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Volume 27
Main Index

Issue 1


Parasite enzymes as potential targets for antiparasitic chemotherapy
Ching Chung Wang
pp 1 - 9; DOI:
10.1021/jm00367a001
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(E)-2-(3,4-dimethoxyphenyl)-3-fluoroallylamine: a selective, enzyme-activated inhibitor of type B monoamine oxidase
Philippe Bey, John Fozard, Jean Michel Lacoste, Ian A. McDonald, Monique Zreika, and Michael G. Palfreyman
pp 9 - 10; DOI:
10.1021/jm00367a002
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Synthesis and biological activity of 5-fluoro-2',3'-dideoxy-3'-fluorouridine and its 5'-phosphate
Sudhir Ajmera, Ashok R. Bapat, Kathleen Danenberg, and Peter V. Danenberg
pp 11 - 14; DOI:
10.1021/jm00367a003
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Structure-activity relationship study of the inhibition of adrenal cortical 11.beta.-hydroxylase by new metyrapone analogs
Sheryl J. Hays, Michael C. Tobes, David L. Gildersleeve, Donald M. Wieland, and William H. Beierwaltes
pp 15 - 19; DOI:
10.1021/jm00367a004
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Stereochemical considerations and the antiinflammatory activity of 6-amino-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ols and related derivatives
Shing Chun Wong, Sandra Sasso, Howard Jones, and James J. Kaminski
pp 20 - 27; DOI:
10.1021/jm00367a005
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Synthesis, resolution, absolute stereochemistry, and enantioselectivity of 3',4'-dihydroxynomifensine
Penelope A. Dandridge, Carl Kaiser, Martin Brenner, Dimitri Gaitanopoulos, Larry D. Davis, R. Lee Webb, James J. Foley, and Henry M. Sarau
pp 28 - 35; DOI:
10.1021/jm00367a006
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Trypanocidal 1,3-arylene diketone bis(guanylhydrazones). Structure-activity relationships among substituted and heterocyclic analogs
Peter Ulrich and Anthony Cerami
pp 35 - 40; DOI:
10.1021/jm00367a007
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Synthesis and evaluation of a novel series of N,N-dimethylisotryptamines
Richard A. Glennon, John M. Jacyno, R. Young, J. D. McKenney, and David Nelson
pp 41 - 45; DOI:
10.1021/jm00367a008
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8-Hydroxy-2-(alkylamino)tetralins and related compounds as central 5-hydroxytryptamine receptor agonists
Lars Erik Arvidsson, Uli Hacksell, Anette Johansson, J. Lars G. Nilsson, Per Lindberg, Domingo Sanchez, Haakan Wikstroem, Kjell Svensson, Stephan Hjorth, and Arvid Carlsson
pp 45 - 51; DOI:
10.1021/jm00367a009
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Palladium(II)-catalyzed olefin-coupling reactions of kainic acid: effects of substitution on the isopropenyl group on receptor binding
Gregory A. Conway, Joon Sup Park, Linda Maggiora, Mathias P. Mertes, Noemi Galton, and Elias K. Michaelis
pp 52 - 56; DOI:
10.1021/jm00367a010
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Effect of tellurium position on the myocardial uptake of radioiodinated 18-iodotellura-17-octadecenoic acid analogs
F. F. Knapp, P. C. Srivastava, A. P. Callahan, E. B. Cunningham, G. W. Kabalka, and K. A. R. Sastry
pp 57 - 63; DOI:
10.1021/jm00367a011
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Electronic structures of cephalosporins and penicillins. 15. Inductive effect of the 3-position side chain in cephalosporins
Donald B. Boyd
pp 63 - 66; DOI:
10.1021/jm00367a012
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A cannabinoid derived prototypical analgesic
Lawrence S. Melvin, M. Ross Johnson, Charles A. Harbert, George M. Milne, and Albert Weissman
pp 67 - 71; DOI:
10.1021/jm00367a013
