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Volume 34
Main Index

Issue 1


An editor's commentary on the birth of a journal
Alfred Burger
pp 2 - 6; DOI:
10.1021/jm00105a001
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Synthesis and antiarrhythmic activity of .alpha.-[(diarylmethoxy)methyl]-1-piperidineethanols
Milton L. Hoefle, L. T. Blouin, R. W. Fleming, S. Hastings, J. M. Hinkley, T. E. Mertz, T. J. Steffe, C. S. Stratton, and L. M. Werbel
pp 7 - 12; DOI:
10.1021/jm00105a002
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Synthesis and antiarrhythmic activity of cis-2,6-dimethyl-.alpha.,.alpha.-diaryl-1-piperidinebutanols
M. L. Hoefle, L. T. Blouin, R. W. Fleming, S. Hastings, J. M. Hinkley, T. E. Mertz, T. J. Steffe, and C. S. Stratton
pp 12 - 19; DOI:
10.1021/jm00105a003
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Long-acting dihydropyridine calcium antagonists. 6. Structure-activity relationships around 4-(2,3-dichlorophenyl)-3-(ethoxycarbonyl)-2-[(2-hydroxyethoxy)methyl]-5-(methoxycarbonyl)-6-methyl-1,4-dihydropyridine
David Alker, Simon F. Campbell, and Peter E. Cross
pp 19 - 24; DOI:
10.1021/jm00105a004
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(R)- and (S)-enantiomers of 11-hydroxy- and 10,11-dihydroxy-N-allylnoraporphine: synthesis and affinity for dopamine receptors in rat brain tissue
John L. Neumeyer, Nora S. Kula, Ross J. Baldessarini, and Yigong Gao
pp 24 - 28; DOI:
10.1021/jm00105a005
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Fluoronaphthyridines and -quinolones as antibacterial agents. 3. Synthesis and structure-activity relationships of new 1-(1,1-dimethyl-2-fluoroethyl), 1-[1-methyl-1-(fluoromethyl)-2-fluoroethyl], and 1-[1,1-(difluoromethyl)-2-fluoroethyl] substituted derivatives
P. Remuzon, D. Bouzard, P. Di Cesare, M. Essiz, J. P. Jacquet, J. R. Kiechel, B. Ledoussal, R. E. Kessler, and J. Fung-Tomc
pp 29 - 37; DOI:
10.1021/jm00105a006
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Heterocyclic quinones. XVII. A new in vivo active antineoplastic drug: 6,7-bis(1-aziridinyl)-4-[[3-(N,N-dimethylamino)propyl]amino]-5,8-quinazolinedione
Sylviane Giorgi-Renault, Jean Renault, Patricia Gebel-Servolles, Michel Baron, Claude Paoletti, Suzanne Cros, Marie Christine Bissery, Francois Lavelle, and Ghanem Atassi
pp 38 - 46; DOI:
10.1021/jm00105a007
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Optimization of hydrophobic and hydrophilic substituent interactions of 2,4-diamino-5-(substituted-benzyl)pyrimidines with dihydrofolate reductase
Cynthia Dias Selassie, Ren-li Li, Martin Poe, and Corwin Hansch
pp 46 - 54; DOI:
10.1021/jm00105a008
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Stereoselective reactions. XVII. Absolute structure-cytotoxic activity relationships of steganacin congeners and analogs
Kiyoshi Tomioka, Tsuneo Ishiguro, Hidemichi Mizuguchi, Nobuyasu Komeshima, Kenji Koga, Shigeru Tsukagoshi, Takashi Tsuruo, Tazuko Tashiro, Seiichi Tanida, and Toyokazu Kishi
pp 54 - 57; DOI:
10.1021/jm00105a009
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Synthesis and antiviral activity of 9-alkoxypurines. 2. 9-(2,3-Dihydroxypropoxy)-, 9-(3,4-dihydroxybutoxy)-, and 9-(1,4-dihydroxybut-2-oxy)purines
Stuart Bailey, Michael R. Harnden, Richard L. Jarvest, Ann Parkin, and Malcolm R. Boyd
pp 57 - 65; DOI:
10.1021/jm00105a010
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Synthesis and structure-activity relationships of benzo[b]thienylallylamine antimycotics
Peter Nussbaumer, Gabor Petranyi, and Anton Stuetz
pp 65 - 73; DOI:
10.1021/jm00105a011
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Design of potent protein kinases inhibitors using the bisubstrate approach
A. Ricouart, J. C. Gesquiere, A. Tartar, and C. Sergheraert
pp 73 - 78; DOI:
10.1021/jm00105a012
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(Acyloxy)alkyl carbamate prodrugs of norfloxacin
Jose Alexander, Robert A. Fromtling, Judith A. Bland, Barbara A. Pelak, and Evamarie C. Gilfillan
pp 78 - 81; DOI:
10.1021/jm00105a013
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A new ionizable chromophore of 1,4-bis(alkylamino)benzo[g]phthalazine which interacts with DNA by intercalation
Miquel Pons, L. Campayo, M. A. Martinez-Balbas, F. Azorin, P. Navarro, and E. Giralt
pp 82 - 86; DOI:
10.1021/jm00105a014
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Nicotinamide ethers: novel inhibitors of calcium-independent phosphodiesterase and [3H]rolipram binding
Fredric J. Vinick, Nicholas A. Saccomano, B. Kenneth Koe, Jann A. Nielsen, Ian H. Williams, Peter F. Thadeio, Stanley Jung, Morgan Meltz, Jonathan Johnson Jr., Lorraine A. Lebel, Lorena L. Russo, and David Helweg
pp 86 - 89; DOI:
10.1021/jm00105a015
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4-(Tetrazolylalkyl)piperidine-2-carboxylic acids. Potent and selective N-methyl-D-aspartic acid receptor antagonists with a short duration of action
Paul L. Ornstein, Darryle D. Schoepp, M. Brian Arnold, J. David Leander, David Lodge, Jonathan W. Paschal, and Tom Elzey
pp 90 - 97; DOI:
10.1021/jm00105a016
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Synthesis of water-soluble (aminoalkyl)camptothecin analogs: inhibition of topoisomerase I and antitumor activity
William D. Kingsbury, Jeffrey C. Boehm, Dalia R. Jakas, Kenneth G. Holden, Sidney M. Hecht, Gregory Gallagher, Mary Jo Caranfa, Francis L. McCabe, Leo F. Faucette, Randall K. Johnson, and Robert P. Hertzberg
pp 98 - 107; DOI:
10.1021/jm00105a017
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Novel, potent aldose reductase inhibitors: 3,4-dihydro-4-oxo-3-[[5-(trifluoromethyl)-2-benzothiazolyl]methyl]-1-phthalazineacetic acid (zopolrestat) and congeners
Banavara L. Mylari, Eric R. Larson, Thomas A. Beyer, William J. Zembrowski, Charles E. Aldinger, Michael F. Dee, Todd W. Siegel, and David H. Singleton
pp 108 - 122; DOI:
10.1021/jm00105a018
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Novel class of amino acid antagonists at non-N-methyl-D-aspartic acid excitatory amino acid receptors. Synthesis, in vitro and in vivo pharmacology, and neuroprotection
Povl Krogsgaard-Larsen, John W. Ferkany, Elsebet O. Nielsen, Ulf Madsen, Bjarke Ebert, Joergen S. Johansen, Nils H. Diemer, Torben Bruhn, David T. Beattie, and David R. Curtis
pp 123 - 130; DOI:
10.1021/jm00105a019
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Three-dimensional structure-activity relationships and receptor mapping of N1-substituents of quinolone antibacterials
Masateru Ohta and Hiroshi Koga
pp 131 - 139; DOI:
10.1021/jm00105a020
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Novel 5-HT3 antagonists. Indole oxadiazoles
C. J. Swain, R. Baker, C. Kneen, J. Moseley, J. Saunders, E. M. Seward, G. Stevenson, M. Beer, J. Stanton, and K. Watling
pp 140 - 151; DOI:
10.1021/jm00105a021
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1,2,4-Triazolo[4,3-a]pyrazine derivatives with human renin inhibitory activity. 3. Synthesis and biological properties of aminodeoxystatine and difluorostatone derivatives
Robert H. Bradbury and Janet E. Rivett
pp 151 - 157; DOI:
10.1021/jm00105a022
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Synthesis and antirhinovirus activity of 8-substituted analogs of 6-(dimethylamino)-9-(4-methylbenzyl)-2-(trifluoromethyl)-9H-purine
James L. Kelley, James A. Linn, and J. W. T. Selway
pp 157 - 160; DOI:
10.1021/jm00105a023
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Synthesis and biological evaluation of cyclopropyl analogs of 2-amino-5-phosphonopentanoic acid
Michael S. Dappen, Roberto Pellicciari, Benedetto Natalini, Joseph B. Monahan, Claudio Chiorri, and Alex A. Cordi
pp 161 - 168; DOI:
10.1021/jm00105a024
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Synthesis, antibacterial activities, and pharmacological properties of enantiomers of temafloxacin hydrochloride
Daniel T. W. Chu, Carl W. Nordeen, Dwight J. Hardy, Robert N. Swanson, William J. Giardina, Andre G. Pernet, and Jacob J. Plattner
pp 168 - 174; DOI:
10.1021/jm00105a025
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Synthesis and biological evaluation of dipeptidyl and tripeptidyl polyoxin and nikkomycin analogs as anticandidal prodrugs
Eduardo Krainer, Jeffrey M. Becker, and Fred Naider
pp 174 - 180; DOI:
10.1021/jm00105a026
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2-(3,4-Dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted-ethyl]-acetamides: the use of conformational analysis in the development of a novel series of potent opioid .kappa. agonists
Gerard F. Costello, Roger James, John S. Shaw, Anthony M. Slater, and Neil C. J. Stutchbury
pp 181 - 189; DOI:
10.1021/jm00105a027
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Highly selective .kappa. opioid analgesics. 4. Synthesis of some conformationally restricted naphthalene derivatives with high receptor affinity and selectivity
Paul R. Halfpenny, David C. Horwell, John Hughes, Christine Humblet, John C. Hunter, David C. Rees, and David Neuhaus
pp 190 - 194; DOI:
10.1021/jm00105a028
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Common stereospecificity of opioid and dopamine systems for N-butyrophenone prodine-like compounds
M. A. Iorio, V. Frigeni, E. R. Bowman, L. S. Harris, E. L. May, and Mario D. Aceto
pp 194 - 197; DOI:
10.1021/jm00105a029
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Aldophosphamide acetal diacetate and structural analogs: synthesis and cytotoxicity studies
Yuqiang Wang and David Farquhar
pp 197 - 203; DOI:
10.1021/jm00105a030
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Analogs of methotrexate and aminopterin with .gamma.-methylene and .gamma.-cyano substitution of the glutamate side chain: synthesis and in vitro biological activity. 40
Andre Rosowsky, Henry Bader, and James H. Freisheim
pp 203 - 208; DOI:
10.1021/jm00105a031
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Synthesis of two cyclopentenyl-3-deazapyrimidine carbocyclic nucleosides related to cytidine and uridine
Richard R. Copp and Victor E. Marquez
pp 208 - 212; DOI:
10.1021/jm00105a032
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Potential anti-AIDS agents. Synthesis and antiviral activity of naphthalenesulfonic acid derivatives against HIV-1 and HIV-2
Prem Mohan, Rajendra Singh, and Masanori Baba
pp 212 - 217; DOI:
10.1021/jm00105a033
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Potential antitumor agents. 61. Structure-activity relationships for in vivo colon 38 activity among disubstituted 9-oxo-9H-xanthene-4-acetic acids
Gordon W. Rewcastle, Graham J. Atwell, Li Zhuang, Bruce C. Baguley, and William A. Denny
pp 217 - 222; DOI:
10.1021/jm00105a034
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Folate analogs. 34. Synthesis and antitumor activity of non-polyglutamylatable inhibitors of dihydrofolate reductase
Ann Abraham, J. J. McGuire, John Galivan, Zenia Nimec, R. L. Kisliuk, Y. Gaumont, and M. G. Nair
pp 222 - 227; DOI:
10.1021/jm00105a035
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Synthesis and biological activity of the 2-desamino and 2-desamino-2-methyl analogs of aminopterin and methotrexate
Andre Rosowsky, Ronald A. Forsch, Richard G. Moran, and James H. Freisheim
pp 227 - 234; DOI:
10.1021/jm00105a036
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Nucleosides and nucleotides. 94. Radical deoxygenation of tert-alcohols in 1-(2-C-alkylpentofuranosyl)pyrimidines: synthesis of (2'S)-2'-deoxy-2'-C-methylcytidine, an antileukemic nucleoside
Akira Matsuda, Kenji Takenuki, Takuma Sasaki, and Tohru Ueda
pp 234 - 239; DOI:
10.1021/jm00105a037
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Synthesis and evaluation of DNA-targeted spatially separated bis(aniline mustards) as potential alkylating agents with enhanced DNA cross-linking capability
Trudi A. Gourdie, A. S. Prakash, Laurence P. G. Wakelin, Paul D. Woodgate, and William A. Denny
pp 240 - 248; DOI:
10.1021/jm00105a038
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Dopamine autoreceptor agonists as potential antipsychotics. 2. (Aminoalkoxy)-4H-1-benzopyran-4-ones
Juan C. Jaen, Lawrence D. Wise, Thomas G. Heffner, Thomas A. Pugsley, and Leonard T. Meltzer
pp 248 - 256; DOI:
10.1021/jm00105a039
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A cardioselective, hydrophilic N,N,N-trimethylethanaminium .alpha.-tocopherol analog that reduces myocardial infarct size
J. Martin Grisar, Margaret A. Petty, Frank N. Bolkenius, James Dow, Joseph Wagner, Eugene R. Wagner, Klaus D. Haegele, and Wybren De Jong
pp 257 - 260; DOI:
10.1021/jm00105a040
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Antidopaminergic effects of the stereoisomers of N-[(1-alkyl-2-pyrrolidinyl)methyl]-5-sulfamoylbenzamides and -2,3-dihydro-benzofuran-7-carboxamides
Shu Murakami, Nobuhiro Marubayashi, Takemi Fukuda, Shuzo Takehara, and Tetsuya Tahara
pp 261 - 267; DOI:
10.1021/jm00105a041
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Dual inhibitors of thromboxane A2 synthase and 5-lipoxygenase with scavenging activity of active oxygen species (AOS). Synthesis of a novel series of (3-pyridylmethyl)benzoquinone derivatives
Shigenori Ohkawa, Shinji Terao, Zenichi Terashita, Yumiko Shibouta, and Kohei Nishikawa
pp 267 - 276; DOI:
10.1021/jm00105a042
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2,3-Dihydrobenzofuran analogs of hallucinogenic phenethylamines
David E. Nichols, Scott E. Snyder, Robert Oberlender, Michael P. Johnson, and Xuemei Huang
pp 276 - 281; DOI:
10.1021/jm00105a043
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Synthesis and benzodiazepine binding activity of a series of novel [1,2,4]triazolo[1,5-c]quinazolin-5(6H)-ones
John E. Francis, William D. Cash, Beverly S. Barbaz, Patrick S. Bernard, Richard A. Lovell, Gerard C. Mazzenga, Robert C. Friedmann, James L. Hyun, Albert F. Braunwalder, and et al.
pp 281 - 290; DOI:
10.1021/jm00105a044
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Calcium-independent phosphodiesterase inhibitors as putative antidepressants: [3-(bicycloalkyloxy)-4-methoxyphenyl-2-imidazolidinones
Nicholas A. Saccomano, Frederic J. Vinick, B. Kenneth Koe, Jann A. Nielsen, William M. Whalen, Morgan Meltz, Douglas Phillips, Peter F. Thadieo, Stanley Jung, Douglas C. Chapin, Lorraine A. Lebel, Lorena L. Russo, David L. Helweg, Jonathan L. Johnson, Jr., Jeffery L. Ives, and Ian H. Williams
pp 291 - 298; DOI:
10.1021/jm00105a045
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Antioxidant activity of probucol and its analogs in hypercholesterolemic Watanabe rabbits
Simon J. T. Mao, Mark T. Yates, Ann E. Rechtin, Richard L. Jackson, and William A. Van Sickle
pp 298 - 302; DOI:
10.1021/jm00105a046
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trans-Hexahydroindolo[4,3-ab]phenanthridines ("benzergolines"), the first structural class of potent and selective dopamine D1 receptor agonists lacking a catechol group
Max P. Seiler, Alexander Hagenbach, Hans Juerg Wuethrich, and Rudolf Markstein
pp 303 - 307; DOI:
10.1021/jm00105a047
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N-[(.omega.-Amino-1-hydroxyalkyl)phenyl]methanesulfonamide derivatives with class III antiarrhythmic activity
Jackson B. Hester, J. Kenneth Gibson, Madeline G. Cimini, D. Edward Emmert, Paula K. Locker, Salvatore C. Perricone, Louis L. Skaletzky, Julie K. Sykes, and Bruce E. West
pp 308 - 315; DOI:
10.1021/jm00105a048
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Boron-containing thiouracil derivatives for neutron-capture therapy of melanoma
Werner Tjarks and Detlef Gabel
pp 315 - 319; DOI:
10.1021/jm00105a049
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Substituted dihydrobenzopyran and dihydrobenzofuran thiazolidine-2,4-diones as hypoglycemic agents
David A. Clark, Steven W. Goldstein, Robert A. Volkmann, James F. Eggler, Gerald F. Holland, Bernard Hulin, Ralph W. Stevenson, David K. Kreutter, E. Michael Gibbs, and et al.
pp 319 - 325; DOI:
10.1021/jm00105a050
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Chemical and biological studies on a series of lipid-soluble (trans-(R,R)- and -(S,S)-1,2-diaminocyclohexane)platinum(II) complexes incorporated in liposomes
Abdul R. Khokhar, Salaam Al-Baker, Trellis Brown, and Roman Perez-Soler
pp 325 - 329; DOI:
10.1021/jm00105a051
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Preparation and anti-HIV activities of aurintricarboxylic acid fractions and analogs: direct correlation of antiviral potency with molecular weight
Mark Cushman, Pinglang Wang, Steve H. Chang, Carl Wild, Erik De Clercq, Dominique Schols, Mark E. Goldman, and Julie A. Bowen
pp 329 - 337; DOI:
10.1021/jm00105a052
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Synthesis and anti-HIV activities of low molecular weight aurintricarboxylic acid fragments and related compounds
Mark Cushman, Suseela Kanamathareddy, Erik De Clercq, Dominique Schols, Mark E. Goldman, and Julie A. Bowen
pp 337 - 342; DOI:
10.1021/jm00105a053
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A ring-enlarged oxetanocin A analog as an inhibitor HIV infectivity
Christopher K. H. Tseng, Victor E. Marquez, George W. A. Milne, Ronald J. Wysocki, Hiroaki Mitsuya, Takuma Shirasaki, and John S. Driscoll
pp 343 - 349; DOI:
10.1021/jm00105a054
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A new class of HIV-1 specific 6-substituted acyclouridine derivatives: synthesis and anti-HIV-1 activity of 5- or 6-substituted analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT)
Hiromichi Tanaka, Masanori Baba, Hiroyuki Hayakawa, Takashi Sakamaki, Tadashi Miyasaka, Masaru Ubasawa, Hideaki Takashima, Kouichi Sekiya, Issei Nitta, Shiro Shigeta, Richard T. Walker, Jan Balzarini, and Eric De Clercq
pp 349 - 357; DOI:
10.1021/jm00105a055
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Inhibitors of cholesterol biosynthesis. 3. Tetrahydro-4-hydroxy-6-[2-(1H-pyrrol-1-yl)ethyl]-2H-pyran 2-one inhibitors of HMG-CoA reductase. 2. Effects of introducing substituents at positions three and four of the pyrrole nucleus
Bruce D. Roth, C. J. Blankley, A. W. Chucholowski, E. Ferguson, M. L. Hoefle, D. F. Ortwine, R. S. Newton, C. S. Sekerke, D. R. Sliskovic, and M. W. Wilson
pp 357 - 366; DOI:
10.1021/jm00105a056
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Inhibitors of cholesterol biosynthesis. 4. trans-6-[2-(Substituted-quinolinyl)ethenyl/ethyl]tetrahydro-4-hydroxy-2H-pyran-2-ones, a novel series of HMG-CoA reductase inhibitors
D. R. Sliskovic, J. A. Picard, W. H. Roark, B. D. Roth, E. Ferguson, B. R. Krause, R. S. Newton, C. Sekerke, and M. K. Shaw
pp 367 - 373; DOI:
10.1021/jm00105a057
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Disubstituted tetrahydrofurans and dioxolanes as platelet activating factor (PAF) antagonists
Javier Bartroli, Elena Carceller, Manuel Merlos, Julian Garcia-Rafanell, and Javier Forn
pp 373 - 386; DOI:
10.1021/jm00105a058
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Synthesis and anticonvulsant activity of imidooxy derivatives
Ivan O. Edafiogho, K. R. Scott, Jacqueline A. Moore, Vida A. Farrar, and Jesse M. Nicholson
pp 387 - 392; DOI:
10.1021/jm00105a059
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Synthesis of chiral and achiral pyranenamine derivatives. Potent agents with topical ocular antiallergic activity
Charles Gluchowski, Trudy E. Bischoff, Michael E. Garst, Lester J. Kaplan, Steven W. Dietrich, Angelika S. Aswad, Mary A. Gaffney, K. Roger Aoki, Carlos Garcia, and Larry A. Wheeler
pp 392 - 397; DOI:
10.1021/jm00105a060
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(2S)-1-(Arylacetyl)-2-(aminomethyl)piperidine derivatives: novel, highly selective .kappa. opioid analgesics
Vittorio Vecchietti, Antonio Giordani, Giuseppe Giardina, Roberto Colle, and Geoffrey D. Clarke
pp 397 - 403; DOI:
10.1021/jm00105a061
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Rationally designed "dipeptoid" analogs of CCK. .alpha.-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties
David C. Horwell, John Hughes, John C. Hunter, Martyn C. Pritchard, Reginald S. Richardson, Edward Roberts, and Geoffrey N. Woodruff
pp 404 - 414; DOI:
10.1021/jm00105a062
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Preparation, characterization, and anticancer activity of a series of cis-PtCl2 complexes linked to anthraquinone intercalators
Dan Gibson, Keria Fiorella Gean, Jehoshua Katzhendle, Raphael Ben-Shoshan, Avner Ramu, and Israel Ringel
pp 414 - 420; DOI:
10.1021/jm00105a063
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Unsaturated and carbocyclic nucleoside analogs: synthesis, antitumor and antiviral activity
Shashikant Phadtare, David Kessel, Thomas H. Corbett, Harold E. Renis, Barbara E. Court, and Jiri Zemlicka
pp 421 - 429; DOI:
10.1021/jm00105a064
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Novel heteroarotinoids: synthesis and biological activity
Lyle W. Spruce, Jonathan B. Gale, K. Darrell Berlin, A. K. Verma, Theodore R. Breitman, Xinhua Ji, and Dick Van der Helm
pp 430 - 439; DOI:
10.1021/jm00105a065
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Design, synthesis, and physicochemical properties of a novel, conformationally restricted 2,3-dihydro-1,3,4-thiadiazole-containing angiotensin converting enzyme inhibitor which is preferentially eliminated by the biliary route in rats
Colin Bennion, Roger C. Brown, Anthony R. Cook, Carol N. Manners, David W. Payling, and David H. Robinson
pp 439 - 447; DOI:
10.1021/jm00105a066
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Non-steroidal antiandrogens. Design of novel compounds based on an infrared study of the dominant conformation and hydrogen-bonding properties of a series of anilide antiandrogens
Jeffrey J. Morris, Leslie R. Hughes, Alasdair T. Glen, and Peter J. Taylor
pp 447 - 455; DOI:
10.1021/jm00105a067
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trans-3-n-propyl-L-proline is a highly favorable, conformationally restricted replacement for methionine in the C-terminal tetrapeptide of cholecystokinin. Stereoselective synthesis of 3-allyl- and 3-n-propyl-L-proline derivatives from 4-hydroxy-L-proline
Mark W. Holladay, Chun Wel Lin, Catherine S. May, David S. Garvey, David G. Witte, Thomas R. Miller, Caroline A. W. Wolfram, and Alex M. Nadzan
pp 455 - 457; DOI:
10.1021/jm00105a068
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Dual antagonists of platelet-activating factor and histamine. Identification of structural requirements for dual activity of N-acyl-4-(5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)piperidines
John J. Piwinski, Jesse K. Wong, Michael J. Green, Ashit K. Ganguly, M. Motasim Billah, Robert E. West, and William Kreutner
pp 457 - 461; DOI:
10.1021/jm00105a069
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Folic acid analogs lacking the 2-carbon are substrates for folylpolyglutamate synthetase and inhibit cell growth
Andre Rosowsky, Ronald A. Forsch, and Richard G. Moran
pp 461 - 463; DOI:
10.1021/jm00105a070
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Relationship between tissue selectivity and lipophilicity for inhibitors of HMG-CoA reductase
Bruce D. Roth, Thomas M. A. Bocan, C. John Blankley, Alexander W. Chucholowski, Paul L. Creger, Mark W. Creswell, Erika Ferguson, Roger S. Newton, Patrick O'Brien, and et al.
pp 463 - 466; DOI:
10.1021/jm00105a071
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8-(Dicyclopropylmethyl)-1,3-dipropylxanthine: a potent and selective adenosine A1 antagonist with renal protective and diuretic activities
Junichi Shimada, Fumio Suzuki, Hiromi Nonaka, Akira Karasawa, Hideaki Mizumoto, Tetsuji Ohno, Kazuhiro Kubo, and Akio Ishii
pp 466 - 469; DOI:
10.1021/jm00105a072
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Design of a well-absorbed renin inhibitor
Saul H. Rosenberg, Hollis D. Kleinert, Herman H. Stein, Donald L. Martin, Marcia A. Chekal, Jerome Cohen, David A. Egan, Karen A. Tricarico, and William R. Baker
pp 469 - 471; DOI:
10.1021/jm00105a073
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Book Reviews

