chemistry, pharmacology, and structure-activity relationships of substituted benzazepinones, a new class of compounds exerting antiischemic properties [Erratum to document cited in CA112(21):198106m]
Manfred Reiffen, Wolfgang Eberlein, Peter Mueller, Manfred Psiorz, Klaus Noll, Joachim Heider, Christian Lillie, Walter Kobinger, and Peter Luger
pp 3229 - 3229; DOI:
10.1021/jm00174a022
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Editorial - Expediting Publication of Communications to the Editor
P. S. Portoghese
pp 3119 - 3119; DOI:
10.1021/jm00174a600
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