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Antiinflammatory activity of 5,6-diaryl-2,3-dihydroimidazo[2,1-b]thiazoles. Isomeric 4-pyridyl and 4-substituted-phenyl derivatives
I. Lantos, P. E. Bender, K. A. Razgaitis, B. M. Sutton, M. J. DiMartino, D. E. Griswold, and D. T. Walz
pp 72 - 75; DOI:
10.1021/jm00367a014
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Structure-activity relationships of phenytoin-like anticonvulsant drugs
Jacques H. Poupaert, Daniel Vandervorst, Pierre Guiot, Mohamed M. M. Moustafa, and Pierre Dumont
pp 76 - 78; DOI:
10.1021/jm00367a015
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Receptor binding sites of hypoglycemic sulfonylureas and related [(acylamino)alkyl]benzoic acids
George R. Brown and Alan J. Foubister
pp 79 - 81; DOI:
10.1021/jm00367a016
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Novel tetracyclic spiropiperidines. 4. Synthesis and pharmacological evaluation of spiro- and 6,7-dihydrospiro[benzo[b]pyrrolo[3,2,1-jk][1,4]benzodiazepine-2H(1H),4'-piperidine]s
Edward J. Glamkowski, James M. Fortunato, Helen H. Ong, Richard C. Allen, Jeffrey C. Wilker, and Harry M. Geyer
pp 81 - 83; DOI:
10.1021/jm00367a017
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2-Acetylpyridine thiosemicarbazones. 8. Derivatives of 1-acetylisoquinoline as potential antimalarial agents
Daniel L. Klayman, John P. Scovill, Joseph Bruce, and Joseph F. Bartosevich
pp 84 - 87; DOI:
10.1021/jm00367a018
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2-Acetylpyridine thiosemicarbazones. 9. Derivatives of 2-acetylpyridine 1-oxide as potential antimalarial agents
John P. Scovill, Daniel L. Klayman, Chris Lambros, George E. Childs, and John D. Notsch
pp 87 - 91; DOI:
10.1021/jm00367a019
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Nucleosides. 129. Synthesis of antiviral nucleosides: 5-alkenyl-1-(2-deoxy-2-fluoro-.beta.-D-arabinofuranosyl)uracils
Kyoichi A. Watanabe, Tsann Long Su, Uri Reichman, Nancy Greenberg, Carlos Lopez, and Jack J. Fox
pp 91 - 94; DOI:
10.1021/jm00367a020
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Synthesis and evaluation of radioiodinated (E)-18-iodo-17-octadecenoic acid as a model iodoalkenyl fatty acid for myocardial imaging
F. F. Knapp, M. M. Goodman, G. W. Kabalka, and K. A. R. Sastry
pp 94 - 97; DOI:
10.1021/jm00367a021
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cis-4-[[[(2-Chloroethyl)nitrosoamino]carbonyl]methylamino]cyclohexanecarboxylic acid, a nitrosourea with latent activity against an experimental solid tumor
Thomas P. Johnston, George S. McCaleb, William C. Rose, and John A. Montgomery
pp 97 - 99; DOI:
10.1021/jm00367a022
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Book Reviews

pp 100 - 102; DOI:
10.1021/jm00367a600
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Issue 2


Design, synthesis, and testing of potential antisickling agents. 3. Ethacrynic acid
Paul E. Kennedy, Franki L. Williams, and Donald J. Abraham
pp 103 - 105; DOI:
10.1021/jm00368a001
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Design, synthesis, and binding characteristics of an opiate receptor mimetic peptide
Willi Kullmann
pp 106 - 115; DOI:
10.1021/jm00368a002
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Replacement of the peptide-backbone amides connecting Tyr-Gly and Gly-Gly in leucine-enkephalin with ketomethylene groups: synthesis and biological activity
Ronald G. Almquist, Cris M. Olsen, Edward T. Uyeno, and Lawrence Toll
pp 115 - 120; DOI:
10.1021/jm00368a003
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Synthesis of 2-(2,3-dihydro-2-oxo-1,3,4-oxadiazol-5-yl) benzo heterocycles. A novel series of orally active antiallergic agents
John H. Musser, Richard E. Brown, Bernard Loev, Kevin Bailey, Howard Jones, Robert Kahen, Fuchih Huang, Atul Khandwala, Mitchell Leibowitz, and et al.