pp 471 - 478; DOI:
10.1021/jm00105a600
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Issue 2


The renewed potential for folate antagonists in contemporary cancer chemotherapy
E. M. Berman and Leslie M. Werbel
pp 479 - 485; DOI:
10.1021/jm00106a001
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Antineoplastic activity of didemnin congeners: nordidemnin and modified chain analogs
Patrick Jouin, Joel Poncet, Marie Noelle Dufour, Andre Aumelas, Antoine Pantaloni, Suzy Cros, and Georgette Francois
pp 486 - 491; DOI:
10.1021/jm00106a002
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Potential antitumor agents. 62. Structure-activity relationships for tricyclic compounds related to the colon tumor active drug 9-oxo-9H-xanthene-4-acetic acid
Gordon W. Rewcastle, Graham J. Atwell, Brian D. Palmer, Peter D. W. Boyd, Bruce C. Baguley, and William A. Denny
pp 491 - 496; DOI:
10.1021/jm00106a003
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A 3 dimensional model for 5-HT1A-receptor agonists based on stereoselective methyl-substituted and conformationally restricted analogs of 8-hydroxy-2-(dipropylamino)tetralin
Charlotta Mellin, Jerk Vallgaarda, David L. Nelson, Lena Bjoerk, Hong Yu, Nils Erik Anden, Ingeborg Csoeregh, Lars Erik Arvidsson, and Uli Hacksell
pp 497 - 510; DOI:
10.1021/jm00106a004
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Molecular and crystal structures of MDL27,467A hydrochloride and quinapril hydrochloride, two ester derivatives of potent angiotensin converting enzyme inhibitors
Roland J. Hausin and Penelope W. Codding
pp 511 - 517; DOI:
10.1021/jm00106a005
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Styrylpyrazoles, styrylisoxazoles, and styrylisothiazoles. Novel 5-lipoxygenase and cyclooxygenase inhibitors
Daniel L. Flynn, Thomas R. Belliotti, Amal M. Boctor, David T. Connor, Catherine R. Kostlan, Donald E. Nies, Daniel F. Ortwine, Denis J. Schrier, and Jagadish C. Sircar
pp 518 - 525; DOI:
10.1021/jm00106a006
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Analysis of the in vitro antitumor activity of novel purine-6-sulfenamide, -sulfinamide, and -sulfonamide nucleosides and certain related compounds using a computer-aided receptor modeling procedure
Vellarkad N. Viswanadhan, Arup K. Ghose, Naeem B. Hanna, Steven S. Matsumoto, Thomas L. Avery, Ganapathi R. Revankar, and Roland K. Robins
pp 526 - 532; DOI:
10.1021/jm00106a007
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Antiulcer agents. 5. Inhibition of gastric H+/K+-ATPase by substituted imidazo[1,2-a]pyridines and related analogs and its implication in modeling the high affinity potassium ion binding site of the gastric proton pump enzyme
James J. Kaminski, Bjorn Wallmark, Carin Briving, and Britt Marie Andersson
pp 533 - 541; DOI:
10.1021/jm00106a008
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Synthesis, peroxidating ability, and antineoplastic evaluation of 1-[(aminoalkyl)amino]-4-hydroxy-10-imino-9-anthracenones
Maria Dzieduszycka, Sante Martelli, Jolanta Tarasiuk, Jolanta Paradziej-Lukowicz, and Edward Borowski
pp 541 - 546; DOI:
10.1021/jm00106a009
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Synthesis and biological activity of bay-region metabolites of a cyclopenta-fused polycyclic aromatic hydrocarbon: benz[j]aceanthrylene
R. Sangaiah, Avram Gold, K. O. Newcomb, and L. M. Ball
pp 546 - 549; DOI:
10.1021/jm00106a010
PDF
2,4-Diamino-5-benzylpyrimidines as antibacterial agents. 14. 2,3-Dihydro-1-(2,4-diamino-5-pyrimidyl)-1H-indenes as conformationally restricted analogs of trimethoprim
Joseph H. Chan and Barbara Roth
pp 550 - 555; DOI:
10.1021/jm00106a011
PDF
Novel pyrrolo[2,3-d]pyrimidine antifolates: synthesis and antitumor activities
Tetsuo Miwa, Takenori Hitaka, Hiroshi Akimoto, and Hiroaki Nomura
pp 555 - 560; DOI:
10.1021/jm00106a012
PDF
Doxorubicin analogs incorporating chemically reactive substituents
David Farquhar, Robert A. Newman, Joan E. Zuckerman, and Borje S. Andersson
pp 561 - 564; DOI:
10.1021/jm00106a013
PDF
Phosphorus-31 NMR and chloride ion kinetics of alkylating monoester phosphoramidates
Kristin M. Fries and Richard F. Borch
pp 565 - 569; DOI:
10.1021/jm00106a014
PDF
Antimalarial polyamine analogs
Michael L. Edwards, D. M. Stemerick, A. J. Bitonti, J. A. Dumont, P. P. McCann, P. Bey, and A. Sjoerdsma
pp 569 - 574; DOI:
10.1021/jm00106a015
PDF
Synthesis and biological activity of methotrexate analogs with two acid groups and a hydrophobic aromatic ring in the side chain
Andre Rosowsky, Henry Bader, and James H. Freisheim
pp 574 - 579; DOI:
10.1021/jm00106a016
PDF
Quantitative structure-activity relationship analysis of cation-substituted polyaromatic compounds as potentiators (amplifiers) of bleomycin-mediated degradation of DNA
Lucjan Strekowski, W. David Wilson, Jerzy L. Mokrosz, Maria J. Mokrosz, Donald B. Harden, Farial A. Tanious, Roman L. Wydra, and Sidney A. Crow
pp 580 - 588; DOI:
10.1021/jm00106a017
PDF
Chemically stable, lipophilic prodrugs of phosphoramide mustard as potential anticancer agents
Chul Hoon Kwon, Ki Young Moon, Nesrine Baturay, and Frances N. Shirota
pp 588 - 592; DOI:
10.1021/jm00106a018
PDF
A new class of calcium antagonists. Synthesis and biological activity of 11-[(.omega.-aminoalkanoyl)amino]-6,6a,7,8,9,10,10a,11-octahydrodibenzo[b,e]thiepin derivatives
Mikio Kurokawa, Fuminori Sato, Naonobu Hatano, Yayoi Honda, and Hitoshi Uno
pp 593 - 599; DOI:
10.1021/jm00106a019
PDF
N-(4-Isoxazolylthiazol-2-yl)oxamic acid derivatives as potent orally active antianaphylactic agents
Dario Chiarino, Giancarlo Grancini, Viviana Frigeni, Ivano Biasini, and Angelo Carenzi
pp 600 - 605; DOI:
10.1021/jm00106a020
PDF
Synthesis and biological evaluation of 5-deazaisofolic acid, 5-deaza-5,6,7,8-tetrahydroisofolic acid, and their N9-substituted analogues
Shyam K. Singh, Inderjit K. Dev, David S. Duch, Robert Ferone, Gary K. Smith, James H. Freisheim, and John B. Hynes
pp 606 - 610; DOI:
10.1021/jm00106a021
PDF
Synthesis and biological activity of 5,11-methylenetetrahydro-5-deazahomofolic acid
Aleem Gangjee, Isaac O. Donkor, Roy L. Kisliuk, Yvette Gaumont, and Janet Thorndike
pp 611 - 616; DOI:
10.1021/jm00106a022
PDF
Novel benzamides as selective and potent gastrokinetic agents. 2. Synthesis and structure-activity relationships of 4-amino-5-chloro-2-ethoxy-N-[[4-(4-fluorobenzyl)-2-morpholinyl]methyl]benzamide citrate (AS-4370) and related compounds
Shiro Kato, Toshiya Morie, Tatsuya Kon, Naoyuki Yoshida, Tadahiko Karasawa, and Junichi Matsumoto
pp 616 - 624; DOI:
10.1021/jm00106a023
PDF
Structure-activity relationship of quinazolinedione inhibitors of calcium-independent phosphodiesterase
John A. Lowe, III, Robert L. Archer, Douglas S. Chapin, John B. Cheng, David Helweg, Jonathan L. Johnson, B. Kenneth Koe, Lorraine A. Lebel, Peter F. Moore, and et al.
pp 624 - 628; DOI:
10.1021/jm00106a024
PDF
Synthesis and anticonvulsant activity of 1-acyl-2-pyrrolidinone derivatives
Hitoshi Sasaki, Yoshiyuki Mori, Junzo Nakamura, and Juichiro Shibasaki
pp 628 - 633; DOI:
10.1021/jm00106a025
PDF
Renin inhibitory peptides. Incorporation of polar, hydrophilic end groups into an active renin inhibitory peptide template and their evaluation in a human renin-infused rat model and in conscious sodium-depleted monkeys
Suvit Thaisrivongs, Donald T. Pals, Donald W. DuCharme, Steve R. Turner, Garry L. DeGraaf, Judy A. Lawson, Sally J. Couch, and Mark V. Williams
pp 633 - 642; DOI:
10.1021/jm00106a026
PDF
Design of potent oxytocin antagonists featuring D-tryptophan at position 2
George Flouret, William Brieher, Kevin Mahan, and Laird Wilson
pp 642 - 646; DOI:
10.1021/jm00106a027
PDF
4'-5'-Unsaturated 5'-halogenated nucleosides. Mechanism-based and competitive inhibitors of S-adenosyl-L-homocysteine hydrolase
Esa T. Jarvi, James R. McCarthy, Shujaath Mehdi, Donald P. Matthews, Michael L. Edwards, Nellikunja J. Prakash, Terry L. Bowlin, Prasad S. Sunkara, and Philippe Bey
pp 647 - 656; DOI:
10.1021/jm00106a028
PDF
Quinolone antibacterials: preparation and activity of bridged bicyclic analogues of the C7-piperazine
John S. Kiely, Marland P. Hutt, Townley P. Culbertson, Ruth A. Bucsh, Donald F. Worth, Lawrence E. Lesheski, Rocco D. Gogliotti, Josephine C. Sesnie, Marjorie Solomon, and Thomas F. Mich
pp 656 - 663; DOI:
10.1021/jm00106a029
PDF
Configuration and preferential solid-state conformations of perindoprilat (S-9780). Comparison with the crystal structures of other ACE inhibitors and conclusions related to structure-activity relationships
Claudine Pascard, Jean Guilhem, Michel Vincent, Georges Remond, Bernard Portevin, and Michel Laubie
pp 663 - 669; DOI:
10.1021/jm00106a030
PDF
Dual-action cephalosporins: cephalosporin 3'-quaternary ammonium quinolones
Harry A. Albrecht, George Beskid, James G. Christenson, Joanne W. Durkin, Virve Fallat, Nafsika H. Georgopapadakou, Dennis D. Keith, Frederick M. Konzelmann, Ellen R. Lipschitz, and et al.
pp 669 - 675; DOI:
10.1021/jm00106a031
PDF
Synthesis of halogen-substituted 1,5-benzothiazepine derivatives and their vasodilating and hypotensive activities
Hirozumi Inoue, Mikihiko Konda, Tomiki Hashiyama, Hisao Otsuka, Kaoru Takahashi, Mitsunori Gaino, Tadamasa Date, Keiichi Aoe, Mikio Takeda, and et al.
pp 675 - 687; DOI:
10.1021/jm00106a032
PDF
Muscarinic cholinergic agonists and antagonists of the 3-(3-alkyl-1,2,4-oxadiazol-5-yl)-1,2,5,6-tetrahydropyridine type. Synthesis and structure-activity relationships
Per Sauerberg, Jens W. Kindtler, Lone Nielsen, Malcolm J. Sheardown, and Tage Honore
pp 687 - 692; DOI:
10.1021/jm00106a033
PDF
Synthesis and anticancer activity of various 3'-deoxy pyrimidine nucleoside analogs, and crystal structure of 1-(3-deoxy-.beta.-D-threo-pentofuranosyl)cytosine
Tai Shun Lin, Jing Hua Yang, Mao Chin Liu, Zhi Yi Shen, Yung Chi Cheng, William H. Prusoff, George I. Birnbaum, Jerzy Giziewicz, Ismail Ghazzouli, and et al.
pp 693 - 701; DOI:
10.1021/jm00106a034
PDF
Synthesis of 3-carbamoylecgonine methyl ester analogs as inhibitors of cocaine binding and dopamine uptake
Richard H. Kline, Jeremy Wright, Amy J. Eshleman, Kristine M. Fox, and Mohyee E. Eldefrawi
pp 702 - 705; DOI:
10.1021/jm00106a035
PDF
Structure-affinity relationships of 12-sulfonyl derivatives of 5,8,8a,9,10,11,12,12a,13,13a-decahydro-6H-isoquino[2,1-g][1,6]naphthyridines at .alpha.-adrenoceptors
Robin D. Clark, David B. Repke, Jacob Berger, Janis T. Nelson, Andrew T. Kilpatrick, Christine M. Brown, Alison C. MacKinnon, Ruth U. Clague, and Michael Spedding
pp 705 - 717; DOI:
10.1021/jm00106a036
PDF
Conformationally defined neurotransmitter analogs. Selective inhibition of glutamate uptake by one pyrrolidine-2,4-dicarboxylate diastereomer
Richard J. Bridges, Mark S. Stanley, Michael W. Anderson, Carl W. Cotman, and A. Richard Chamberlin
pp 717 - 725; DOI:
10.1021/jm00106a037
PDF
Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease
L. J. Browne, C. Gude, H. Rodriguez, R. E. Steele, and A. Bhatnager
pp 725 - 736; DOI:
10.1021/jm00106a038
PDF
4'-Hydroxy-3-methoxyflavones with potent antipicornavirus activity
Nadine De Meyer, Achiel Haemers, Lallan Mishra, Hrishi Kesh Pandey, L. A. C. Pieters, Dirk A. Vanden Berghe, and Arnold J. Vlietinck
pp 736 - 746; DOI:
10.1021/jm00106a039
PDF
Synthesis and anti-HIV-1 activity of 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one (TIBO) derivatives
Michael J. Kukla, Henry J. Breslin, Rudi Pauwels, Cynthia L. Fedde, Milton Miranda, Malcolm K. Scott, Ronald G. Sherrill, Alfons Raeymaekers, Jozef Van Gelder, and et al.
pp 746 - 751; DOI:
10.1021/jm00106a040
PDF
Allosteric modifiers of hemoglobin. 1. Design, synthesis, testing, and structure-allosteric activity relationship of novel hemoglobin oxygen affinity decreasing agents
Ramnarayan S. Randad, Mona A. Mahran, Ahmed S. Mehanna, and Donald J. Abraham
pp 752 - 757; DOI:
10.1021/jm00106a041
PDF
Allosteric modifiers of hemoglobin. 2. Crystallographically determined binding sites and hydrophobic binding/interaction analysis of novel hemoglobin oxygen effectors
Fred C. Wireko, Glen E. Kellogg, and Donald J. Abraham
pp 758 - 767; DOI:
10.1021/jm00106a042
PDF
Synthesis of high specific activity (+)- and (-)-6-[18F]fluoronorepinephrine via the nucleophilic aromatic substitution reaction
Yu Shin Ding, Joanna S. Fowler, S. John Gatley, Stephen L. Dewey, and Alfred P. Wolf
pp 767 - 771; DOI:
10.1021/jm00106a043
PDF
Romazarit. A potential disease-modifying antirheumatic drug
Christopher R. Self, William E. Barber, Peter J. Machin, John M. Osbond, Carey E. Smithen, Brian P. Tong, James C. Wickens, David P. Bloxham, David Bradshaw, and et al.
pp 772 - 777; DOI:
10.1021/jm00106a044
PDF
Nucleosides and nucleotides. 96. Synthesis and antitumor activity of 5-ethynyl-1-.beta.-D-ribofuranosylimidazole-4-carboxamide (EICAR) and its derivatives
Noriaki Minakawa, Takayuki Takeda, Takuma Sasaki, Akira Matsuda, and Tohru Ueda
pp 778 - 786; DOI:
10.1021/jm00106a045
PDF
Structure-activity relationship of mutagenic aromatic and heteroaromatic nitro compounds. Correlation with molecular orbital energies and hydrophobicity
Asim Kumar Debnath, Rosa L. Lopez de Compadre, Gargi Debnath, Alan J. Shusterman, and Corwin Hansch
pp 786 - 797; DOI:
10.1021/jm00106a046
PDF
Synthesis and protein-tyrosine kinase inhibitory activities of flavonoid analogs
Mark Cushman, Dhanapalan Nagarathnam, Debra L. Burg, and Robert L. Geahlen
pp 798 - 806; DOI:
10.1021/jm00106a047
PDF
Dihydropyrimidine calcium channel blockers. 3. 3-Carbamoyl-4-aryl-1,2,3,4-tetrahydro-6-methyl-5-pyrimidinecarboxylic acid esters as orally effective antihypertensive agents
Karnail S. Atwal, Brian N. Swanson, Steven E. Unger, David M. Floyd, Suzanne Moreland, Anders Hedberg, and Brian C. O'Reilly
pp 806 - 811; DOI:
10.1021/jm00106a048
PDF
Nucleosides and nucleotides. 97. Synthesis of new broad spectrum antineoplastic nucleosides, 2'-deoxy-2'-methylidenecytidine (DMDC) and its derivatives
Akira Matsuda, Kenji Takenuki, Motohiro Tanaka, Takuma Sasaki, and Tohru Ueda
pp 812 - 819; DOI:
10.1021/jm00106a049
PDF
Structure-stability relationships of gadolinium(III) ion complexes for magnetic resonance imaging
Rune Fossheim, Harald Dugstad, and Svein G. Dahl
pp 819 - 826; DOI:
10.1021/jm00106a050
PDF
New 1-(heterocyclylalkyl)-4-(propionanilido)-4-piperidinyl methyl ester and methylene methyl ether analgesics
Jerome R. Bagley, Sheela A. Thomas, Frieda G. Rudo, H. Kenneth Spencer, Brian M. Doorley, Michael H. Ossipov, Thomas P. Jerussi, Mark J. Benvenga, and Theodore Spaulding
pp 827 - 841; DOI:
10.1021/jm00106a051
PDF
Synthesis and biological evaluation of a series of 1,1-dichloro-2,2,3-triarylcyclopropanes as pure antiestrogens
Billy W. Day, Robert A. Magarian, Pramod T. Jain, J. Thomas Pento, Gorgin K. Mousissian, and Karen L. Meyer
pp 842 - 851; DOI:
10.1021/jm00106a052
PDF
Synthesis and biological activity of D3-trishomocubyl-4-amines
Douglas W. Oliver, Theodor G. Dekker, Friedrich O. Snyckers, and Theunis G. Fourie
pp 851 - 854; DOI:
10.1021/jm00106a053
PDF
Synthesis, receptor binding, and tissue distribution of 7.alpha.- and 11.beta.-substituted (17.alpha.,20E)- and (17.alpha.,20Z)-21-[125I]iodo-19-norpregna-1,3,5(10),20-tetraene-3,17-diols
H. Ali, J. Rousseau, M. A. Ghaffari, and Johan E. Van Lier
pp 854 - 860; DOI:
10.1021/jm00106a054
PDF
Synthesis of high specific activity 6-[18F]fluorodopamine for positron emission tomography studies of sympathetic nervous tissue
Yu Shin Ding, Joanna S. Fowler, S. John Gatley, Stephen L. Dewey, Alfred P. Wolf, and David J. Schlyer
pp 861 - 863; DOI:
10.1021/jm00106a055
PDF
Hydrophobicity parameters for platinum complexes
Jean Pierre Souchard, Tam T. B. Ha, S. Cros, and Neil P. Johnson
pp 863 - 864; DOI:
10.1021/jm00106a056
PDF
Book Reviews

pp 864 - 868; DOI:
10.1021/jm00106a600
PDF

Issue 3


Reevaluating equilibrium and kinetic binding parameters for lipophilic drugs based on a structural model for drug interactions with biological membranes
R. Preston Mason, David G. Rhodes, and Leo G. Herbette
pp 869 - 877; DOI:
10.1021/jm00107a001
PDF
Synthesis and resolution of (.+-.)-7-chloro-8-hydroxy-1-(3'-iodophenyl)-3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine (TISCH): a high affinity and selective iodinated ligand for CNS D1 dopamine receptor
Sumalee Chumpradit, Mei Pung Kung, Jeffrey J. Billings, and Hank F. Kung
pp 877 - 883; DOI:
10.1021/jm00107a002
PDF
Synthesis and ligand binding of cocaine isomers at the cocaine receptor
F. Ivy Carroll, Anita H. Lewin, Philip Abraham, Karol Parham, John W. Boja, and Michael J. Kuhar
pp 883 - 886; DOI:
10.1021/jm00107a003
PDF
Renin inhibitors containing conformationally restricted P1-P1' dipeptide mimetics
Peter D. Williams, Debra S. Perlow, Linda S. Payne, M. Katherine Holloway, Peter K. S. Siegl, Terry W. Schorn, Robert J. Lynch, John J. Doyle, John F. Strouse, and et al.
pp 887 - 900; DOI:
10.1021/jm00107a004
PDF
Syntheses and in vitro evaluation of water-soluble "cationic metalloporphyrin-ellipticine" molecules having a high affinity for DNA
Li Ding, Guita Etemad-Moghadam, Suzy Cros, Christian Auclair, and Bernard Meunier
pp 900 - 906; DOI:
10.1021/jm00107a005
PDF
Fluorocarbocyclic nucleosides: synthesis and antiviral activity of 2'- and 6'-fluorocarbocyclic 2'-deoxyguanosines
Alan D. Borthwick, Barrie E. Kirk, Keith Biggadike, Anne M. Exall, Suzanne Butt, Stanley M. Roberts, David J. Knight, Jonathan A. V. Coates, and D. Michael Ryan
pp 907 - 914; DOI:
10.1021/jm00107a006
PDF
N-(5-fluorobenzothiazol-2-yl)-2-guanidinothiazole-4-carboxamide. A novel, systemically active antitumor agent effective against 3LL Lewis Lung carcinoma
Rodney C. Schnur, Anton F. J. Fliri, Shama Kajiji, and Vincent A. Pollack
pp 914 - 918; DOI:
10.1021/jm00107a007
PDF
Synthesis and smooth muscle relaxant activity of a new series of potassium channel activators: 3-amido-1,1-dimethylindan-2-ols
Derek R. Buckle, Jonathan R. S. Arch, Colin Edge, Keith A. Foster, Catherine S. V. Houge-Frydrych, Ivan L. Pinto, David G. Smith, John F. Taylor, Stephen G. Taylor, and et al.
pp 919 - 926; DOI:
10.1021/jm00107a008
PDF
A new class of calcium antagonists. 2. Synthesis and biological activity of 11-[4-[4-(4-fluorophenyl)-1-piperazinyl]butyryl]amino]-6,11-dihydrodibenzo[b,e]thiepin maleate and related compounds
Mikio Kurokawa, Fuminori Sato, Iwao Fujiwara, Naonobu Hatano, Yayoi Honda, Takayuki Yoshida, Shunsuke Naruto, Junichi Mastumoto, and Hitoshi Uno
pp 927 - 934; DOI:
10.1021/jm00107a009
PDF
Modeling alcohol metabolism with the DARC/CALPHI system
Christiane Mercier, Veronique Fabart, Yves Sobel, and Jacques Emile Dubois
pp 934 - 942; DOI:
10.1021/jm00107a010
PDF
Specific bradycardic agents. 2. Heteroaromatic modifications in the side chain of specific bradycardic benzazepinones: chemistry, pharmacology, and structure-activity relationships
Andreas Bomhard, Manfred Reiffen, Joachim Heider, Manfred Psiorz, and Christian Lillie
pp 942 - 947; DOI:
10.1021/jm00107a011
PDF
Potential antipsychotic agents. 9. Synthesis and stereoselective dopamine D-2 receptor blockade of a potent class of substituted (R)-N-[(1-benzyl-2-pyrrolidinyl)methyl]benzamides. Relations to other side chain congeners
Thomas Hoegberg, Peter Stroem, Tomas De Paulis, Birgitta Stensland, Ingeborg Csoeregh, Kerstin Lundin, Haakan Hall, and Sven Ove Oegren
pp 948 - 955; DOI:
10.1021/jm00107a012
PDF
Synthesis and siderophore activity of albomycin-like peptides derived from N5-acetyl-N5-hydroxy-L-ornithine
E. Kurt Dolence, Chia En Lin, Marvin J. Miller, and Shelley M. Payne
pp 956 - 968; DOI:
10.1021/jm00107a013
PDF
Synthesis and siderophore and antibacterial activity of N5-acetyl-N5-hydroxyl-L-ornithine derived siderophore-.beta.-lactam conjugates: iron transport mediated drug delivery
E. Kurt Dolence, Albert A. Minnick, Chia En Lin, Marvin J. Miller, and Shelley M. Payne
pp 968 - 978; DOI:
10.1021/jm00107a014
PDF
Quinazoline antifolates inhibiting thymidylate synthase: 4-thio-substituted analogs
Timothy J. Thornton, Terence R. Jones, Ann L. Jackman, Anthony Flinn, Breda M. O'Connor, Peter Warner, and A. Hilary Calvert
pp 978 - 984; DOI:
10.1021/jm00107a015
PDF
Synthesis and antitumor activity of structural analogs of the epipodophyllotoxins
Larry L. Klein, Clinton M. Yeung, Daniel T. Chu, Edith J. McDonald, Jacob J. Clement, and Jacob J. Plattner
pp 984 - 992; DOI:
10.1021/jm00107a016
PDF
Relationships between the structure of taxol analogs and their antimitotic activity
Francoise Gueritte-Voegelein, Daniel Guenard, Francois Lavelle, Marie Therese Le Goff, Lydie Mangatal, and Pierre Potier
pp 992 - 998; DOI:
10.1021/jm00107a017
PDF
Nucleosides and nucleotides. 95. Improved synthesis of 1-(2-azido-2-deoxy-.beta.-D-arabinofuranosyl)cytosine (Cytarazid) and -thymine. Inhibitory spectrum of Cytarazid on the growth of various human tumor cells in vitro
Akira Matsuda, Johji Yasuoka, Takuma Sasaki, and Tohru Ueda
pp 999 - 1002; DOI:
10.1021/jm00107a018
PDF
Synthesis of 2-exo- and 2-endo-mecamylamine analogs. Structure-activity relationships for nicotinic antagonism in the central nervous system
John A. Suchocki, Everette L. May, Thomas J. Martin, Clifford George, and Billy R. Martin
pp 1003 - 1010; DOI:
10.1021/jm00107a019
PDF
A highly specific aldose reductase inhibitor, ethyl 1-benzyl-3-hydroxy-2(5H)-oxopyrrole-4-carboxylate and its congeners
Banavara L. Mylari, Thomas A. Beyer, and Todd W. Siegel
pp 1011 - 1018; DOI:
10.1021/jm00107a020
PDF
A potential radioiodinated ligand for androgen receptor: 7.alpha.-methyl-17.alpha.-[2'-(E)-iodovinyl]-19-nortestosterone
Mohammad Salman and Gary C. Chamness
pp 1019 - 1024; DOI:
10.1021/jm00107a021
PDF
Perfluorinated analogs of poison ivy allergens. Synthesis and skin tolerogenic activity in mice
Rossana Fraginals, Marcel Schaeffer, Jean Luc Stampf, and Claude Benezra
pp 1024 - 1027; DOI:
10.1021/jm00107a022
PDF
Indazolinones, a new series of redox-active 5-lipoxygenase inhibitors with built-in selectivity and oral activity
P. Bruneau, C. Delvare, M. P. Edwards, and R. M. McMillan
pp 1028 - 1036; DOI:
10.1021/jm00107a023
PDF
Water-soluble cholesteryl-containing phosphorothioate monogalactosides: synthesis, properties, and use in lowering blood cholesterol by directing plasma lipoproteins to the liver
Harlof C. P. F. Roelen, Martin K. Bijsterbosch, Hille F. Bakkeren, Theo J. C. Van Berkel, Herman J. M. Kempen, Marinus Buytenhek, Gijs A. Van der Marel, and Jacques H. Van Boom
pp 1036 - 1042; DOI:
10.1021/jm00107a024
PDF
N6-Substituted adenosine receptor agonists: potential antihypertensive agents
B. K. Trivedi, C. J. Blankley, J. A. Bristol, H. W. Hamilton, W. C. Patt, W. J. Kramer, S. A. Johnson, R. F. Bruns, D. M. Cohen, and M. J. Ryan
pp 1043 - 1049; DOI:
10.1021/jm00107a025
PDF
Studies on (H+-K+)-ATPase inhibitors of gastric acid secretion. Prodrugs of 2-[(2-pyridinylmethyl)sulfinyl]benzimidazole proton-pump inhibitors
John C. Sih, Wha bin Im, Andre Robert, David R. Graber, and David P. Blakeman
pp 1049 - 1062; DOI:
10.1021/jm00107a026
PDF
Effect of fluorine substitution on the adrenergic properties of 3-(tert-butylamino)-1-(3,4-dihydroxyphenoxy)-2-propanol
Adeboye Adejare, Jun Ying Nie, David Hebel, L. Ellen Brackett, Oksoon Choi, Fabian Gusovsky, William L. Padgett, John W. Daly, Cyrus R. Creveling, and Kenneth L. Kirk
pp 1063 - 1068; DOI:
10.1021/jm00107a027
PDF
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents
Nicholas J. Hrib, John G. Jurcak, Francis P. Huger, Cheri L. Errico, and Robert W. Dunn
pp 1068 - 1072; DOI:
10.1021/jm00107a028
PDF
Muscarinic receptor binding and activation of second messengers by substituted N-methyl-N-[4-(1-azacycloalkyl)-2-butynyl]acetamides
Barton J. Bradbury, Jesse Baumgold, Robert Paek, Udai Kammula, Jeff Zimmet, and Kenneth A. Jacobson
pp 1073 - 1079; DOI:
10.1021/jm00107a029
PDF
Isomeric monomethyl ether derivatives of (RS)-9,10-dihydroxyaporphine ("isoapomorphine") as possible products of metabolism by catechol-O-methyltransferase
Joseph G. Cannon and Pang Qijie
pp 1079 - 1082; DOI:
10.1021/jm00107a030
PDF
The enantiomeric specificity of the antihypertensive activity of 1-(phenylthio)-2-aminopropane, a synthetic substrate analog for dopamine .beta.-monooxygenase
Heath H. Herman, Philip A. Husain, James E. Colbert, Margaret M. Schweri, Stanley H. Pollock, Lydia C. Fowler, and Sheldon W. May
pp 1082 - 1085; DOI:
10.1021/jm00107a031
PDF
Tetrahydropyridyloxadiazoles: semi-rigid muscarinic ligands
Graham A. Showell, Tracey L. Gibbons, Clare O. Kneen, Angus M. MacLeod, Kevin Merchant, John Saunders, Stephen B. Freedman, Shailendra Patel, and Raymond Baker
pp 1086 - 1094; DOI:
10.1021/jm00107a032
PDF
Identification and exploitation of the .sigma.-opiate pharmacophore
Richard A. Glennon, J. Doyle Smith, Abd M. Ismaiel, Mahmoud El-Ashmawy, George Battaglia, and James B. Fischer
pp 1094 - 1098; DOI:
10.1021/jm00107a033
PDF
Antinociceptive (aminoalkyl)indoles
Malcolm R. Bell, Thomas E. D'Ambra, Virendra Kumar, Michael A. Eissenstat, John L. Herrmann Jr., Joseph R. Wetzel, David Rosi, Richard E. Philion, Sol J. Daum, and et al.
pp 1099 - 1110; DOI:
10.1021/jm00107a034
PDF
Synthesis and structure-activity relationship of new cephalosporins with amino heterocycles at C-7. Dependence of the antibacterial spectrum and .beta.-lactamase stability on the pKa of the C-7 heterocycle
F. Jung, C. Delvare, D. Boucherot, A. Hamon, N. Ackerley, and M. J. Betts
pp 1110 - 1116; DOI:
10.1021/jm00107a035
PDF
A comparative NMR study between the macrolide antibiotic roxithromycin and erythromycin A with different biological properties
Josyane Gharbi-Benarous, Marcel Delaforge, Christophe K. Jankowski, and Jean Pierre Girault
pp 1117 - 1125; DOI:
10.1021/jm00107a036
PDF
Carboxylic acids and tetrazoles as isosteric replacements for sulfate in cholecystokinin analogs
Jefferson W. Tilley, Waleed Danho, Kathleen Lovey, Rolf Wagner, Joseph Swistok, Raymond Makofske, Joseph Michalewsky, Joseph Triscari, David Nelson, and Sally Weatherford
pp 1125 - 1136; DOI:
10.1021/jm00107a037
PDF
Neoglycoproteins as carriers for antiviral drugs: synthesis and analysis of protein-drug conjugates
Grietje Molema, Robert W. Jansen, Jan Visser, Piet Herdewijn, Frits Moolenaar, and Dirk K. F. Meijer
pp 1137 - 1141; DOI:
10.1021/jm00107a038
PDF
Synthesis and biological activity of 5-amino- and 5-hydroxyquinolones, and the overwhelming influence of the remote N1-substituent in determining the structure-activity relationship
John M. Domagala, Alex J. Bridges, Townley P. Culbertson, Laura Gambino, Susan E. Hagen, Gregory Karrick, Kenneth Porter, Joseph P. Sanchez, Josephine A. Sesnie, and et al.
pp 1142 - 1154; DOI:
10.1021/jm00107a039
PDF
Synthesis and biological activity of 5-alkyl-1,7,8-trisubstituted-6-fluoroquinoline-3-carboxylic acids
Susan E. Hagen, John M. Domagala, Carl L. Heifetz, and Judith Johnson
pp 1155 - 1161; DOI:
10.1021/jm00107a040
PDF
.beta.-Substituted .beta.-phenylpropionyl chymotrypsins. Structural and stereochemical features in stable acyl enzymes
Peter E. Reed and John A. Katzenellenbogen
pp 1162 - 1176; DOI:
10.1021/jm00107a041
PDF
Biologically active taxol analogs with deleted A-ring side chain substituents and variable C-2' configurations
Charles S. Swindell, Nancy E. Krauss, Susan B. Horwitz, and Israel Ringel
pp 1176 - 1184; DOI:
10.1021/jm00107a042
PDF
Positional effects of sulfation in hirudin and hirudin PA related anticoagulant peptides
Marguerite H. Payne, John L. Krstenansky, Mark T. Yates, and Simon J. T. Mao
pp 1184 - 1187; DOI:
10.1021/jm00107a043
PDF
Adenosine deaminase inhibitors: synthesis and structure activity relationships of imidazole analogs of erythro-9-(2-hydroxy-3-nonyl)adenine
Gloria Cristalli, Alessandra Eleuteri, Palmarisa Franchetti, Mario Grifantini, Sauro Vittori, and Giulio Lupidi
pp 1187 - 1192; DOI:
10.1021/jm00107a044
PDF
Synthesis and copper-dependent antimycoplasmal activity of amides and amidines derived from 2-amino-1,10-phenanthroline
Marcel A. H. De Zwart, Henricus M. M. Bastiaans, Henk Van der Goot, and Hendrik Timmerman
pp 1193 - 1201; DOI:
10.1021/jm00107a045
PDF
1H-Imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists
Philip J. M. Van Galen, Peter Nissen, Ineke Van Wijngaarden, Adriaan P. Ijzerman, and Willem Soudijn
pp 1202 - 1206; DOI:
10.1021/jm00107a046
PDF
Dual-function radiosensitizers. .alpha.-[[(2-Bromoethyl)amino]methyl]-2-nitro-1H-imidazole-1-ethanol and related compounds: preparation via an aziridine equivalent
Mark J. Suto, Michael A. Stier, and Leslie M. Werbel
pp 1207 - 1209; DOI:
10.1021/jm00107a047
PDF
Triazolobenzo- and triazolothienodiazepines as potent antagonists of platelet activating factor
Armin Walser, Thomas Flynn, Carl Mason, Herman Crowley, Catherine Maresca, Bob Yaremko, and Margaret O'Donnell
pp 1209 - 1221; DOI:
10.1021/jm00107a048
PDF
Effect of hydroxyl group configuration in hydroxyethylamine dipeptide isosteres on HIV protease inhibition. Evidence for multiple binding modes
Daniel H. Rich, Chong Qing Sun, J. V. N. Vara Prasad, Ahammadunny Pathiasseril, Mihaly V. Toth, Garland R. Marshall, Michael Clare, Richard A. Mueller, and Kathryn Houseman
pp 1222 - 1225; DOI:
10.1021/jm00107a049
PDF
L-687,908, a potent hydroxyethylene containing HIV protease inhibitor
Joseph P. Vacca, J. P. Guare, S. J. DeSolms, W. M. Sanders, E. A. Giuliani, S. D. Young, P. L. Darke, I. S. Sigal, W. A. Schleif, and et al.
pp 1225 - 1228; DOI:
10.1021/jm00107a050
PDF
Benzocycloalkyl amines as novel C-termini for HIV protease inhibitors
Terry A. Lyle, Catherine M. Wiscount, James P. Guare, Wayne J. Thompson, Paul S. Anderson, Paul L. Darke, Joan A. Zugay, Emilio A. Emini, William A. Schleif, and et al.
pp 1228 - 1230; DOI:
10.1021/jm00107a051
PDF
Design and conformational analysis of several highly potent bradykinin receptor antagonists
Donald J. Kyle, Jennifer A. Martin, Stephen G. Farmer, and Ronald M. Burch
pp 1230 - 1233; DOI:
10.1021/jm00107a052
PDF
Book Reviews