pp 121 - 125; DOI:
10.1021/jm00368a004
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Antiallergic agents. 3. N-(1H-tetrazol-5-yl)-2-pyridinecarboxamides
Yasushi Honma, Kyoji Hanamoto, Tomiki Hashiyama, Yasuo Sekine, Mikio Takeda, Yasutoshi Ono, and Kei Tsuzurahara
pp 125 - 128; DOI:
10.1021/jm00368a005
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Crystallography, quantitative structure-activity relationships, (QSAR) and molecular graphics in a comparative analysis of the inhibition of dihydrofolate reductase from chicken liver and Lactobacillus casei by 4,6-diamino-1,2-dihydro-2,2-dimethyl-1-(substituted-phenyl)-s-triazines
Corwin Hansch, Bruce A. Hathaway, Zongru Guo, Cynthia Dias Selassie, Stephen W. Dietrich, Jeffrey M. Blaney, Robert Langridge, Karl W. Volz, and Bernard T. Kaufman
pp 129 - 143; DOI:
10.1021/jm00368a006
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Inhibition of human dihydrofolate reductase by 4,6-diamino-1,2-dihydro-2,2-dimethyl-1-(substituted-phenyl)-s-triazines. A quantitative structure-activity relationship analysis
Bruce A. Hathaway, Zong Ru Guo, Corwin Hansch, Tavner J. Delcamp, Sandra S. Susten, and James H. Freisheim
pp 144 - 149; DOI:
10.1021/jm00368a007
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Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines
Donald M. Wieland, Thomas J. Mangner, Muthiah N. Inbasekaran, Lawrence E. Brown, and Jiann Long Wu
pp 149 - 155; DOI:
10.1021/jm00368a008
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Synthesis and evaluation of radioiodinated derivatives of 1-azabicyclo[2.2.2]oct-3-yl .alpha.-hydroxy-.alpha.-(4-iodophenyl)-.alpha.-phenylacetate as potential radiopharmaceuticals
W. J. Rzeszotarski, W. C. Eckelman, B. E. Francis, D. A. Simms, R. E. Gibson, E. M. Jagoda, M. P. Grissom, R. R. Eng, J. J. Conklin, and R. C. Reba
pp 156 - 160; DOI:
10.1021/jm00368a009
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Synthesis of 3-hydroxy-2- and -4-pyridone nucleosides as potential antitumor agents
David T. Mao, John S. Driscoll, and Victor E. Marquez
pp 160 - 164; DOI:
10.1021/jm00368a010
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Design, synthesis, and x-ray data of novel potential antipsychotic agents. Substituted 7-phenylquinolizidines: stereospecific, neuroleptic, and antinociceptive properties
Rene Imhof, Emilio Kyburz, and John J. Daly
pp 165 - 175; DOI:
10.1021/jm00368a011
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Synthesis and characterization of N2-(p-n-butylphenyl)-2'-deoxyguanosine and its 5'-triphosphate and their inhibition of HeLa DNA polymerase .alpha.
George E. Wright and Lech W. Dudycz
pp 175 - 181; DOI:
10.1021/jm00368a012
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Quantitative structure-activity relationships of 6-anilinouracils as inhibitors of Bacillus subtilis DNA polymerase III
George E. Wright and Joseph J. Gambino
pp 181 - 185; DOI:
10.1021/jm00368a013
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Resorcinol congeners of dopamine derived from benzocycloheptene and indan
Joseph G. Cannon, Jonathan P. Pease, Richard L. Hamer, Mustafa Ilhan, Ranbir K. Bhatnagar, and John P. Long
pp 186 - 189; DOI:
10.1021/jm00368a014
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Conformationally restricted congeners of dopamine derived from octahydrobenzo[g]quinoline and octahydrobenzo[f]quinoline
Joseph G. Cannon, Richard L. Hamer, Mustafa Ilhan, Ranbir K. Bhatnagar, and John P. Long
pp 190 - 195; DOI:
10.1021/jm00368a015
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Antitumour imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3H)-one, a novel broad-spectrum antitumor agent
Malcolm F. G. Stevens, John A. Hickman, Robert Stone, Neil W. Gibson, Ghouse Unissa Baig, Edward Lunt, and Christopher G. Newton
pp 196 - 201; DOI:
10.1021/jm00368a016
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Synthesis and anticonvulsant activity of some substituted lactams and amides
Wayne J. Brouillette and Gary L. Grunewald
pp 202 - 206; DOI:
10.1021/jm00368a017
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Synthesis of imidazo[1,2-a]pyrazine derivatives with uterine-relaxing, antibronchospastic, and cardiac-stimulating properties
Claire Sablayrolles, Jean Claude Milhavet, Eliane Rechenq, Jean Pierre Chapat, Gerard H. Cros, Maurice Boucard, Jean J. Serrano, and John H. McNeill
pp 206 - 212; DOI:
10.1021/jm00368a018