pp 1233 - 1234; DOI:
10.1021/jm00107a600
PDF

Issue 4


Peptide leukotrienes: current status of research
A. Shaw and R. D. Krell
pp 1235 - 1242; DOI:
10.1021/jm00108a001
PDF
Kynurenic acid derivatives. Structure-activity relationships for excitatory amino acid antagonism and identification of potent and selective antagonists at the glycine site on the N-methyl-D-aspartate receptor
Paul D. Leeson, Raymond Baker, Robert W. Carling, Neil R. Curtis, Kevin W. Moore, Brian J. Williams, Alan C. Foster, Angus E. Donald, John A. Kemp, and George R. Marshall
pp 1243 - 1252; DOI:
10.1021/jm00108a002
PDF
Synthesis and pharmacological evaluation of a major metabolite of ameltolide, a potent anticonvulsant
David W. Robertson, E. E. Beedle, Joseph H. Krushinski, Ronald R. Lawson, C. John Parli, Brian Potts, and J. David Leander
pp 1253 - 1257; DOI:
10.1021/jm00108a003
PDF
New inhibitors of human renin that contain novel replacements at the P2 site
Annette M. Doherty, James S. Kaltenbronn, James P. Hudspeth, Joseph T. Repine, William H. Roark, Ila Sircar, Frank J. Tinney, Cleo J. Connolly, John C. Hodges, and et al.
pp 1258 - 1271; DOI:
10.1021/jm00108a004
PDF
Morphine 6-glucuronide and morphine 3-glucuronide as molecular chameleons with unexpected lipophilicity
Pierre Alain Carrupt, Bernard Testa, Antoine Bechalany, Nabil El Tayar, Patrick Descas, and Daniel Perrissoud
pp 1272 - 1275; DOI:
10.1021/jm00108a005
PDF
Conformationally constrained renin inhibitory peptides: cyclic (3-1)-1-(carboxymethyl)-L-prolyl-L-phenylalanyl-L-histidinamide as a conformational restriction at the P2-P4 tripeptide portion of the angiotensinogen template
Suvit Thaisrivongs, James R. Blinn, Donald T. Pals, and Steve R. Turner
pp 1276 - 1282; DOI:
10.1021/jm00108a006
PDF
Novel indole-2-carboxylates as ligands for the strychnine-insensitive N-methyl-D-aspartate-linked glycine receptor
Nancy M. Gray, Michael S. Dappen, Brian K. Cheng, Alexis A. Cordi, John P. Biesterfeldt, William F. Hood, and Joseph B. Monahan
pp 1283 - 1292; DOI:
10.1021/jm00108a007
PDF
Role of the spacer in conferring .kappa. opioid receptor selectivity to bivalent ligands related to norbinaltorphimine
P. S. Portoghese, A. Garzon-Aburbeh, H. Nagase, C. E. Lin, and A. E. Takemori
pp 1292 - 1296; DOI:
10.1021/jm00108a008
PDF
Synthesis and properties of some peptide analogs of actinomycin D
Anthony B. Mauger, Oswald A. Stuart, and Edward Katz
pp 1297 - 1301; DOI:
10.1021/jm00108a009
PDF
Interaction of GTP derivatives with cellular and oncogenic ras-p21 proteins
Timothy Noonan, Neal Brown, Lech Dudycz, and George Wright
pp 1302 - 1307; DOI:
10.1021/jm00108a010
PDF
Synthesis and biochemical evaluation of baclofen analogs locked in the baclofen solid-state conformation
Andre Mann, Thierry Boulanger, Barbara Brandau, Francois Durant, Guy Evrard, Michel Heaulme, Eric Desaulles, and Camille Georges Wermuth
pp 1307 - 1313; DOI:
10.1021/jm00108a011
PDF
Optical isomers of rocastine and close analogs: synthesis and H1 antihistaminic activity of its enantiomers and their structural relationship to the classical antihistamines
Mark C. Sleevi, Albert D. Cale, Thomas W. Gero, Larry W. Jaques, William J. Welstead, Ashby F. Johnson, Brian F. Kilpatrick, Iulia Demian, Joseph C. Nolan, and Herndon Jenkins
pp 1314 - 1328; DOI:
10.1021/jm00108a012
PDF
Synthesis and aromatase inhibitory activity of novel 1-(4-aminophenyl)-3-azabicyclo[3.1.0]hexane- and -[3.1.1]heptane-2,4-diones
Jaroslav Stanek, Alex Alder, Daniel Bellus, Ajay S. Bhatnagar, Albert Haeusler, and Klaus Schieweck
pp 1329 - 1334; DOI:
10.1021/jm00108a013
PDF
2-Alkoxyadenosines: potent and selective agonists at the coronary artery A2 adenosine receptor
Masayuki Ueeda, Robert D. Thompson, Luis H. Arroyo, and Ray A. Olsson
pp 1334 - 1339; DOI:
10.1021/jm00108a014
PDF
2-Aralkoxyadenosines: potent and selective agonists at the coronary artery A2 adenosine receptor
Masayuki Ueeda, Robert D. Thompson, Luis H. Arroyo, and Ray A. Olsson
pp 1340 - 1344; DOI:
10.1021/jm00108a015
PDF
Inhibition of human placental aromatase by novel homologated 19-oxiranyl and 19-thiiranyl steroids
Wayne E. Childers, James V. Silverton, James T. Kellis, Larry E. Vickery, and Cecil H. Robinson
pp 1344 - 1349; DOI:
10.1021/jm00108a016
PDF
Function of negative charge in the "address domain" of deltorphins
L. H. Lazarus, S. Salvadori, V. Santagada, R. Tomatis, and W. E. Wilson
pp 1350 - 1355; DOI:
10.1021/jm00108a017
PDF
New dibenzothiadiazepine derivatives with antidepressant activities
Danilo Giannotti, Giovanni Viti, Piero Sbraci, Vittorio Pestellini, Giovanna Volterra, Franco Borsini, Alessandro Lecci, Alberto Meli, Paolo Dapporto, and Paola Paoli
pp 1356 - 1362; DOI:
10.1021/jm00108a018
PDF
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 4. Effect of various side-chain substituents on therapeutic activity against anticholinesterase intoxication
Dane A. Goff, Gary A. Koolpe, Andrew B. Kelson, Huynh M. Vu, Dorris L. Taylor, Clifford D. Bedford, Ralph N. Harris, H. A. Mussalam, and Irwin Koplovitz
pp 1363 - 1368; DOI:
10.1021/jm00108a019
PDF
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 5. Structure-activity relationships for side-chain nitro-, sulfone-, amino-, and aminosulfonyl-substituted analogs for therapy against anticholinesterase intoxication
Gary A. Koolpe, Steven M. Lovejoy, Dane A. Goff, Kuei Ying Lin, Doris S. Leung, Clifford D. Bedford, Ralph N. Harris, H. A. Musallam, and Irwin Koplovitz
pp 1368 - 1376; DOI:
10.1021/jm00108a020
PDF
In vitro evaluation of phosphocholine and quaternary ammonium containing lipids as novel anti-HIV agents
Karen L. Meyer, Canino J. Marasco, Susan L. Morris-Natschke, Khalid S. Ishaq, Claude Piantadosi, and Louis S. Kucera
pp 1377 - 1383; DOI:
10.1021/jm00108a021
PDF
Receptor-based design of novel dihydrofolate reductase inhibitors: benzimidazole and indole derivatives
Kwasi A. Ohemeng and Barbara Roth
pp 1383 - 1394; DOI:
10.1021/jm00108a022
PDF
Synthesis and anti-HIV activity of 2-, 3-, and 4-substituted analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT)
Hiromichi Tanaka, Masanori Baba, Masaru Ubasawa, Hideaki Takashima, Kouichi Sekiya, Issei Nitta, Shiro Shigeta, Richard T. Walker, Erik De Clercq, and Tadashi Miyasaka
pp 1394 - 1399; DOI:
10.1021/jm00108a023
PDF
Synthesis of potential dual-acting radiation sensitizer antineoplastic agents: 2,2-dimethylphosphoraziridines containing 2-nitroimidazoles or other electron-affinic moieties
Michael E. Perlman, Joseph A. Dunn, Thomas A. Piscitelli, Julie Earle, William C. Rose, Galen L. Wampler, Joan E. MacDiarmid, and Thomas J. Bardos
pp 1400 - 1407; DOI:
10.1021/jm00108a024
PDF
Synthesis and evaluation of novel ether lipid nucleoside conjugates for anti-HIV-1 activity
Claude Piantadosi, Canio J. Marasco Jr., Susan L. Morris-Natschke, Karen L. Meyer, Fatma Gumus, Jefferson R. Surles, Khalid S. Ishaq, Louis S. Kucera, Nathan Iyer, and et al.
pp 1408 - 1414; DOI:
10.1021/jm00108a025
PDF
Synthesis and antiviral activity of enantiomeric forms of cyclobutyl nucleoside analogs
Gregory S. Bisacchi, Abbe Braitman, Christopher W. Cianci, Junius M. Clark, A. Kirk Field, Moira E. Hagen, Deborah R. Hockstein, Mary F. Malley, Toomas Mitt, and et al.
pp 1415 - 1421; DOI:
10.1021/jm00108a026
PDF
2-Acetylpyridine thiosemicarbazones. 13. Derivatives with antifilarial activity
Daniel L. Klayman, Ai J. Lin, John W. McCall, Shao Yin Wang, Simon Townson, Max Grogl, and Kenneth E. Kinnamon
pp 1422 - 1425; DOI:
10.1021/jm00108a027
PDF
Synthesis and antiretrovirus properties of 5'-isocyano-5'-deoxythymidine,5'-isocyano-2',5'-dideoxyuridine,3'-azido-5'-isocyano-3',5'-dideoxythymidine, and 3'-azido-5'-isocyano-2',3',5'-trideoxyuridine
Johann Hiebl, Erich Zbiral, Jan Balzarini, and Erik De Clercq
pp 1426 - 1430; DOI:
10.1021/jm00108a028
PDF
1,3,8-Trisubstituted xanthines. Effects of substitution pattern upon adenosine receptor A1/A2 affinity
Ronald H. Erickson, Roger N. Hiner, Scott W. Feeney, Paul R. Blake, Waclaw J. Rzeszotarski, Rickey P. Hicks, Diane G. Costello, and Mary E. Abreu
pp 1431 - 1435; DOI:
10.1021/jm00108a029
PDF
Crystal, solution, and molecular modeling structural properties and muscarinic antagonist activity of azaprophen
F. Ivy Carroll, Philip Abraham, S. Wayne Mascarella, P. Singh, Charles G. Moreland, S. S. Sankar, Yong Wha Kwon, and David J. Triggle
pp 1436 - 1440; DOI:
10.1021/jm00108a030
PDF
Thienotriazolodiazepines as platelet-activating factor antagonists. Steric limitations for the substituent in position 2
Armin Walser, Thomas Flynn, Carl Mason, Herman Crowley, Catherine Maresca, and Margaret O'Donnell
pp 1440 - 1446; DOI:
10.1021/jm00108a031
PDF
Synthesis and in vitro biological activity of new deaza analogs of folic acid, aminopterin, and methotrexate with an L-ornithine side chain
Andre Rosowsky, Ronald A. Forsch, Henry Bader, and James H. Freisheim
pp 1447 - 1454; DOI:
10.1021/jm00108a032
PDF
Recognition of cholinergic agonists by the muscarinic receptor. 2. Pilocarpine
Jerome M. Schulman, Rosalie C. Peck, and Raymond L. Disch
pp 1455 - 1459; DOI:
10.1021/jm00108a033
PDF
Synthesis and structure-activity studies of alkyl-substituted .gamma.-butyrolactones and .gamma.-thiobutyrolactones: ligands for the picrotoxin receptor
Daniel J. Canney, Katherine D. Holland, Jeffrey A. Levine, Ann C. McKeon, James A. Ferrendelli, and Douglas F. Covey
pp 1460 - 1467; DOI:
10.1021/jm00108a034
PDF
New derivatives of kanamycin B obtained by modifications and substitutions in position 6''. 1. Synthesis and microbiological evaluation
A. Van Schepdael, J. Delcourt, M. Mulier, R. Busson, L. Verbist, H. J. Vanderhaeghe, M. P. Mingeot-Leclercq, P. M. Tulkens, and P. J. Claes
pp 1468 - 1475; DOI:
10.1021/jm00108a035
PDF
New derivatives of kanamycin B obtained by modifications and substitutions in position 6''. 2. In vitro and computer-aided toxicological evaluation with respect to interactions with phosphatidylinositol
M. P. Mingeot-Leclercq, A. Van Schepdael, R. Brasseur, R. Busson, H. J. Vanderhaeghe, P. J. Claes, and P. M. Tulkens
pp 1476 - 1482; DOI:
10.1021/jm00108a036
PDF
New derivatives of kanamycin B obtained by combined modifications in positions 1 and 6". Synthesis, microbiological properties, and in vitro and computer-aided toxicological evaluation
A. Van Schepdael, R. Busson, H. J. Vanderhaeghe, P. J. Claes, L. Verbist, M. P. Mingeot-Leclercq, R. Brasseur, and P. M. Tulkens
pp 1483 - 1492; DOI:
10.1021/jm00108a037
PDF
Quinazolineacetic acids and related analogs as aldose reductase inhibitors
Michael S. Malamas and Jane Millen
pp 1492 - 1503; DOI:
10.1021/jm00108a038
PDF
Novel caffeic acid derivatives: extremely potent inhibitors of 12-lipoxygenase
Hidetsura Cho, Masaru Ueda, Mie Tamaoka, Mikiko Hamaguchi, Kazuo Aisaka, Yoshinobu Kiso, Teruyoshi Inoue, Ryoko Ogino, Toshio Tatsuoka, and et al.
pp 1503 - 1505; DOI:
10.1021/jm00108a039
PDF
Quinazolinone cholecystokinin-B receptor ligands
Melvin J. Yu, K. Jeff Thrasher, Jefferson R. McCowan, Norma R. Mason, and Laurane G. Mendelsohn
pp 1505 - 1508; DOI:
10.1021/jm00108a040
PDF
Specific anti-HIV-1 acyclonucleosides which cannot be phosphorylated: synthesis of some deoxy analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine
Hiromichi Tanaka, Masanori Baba, Shigeru Saito, Tadashi Miyasaka, Hideaki Takashima, Kouichi Sekiya, Masaru Ubasawa, Issei Nitta, Richard T. Walker, and et al.
pp 1508 - 1511; DOI:
10.1021/jm00108a041
PDF
Novel synthesis and biochemical properties of an [125I]-labeled photoaffinity probe for thromboxane A2/prostaglandin H2 receptors
Dale E. Mais, Nancy L. Bowling, Timothy A. True, Masao Naka, Thomas A. Morinelli, John E. Oatis, Nobuyuki Hamanaka, and Perry V. Halushka
pp 1511 - 1514; DOI:
10.1021/jm00108a042
PDF
1-(Carboxybenzyl)imidazole-5-acrylic acids: potent and selective angiotensin II receptor antagonists
Joseph Weinstock, Richard M. Keenan, James Samanen, Judith Hempel, Joseph A. Finkelstein, Robert G. Franz, Dimitri E. Gaitanopoulos, Gerald R. Girard, John G. Gleason, and et al.
pp 1514 - 1517; DOI:
10.1021/jm00108a043
PDF
Synthesis and pharmacology of the enantiomers of cis-7-hydroxy-3-methyl-2-(dipropylamino)tetralin [Erratum to document cited in CA113(21):190865h]
Anette M. Johansson, Karin Fredriksson, Uli Hacksell, Cor J. Grol, Kjell Svensson, Arvid Carlsson, and Staffan Sundell
pp 1517 - 1517; DOI:
10.1021/jm00108a044
PDF
Book Reviews

pp 1518 - 1520; DOI:
10.1021/jm00108a600
PDF

Issue 5


S-Adenosyl-L-homocysteine hydrolase as a target for antiviral chemotherapy
Michael S. Wolfe and Ronald T. Borchardt
pp 1521 - 1530; DOI:
10.1021/jm00109a001
PDF
Novel site-directed affinity ligands for GABA-gated chloride channels: synthesis, characterization, and molecular modeling of 1-(isothiocyanatophenyl)-4-tert-butyl-2,6,7-trioxabicyclo[2.2.2]octanes
Brian R. De Costa, Anita H. Lewin, Kenner C. Rice, Phil Skolnick, and Joyce A. Schoenheimer
pp 1531 - 1538; DOI:
10.1021/jm00109a002
PDF
Benzyloxazolidine-2,4-diones as potent hypoglycemic agents
Robert L. Dow, Bruce M. Bechle, Thomas T. Chou, David A. Clark, Bernard Hulin, and Ralph W. Stevenson
pp 1538 - 1544; DOI:
10.1021/jm00109a003
PDF
(Benzoylphenyl)piperidines: a new class of immunomodulators
Francois D. Bellamy, Jean B. Chazan, Pierre Dodey, Patrick Dutartre, Khan Ou, Marc Pascal, and Jacques Robin
pp 1545 - 1552; DOI:
10.1021/jm00109a004
PDF
DNA-directed alkylating agents. 4. 4-Anilinoquinoline-based minor groove directed aniline mustards
G. Lance Gravatt, Bruce C. Baguley, William R. Wilson, and William A. Denny
pp 1552 - 1560; DOI:
10.1021/jm00109a005
PDF
5-Lipoxygenase inhibitors: the synthesis and structure-activity relationships of a series of 1-phenyl-3-pyrazolidinones
Dennis J. Hlasta, Francis B. Casey, Edward W. Ferguson, Sally J. Gangell, Martha R. Heimann, Edward P. Jaeger, Rudolph K. Kullnig, and Robert J. Gordon
pp 1560 - 1570; DOI:
10.1021/jm00109a006
PDF
The synthesis and potassium channel blocking activity of some (4-methanesulfonamidophenoxy)propanolamines as potential class III antiarrhythmic agents
Sean P. Connors, Paul D. Dennis, Edward W. Gill, and Derek A. Terrar
pp 1570 - 1577; DOI:
10.1021/jm00109a007
PDF
Phosphonate-containing inhibitors of tyrosine-specific protein kinases
Terrence R. Burke, Zhen Hong Li, Joseph B. Bolen, and Victor E. Marquez
pp 1577 - 1581; DOI:
10.1021/jm00109a008
PDF
Structure-activity studies on a potent antagonist to organophosphate-induced toxicity
Joseph G. Cannon, M. Fethi Sahin, Ranbir K. Bhatnagar, Jan R. Flynn, and John Paul Long
pp 1582 - 1584; DOI:
10.1021/jm00109a009
PDF
Aminoalkynyldithianes. A new class of calcium channel blockers
Theodore C. Adams, Andrea C. Dupont, J. Paul Carter, James F. Kachur, Maria E. Guzewska, W. Janusz Rzeszotarski, Stephen G. Farmer, Lalita Noronha-Blob, and Carl Kaiser
pp 1585 - 1593; DOI:
10.1021/jm00109a010
PDF
Quinazoline antifolate thymidylate synthase inhibitors: heterocyclic benzoyl ring modifications
Peter R. Marsham, Leslie R. Hughes, Ann L. Jackman, Anthony J. Hayter, John Oldfield, J. Michael Wardleworth, Joel A. M. Bishop, Brigid M. O'Connor, and A. Hilary Calvert
pp 1594 - 1605; DOI:
10.1021/jm00109a011
PDF
Escherichia coli mediated biosynthesis and in vitro anti-HIV activity of lipophilic 6-halo-2',3'-dideoxypurine nucleosides
Kunichika Murakami, Takuma Shirasaka, Hidetoshi Yoshioka, Eiji Kojima, Shizuko Aoki, Harry Ford, John S. Driscoll, James A. Kelley, and Hiroaki Mitsuya
pp 1606 - 1612; DOI:
10.1021/jm00109a012
PDF
Synthesis and in vitro evaluation of 2,3-dimethoxy-5-(fluoroalkyl)-substituted benzamides: high-affinity ligands for CNS dopamine D2 receptors
John E. Bishop, Chester A. Mathis, John M. Gerdes, John M. Whitney, Allison M. Eaton, and Richard B. Mailman
pp 1612 - 1624; DOI:
10.1021/jm00109a013
PDF
Synthesis and biological activity of new halo-steroidal antiestrogens
Charles Levesque, Yves Merand, Jean Marc Dufour, Claude Labrie, and Fernand Labrie
pp 1624 - 1630; DOI:
10.1021/jm00109a014
PDF
Synthesis and anthelmintic activity of 3'-benzoylurea derivatives of 6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole
Robert J. Weikert, Stanford Bingham, Mark A. Emanuel, Elizabeth B. Fraser-Smith, David G. Loughhead, Peter H. Nelson, and Anthony L. Poulton
pp 1630 - 1633; DOI:
10.1021/jm00109a015
PDF
Synthesis and antimalarial activity of 2-aziridinyl- and 2,3-bis(aziridinyl)-1,4-naphthoquinonyl sulfonate and acylate derivatives
Tai Shun Lin, Li Ya Zhu, Shi Ping Xu, Alan A. Divo, and Alan C. Sartorelli
pp 1634 - 1639; DOI:
10.1021/jm00109a016
PDF
Fluorinated sugar analogs of potential anti-HIV-1 nucleosides
Jai Tung Huang, Ling Ching Chen, Liben Wang, Moon Hwan Kim, James A. Warshaw, Donald Armstrong, Qing Yu Zhu, Ting Chao Chou, Kyoichi A. Watanabe, and et al.
pp 1640 - 1646; DOI:
10.1021/jm00109a017
PDF
Potential anti-AIDS drugs. Lipophilic, adenosine deaminase-activated prodrugs
Joseph J. Barchi, Victor E. Marquez, John S. Driscoll, Harry Ford, Hiroaki Mitsuya, Takuma Shirasaka, Shizuko Aoki, and James A. Kelley
pp 1647 - 1655; DOI:
10.1021/jm00109a018
PDF
Synthesis and structure-activity relationships of deltorphins analogs
Severo Salvadori, Mauro Marastoni, Gianfranco Balboni, Pier Andrea Borea, Michele Morari, and Roberto Tomatis
pp 1656 - 1661; DOI:
10.1021/jm00109a019
PDF
Synthesis and pharmacological examination of 1-(3-methoxy-4-methylphenyl)-2-aminopropane and 5-methoxy-6-methyl-2-aminoindan: similarities to 3,4-(methylenedioxy)methamphetamine (MDMA)
Michael P. Johnson, Stewart P. Frescas, Robert Oberlender, and David E. Nichols
pp 1662 - 1668; DOI:
10.1021/jm00109a020
PDF
Using theoretical descriptors in quantitative structure-activity relationships: some toxicological indices
Leland Y. Wilson and George R. Famini
pp 1668 - 1674; DOI:
10.1021/jm00109a021
PDF
Compounds from Danshen. Part 4. Structure-activity relationship of miltirone, an active central benzodiazepine receptor ligand isolated from Salvia miltiorrhiza Bunge (Danshen)
Hson Mou Chang, Kuk Ying Chui, Fan Wah Lau Tan, Yun Yang, Zeng Pei Zhong, Chi Ming Lee, Hing Leung Sham, and Henry N. C. Wong
pp 1675 - 1692; DOI:
10.1021/jm00109a022
PDF
Synthesis of the 2-amino-4-phosphonobutanoic acid analogs (E)- and (Z)-2-amino-2,3-methano-4-phosphonobutanoic acid and their evaluation as inhibitors of hippocampal excitatory neurotransmission
Heather B. Kroona, Nancy L. Peterson, James F. Koerner, and Rodney L. Johnson
pp 1692 - 1699; DOI:
10.1021/jm00109a023
PDF
Anesthetic steroid mobility in model membrane preparations examined by high-resolution proton and deuterium NMR spectroscopy
Alexandros Makriyannis, Christine M. DiMeglio, and Stephen W. Fesik
pp 1700 - 1703; DOI:
10.1021/jm00109a024
PDF
Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene D4 receptor antagonists. 4. Addition of chromone moiety enhances leukotriene D4 receptor binding affinity
Fu Chih Huang, Robert A. Galemmo, Gregory B. Poli, Keith S. Learn, Mathew M. Morrissette, William H. Johnson, William P. Dankulich, Henry F. Campbell, Gilbert W. Carnathan, and Richard G. Van Inwegen
pp 1704 - 1707; DOI:
10.1021/jm00109a025
PDF
Conformational properties of semirigid antipsychotic drugs: the pharmacophore for dopamine D2 antagonist activity
Mark Froimowitz and Sten Raemsby
pp 1707 - 1714; DOI:
10.1021/jm00109a026
PDF
Role of spacer and address components in peptidomimetic .delta.-opioid receptor antagonists related to naltrindole
P. S. Portoghese, H. Nagase, K. E. MaloneyHuss, C. E. Lin, and A. E. Takemori
pp 1715 - 1720; DOI:
10.1021/jm00109a027
PDF
Synthesis and hypocholesterolemic activity of 6,7-dihydro-4H-pyrazolo[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-diones, novel inhibitors of acylCoA: cholesterol O-acyltransferase
Scott D. Larsen, Charles H. Spilman, Frank P. Bell, Dac M. Dinh, Esther Martinborough, and Gracella J. Wilson
pp 1721 - 1727; DOI:
10.1021/jm00109a028
PDF
Synthesis and receptor binding of N-substituted tropane derivatives. High-affinity ligands for the cocaine receptor
Richard A. Milius, Jayanta K. Saha, Bertha K. Madras, and John L. Neumeyer
pp 1728 - 1731; DOI:
10.1021/jm00109a029
PDF
Synthesis, hydrolysis rates, supercomputer modeling, and antibacterial activity of bicyclic tetrahydropyridazinones
Louis N. Jungheim, Donald B. Boyd, Joseph M. Indelicato, Carol E. Pasini, David A. Preston, and William E. Alborn
pp 1732 - 1739; DOI:
10.1021/jm00109a030
PDF
Synthesis and quantitative structure-activity relationship analysis of 2-(aryl or heteroaryl)quinolin-4-amines, a new class of anti-HIV-1 agents
Lucjan Strekowski, Jerzy L. Mokrosz, Vidya A. Honkan, Agnieszka Czarny, Marek T. Cegla, Roman L. Wydra, Steven E. Patterson, and Raymond F. Schinazi
pp 1739 - 1746; DOI:
10.1021/jm00109a031
PDF
Synthesis and bioactivity of N.omega.-hydroxyarginine: a possible intermediate in the biosynthesis of nitric oxide from arginine
Guillermo C. Wallace and Jon M. Fukuto
pp 1746 - 1748; DOI:
10.1021/jm00109a032
PDF
Novel time-dependent inhibitors of human placental aromatase
Joseph P. Burkhart, Norton P. Peet, C. Lee Wright, and J. O'Neal Johnston
pp 1748 - 1750; DOI:
10.1021/jm00109a033
PDF
Imidazo[4,5-b]quinoxaline cyanines as neurokinin antagonists
Kenneth C. Appell, Bruce E. Babb, Ramanuj Goswami, Patricia L. Hall, Kristine B. Lawrence, Margaret E. Logan, Rose Przyklek-Elling, Bruce E. Tomczuk, Bhaskar R. Venepalli, and John M. Yanni
pp 1751 - 1753; DOI:
10.1021/jm00109a034
PDF
The agonist pharmacophore of the benzodiazepine receptor. Synthesis of a selective anticonvulsant/anxiolytic
Hernando Diaz-Arauzo, Gary E. Evoniuk, Phil Skolnick, and James M. Cook
pp 1754 - 1756; DOI:
10.1021/jm00109a035
PDF

Issue 6


An approach to the design of receptor-type-selective nonpeptide antagonists of peptidergic receptors: .delta. opioid antagonists
Philip S. Portoghese
pp 1757 - 1762; DOI:
10.1021/jm00110a001
PDF
Dexamethasone 21-(.beta.-isothiocyanatoethyl)thio ether: a new affinity label for glucocorticoid receptors
Susana Lopez and S. Stoney Simons
pp 1762 - 1767; DOI:
10.1021/jm00110a002
PDF
Synthesis and antiviral activity of 5-heteroaryl-substituted 2'-deoxyuridines
P. Wigerinck, R. Snoeck, P. Claes, E. De Clercq, and P. Herdewijn
pp 1767 - 1772; DOI:
10.1021/jm00110a003
PDF
Substituent effect on the stereochemistry of H2-receptor antagonists of the phenylformamidine series. A conformation-dependent mode of interaction with the H2 receptor
Arturo Donetti, Harold M. M. Bastiaans, Klaas Kramer, Giuseppe Bietti, Enzo Ceeda, Enrica Dubini, Maurizio Mondoni, Aalt Bast, and Hendrik Timmerman
pp 1772 - 1776; DOI:
10.1021/jm00110a004
PDF
Synthesis, conformational properties, and antibody recognition of peptides containing .beta.-turn mimetics based on .alpha.-alkylproline derivatives
Mark G. Hinds, John H. Welsh, David M. Brennand, J. Fisher, Martin J. Glennie, Nigel G. J. Richards, David L. Turner, and John A. Robinson
pp 1777 - 1789; DOI:
10.1021/jm00110a005
PDF
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 1. (.+-.)-(3-Pyridinylbicycloheptyl)alkanoic acids
Shripad S. Bhagwat, Candido Gude, David S. Cohen, Warren Lee, Patricia Furness, and Frank H. Clarke
pp 1790 - 1797; DOI:
10.1021/jm00110a006
PDF
Structure/activity and molecular modeling studies of the lophotoxin family of irreversible nicotinic receptor antagonists
Stewart N. Abramson, Jacqueline A. Trischman, Dianne M. Tapiolas, Edward E. Harold, William Fenical, and Palmer Taylor
pp 1798 - 1804; DOI:
10.1021/jm00110a007
PDF
New isomeric classes of topically active ocular hypotensive carbonic anhydrase inhibitors: 5-substituted thieno[2,3-b]thiophene-2-sulfonamides and 5-substituted thieno[3,2-b]thiophene-2-sulfonamides
John D. Prugh, George D. Hartman, Pierre J. Mallorga, Brian M. McKeever, Stuart R. Michelson, Mark A. Murcko, Harvey Schwam, Robert L. Smith, John M. Sondey, and et al.
pp 1805 - 1818; DOI:
10.1021/jm00110a008
PDF
Flavins as potential antimalarials. 2. 3-Methyl-10-(substituted-phenyl)flavins
William B. Cowden, Peter K. Halladay, Ross B. Cunningham, Nicholas H. Hunt, and Ian A. Clark
pp 1818 - 1822; DOI:
10.1021/jm00110a009
PDF
Topographically designed analogs of [cyclic] [D-Pen2,D-Pen5]enkephalin
Victor J. Hruby, Geza Toth, Catherine A. Gehrig, Lung Fa Kao, Richard Knapp, George K. Lui, Henry I. Yamamura, Thomas H. Kramer, P. Davis, and Thomas F. Burks
pp 1823 - 1830; DOI:
10.1021/jm00110a010
PDF
Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study and antiviral activity
Yvette Henin, Catherine Gouyette, Olivier Schwartz, Jean Claude Debouzy, Jean Michel Neumann, and Huynh Dinh Tam
pp 1830 - 1837; DOI:
10.1021/jm00110a011
PDF
Oxidation of dihydropyridine calcium channel blockers and analogs by human liver cytochrome P-450 IIIA4
F. Peter Guengerich, William R. Brian, Masahiko Iwasaki, Marie Agnes Sari, Catharina Baeaernhielm, and Peder Berntsson
pp 1838 - 1844; DOI:
10.1021/jm00110a012
PDF
Synthesis and anticonvulsant activity of 2-iminohydantoins
Chul Hoon Kwon, Muhammad Tahir Iqbal, and John N. D. Wurpel
pp 1845 - 1849; DOI:
10.1021/jm00110a013
PDF
Pyrimido[5,4-b]indole derivatives. 1. A new class of potent and selective .alpha.1 adrenoceptor ligands
Filippo Russo, Giuseppe Romeo, Salvatore Guccione, and Antonio De Blasi
pp 1850 - 1854; DOI:
10.1021/jm00110a014
PDF
Binding of substituted and conformationally restricted derivatives of N-(3-phenyl-n-propyl)-1-phenyl-2-aminopropane at .sigma.-receptors
Richard A. Glennon, Abd M. Ismaiel, J. Doyle Smith, Mamoun Yousif, Mahmoud El-Ashmawy, J. L. Herndon, James B. Fischer, Kathleen J. Burke Howie, and Alfred C. Server
pp 1855 - 1859; DOI:
10.1021/jm00110a015
PDF
1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents
John A. Lowe, III, Thomas F. Seeger, Arthur A. Nagel, Harry R. Howard, Patricia A. Seymour, James H. Heym, Frank E. Ewing, Michael E. Newman, Anne W. Schmidt, and et al.
pp 1860 - 1866; DOI:
10.1021/jm00110a016
PDF
Radiosynthesis of .sigma. receptor ligands for positron emission tomography: carbon-11 and fluorine-18 labeled guanidines
Alan A. Wilson, Robert F. Dannals, Hayden T. Ravert, Mark S. Sonders, Eckard Weber, and Henry N. Wagner
pp 1867 - 1870; DOI:
10.1021/jm00110a017
PDF
Streptonigrin and related compounds. 5. Synthesis and evaluation of some isoquinoline analogs
Koppaka V. Rao and Joseph W. Beach
pp 1871 - 1879; DOI:
10.1021/jm00110a018
PDF
2'-Deoxy-2'-methylenecytidine and 2'-deoxy-2',2'-difluorocytidine 5'-diphosphates: potent mechanism-based inhibitors of ribonucleotide reductase
C. H. Baker, J. Banzon, J. M. Bollinger, J. Stubbe, V. Samano, M. J. Robins, B. Lippert, E. Jarvi, and R. Resvick
pp 1879 - 1884; DOI:
10.1021/jm00110a019
PDF
FTIR spectral study of intramolecular hydrogen bonding in thromboxane A2 receptor antagonist S-145 and related compounds. 3. Conformation and activity of S-145 analogs
Mamoru Takasuka, Masumi Yamakawa, and Mitsuaki Ohtani
pp 1885 - 1891; DOI:
10.1021/jm00110a020
PDF
Naphtho and benzo analogs of the .kappa. opioid agonist trans-(.+-.)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzeneacetamide
Jeremiah P. Freeman, Eric T. Michalson, Stan V. D'Andrea, Lubomir Baczynskyj, Philip F. VonVoigtlander, R. A. Lahti, Martin W. Smith, Charles F. Lawson, Terrence A. Scahill, and et al.
pp 1891 - 1896; DOI:
10.1021/jm00110a021
PDF
Tyrphostins. II. Heterocyclic and .alpha.-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases
Aviv Gazit, Nir Osherov, Israel Posner, Pnina Yaish, Enrique Poradosu, Chaim Gilon, and Alexander Levitzki
pp 1896 - 1907; DOI:
10.1021/jm00110a022
PDF
Linear discriminant and multiple regression analyses of anticoccidial triazines
James W. McFarland, Christopher B. Cooper, and Deborah M. Newcomb
pp 1908 - 1911; DOI:
10.1021/jm00110a023
PDF
Isoprenyl phosphinylformates: new inhibitors of squalene synthetase
Scott A. Biller, Cornelia Forster, Eric M. Gordon, Thomas Harrity, Lois C. Rich, Joseph Marretta, and Carl P. Ciosek
pp 1912 - 1914; DOI:
10.1021/jm00110a024
PDF
Targeting renal dipeptidase (dehydropeptidase I) for inactivation by mechanism-based inactivators
Yong Qian Wu and Shahriar Mobashery
pp 1914 - 1916; DOI:
10.1021/jm00110a025
PDF
Book Reviews

pp 1916 - 1924; DOI:
10.1021/jm00110a600
PDF

Issue 7


Design of enzyme inhibitors using iterative protein crystallographic analysis
Krzysztof Appelt, Russell J. Bacquet, Charlotte A. Bartlett, Carol L. J. Booth, Stephan T. Freer, Mary Ann M. Fuhry, Michael R. Gehring, Steven M. Herrmann, Eleanor F. Howland, and et al.
pp 1925 - 1934; DOI:
10.1021/jm00111a001
PDF
Renin inhibitors containing esters at the P2-position. Oral activity in a derivative of methyl aminomalonate
Joseph T. Repine, Richard J. Himmelsbach, John C. Hodges, James S. Kaltenbronn, Ila Sircar, Richard W. Skeean, Sean T. Brennan, Timothy R. Hurley, Elizabeth Lunney, and et al.
pp 1935 - 1943; DOI:
10.1021/jm00111a002
PDF
Structural studies on tazobactam
Carol A. Toomer, Carl H. Schwalbe, Neil S. Ringan, Peter A. Lambert, Philip R. Lowe, and Ving J. Lee
pp 1944 - 1947; DOI:
10.1021/jm00111a003
PDF
Additional nucleotide derivatives of mitosenes. Synthesis and activity against parental and multidrug resistant L1210 leukemia
Bhashyam S. Iyengar, Robert T. Dorr, and William A. Remers
pp 1947 - 1951; DOI:
10.1021/jm00111a004
PDF
Synthetic approaches to the guanosine and xanthosine analogs 5-amino-3-.beta.-D-ribofuranosylpyrazolo[3,4-e][1,3]oxazin-7-one and 3-.beta.-D-ribofuranosylpyrazolo[3,4-e][1,3]oxazine-5,7-dione and studies of their antitumor potential
Ruiming Zou, Vladimir G. Beylin, Michael P. Groziak, Linda L. Wotring, and Leroy B. Townsend
pp 1951 - 1959; DOI:
10.1021/jm00111a005
PDF
Synthesis and biological evaluation of quinocarcin derivatives: thioalkyl-substituted quinones and hydroquinones
Hiromitsu Saito, Tadashi Hirata, Masaji Kasai, Kazuhisa Fujimoto, Tadashi Ashizawa, Makoto Morimoto, and Akira Sato
pp 1959 - 1966; DOI:
10.1021/jm00111a006
PDF
Persistent binding of fatty acyl derivatives of naltrexamine to opioid receptors
P. S. Portoghese, A. Garzon-Aburbeh, and D. L. Larson
pp 1966 - 1969; DOI:
10.1021/jm00111a007
PDF
Lipopeptides containing 2-(palmitoylamino)-6,7-bis(palmitoyloxy)heptanoic acid: synthesis, stereospecific stimulation of B-lymphocytes and macrophages and adjuvanticity in vivo and in vitro
Joerg Metzger, Guenther Jung, Wolfgang G. Bessler, Petra Hoffmann, Marianne Strecker, Albrecht Lieberknecht, and Ulrich Schmidt
pp 1969 - 1974; DOI:
10.1021/jm00111a008
PDF
Quantitative structure-activity relationships of antitumor guanidinothiazolecarboxamides with survival enhancement for therapy in the 3LL Lewis lung carcinoma model
Rodney C. Schnur, Randall J. Gallaschun, David H. Singleton, Martin Grissom, Donald E. Sloan, Peter Goodwin, Patricia A. McNiff, Anton F. J. Fliri, F. Michael Mangano, and et al.
pp 1975 - 1982; DOI:
10.1021/jm00111a009
PDF
2-[(Arylmethyl)amino]-2-methyl-1,3-propanediol DNA intercalators. An examination of the effects of aromatic ring variation on antitumor activity and DNA binding
Kenneth W. Bair, C. Webster Andrews, Richard L. Tuttle, Vincent C. Knick, Michael Cory, and David D. McKee
pp 1983 - 1990; DOI:
10.1021/jm00111a010
PDF
Computer simulation of the binding of saframycin A to d(GATGCATC)2
G. Craig Hill and William A. Remers
pp 1990 - 1998; DOI:
10.1021/jm00111a011
PDF
New .alpha.-amino phosphonic acid derivatives of vinblastine: chemistry and antitumor activity
Gilbert Lavielle, Patrick Hautefaye, Corinne Schaeffer, Jean A. Boutin, Claude A. Cudennec, and Alain Pierre
pp 1998 - 2003; DOI:
10.1021/jm00111a012
PDF
Novel cerebroprotective agents with central nervous system stimulating activity. 1. Synthesis and pharmacology of the 1-amino-7-hydroxyindan derivatives
Yasuo Oshiro, Youji Sakurai, Tatsuyoshi Tanaka, Hiraki Ueda, Tetsuro Kikuchi, and Katura Tottori
pp 2004 - 2013; DOI:
10.1021/jm00111a013
PDF
Novel cerebroprotective agents with central nervous system stimulating activity. 2. Synthesis and pharmacology of the 1-(acylamino)-7-hydroxyindan derivatives
Yasuo Oshiro, Youji Sakurai, Tatsuyoshi Tanaka, Tetsuro Kikuchi, Tsuyoshi Hirose, and Katsura Tottori
pp 2014 - 2023; DOI:
10.1021/jm00111a014
PDF
Octoclothepin enantiomers. A reinvestigation of their biochemical and pharmacological activity in relation to a new receptor-interaction model for dopamine D-2 receptor antagonists
Klaus P. Boegesoe, Tommy Liljefors, Joern Arnt, John Hyttel, and Henrik Pedersen
pp 2023 - 2030; DOI:
10.1021/jm00111a015
PDF
Neurochemistry of aging. 2. Design, synthesis and biological evaluation of halomethyl analogs of choline with high affinity choline transport inhibitory activity
Jehangir S. Mistry, Donald J. Abraham, Alan P. Kozikowski, and Israel Hanin
pp 2031 - 2036; DOI:
10.1021/jm00111a016
PDF
An NMR and theoretical study of the conformation and internal flexibility of butaclamol hydrochloride
Marco G. Casarotto, David J. Craik, Edward J. Lloyd, and Ashton C. Partridge
pp 2036 - 2043; DOI:
10.1021/jm00111a017
PDF
NMR studies of the conformational interconversion of butaclamol in solution
Marco G. Casarotto, David J. Craik, and Edward J. Lloyd
pp 2043 - 2049; DOI:
10.1021/jm00111a018
PDF
Electron-deficient isoalloxazines: model systems for disulfide prodrug formation
John R. Cashman and Yan Liu
pp 2049 - 2055; DOI:
10.1021/jm00111a019
PDF
Direct prediction of dissociation constants (pKa's) of clonidine-like imidazolines, 2-substituted imidazoles and 1-methyl-2-substituted-imidazoles from 3D structures using a comparative molecular field analysis (CoMFA) approach
Ki H. Kim and Yvonne C. Martin
pp 2056 - 2060; DOI:
10.1021/jm00111a020
PDF
2-(Oxadiazolyl)- and 2-(thiazolyl)imidazo[1,2-a]pyrimidines as agonists and inverse agonists at benzodiazepine receptors
W. Roger Tully, Colin R. Gardner, Roger J. Gillespie, and Robert Westwood
pp 2060 - 2067; DOI:
10.1021/jm00111a021
PDF
Identification and synthesis of a receptor binding site of human anaphylatoxin C5a
Megumi Kawai, David A. Quincy, Benjamin Lane, Karl W. Mollison, Jay R. Luly, and George W. Carter
pp 2068 - 2071; DOI:
10.1021/jm00111a022
PDF
Evaluation of desferrithiocin and its synthetic analogs as orally effective iron chelators
Raymond J. Bergeron, Jan Wiegand, John B. Dionis, Majia Egli-Karmakka, Joerg Frei, Alica Huxley-Tencer, and Heinrich H. Peter
pp 2072 - 2078; DOI:
10.1021/jm00111a023
PDF
Computer simulation of the binding of naphthyridinomycin and cyanocycline A to DNA
G. Craig Hill, Timothy P. Wunz, Neil E. MacKenzie, Paul R. Gooley, and William A. Remers
pp 2079 - 2088; DOI:
10.1021/jm00111a024
PDF
Improvement in potency of an oxytocin antagonist after systematic substitutions with L-tryptophan
George Flouret, William Brieher, Tadeusz Majewski, Kevin Mahan, and Laird Wilson
pp 2089 - 2094; DOI:
10.1021/jm00111a025
PDF
Stereospecific synthesis of (R)- and (S)-S-adenosyl-1,8-diamino-3-thiooctane, a potent inhibitor of polyamine biosynthesis. Comparison of asymmetric induction vs enantiomeric synthesis
Chin Liu and James K. Coward
pp 2094 - 2101; DOI:
10.1021/jm00111a026
PDF
Gastrin releasing peptide antagonists with improved potency and stability
David C. Heimbrook, Walfred S. Saari, Nancy L. Balishin, Thorsten W. Fisher, Arthur Friedman, David M. Kiefer, Nicola S. Rotberg, John W. Wallen, and Allen Oliff
pp 2102 - 2107; DOI:
10.1021/jm00111a027
PDF
Determination of dissociation constants of high affinity (pM) human renin inhibitors: application to analogs of ditekiren (U-71,038)
D. E. Epps, R. A. Poorman, F. Mandel, and H. J. Schostarez
pp 2107 - 2112; DOI:
10.1021/jm00111a028
PDF
Synthesis of a series of nitrothiophenes with basic or electrophilic substituents and evaluation as radiosensitizers and as bioreductively activated cytotoxins
Michael D. Threadgill, Paul Webb, Peter O'Neill, Matthew A. Naylor, Miriam A. Stephens, Ian J. Stratford, Shirley Cole, Gerald E. Adams, and E. Martin Fielden
pp 2112 - 2120; DOI:
10.1021/jm00111a029
PDF
Relative structure-inhibition analyses of the N-benzoyl and N-(phenylsulfonyl) amino acid aldose reductase inhibitors
Jack DeRuiter, R. Alan Davis, Vinay G. Wandrekar, and Charles A. Mayfield
pp 2120 - 2126; DOI:
10.1021/jm00111a030
PDF
Synthesis and in vivo photodynamic activity of some bacteriochlorin derivatives against bladder tumors in rodents
Alan R. Morgan, Greta M. Garbo, Rick W. Keck, Steven H. Selman, and Dimitris Skalkos
pp 2126 - 2133; DOI:
10.1021/jm00111a031
PDF
Functionalized congener approach to muscarinic antagonists: analogs of pirenzepine
Yishai Karton, Barton J. Bradbury, Jesse Baumgold, Robert Paek, and Kenneth A. Jacobson
pp 2133 - 2145; DOI:
10.1021/jm00111a032
PDF
2-Phenylindole-linked [2-(aminoalkyl)pyridine]dichloroplatinum(II): complexes with a selective action on estrogen receptor positive mammary tumors
Norbert G. Knebel and Erwin Von Angerer
pp 2145 - 2152; DOI:
10.1021/jm00111a033
PDF
3-O-Alkylascorbic acids as free-radical quenchers: synthesis and inhibitory effect on lipid peroxidation
Yasunori Nihro, Hideki Miyataka, Tadamitsu Sudo, Hitoshi Matsumoto, and Toshio Satoh
pp 2152 - 2157; DOI:
10.1021/jm00111a034
PDF
4-Hydroxythiazole inhibitors of 5-lipoxygenase
Francis A. J. Kerdesky, James H. Holms, Jimmie L. Moore, Randy L. Bell, Richard D. Dyer, George W. Carter, and Dee W. Brooks
pp 2158 - 2165; DOI:
10.1021/jm00111a035
PDF
Synthesis of an (iodovinyl)misonidazole derivative for hypoxia imaging
Joseph E. Biskupiak, John R. Grierson, Janet S. Rasey, Gary V. Martin, and Kenneth A. Krohn
pp 2165 - 2168; DOI:
10.1021/jm00111a036
PDF
Syntheses of 5,7,8- and 5,6,7-trioxygenated 3-alkyl-3',4'-dihydroxyflavones and their inhibitory activities against arachidonate 5-lipoxygenase
Tokunaru Horie, Hideaki Tominaga, Yasuhiko Kawamura, Takahiko Hada, Natsuo Ueda, Yumi Amano, and Shozo Yamamoto
pp 2169 - 2176; DOI:
10.1021/jm00111a037
PDF
(Methoxyalkyl)thiazoles: a new series of potent, selective, and orally active 5-lipoxygenase inhibitors displaying high enantioselectivity
T. Geoffrey C. Bird, Pierre Bruneau, Graham C. Crawley, Martin P. Edwards, Stephen J. Foster, Jean Marc Girodeau, John F. Kingston, and Rodger M. McMillan
pp 2176 - 2186; DOI:
10.1021/jm00111a038
PDF
Novel thiophene-, pyrrole-, furan-, and benzene carboxamidotetrazoles as potential antiallergy agents
Michael D. Mullican, Roderick J. Sorenson, David T. Connor, David O. Thueson, John A. Kennedy, and Mary Carol Conroy
pp 2186 - 2194; DOI:
10.1021/jm00111a039
PDF
Synthesis and antiviral and cytostatic properties of 3'-deoxy-3'-fluoro- and 2'-azido-3'-fluoro-2',3'-dideoxy-D-ribofuranosides of natural heterocyclic bases
I. A. Mikhailopulo, N. E. Poopeiko, T. I. Prikota, G. G. Sivets, E. I. Kvasyuk, J. Balzarini, and Erik De Clercq
pp 2195 - 2202; DOI:
10.1021/jm00111a040
PDF
Design, synthesis, and pharmacological evaluation of ultrashort- to long-acting opioid analgesics
Paul L. Feldman, Michael K. James, Marcus F. Brackeen, Joanne M. Bilotta, Suzanne V. Schuster, Avis P. Lahey, Michael W. Lutz, M. Ross Johnson, and H. Jeff Leighton
pp 2202 - 2208; DOI:
10.1021/jm00111a041
PDF
Quinazoline antifolate thymidylate synthase inhibitors: bridge modifications and conformationally restricted analogs in the C2-methyl series
Peter R. Marsham, Ann L. Jackman, Anthony J. Hayter, Melanie R. Daw, Jayne L. Snowden, Brigid M. O'Connor, Joel A. M. Bishop, A. Hilary Calvert, and Leslie R. Hughes
pp 2209 - 2218; DOI:
10.1021/jm00111a042
PDF
Verapamil analog with restricted molecular flexibility
Silvia Dei, M. Novella Romanelli, Serena Scapecchi, Elisabetta Teodori, Alberto Chiarini, and Fulvio Gualtieri
pp 2219 - 2225; DOI:
10.1021/jm00111a043
PDF
Purine and 1-deazapurine ribonucleosides and deoxyribonucleosides: synthesis and biological activity
Gloria Cristalli, Sauro Vittori, Alessandra Eleuteri, Mario Grifantini, Rosaria Volpini, Giulio Lupidi, Laura Capolongo, and Enrico Pesenti
pp 2226 - 2230; DOI:
10.1021/jm00111a044
PDF
Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones
Karl D. Hargrave, John R. Proudfoot, Karl G. Grozinger, Ernest Cullen, Suresh R. Kapadia, Usha R. Patel, Victor U. Fuchs, Scott C. Mauldin, Jana Vitous, and et al.
pp 2231 - 2241; DOI:
10.1021/jm00111a045
PDF
Synthesis and antidopaminergic activity of some 3-(aminomethyl)tetralones as analogs of butyrophenone
Lourdes Cortizo, Lourdes Santana, Enrique Ravina, Francisco Orallo, Jose A. Fontenla, Elena Castro, Jose M. Calleja, and Maria L. De Ceballos
pp 2242 - 2247; DOI:
10.1021/jm00111a046
PDF
Calcium channel blocking and positive inotropic activities of ethyl 5-cyano-1,4-dihydro-6-methyl-2-[(phenylsulfonyl)methyl]-4-aryl-3-pyridinecarboxylate and analogs. Synthesis and structure-activity relationships
Ila Sircar, Eva K. Gregor, K. R. Anderson, Stehen J. Haleen, Yu Hsin Shih, Ronald E. Weishaar, Robert P. Steffen, Thomas A. Pugsley, and M. D. Taylor
pp 2248 - 2260; DOI:
10.1021/jm00111a047
PDF
Synthesis and biological evaluation of substituted benzenesulfonamides as novel potent membrane-bound phospholipase A2 inhibitors
Hitoshi Oinuma, Tadanobu Takamura, Takashi Hasegawa, Kenichi Nomoto, Toshihiko Naitoh, Yoshiharu Daiku, Sachiyuki Hamano, Hiroshi Kakisawa, and Norio Minami
pp 2260 - 2267; DOI:
10.1021/jm00111a048
PDF
Fluorescent markers for hypoxic cells: a study of nitroaromatic compounds, with fluorescent heterocyclic side chains, that undergo bioreductive binding
Richard J. Hodgkiss, Gareth W. Jones, Anthony Long, Richard W. Middleton, John Parrick, Michael R. L. Stratford, Peter Wardman, and George D. Wilson
pp 2268 - 2274; DOI:
10.1021/jm00111a049
PDF
Nucleic acid related compounds. 65. New syntheses of 1-(.beta.-D-arabinofuranosyl)-5(E)-(2-iodovinyl)uracil (IVAraU) from vinylsilane precursors. Radioiodine uptake as a marker for thymidine kinase herpes viral infections
Morris J. Robins, Stefano Manfredini, Steven G. Wood, R. James Wanklin, Bruce A. Rennie, and Stephen L. Sacks
pp 2275 - 2280; DOI:
10.1021/jm00111a050
PDF
Structure activity relationship for mitomycin C and mitomycin A analogs
Kenneth R. Kunz, Bhashyam S. Iyengar, Robert T. Dorr, David S. Alberts, and William A. Remers
pp 2281 - 2286; DOI:
10.1021/jm00111a051
PDF
A new class of acyclic phosphonate nucleotide analogs: Phosphonate isosteres of acyclovir and ganciclovir monophosphates as antiviral agents
Choung Un Kim, Peter F. Misco, Bing Yu Luh, Michael J. M. Hitchcock, Ismail Ghazzouli, and John C. Martin
pp 2286 - 2294; DOI:
10.1021/jm00111a052
PDF
3-Alkyl-4-aminobutyric acids: the first class of anticonvulsant agents that activates L-glutamic acid decarboxylase
Richard B. Silverman, Ryszard Andruszkiewicz, Shrenik M. Nanavati, Charles P. Taylor, and Mark G. Vartanian
pp 2295 - 2298; DOI:
10.1021/jm00111a053
PDF
New pepstatin analogs: synthesis and pepsin inhibition
Rose M. McConnell, Donna Frizzell, Amanda Camp, Anissa Evans, Wanda Jones, and Cathy Cagle
pp 2298 - 2300; DOI:
10.1021/jm00111a054
PDF
Potent inhibitory effect of a series of modified cyclodextrin sulfates on the replication of HIV-1 in vitro
Tamon Moriya, Hironori Kurita, Kazuo Matsumoto, Toru Otake, Haruyo Mori, Motoko Morimoto, Noboru Ueba, and Nobuharu Kunita
pp 2301 - 2304; DOI:
10.1021/jm00111a055
PDF
Rationally designed "dipeptoid" analogs of CCK. .alpha.-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties [Erratum to document cited in CA114(5):43545w]
David C. Horwell, John Hughes, John C. Hunter, Martyn C. Pritchard, Reginald S. Richardson, Edward Roberts, and Geoffrey N. Woodruff
pp 2304 - 2304; DOI:
10.1021/jm00111a056
PDF