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Synthesis and antiinflammatory activity of [(cycloalkylmethyl)phenyl]acetic acids and related compounds
Atsusuke Terada, Shunji Naruto, Kazuyuki Wachi, Shigeru Tanaka, Yoshio Iizuka, and Eiichi Misaka
pp 212 - 216; DOI:
10.1021/jm00368a019
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Synthesis and antimicrobial activity of clindamycin analogs: pirlimycin, a potent antibacterial agent
Robert D. Birkenmeyer, Stephen J. Kroll, Charles Lewis, Kurt F. Stern, and Gary E. Zurenko
pp 216 - 223; DOI:
10.1021/jm00368a020
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Studies on 1,2,3,-triazoles. 10. Synthesis and antiallergic properties of 9-oxo-1H,9H-benzothiopyrano[2,3-d]-1,2,3-triazoles and their S-oxides
Derek R. Buckle, Caroline J. M. Rockell, Harry Smith, and Barbara A. Spicer
pp 223 - 227; DOI:
10.1021/jm00368a021
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Design and synthesis of tetrahedral intermediate analogs as potential dihydroorotase inhibitors
Corey H. Levenson and Rich B. Meyer
pp 228 - 232; DOI:
10.1021/jm00368a022
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Improved synthesis and antitumor evaluation of 5,8-dideazaisofolic acid and closely related analogs
J. B. Hynes, Y. C. S. Yang, J. E. McGill, S. J. Harmon, and W. L. Washtien
pp 232 - 235; DOI:
10.1021/jm00368a023
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Novel N-hydroxyguanidine derivatives as anticancer and antiviral agents
Anna W. Tai, Eric J. Lien, Michael M. C. Lai, and Tasneem A. Khwaja
pp 236 - 238; DOI:
10.1021/jm00368a024
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Antileukemic compounds derived by chemical modification of macrocyclic trichothecenes. 2. Derivatives of roridins A and H and verrucarins A and J
Bruce B. Jarvis, Jacob O. Midiwo, and Eugene P. Mazzola
pp 239 - 244; DOI:
10.1021/jm00368a025
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Book Reviews

pp 244 - 246; DOI:
10.1021/jm00368a600
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Issue 3


Dependence of .beta.-lactamase stability on substructures within .beta.-lactam antibiotics
Christopher M. Cimarusti
pp 247 - 253; DOI:
10.1021/jm00369a001
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5-[(Aminoalkyl)amino]-substituted anthra[1,9-cd]pyrazol-6(2H)-ones as novel anticancer agents. Synthesis and biological evaluation
H. D. Hollis Showalter, Judith L. Johnson, Leslie M. Werbel, Wilbur R. Leopold, Robert C. Jackson, and Edward F. Elslager
pp 253 - 255; DOI:
10.1021/jm00369a002
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N-[[5-(Trifluoromethyl)-6-methoxy-1-naphthalenyl]thioxomethyl]-N-methylglycine (Tolrestat), a potent, orally active aldose reductase inhibitor
Kazimir Sestanj, Francesco Bellini, Steven Fung, Nedumparambil Abraham, Adi Treasurywala, Leslie Humber, Nicole Simard-Dequesne, and Dushan Dvornik
pp 255 - 256; DOI:
10.1021/jm00369a003
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Cardiac glycosides. 1. A systematic study of digitoxigenin D-glycosides
Dwight S. Fullerton, Masaru Kihara, Tamboue Deffo, Eitaro Kitatsuji, Khalil Ahmed, Bruce Simat, and Arthur H. L. From
pp 256 - 261; DOI:
10.1021/jm00369a004
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A colon-specific drug-delivery system based on drug glycosides and the glycosidases of colonic bacteria
David R. Friend and George W. Chang
pp 261 - 266; DOI:
10.1021/jm00369a005
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Synthesis and biological activity of nucleosides and nucleotides related to the antitumor agent 2-.beta.-D-ribofuranosylthiazole-4-carboxamide
Prem C. Srivastava, Ganapathi R. Revankar, and Roland K. Robins
pp 266 - 269; DOI:
10.1021/jm00369a006
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Synthesis and evaluation of a series of 2'-O-acyl derivatives of 9-.beta.-D-arabinofuranosyladenine as antiherpes agents
David C. Baker, S. D. Kumar, William J. Waites, Gussie Arnett, William M. Shannon, William I. Higuchi, and W. J. Lambert
pp 270 - 274; DOI:
10.1021/jm00369a007
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Adenosine deaminase inhibitors. Synthesis of deaza analogs of erythro-9-(2-hydroxy-3-nonyl) adenine
Ippolito Antonini, Gloria Cristalli, Palmarisa Franchetti, Mario Grifantini, Sante Martelli, Giulio Lupidi, and Francesca Riva
pp 274 - 278; DOI:
10.1021/jm00369a008