Issue 8


HIV protease: a novel chemotherapeutic target for AIDS
Joel R. Huff
pp 2305 - 2314; DOI:
10.1021/jm00112a001
PDF
Cholinergic activity of acetylenic imidazoles and related compounds
Malcolm W. Moon, Connie G. Chidester, Richard F. Heier, Jeanette K. Morris, R. James Collins, Roland R. Russell, Jonathan W. Francis, G. Patrick Sage, and Vimala H. Sethy
pp 2314 - 2327; DOI:
10.1021/jm00112a002
PDF
Sulfonylbenzoyl-nitrostyrenes: Potential bisubstrate type inhibitors of the EGF-receptor tyrosine protein kinase
Peter M. Traxler, Oskar Wacker, Ha L. Bach, Johanna F. Geissler, Wilhelm Kump, Thomas Meyer, Urs Regenass, Johannes L. Roesel, and Nicholas Lydon
pp 2328 - 2337; DOI:
10.1021/jm00112a003
PDF
Comparative molecular field analysis of some clodronic acid esters
J. P. Bjorkroth, T. A. Pakkanen, J. Lindroos, E. Pohjala, H. Hanhijarvi, L. Lauren, R. Hannuniemi, A. Juhakoski, K. Kippo, and T. Kleimola
pp 2338 - 2343; DOI:
10.1021/jm00112a004
PDF
Inhibitors of the protease from human immunodeficiency virus: design and modeling of a compound containing a dihydroxyethylene isostere insert with high binding affinity and effective antiviral activity
Suvit Thaisrivongs, Alfredo G. Tomasselli, Joseph B. Moon, John Hui, Thomas J. McQuade, Steve R. Turner, Joseph W. Strohbach, W. Jeffrey Howe, W. Gary Tarpley, and Robert L. Heinrikson
pp 2344 - 2356; DOI:
10.1021/jm00112a005
PDF
2-Chloro-1-(2,4-dichlorophenyl)-3-(1H-imidazol-1-yl)-2-phenylpropan-1-one hydrochloride, a novel, nonmutagenic antibacterial with specific activity against anaerobic bacteria
Jon P. Dickens, George J. Ellames, Nigel J. Hare, Kevin R. Lawson, William R. McKay, Anthony P. Metters, Peter L. Myers, Anthony M. S. Pope, and Roger M. Upton
pp 2356 - 2360; DOI:
10.1021/jm00112a006
PDF
Synthesis and biological activity of 2'-deoxy-4'-thio pyrimidine nucleosides
John A. Secrist, Kamal N. Tiwari, James M. Riordan, and John A. Montgomery
pp 2361 - 2366; DOI:
10.1021/jm00112a007
PDF
Modeling study of the structure of the macromolecular antitumor antibiotic neocarzinostatin. Origin of the stabilization of the chromophore
Masaji Ishiguro, Seiichi Imajo, and Masahiro Hirama
pp 2366 - 2373; DOI:
10.1021/jm00112a008
PDF
Synthesis and antitumor evaluations of symmetrically and unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones and 1,4-bis[(aminoalkyl)amino]-5,8-dihydroxyanthracene-9,10-diones
A. Paul Krapcho, Zelleka Getahun, Kenneth L. Avery, Kevin J. Vargas, Miles P. Hacker, Silvano Spinelli, Gabriella Pezzoni, and Carla Manzotti
pp 2373 - 2380; DOI:
10.1021/jm00112a009
PDF
Synthesis and antiviral activity of 3-substituted derivatives of 3,9-dihydro-9-oxo-5H-imidazo[1,2-a]purines, tricyclic analogs of acyclovir and ganciclovir
Jerzy Boryski, Bozenna Golankiewicz, and Erik De Clercq
pp 2380 - 2383; DOI:
10.1021/jm00112a010
PDF
5-(5-Bromothien-2-yl)-2'-deoxyuridine and 5-(5-chlorothien-2-yl)-2'-deoxyuridine are equipotent to (E)-5-(2-bromovinyl)-2'-deoxyuridine in the inhibition of herpes simplex virus type I replication
P. Wigerinck, C. Pannecouque, R. Snoeck, P. Claes, E. De Clercq, and P. Herdewijn
pp 2383 - 2389; DOI:
10.1021/jm00112a011
PDF
Synthesis and binding of [125I2]philanthotoxin-343, [125I2]philanthotoxin-343-lysine, and [125I2]philanthotoxin-343-arginine to rat brain membranes
R. A. Goodnow, R. Bukownik, K. Nakanishi, P. N. R. Usherwood, A. T. Eldefrawi, N. A. Anis, and M. E. Eldefrawi
pp 2389 - 2394; DOI:
10.1021/jm00112a012
PDF
Novel gonadotropin-releasing hormone antagonists: peptides incorporating modified N.omega.-cyanoguanidino moieties
Paula Theobald, John Porter, Catherine Rivier, Anne Corrigan, Marilyn Perrin, Wylie Vale, Jean Rivier, William Hook, and Reuben Siraganian
pp 2395 - 2402; DOI:
10.1021/jm00112a013
PDF
Synthesis and biological activity of angiotensin II analog containing a Val-His replacement, Val.psi.[CH(CONH2)HN]His
Raju Mohan, Yuo Ling Chou, Ron Bihovsky, William C. Lumma, Paul W. Erhardt, and Kenneth J. Shaw
pp 2402 - 2410; DOI:
10.1021/jm00112a014
PDF
Conformationally restricted polysubstituted biphenyl derivatives with angiotensin II receptors antagonist properties
P. R. Bovy, J. T. Collins, G. M. Olins, E. G. McMahon, and W. C. Hutton
pp 2410 - 2414; DOI:
10.1021/jm00112a015
PDF
Synthesis and DNA-binding properties of polyamine analogs
Michael L. Edwards, Ronald D. Snyder, and David M. Stemerick
pp 2414 - 2420; DOI:
10.1021/jm00112a016
PDF
Synthesis of structural analogs of lyngbyatoxin A and their evaluation as activators of protein kinase C
Alan P. Kozikowski, Patrick W. Shum, Alakananda Basu, and John S. Lazo
pp 2420 - 2430; DOI:
10.1021/jm00112a017
PDF
Pseudopeptide analogs of substance P and leucine enkephalinamide containing the .psi.(methyleneoxy) modification: synthesis and biological activity
Eli Roubini, Ralph Laufer, Chaim Gilon, Zvi Selinger, Bernard P. Roques, and Michael Chorev
pp 2430 - 2438; DOI:
10.1021/jm00112a018
PDF
Electrophilic .gamma.-lactone .kappa.-opioid receptor probes. Analogs of 2'-hydroxy-2-(tetrahydrofurfuryl)-5,9-dimethyl-6,7-benzomorphan diastereomers
Peter Klein and Wendel L. Nelson
pp 2438 - 2444; DOI:
10.1021/jm00112a019
PDF
Preparation and anticonvulsant activity of a series of functionalized .alpha.-heteroatom-substituted amino acids
Harold Kohn, Kailash N. Sawhney, Philippe LeGall, David W. Robertson, and J. David Leander
pp 2444 - 2452; DOI:
10.1021/jm00112a020
PDF
Studies of vitamin D (calciferol) and its analogs. 39. Arocalciferols: synthesis and biological evaluation of aromatic side-chain analogs of 1.alpha.,25-dihydroxyvitamin D3
Bruno Figadere, Anthony W. Norman, Helen L. Henry, H. Phillip Koeffler, Jian Yuan Zhou, and William H. Okamura
pp 2452 - 2463; DOI:
10.1021/jm00112a021
PDF
Aldosterone antagonists. 4. Synthesis and activities of steroidal 6,6-ethylene-15,16-methylene 17-spirolactones
Klaus Nickisch, Sybille Beier, Dieter Bittler, Walter Elger, Henry Laurent, Wolfgang Losert, Yukishige Nishino, Ekkehard Schillinger, and Rudolf Wiechert
pp 2464 - 2468; DOI:
10.1021/jm00112a022
PDF
Synthesis and evaluation of antiinflammatory activities of a series of corticosteroid 17.alpha.-esters containing a functional group
Hiroaki Ueno, Akira Maruyama, Motoyoshi Miyake, Etsuko Nakao, Kenichiro Nakao, Kohei Umezu, and Issei Nitta
pp 2468 - 2473; DOI:
10.1021/jm00112a023
PDF
3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 8. Side chain ether analogs of lovastatin
Ta Jyh Lee, W. J. Holtz, R. L. Smith, A. W. Alberts, and J. L. Gilfillan
pp 2474 - 2477; DOI:
10.1021/jm00112a024
PDF
Naphthosultam derivatives: a new class of potent and selective 5-HT2 antagonists
Jean Luc Malleron, Marie Therese Comte, Claude Gueremy, Jean Francis Peyronel, Alain Truchon, Jean Charles Blanchard, Adam Doble, Odile Piot, Jean Luc Zundel, and et al.
pp 2477 - 2483; DOI:
10.1021/jm00112a025
PDF
A new class of analog of the bifunctional radiosensitizer .alpha.-(1-aziridinylmethyl)-2-nitro-1H-imidazole-1-ethanol (RSU 1069): the cycloalkylaziridines
Mark J. Suto, Michael A. Stier, Leslie M. Werbel, Carla M. Arundel-Suto, Wilbur R. Leopold, William E. Elliott, and Judith S. Sebolt-Leopold
pp 2484 - 2488; DOI:
10.1021/jm00112a026
PDF
3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 7. Modification of the hexahydronaphthalene moiety of simvastatin: 5-oxygenated and 5-oxa derivatives
Mark E. Duggan, Alfred W. Alberts, Rick Bostedor, Yu Sheng Chao, John I. Germershausen, James L. Gilfillan, Wasyl Halczenko, George D. Hartman, Vincent Hunt, and et al.
pp 2489 - 2495; DOI:
10.1021/jm00112a027
PDF
Synthesis and biochemical studies of 16- or 19-substituted androst-4-enes as aromatase inhibitors
Mitsuteru Numazawa, Ayako Mutsumi, Kumiko Hoshi, Mariko Oshibe, Etsushi Ishikawa, and Hiroki Kigawa
pp 2496 - 2504; DOI:
10.1021/jm00112a028
PDF
Syntheses of tolrestat analogs containing additional substituents in the ring and their evaluation as aldose reductase inhibitors. Identification of potent, orally active 2-fluoro derivatives
Jay Wrobel, Jane Millen, Janet Sredy, Arlene Dietrich, Beverly J. Gorham, Michael Malamas, Joseph M. Kelly, John G. Bauman, Maria C. Harrison, and et al.
pp 2504 - 2520; DOI:
10.1021/jm00112a029
PDF
Active conformation of 1,4-dihydropyridine calcium entry blockers. Effect of size of 2-aryl substituent on rotameric equilibria and receptor binding
George Rovnyak, Niels Andersen, Jack Gougoutas, Anders Hedberg, S. David Kimball, Mary Malley, Suzanne Moreland, Michael Porubcan, and Andrew Pudzianowski
pp 2521 - 2524; DOI:
10.1021/jm00112a030
PDF
Nonpeptide angiotensin II receptor antagonists: the discovery of a series of N-(biphenylylmethyl)imidazoles as potent, orally active antihypertensives
David J. Carini, John V. Duncia, Paul E. Aldrich, Andrew T. Chiu, Alexander L. Johnson, Michael E. Pierce, William A. Price, Joseph B. Santella, III, Gregory J. Wells, and et al.
pp 2525 - 2547; DOI:
10.1021/jm00112a031
PDF
GABA-uptake inhibitors: construction of a general pharmacophore model and successful prediction of a new representative
Victor N'Goka, Gilbert Schlewer, Jean Michel Linget, Jean Pierre Chambon, and Camille Georges Wermuth
pp 2547 - 2557; DOI:
10.1021/jm00112a032
PDF
3-Thienyl- and 3-furylaminobutyric acids. Synthesis and binding GABAB receptor studies
Pascal Berthelot, Claude Vaccher, Nathalie Flouquet, Michel Debaert, Michel Luyckx, and Claude Brunet
pp 2557 - 2560; DOI:
10.1021/jm00112a033
PDF
Synthesis and dopaminergic activity of 3-substituted 1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-1H-2-benzopyrans: characterization of an auxiliary binding region in the D1 receptor
Michael P. DeNinno, Robert Schoenleber, Richard J. Perner, Linda Lijewski, Karen E. Asin, Donald R. Britton, Robert MacKenzie, and John W. Kebabian
pp 2561 - 2569; DOI:
10.1021/jm00112a034
PDF
Highly selective adenosine A2 receptor agonists in a series of N-alkylated 2-aminoadenosines
John E. Francis, Randy L. Webb, Geetha R. Ghai, Alan J. Hutchison, Michael A. Moskal, Reynalda DeJesus, Rina Yokoyama, Stephen L. Rovinski, Nicolina Contardo, and et al.
pp 2570 - 2579; DOI:
10.1021/jm00112a035
PDF
Synthesis and evaluation of stilbene and dihydrostilbene derivatives as potential anticancer agents that inhibit tubulin polymerization
Mark Cushman, Dhanapalan Nagarathnam, D. Gopal, Asit K. Chakraborti, Chii M. Lin, and Ernest Hamel
pp 2579 - 2588; DOI:
10.1021/jm00112a036
PDF
Relaxant activity of 6-cyano-2,2-dimethyl-2H-1-benzopyran-4-carboxamides and -thiocarboxamides and their analogs in guinea pig trachealis
Jonathan R. S. Arch, Derek R. Buckle, Claire Carey, Hilary Parr-Dobrzanski, Andrew Faller, Keith A. Foster, Catherine S. V. Houge-Frydrych, Ivan L. Pinto, David G. Smith, and Stephen G. Taylor
pp 2588 - 2594; DOI:
10.1021/jm00112a037
PDF
Solid-state and solution conformation of 3'-amino-3'-deoxythymidine, precursor to a noncompetitive inhibitor of HIV-1 reverse transcriptase
Terez Kovacs, Laszlo Parkanyi, Istvan Pelczer, Francisco Cervantes-Lee, Keith H. Pannell, and Paul F. Torrence
pp 2595 - 2600; DOI:
10.1021/jm00112a038
PDF
Targeting 5'-deoxy-5'-(methylthio)adenosine phosphorylase by 5'-haloalkyl analogs of 5'-deoxy-5'-(methylthio)adenosine
Janice R. Sufrin, Arthur J. Spiess, Debora L. Kramer, Paul R. Libby, John T. Miller, Ralph J. Bernacki, Younha Lee, Ronald T. Borchardt, and Carl W. Porter
pp 2600 - 2606; DOI:
10.1021/jm00112a039
PDF
Synthesis and anticancer and antiviral activities of various 2'- and 3'-methylidene-substituted nucleoside analogs and crystal structure of 2'-deoxy-2'-methylidenecytidine hydrochloride
Tai Shun Lin, Mei Zhen Luo, Mao Chin Liu, Regina H. Clarke-Katzenburg, Yung Chi Cheng, William H. Prusoff, William R. Mancini, George I. Birnbaum, Eric J. Gabe, and Jerzy Giziewicz
pp 2607 - 2615; DOI:
10.1021/jm00112a040
PDF
Synthesis, stereochemistry, and biological activity of the 1-(1-phenyl-2-methylcyclohexyl)piperidines and the 1-(1-phenyl-4-methylcyclohexyl)piperidines. Absolute configuration of the potent trans-(-)-1-(1-phenyl-2-methylcyclohexyl)piperidine
Maria A. Iorio, Lamberto Tomassini, Mariena V. Mattson, Clifford George, and Arthur E. Jacobson
pp 2615 - 2623; DOI:
10.1021/jm00112a041
PDF
(1S)-1-(Aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinoline and heterocycle-condensed tetrahydropyridine derivatives: members of a novel class of very potent .kappa. opioid analgesics
Vittorio Vecchietti, Geoffrey D. Clarke, Roberto Colle, Giuseppe Giardina, Giuseppe Petrone, and Massimo Sbacchi
pp 2624 - 2633; DOI:
10.1021/jm00112a042
PDF
Analogs of the 5-HT1A serotonin antagonist 1-(2-methoxyphenyl)-4-[4-(2-phthalimido)butyl]piperazine with reduced .alpha.1-adrenergic affinity
Revathi K. Raghupathi, Laura Rydelek-Fitzgerald, Milt Teitler, and Richard A. Glennon
pp 2633 - 2638; DOI:
10.1021/jm00112a043
PDF
Acyclic analogs of 2-(4-phenylpiperidino)cyclohexanol (vesamicol): conformationally mobile inhibitors of vesicular acetylcholine transport
S. M. N. Efange, R. H. Michelson, A. K. Dutta, and S. M. Parsons
pp 2638 - 2643; DOI:
10.1021/jm00112a044
PDF
Synthesis of 2-deoxy-2-[(2,2-difluoro-3-hydroxytetradecanoyl)amino]-3-O-[(R)-3-(tetradecanoyloxy)tetradecanoyl]-D-glucopyranose 4-phosphate
Masao Shiozaki, Yoshiyuki Kobayashi, Masami Arai, Takashi Watanabe, Tetsuo Hiraoka, Masahiro Nishijima, Sayuri Kuge, Toshiaki Otsuka, and Yuzuru Akamatsu
pp 2643 - 2646; DOI:
10.1021/jm00112a045
PDF
3-(5-Alkyl-4-hydroxy-3-methoxy-1-naphthalenyl)-2-methyl-2-propenoic acids as orally active inhibitors of IL-1 generation
Masayuki Tanaka, Kenichi Chiba, Makoto Okita, Toshihiko Kaneko, Katsuya Tagami, Shigeki Hibi, Yasushi Okamoto, Hiroshi Shirota, Masaki Goto, and et al.
pp 2647 - 2649; DOI:
10.1021/jm00112a046
PDF
Probing the bradykinin receptor: mapping the geometric topography using ethers of hydroxyproline in novel peptides
Donald J. Kyle, Jennifer A. Martin, Ronald M. Burch, John P. Carter, Songfeng Lu, Sonya Meeker, Judith C. Prosser, James P. Sullivan, James Togo, and et al.
pp 2649 - 2653; DOI:
10.1021/jm00112a047
PDF
Determination of the relative binding free energies of peptide inhibitors to the HIV-1 protease
David M. Ferguson, Randall J. Radmer, and Peter A. Kollman
pp 2654 - 2659; DOI:
10.1021/jm00112a048
PDF
Book Reviews

pp 2660 - 2664; DOI:
10.1021/jm00112a600
PDF

Issue 9


My odyssey in drug discovery
George DeStevens
pp 2665 - 2670; DOI:
10.1021/jm00113a001
PDF
Novel compounds possessing potent cAMP and cGMP phosphodiesterase inhibitory activity. Synthesis and cardiovascular effects of a series of imidazo[1,2-a]quinoxalinones and imidazo[1,5-a]quinoxalinones and their aza analogs
David D. Davey, P. W. Erhardt, E. H. Cantor, S. S. Greenberg, W. R. Ingebretsen, and J. Wiggins
pp 2671 - 2677; DOI:
10.1021/jm00113a002
PDF
Spatial requirements of the sodium channel binding site for class I antiarrhythmics as derived from the crystal structures of 4-substituted 2,6-bis(1-pyrrolidinylmethyl)phenols
Marek L. Glowka, Robin L. Dargie, and Penelope W. Codding
pp 2678 - 2684; DOI:
10.1021/jm00113a003
PDF
New aromatase inhibitors. Synthesis and biological activity of pyridyl-substituted tetralone derivatives
Herbert Bayer, Christine Batzl, Rolf W. Hartman, and Albrecht Mannschreck
pp 2685 - 2691; DOI:
10.1021/jm00113a004
PDF
Design and synthesis of P2-P1'-linked macrocyclic human renin inhibitors
Ann E. Weber, Thomas A. Halgren, John J. Doyle, Robert J. Lynch, Peter K. S. Siegl, William H. Parsons, William J. Greenlee, and Arthur A. Patchett
pp 2692 - 2701; DOI:
10.1021/jm00113a005
PDF
Studies on uricosuric diuretics. 4. Three-dimensional structure-activity relationships and receptor mapping of (aryloxy)acetic acid diuretics
Hiroshi Koga, Haruhiko Sato, Takashi Dan, and Bunya Aoki
pp 2702 - 2708; DOI:
10.1021/jm00113a006
PDF
Crystallographic and molecular modeling studies on trypanosomal triosephosphate isomerase: a critical assessment of the predicted and observed structures of the complex with 2-phosphoglycerate
Martin E. M. Noble, Christophe L. M. J. Verlinde, Hillie Groendijk, Kor H. Kalk, Rik K. Wierenga, and Wim G. J. Hol
pp 2709 - 2718; DOI:
10.1021/jm00113a007
PDF
Synthesis, ligand binding, QSAR, and CoMFA study of 3.beta.-(p-substituted phenyl)tropane-2.beta.-carboxylic acid methyl esters
F. Ivy Carroll, Yigong Gao, M. Abdur Rahman, Philip Abraham, Karol Parham, Anita H. Lewin, John W. Boja, and Michael J. Kuhar
pp 2719 - 2725; DOI:
10.1021/jm00113a008
PDF
Comparison of azabicyclic esters and oxadiazoles as ligands for the muscarinic receptor
Barry S. Orlek, Frank E. Blaney, Frank Brown, Michael S. G. Clark, Michael S. Hadley, John Hatcher, Graham J. Riley, Howard E. Rosenberg, Harry J. Wadsworth, and Paul Wyman
pp 2726 - 2735; DOI:
10.1021/jm00113a009
PDF
Dopamine autoreceptor agonists as potential antipsychotics. 3. 6-Propyl-4,5,5a,6,7,8-hexahydrothiazolo[4,5-f]quinolin-2-amine
Bradley W. Caprathe, Juan C. Jaen, Lawrence D. Wise, Thomas G. Heffner, Thomas A. Pugsley, Leonard T. Meltzer, and Masood Parvez
pp 2736 - 2746; DOI:
10.1021/jm00113a010
PDF
Folate analogs. 35. Synthesis and biological evaluation of 1-deaza, 3-deaza, and bridge-elongated analogs of N10-propargyl-5,8-dideazafolic acid
Shu Wen Li, M. G. Nair, Donna M. Edwards, R. L. Kisliuk, Y. Gaumont, I. K. Dev, D. S. Duch, J. Humphreys, G. K. Smith, and Robert Ferone
pp 2746 - 2754; DOI:
10.1021/jm00113a011
PDF
Structure-activity relationships of estrogenic ligands: synthesis and evaluation of (17.alpha.,20E)- and (17.alpha.,20Z)-21-halo-19-norpregna-1,3,5(10),20-tetraene-3,17.beta.-diols
Elio Napolitano, Rita Fiaschi, and Robert N. Hanson
pp 2754 - 2759; DOI:
10.1021/jm00113a012
PDF
C-Glycosidic analogs of lipid A and lipid X: synthesis and biological activities
Hermann Vyplel, Dieter Scholz, Ingolf Macher, Karl Schindlmaier, and Eberhard Schuetze
pp 2759 - 2767; DOI:
10.1021/jm00113a013
PDF
(Phenylmethoxy)phenyl derivatives of w-oxo- and w-tetrazolylalkanoic acids and related tetrazoles. Synthesis and evaluation as leukotriene D4 receptor antagonists
Robert D. Dillard, Richard A. Hahn, Doris McCullough, F. Patrick Carr, Lynn E. Rinkema, Carlos R. Roman, and Jerome H. Fleisch
pp 2768 - 2778; DOI:
10.1021/jm00113a014
PDF
Pregnanes that bind to the digitalis receptor: synthesis of 14-hydroxy-5.beta.,14.beta.-pregnane glycosides from digitoxin and digitoxigenin
John F. Templeton, Peter Setiloane, V. P. Sashi Kumar, Yulan Yan, Talal H. Zeglam, and Frank S. LaBella
pp 2778 - 2782; DOI:
10.1021/jm00113a015
PDF
The synthesis and antiviral activity of some 4'-thio-2'-deoxy nucleoside analogs
Michael R. Dyson, Paul L. Coe, and Richard T. Walker
pp 2782 - 2786; DOI:
10.1021/jm00113a016
PDF
Synthesis and biological evaluation of 4-purinylpyrrolidine nucleosides
Mark L. Peterson and Robert Vince
pp 2787 - 2797; DOI:
10.1021/jm00113a017
PDF
Synthesis and biological activity of sinefungin analogs
Pierre Blanchard, Nerina Dodic, Jean Louis Fourrery, Francoise Lawrence, Abdel Malek Mouna, and Malka Robert-Gero
pp 2798 - 2803; DOI:
10.1021/jm00113a018
PDF
Phosphorus-containing inhibitors of HMG-CoA reductase. 2. Synthesis and biological activities of a series of substituted pyridines containing a hydroxyphosphinyl moiety
Jeffrey A. Robl, Laurelee A. Duncan, Jelka Pluscec, Donald S. Karanewsky, Eric M. Gordon, Carl P. Ciosek Jr., Lois C. Rich, Viviane C. Dehmel, Dorothy A. Slusarchyk, and et al.
pp 2804 - 2815; DOI:
10.1021/jm00113a019
PDF
Modification of the enkephalin "message" with an artificial polycationic C-terminus
Alan R. Jacobson, S. William Tam, and Lawrence M. Sayre
pp 2816 - 2821; DOI:
10.1021/jm00113a020
PDF
Monoterpenic fragment analogs of aplasmomycin as potential antimalarials
N. Balu, Jacob V. Thomas, and Sujata V. Bhat
pp 2821 - 2823; DOI:
10.1021/jm00113a021
PDF
Applications of neural networks in quantitative structure-activity relationships of dihydrofolate reductase inhibitors
T. A. Andrea and Hooshmand Kalayeh
pp 2824 - 2836; DOI:
10.1021/jm00113a022
PDF
Boc-CCK-4 derivatives containing side-chain ureas as potent and selective CCK-A receptor agonists
Kazumi Shiosaki, Chun Wel Lin, Hana Kopecka, Michael D. Tufano, Bruce R. Bianchi, Thomas R. Miller, David G. Witte, and Alex M. Nadzan
pp 2837 - 2842; DOI:
10.1021/jm00113a023
PDF
Benzylated 1,2,3-triazoles as anticoccidiostats
Richard J. Bochis, John C. Chabala, Ellwood Harris, Louis H. Peterson, Louis Barash, Thomas Beattie, Jeannette E. Brown, Donald W. Graham, Frank S. Waksmunski, and et al.
pp 2843 - 2852; DOI:
10.1021/jm00113a024
PDF
Design and synthesis of HIV protease inhibitors. Variations of the carboxyterminus of the HIV protease inhibitor L-682,679
S. Jane DeSolms, Elizabeth A. Giuliani, James P. Guare, Joseph P. Vacca, William M. Sanders, Samuel L. Graham, J. Mark Wiggins, Paul L. Darke, Irving S. Sigal, and et al.
pp 2852 - 2857; DOI:
10.1021/jm00113a025
PDF
Dual-action cephalosporins: cephalosporin 3'-quinolone carbamates
Harry A. Albrecht, George Beskid, Nafsika H. Georgopapadakou, Dennis D. Keith, Frederick M. Konzelmann, David L. Pruess, Pamela L. Rossman, Chung Chen Wei, and James G. Christenson
pp 2857 - 2864; DOI:
10.1021/jm00113a026
PDF
Potential antitumor agents. 63. Structure-activity relationships for side-chain analogs of the colon 38 active agent 9-oxo-9H-xanthene-4-acetic acid
Gordon W. Rewcastle, Graham J. Atwell, Bruce C. Baguley, Maruta Boyd, Lindy L. Thomsen, Li Zhuang, and William A. Denny
pp 2864 - 2870; DOI:
10.1021/jm00113a027
PDF
Determination of the mechanism of demethylenation of (methylenedioxy)phenyl compounds by cytochrome P450 using deuterium isotope effects
Jon M. Fukuto, Yoshito Kumagai, and Arthur K. Cho
pp 2871 - 2876; DOI:
10.1021/jm00113a028
PDF
N6,9-Disubstituted adenines: potent, selective antagonists at the A1 adenosine receptor
Robert D. Thompson, Sherrie Secunda, John W. Daly, and Ray A. Olsson
pp 2877 - 2882; DOI:
10.1021/jm00113a029
PDF
Interphenylene 7-oxabicyclo[2.2.1]heptane thromboxane A2(TxA2)antagonists. Semicarbazone .omega.-chains
Raj N. Misra, Baerbel R. Brown, Wen Ching Han, Don N. Harris, Anders Hedberg, Maria L. Webb, and Steven E. Hall
pp 2882 - 2891; DOI:
10.1021/jm00113a030
PDF
Synthesis and adenosine receptor affinity of a series of pyrazolo[3,4-d]pyrimidine analogs of 1-methylisoguanosine
Fiona A. Harden, Ronald J. Quinn, and Peter J. Scammells
pp 2892 - 2898; DOI:
10.1021/jm00113a031
PDF
Anxiolytic properties of certain annelated [1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-ones
John E. Francis, Debra A. Bennett, James L. Hyun, Stephen L. Rovinski, Caryl L. Amrick, Patricia S. Loo, Deborah Murphy, Robert F. Neale, and Douglas E. Wilson
pp 2899 - 2906; DOI:
10.1021/jm00113a032
PDF
1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-ones - inhibitors of blood platelet cAMP phosphodiesterase and induced aggregation
Nicholas A. Meanwell, Herbert R. Roth, Edward C. R. Smith, Donald L. Wedding, J. J. Kim Wright, J. Stuart Fleming, and Elizabeth Gillespie
pp 2906 - 2916; DOI:
10.1021/jm00113a033
PDF
Nucleosides and nucleotides. 100. 2'-C-Cyano-2'-deoxy-1-.beta.-D-arabinofuranosylcytosine (CNDAC): design of a potential mechanism-based DNA-strand-breaking antineoplastic nucleoside
Akira Matsuda, Yuki Nakajima, Atsushi Azuma, Motohiro Tanaka, and Takuma Sasaki
pp 2917 - 2919; DOI:
10.1021/jm00113a034
PDF
Potent, orally active imidazo[4,5-b]pyridine-based angiotensin II receptor antagonists
Nathan B. Mantlo, Prasun K. Chakravarty, Debra L. Ondeyka, Peter K. S. Siegl, Raymond S. Chang, Victor J. Lotti, Kristie A. Faust, Terry W. Schorn, Tsing Bau Chen, and et al.
pp 2919 - 2922; DOI:
10.1021/jm00113a035
PDF
2-Pyridinone derivatives: a new class of nonnucleoside, HIV-1-specific reverse transcriptase inhibitors
Walfred S. Saari, Jacob M. Hoffman, John S. Wai, Thorsten E. Fisher, Clarence S. Rooney, Anthony M. Smith, Craig M. Thomas, Mark E. Goldman, Julie A. O'Brien, and et al.
pp 2922 - 2925; DOI:
10.1021/jm00113a036
PDF
NMR studies of an FK-506 analog [U-13C]ascomycin, bound to FKBP: conformation and regions of ascomycin involved in binding
A. M. Petros, R. T. Gampe Jr., G. Gemmecker, P. Neri, T. F. Holzman, R. Edalji, J. Hochlowski, M. Jackson, J. McAlpine, and et al.
pp 2925 - 2928; DOI:
10.1021/jm00113a037
PDF
Substituted 2-(aminomethyl)piperidines: a novel class of selective protein kinase C inhibitors
Barry G. Shearer, James P. Sullivan, J. Paul Carter, Rose M. Mathew, Phillip Waid, Jane R. Connor, Raymond J. Patch, and Ronald M. Burch
pp 2928 - 2931; DOI:
10.1021/jm00113a038
PDF
A selective, reversible, competitive inhibitor of monoamine oxidase A containing no nitrogen, with negligible potentiation of tyramine-induced blood pressure rise
Morton Harfenist, Daniel P. C. McGee, and Helen L. White
pp 2931 - 2933; DOI:
10.1021/jm00113a039
PDF
Nitroheterocycle reduction as a paradigm for intramolecular catalysis of drug delivery to hypoxic cells
Albert Firestone, R. Timothy Mulcahy, and Richard F. Borch
pp 2933 - 2935; DOI:
10.1021/jm00113a040
PDF
Book Reviews

pp 2936 - 2936; DOI:
10.1021/jm00113a600
PDF

Issue 10


NMR studies of molecular complexes as a tool in drug design
Stephen W. Fesik
pp 2937 - 2945; DOI:
10.1021/jm00114a001
PDF
Synthesis and pharmacological evaluation of 1-(aminomethyl)-3,4-dihydro-5-hydroxy-1H-2-benzopyrans as dopamine D1 selective ligands
Michael R. Michaelides, Robert Schoenleber, Sheela Thomas, Diane M. Yamamoto, Donald R. Britton, Robert MacKenzie, and John W. Kebabian
pp 2946 - 2953; DOI:
10.1021/jm00114a002
PDF
Structure-activity studies of antitumor agents based on pyrrolo[1,2-a]benzimidazoles: new reductive alkylating DNA cleaving agents
Imadul Islam, Edward B. Skibo, Robert T. Dorr, and David S. Alberts
pp 2954 - 2961; DOI:
10.1021/jm00114a003
PDF
Synthesis and biological activity of new HMG-CoA reductase inhibitors. 3. Lactones of 6-phenoxy-3,5-dihydroxyhexanoic acids
H. Jendralla, E. Granzer, B. Von Kerekjarto, R. Krause, U. Schacht, E. Baader, W. Bartmann, G. Beck, A. Bergmann, and et al.
pp 2962 - 2983; DOI:
10.1021/jm00114a004
PDF
Muscarinic receptor binding profile of para-substituted caramiphen analogs
Robert L. Hudkins, Diane L. DeHaven-Hudkins, and James F. Stubbins
pp 2984 - 2989; DOI:
10.1021/jm00114a005
PDF
Synthesis and muscarinic cholinergic receptor affinities of 3-quinuclidinyl .alpha.-(alkoxyalkyl)-.alpha.-aryl-.alpha.-hydroxyacetates
Victor I. Cohen, Raymond E. Gibson, Linda H. Fan, Rosanna De la Cruz, Miriam S. Gitler, Erin Hariman, and Richard C. Reba
pp 2989 - 2993; DOI:
10.1021/jm00114a006
PDF
2-Phenyl-3H-imidazo[4,5-b]pyridine-3-acetamides as nonbenzodiazepine anticonvulsants and anxiolytics
Bruce E. Tomczuk, C. R. Taylor, L. Meredith Moses, Deborah B. Sutherland, Young S. Lo, David N. Johnson, William B. Kinnier, and Brian F. Kilpatrick
pp 2993 - 3006; DOI:
10.1021/jm00114a007
PDF
Synthesis and antiviral activity of certain guanosine analogs in the thiazolo[4,5-d]pyrimidine ring system
Ganesh D. Kini, Jack D. Anderson, Yogesh S. Sanghvi, Arthur F. Lewis, Donald F. Smee, Ganapathi R. Revankar, Roland K. Robins, and Howard B. Cottam
pp 3006 - 3010; DOI:
10.1021/jm00114a008
PDF
Synthesis, calcium-channel-blocking activity, and antihypertensive activity of 4-(diarylmethyl)-1-[3-(aryloxy)propyl]piperidines and structurally related compounds
James R. Shanklin, Christopher P. Johnson, Anthony G. Proakis, and Richard J. Barrett
pp 3011 - 3022; DOI:
10.1021/jm00114a009
PDF
New 5H-pyridazino[4,5-b]indole derivatives. Synthesis and studies as inhibitors of blood platelet aggregation and inotropics
A. Monge, I. Aldana, T. Alvarez, M. Font, E. Santiago, J. A. Latre, M. J. Bermejillo, M. J. Lopez-Unzu, and E. Fernandez-Alvarez
pp 3023 - 3029; DOI:
10.1021/jm00114a010
PDF
Peptide derivatives specific for a Plasmodium falciparum proteinase inhibit the human erythrocyte invasion by merozoites
Roger Mayer, Isabelle Picard, Philippe Lawton, Philippe Grellier, Christine Barrault, Michel Monsigny, and Joseph Schrevel
pp 3029 - 3035; DOI:
10.1021/jm00114a011
PDF
An investigation of angiotensin II agonist and antagonist analogs with 5,5-dimethylthiazolidine-4-carboxylic acid and other constrained amino acids
J. Samanen, T. Cash, D. Narindray, E. Brandeis, W. Adams, H. Weideman, T. Yellin, and D. Regoli
pp 3036 - 3043; DOI:
10.1021/jm00114a012
PDF
Synthesis and antitumor properties of activated cyclophosphamide analogs
Richard F. Borch and Gregory W. Canute
pp 3044 - 3052; DOI:
10.1021/jm00114a013
PDF
Synthesis, activation, and cytotoxicity of aldophosphamide analogs
Richard F. Borch and Ronald R. Valente
pp 3052 - 3058; DOI:
10.1021/jm00114a014
PDF
Synthesis and receptor binding of enantiomeric N-substituted cis-N-[2-(3,4-dichlorophenyl)ethyl]-2-(1-pyrrolidinyl)cyclohexylamines as high-affinity .sigma. receptor ligands
Lilian Radesca, Wayne D. Bowen, Lisa Di Paolo, and Brian R. De Costa
pp 3058 - 3065; DOI:
10.1021/jm00114a015
PDF
Analogs of oxybutynin. Synthesis and antimuscarinic and bladder activity of some substituted 7-amino-1-hydroxy-5-heptyn-2-ones and related compounds
J. Paul Carter, Lalita Noronha-Blob, Vicki H. Audia, Andrea C. Dupont, Daniel W. McPherson, Kenneth J. Natalie, W. Janusz Rzeszotarski, Ciro J. Spagnuolo, Philip P. Waid, and Carl Kaiser
pp 3065 - 3074; DOI:
10.1021/jm00114a016
PDF
3-Methyl-2H-1-benzopyran potassium channel activators
Rolf Gericke, Juergen Harting, Inge Lues, and Christine Schittenhelm
pp 3074 - 3085; DOI:
10.1021/jm00114a017
PDF
Separation of .alpha.1-adrenergic and N-methyl-D-aspartate antagonist activity in a series of ifenprodil compounds
B. L. Chenard, I. A. Shalaby, B. K. Koe, R. T. Ronau, T. W. Butler, M. A. Prochniak, A. W. Schmidt, and C. B. Fox
pp 3085 - 3090; DOI:
10.1021/jm00114a018
PDF
Enantioselective and diastereoselective hydroxylation of bufuralol. Absolute configuration of the 7-(1-hydroxyethyl)-2-[1-hydroxy-2-(tert-butylamino)ethyl]benzofurans, the benzylic hydroxylation metabolites
S. Ananda Weerawarna, Stefan M. Geisshusler, Satya S. Murthy, and Wendel L. Nelson
pp 3091 - 3097; DOI:
10.1021/jm00114a019
PDF
Topically active carbonic anhydrase inhibitors. 4. [(Hydroxyalkyl)sulfonyl]benzene and [(hydroxyalkyl)sulfonyl]thiophenesulfonamides
Kenneth L. Shepard, Samuel L. Graham, Ronald J. Hudcosky, Stuart R. Michelson, Thomas H. Scholz, Harvey Schwam, Anthony M. Smith, John M. Sondey, Kim M. Strohmaier, and et al.
pp 3098 - 3105; DOI:
10.1021/jm00114a020
PDF
Nonpeptidic angiotensin II antagonists: synthesis and in vitro activity of a series of novel naphthalene and tetrahydronaphthalene derivatives
Peter Buehlmayer, Leoluca Criscione, Walter Fuhrer, Pascal Furet, Marc De Gasparo, Stefan Stutz, and Steven Whitebread
pp 3105 - 3114; DOI:
10.1021/jm00114a021
PDF
Development of a small RGD peptide fibrinogen receptor antagonist with potent antiaggregatory activity in vitro
J. Samanen, F. Ali, T. Romoff, R. Calvo, E. Sorenson, J. Vasko, B. Storer, D. Berry, D. Bennett, and et al.
pp 3114 - 3125; DOI:
10.1021/jm00114a022
PDF
Conformational restriction of the phenylalanine residue in a cyclic opioid peptide analog: effects on receptor selectivity and stereospecificity
Peter W. Schiller, Grazyna Weltrowska, Nguyen Thi Mai Dung, Carole Lemieux, Nga N. Chung, Brian J. Marsden, and Brian C. Wilkes
pp 3125 - 3132; DOI:
10.1021/jm00114a023
PDF
Synthesis and evaluation of some nitrobenzenesulfonamides containing nitroisopropyl and (ureidooxy)methyl groups as novel hypoxic cell-selective cytotoxic agents
Walfred S. Saari, John E. Schwering, Paulette A. Lyle, Edward L. Engelhardt, Alan C. Sartorelli, and Sara Rockwell
pp 3132 - 3138; DOI:
10.1021/jm00114a024
PDF
Monovalent sialosides that bind tightly to influenza A virus
Peter L. Toogood, Peter K. Galliker, Gary D. Glick, and Jeremy R. Knowles
pp 3138 - 3140; DOI:
10.1021/jm00114a025
PDF
Peptide to glycopeptide: glycosylated oligopeptide renin inhibitors with attenuated in vivo clearance properties
Jed F. Fisher, Allen W. Harrison, Gordon L. Bundy, Karen F. Wilkinson, Bob D. Rush, and Mary J. Ruwart
pp 3140 - 3143; DOI:
10.1021/jm00114a026
PDF
[123I]-2.beta.-carbomethoxy-3.beta.-(4-iodophenyl)tropane: high-affinity SPECT (single photon emission computed tomography) radiotracer of monoamine reuptake sites in brain
John L. Neumeyer, Shaoyin Wang, Richard A. Milius, Ronald M. Baldwin, Yolanda Zea-Ponce, Paul B. Hoffer, Elzbieta Sybirska, Mohammed Al-Tikriti, Dennis S. Charney, and et al.
pp 3144 - 3146; DOI:
10.1021/jm00114a027
PDF
Book Reviews

pp 3147 - 3148; DOI:
10.1021/jm00114a600
PDF

Issue 11


Structure activity studies related to 2-(3,4-dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted-ethyl]acetamides: a novel series of potent and selective .kappa.-opioid agonists
Jeffrey J. Barlow, Thomas P. Blackburn, Gerard F. Costello, Roger James, David J. Le Count, Brian G. Main, Robert J. Pearce, Keith Russell, and John S. Shaw
pp 3149 - 3158; DOI:
10.1021/jm00115a001
PDF
Novel 1-phenylcycloalkanecarboxylic acid derivatives as potential anticonvulsant agents
Silvia N. Calderon, Amy Hauck Newman, and Frank C. Tortella
pp 3159 - 3164; DOI:
10.1021/jm00115a002
PDF
Synthesis, molecular modeling studies, and muscarinic receptor activity of azaprophen analogs
David J. Triggle, Yong Who Kwon, Philip Abraham, J. Bruce Pitner, S. Wayne Mascarella, and F. I. Carroll
pp 3164 - 3171; DOI:
10.1021/jm00115a003
PDF
Geiparvarin analogs. 2. Synthesis and cytostatic activity of 5-(4-arylbutadienyl)-3(2H)-furanones and of N-substituted 3-(4-oxo-2-furanyl)-2-buten-2-yl carbamates
Daniele Simoni, Stefano Manfredini, Mojgan Aghazadeh Tabrizi, Rita Bazzanini, Pier G. Baraldi, Jan Balzarini, and Erik De Clercq
pp 3172 - 3176; DOI:
10.1021/jm00115a004
PDF
Antimitotic agents. Alterations at the 2,3-positions of ethyl (5-amino-1,2-dihydropyrido[3,4-b]pyrazin-7-yl)carbamates
Carroll Temple, Gregory A. Rener, Robert N. Comber, and William R. Waud
pp 3176 - 3181; DOI:
10.1021/jm00115a005
PDF
Synthesis and biological evaluation of hydroxamate-based iron chelators
Raymond J. Bergeron, Jan Wiegand, James S. McManis, and P. Thirumalai Perumal
pp 3182 - 3187; DOI:
10.1021/jm00115a006
PDF
Synthesis and anti-HIV-1 activity of 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one (TIBO) derivatives. 2
Michael J. Kukla, Henry J. Breslin, Craig J. Diamond, Philip P. Grous, Chih Y. Ho, Milton Miranda, James D. Rodgers, Ronald G. Sherrill, Erik De Clercq, and et al.
pp 3187 - 3197; DOI:
10.1021/jm00115a007
PDF
Synthesis and ocular antihypertensive activity of new imidazolidine derivatives containing a .beta.-blocking side chain
D. Huber, J. D. Ehrhardt, N. Decker, J. Himber, G. Andermann, and G. Leclerc
pp 3197 - 3204; DOI:
10.1021/jm00115a008
PDF
(Aminoalkyl)carbamates of forskolin: intermediates for the synthesis of functionalized derivatives of forskolin with different specificities for adenylyl cyclase and the glucose transporter
Joan D. Robbins, Antonio Laurenza, Raymond W. Kosley, Gerard J. O'Malley, Bettina Spahl, and Kenneth B. Seamon
pp 3204 - 3212; DOI:
10.1021/jm00115a009
PDF
Synthesis and selective class III antiarrhythmic activity of novel N-heteroaralkyl-substituted 1-(aryloxy)-2-propanolamine and related propylamine derivatives
John A. Butera, Walter Spinelli, Viji Anantharaman, Nicholas Marcopulos, Roderick W. Parsons, Issam F. Moubarak, Catherine Cullinan, and Jehan F. Bagli
pp 3212 - 3228; DOI:
10.1021/jm00115a010
PDF
Spiro[fluoreneisothiazolidin]one dioxides: new aldose reductase and L-hexonate dehydrogenase inhibitors
Mark T. DuPriest, Brenda W. Griffin, Daniel Kuzmich, and Loretta G. McNatt
pp 3229 - 3234; DOI:
10.1021/jm00115a011
PDF
Fluorescent probes for dopamine receptors: synthesis and characterization of fluorescein and 7-nitrobenz-2-oxa-1,3-diazol-4-yl conjugates of D-1 and D-2 receptor ligands
Venkatesalu Bakthavachalam, Nandkishore Baindur, Bertha K. Madras, and John L. Neumeyer
pp 3235 - 3241; DOI:
10.1021/jm00115a012
PDF
Complexes of .NO with nucleophiles as agents for the controlled biological release of nitric oxide. Vasorelaxant effects
Chris M. Maragos, Deborah Morley, David A. Wink, Tambra M. Dunams, Joseph E. Saavedra, Aaron Hoffman, Alfred A. Bove, Lawrence Isaac, Joseph A. Hrabie, and Larry K. Keefer
pp 3242 - 3247; DOI:
10.1021/jm00115a013
PDF
Synthesis and structure-activity relationships of a novel series of non-peptide angiotensin II receptor binding inhibitors specific for the AT2 subtype
C. John Blankley, John C. Hodges, Sylvester R. Klutchko, Richard J. Himmelsbach, Alexander Chucholowski, Cleo J. Connolly, Sandra J. Neergaard, Michael S. Van Nieuwenhze, Alan Sebastian, and et al.
pp 3248 - 3260; DOI:
10.1021/jm00115a014
PDF
Synthesis and antihypertensive activity of pyran oxygen and amide nitrogen replacement analogs of the potassium channel activator cromakalim
Valerie A. Ashwood, Frederick Cassidy, John M. Evans, Stefania Gagliardi, and Geoffrey Stemp
pp 3261 - 3267; DOI:
10.1021/jm00115a015
PDF
Substrate analog renin inhibitors containing replacements of histidine in P2 or isosteres of the amide bond between P3 and P2 sites
Peter Raddatz, Alfred Jonczyk, Klaus Otto Minck, Claus Jochen Schmitges, and Jan Sombroek
pp 3267 - 3280; DOI:
10.1021/jm00115a016
PDF
Antitumor properties of 2(1H)-pyrimidinone riboside (zebularine) and its fluorinated analogs
John S. Driscoll, Victor E. Marquez, Jacqueline Plowman, Paul S. Liu, James A. Kelley, and Joseph J. Barchi
pp 3280 - 3284; DOI:
10.1021/jm00115a017
PDF
Synthesis, characterization and myocardial uptake of cationic bis(arene)technetium(I) complexes
Dennis W. Wester, Joseph R. Coveney, Dennis L. Nosco, Mark S. Robbins, and Richard T. Dean
pp 3284 - 3290; DOI:
10.1021/jm00115a018
PDF
Synthesis and evaluation of a series of 3,5-disubstituted benzisoxazole-4,7-diones. Potent radiosensitizers in vitro
Mark J. Suto, Michael A. Stier, R. Thomas Winters, William R. Turner, Cheryl D. Pinter, William E. Elliott, and Judith S. Sebolt-Leopold
pp 3290 - 3294; DOI:
10.1021/jm00115a019
PDF
Synthesis and biological activity of a series of diaryl-substituted .alpha.-cyano-.beta.-hydroxypropenamides, a new class of anthelmintic agents
Eric B. Sjogren, Michael A. Rider, Peter H. Nelson, Stanford Bingham, Anthony L. Poulton, Mark A. Emanuel, and Richard Komuniecki
pp 3295 - 3301; DOI:
10.1021/jm00115a020
PDF
Gossypol and derivatives: a new class of aldose reductase inhibitors
Lorraine M. Deck, David L. Vander Jagt, and Robert E. Royer
pp 3301 - 3305; DOI:
10.1021/jm00115a021
PDF
Activity of acyclic 6-(phenylselenenyl)pyrimidine nucleosides against human immunodeficiency viruses in primary lymphocytes
Naganna M. Goudgaon and Raymond F. Schinazi
pp 3305 - 3309; DOI:
10.1021/jm00115a022
PDF
Synthesis and pharmacological evaluation of ether and related analogs of .DELTA.8-, .DELTA.9-, and .DELTA.9,11-tetrahydrocannabinol
David R. Compton, W. Roy Prescott, Billy R. Martin, Craig Siegel, Patrick M. Gordon, and Raj K. Razdan
pp 3310 - 3316; DOI:
10.1021/jm00115a023
PDF
Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone
Joseph A. Cipollina, Edward H. Ruediger, James S. New, Mary E. Wire, Timothy A. Shepherd, David W. Smith, and Joseph P. Yevich
pp 3316 - 3328; DOI:
10.1021/jm00115a024
PDF
Design of potent linear PAF antagonists
Javier Bartroli, Elena Carceller, Manuel Merlos, Marta Giral, Julian Garcia-Rafanell, and Javier Forn
pp 3328 - 3334; DOI:
10.1021/jm00115a025
PDF
Fluorinated colchicinoids: antitubulin and cytotoxic properties
Israel Ringel, Dena Jaffe, Sara Alerhand, Oliver Boye, Anjum Muzaffar, and Arnold Brossi
pp 3334 - 3338; DOI:
10.1021/jm00115a026
PDF
Antineoplastic agents. 219. Isolation and structure of the cell growth inhibitory constituents from the western Pacific marine sponge Axinella sp
George R. Pettit, Cherry L. Herald, Michael R. Boyd, John E. Leet, Claude Dufresne, Dennis L. Doubek, Jean M. Schmidt, Ronald L. Cerny, John N. A. Hooper, and Klaus C. Rutzler
pp 3339 - 3340; DOI:
10.1021/jm00115a027
PDF
Novel binding mode of highly potent HIV-proteinase inhibitors incorporating the (R)-hydroxyethylamine isostere
Antonin Krohn, Sally Redshaw, Jenny C. Ritchie, Bradford J. Graves, and Marcos H. Hatada
pp 3340 - 3342; DOI:
10.1021/jm00115a028
PDF
Book Reviews

pp 3343 - 3344; DOI:
10.1021/jm00115a600
PDF

Issue 12


Antitumor agents. 120. New 4-substituted benzylamine and benzyl ether derivatives of 4'-O-demethylepipodophyllotoxin as potent inhibitors of human DNA topoisomerase II
Xiao Ming Zhou, Zhe Qing Wang, Jang Yang Chang, Hong Xing Chen, Yung Chi Cheng, and Kuo Hsiung Lee
pp 3346 - 3350; DOI:
10.1021/jm00116a001
PDF
Cholecystokinin (CCK) antagonists: (R)-tryptophan-based hybrid antagonists of high affinity and selectivity for CCK-A receptors
James F. Kerwin, Frank Wagenaar, Hana Kopecka, Chun Wel Lin, Thomas Miller, David Witte, Michael Stashko, and Alex M. Nadzan
pp 3350 - 3359; DOI:
10.1021/jm00116a002
PDF
Novel 1-phenylpiperazine and 4-phenylpiperidine derivatives as high-affinity .sigma. ligands
Richard A. Glennon, Mamoun Y. Yousif, Abd M. Ismaiel, Mahmoud B. El-Ashmawy, J. L. Herndon, James B. Fischer, Alfred C. Server, and Kathleen J. Burke Howie
pp 3360 - 3365; DOI:
10.1021/jm00116a003
PDF
(.+-.)-3-Allyl-6-bromo-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine, a new high affinity D1 dopamine receptor ligand: synthesis and structure-activity relationship
John L. Neumeyer, Nandkishore Baindur, Hyman B. Niznik, H. C. Guan, and Philip Seeman
pp 3366 - 3371; DOI:
10.1021/jm00116a004
PDF
Immunostimulation by a partially modified retro-inverso-tuftsin analog containing Thr1.sum..psi.[NHCO](R,S)Lys2 modification
Antonio S. Verdini, Sergio Silvestri, Cristina Becherucci, Maria G. Longobardi, Luca Parente, Samuele Peppoloni, Mauro Perretti, Piero Pileri, Massimo Pinori, and et al.
pp 3372 - 3379; DOI:
10.1021/jm00116a005
PDF
Molecular mechanics simulations on covalent complexes of mitomycin C and its analogs with left-handed DNA duplexes
Shashidhar N. Rao, Bhashyam S. Iyengar, Timothy P. Wunz, and William A. Remers
pp 3380 - 3388; DOI:
10.1021/jm00116a006
PDF
Activity of N6-substituted 2-chloroadenosines at A1 and A2 adenosine receptors
Robert D. Thompson, Sherrie Secunda, John W. Daly, and Ray A. Olsson
pp 3388 - 3390; DOI:
10.1021/jm00116a007
PDF
Synthesis and antibacterial activities of C-21 functionalized derivatives of (9R)-9-amino-9-deoxoerythromycins A and B
Paul A. Lartey, Shari L. DeNinno, Ramin Faghih, Dwight J. Hardy, Jacob J. Clement, Jacob J. Plattner, and Richard L. Stephens
pp 3390 - 3395; DOI:
10.1021/jm00116a008
PDF
Examination of HIV-1 protease secondary structure specificity using conformationally constrained inhibitors
Michael Kahn, Hiroshi Nakanishi, R. Alan Chrusciel, Dennis Fitzpatrick, and Michael E. Johnson
pp 3395 - 3399; DOI:
10.1021/jm00116a009
PDF
Delineating the pharmacophoric elements of huperzine A: importance of the unsaturated three-carbon bridge to its AChE inhibitory activity
Alan P. Kozikowski, Chris P. Miller, Fumio Yamada, Yuan Ping Pang, Jacqueline H. Miller, Michael McKinney, and Richard G. Ball
pp 3399 - 3402; DOI:
10.1021/jm00116a010
PDF
Novel alkaloids from the tropical plant Ancistrocladus abbreviatus inhibit cell killing by HIV-1 and HIV-2
Kirk P. Manfredi, John W. Blunt, John H. Cardellina, James B. McMahon, Lewis L. Pannell, Gordon M. Cragg, and Michael R. Boyd
pp 3402 - 3405; DOI:
10.1021/jm00116a011
PDF
1,3,8-Trisubstituted xanthines. Effects of substitution pattern upon adenosine receptor A1/A2 affinity [Erratum to document cited in CA114(19):185119j]
Ronald H. Erickson, Roger N. Hiner, Scott W. Feeney, Paul R. Blake, Waclaw J. Rzeszotarski, Rickey P. Hicks, Diane G. Costello, and Mary E. Abreu
pp 3405 - 3405; DOI:
10.1021/jm00116a012
PDF
Synthesis and resolution of (.+-.)-7-chloro-8-hydroxy-1-(3'-iodophenyl)-3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine (TISCH): a high affinity and selective iodinated ligand for CNS D1 dopamine receptor [Erratum to document cited in CA114(13):122017d]
Sumalee Chumpradit, Mei Pung Kung, Jeffrey J. Billings, and Hank F. Kung
pp 3405 - 3405; DOI:
10.1021/jm00116a013
PDF
Stereospecific synthesis of (R)- and (S)-S-adenosyl-1,8-diamino-3-thiooctane, a potent inhibitor of polyamine biosynthesis. Comparison of asymmetric induction vs enantiomeric synthesis [Erratum to document cited in CA115(5):50181y]
Chin Liu and James K. Coward
pp 3406 - 3408; DOI:
10.1021/jm00116a014
PDF
Editorial - The Journal of Medicinal Chemistry Becomes a Biweekly Publication in 1992
Philip S. Portoghese
pp 3345 - 3345; DOI:
10.1021/jm00116a600
PDF
Book Reviews

pp 3408 - 3410; DOI:
10.1021/jm00116a601
PDF