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Synthesis of (E)-5-(3,3,3-trifluoro-1-propenyl)-2'-deoxyuridine and related analogs: potent and unusually selective antiviral activity of (E)-5-(3,3,3-trifluoro-1-propenyl)-2'-deoxyridine against herpes simplex virus type 1
Donald E. Bergstrom, Jerry L. Ruth, P. Anantha Reddy, and Erik De Clercq
pp 279 - 284; DOI:
10.1021/jm00369a009
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Antiviral activity of C-5 substituted tubercidin analogs
Donald E. Bergstrom, Alan J. Brattesani, Mark K. Ogawa, P. Anantha Reddy, Michael J. Schweickert, Jan Balzarini, and Erik De Clercq
pp 285 - 292; DOI:
10.1021/jm00369a010
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1,4-Dihydro-4-oxopyridinecarboxylic acids as antibacterial agents. 2. Synthesis and structure-activity relationships of 1,6,7-trisubstituted 1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acids, including enoxacin, a new antibacterial agent
Junichi Matsumoto, Teruyuki Miyamoto, Akira Minamida, Yoshiro Nishimura, Hiroshi Egawa, and Haruki Nishimura
pp 292 - 301; DOI:
10.1021/jm00369a011
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Structure-activity relationships of sparsomycin and its analogs: octylsparsomycin: The first analog more active than sparsomycin
Rob M. J. Liskamp, J. Hans Colstee, Harry C. J. Ottenheijm, Peter Lelieveld, and Wil Akkerman
pp 301 - 306; DOI:
10.1021/jm00369a012
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Structure-activity relationships among DNA gyrase inhibitors. Synthesis and biological evaluation of 1,2-dihydro-4,4-dimethyl-1-oxo-2-naphthalenecarboxylic acids as 1-carba bioisosteres of oxolinic acid
Thomas Hogberg, Ish Khanna, Steven D. Drake, Lester A. Mitscher, and Linus L. Shen
pp 306 - 310; DOI:
10.1021/jm00369a013
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Structure activity studies on the N-terminal region of glucagon
Javier Sueiras-Diaz, Valentine A. Lance, William A. Murphy, and David H. Coy
pp 310 - 315; DOI:
10.1021/jm00369a014
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Angiotensin II: dependence of hormone affinity on the electronegativity of a single side chain
Gaetan Guillemette, Michel Bernier, Paul Parent, Richard Leduc, and Emanuel Escher
pp 315 - 320; DOI:
10.1021/jm00369a015
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Synthesis of a novel class of heteroaromatic amino acids and their use in the preparation of analogs of luteinizing hormone-releasing hormone
John J. Nestor, Bonnie L. Horner, Teresa L. Ho, Gordon H. Jones, Georgia I. McRae, and Brian H. Vickery
pp 320 - 325; DOI:
10.1021/jm00369a016
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Tri- and tetrapeptide analogs of kinins as potential renal vasodilators
Francis R. Pfeiffer, Pamela A. Chambers, Eileen E. Hilbert, Paul W. Woodward, and Dennis M. Ackerman
pp 325 - 341; DOI:
10.1021/jm00369a017
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Cytochrome P-450 complex formation in the metabolism of phenylalkylamines. 8. Stereoselectivity in metabolic intermediary complex formation with a series of chiral 2-substituted 1-phenyl-2-aminoethanes
Ulla B. Paulsen-Soerman, Karl Henrik Joensson, and Bjoern G. A. Lindeke
pp 342 - 346; DOI:
10.1021/jm00369a018
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Comparative structure-activity relationships of antifolate triazines inhibiting murine tumor cells sensitive and resistant to methotrexate
Cynthia Dias Selassie, Corwin Hansch, Tasneem A. Khwaja, Cecilia B. Dias, and Stephanie Pentecost
pp 347 - 357; DOI:
10.1021/jm00369a019
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Studies of the mode of action of antitumor triazenes and triazines. 6. 1-Aryl-3-(hydroxymethyl)-3-methyltriazenes: synthesis, chemistry, and antitumor properties
Keith Vaughan, York Tang, Gerard Llanos, Julie K. Horton, Richard J. Simmonds, John A. Hickman, and Malcolm F. G. Stevens
pp 357 - 363; DOI:
10.1021/jm00369a020
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Potential antitumor agents. 40. Orally active 4,5-disubstituted derivatives of amsacrine
William A. Denny, Graham J. Atwell, and Bruce C. Baguley
pp 363 - 367; DOI:
10.1021/jm00369a021
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Potential antitumor agents. 41. Analogs of amsacrine with electron-donor substituents in the anilino ring
Graham J. Atwell, Gordon W. Rewcastle, William A. Denny, Bruce F. Cain, and Bruce C. Baguley
pp 367 - 372; DOI:
10.1021/jm00369a022
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Dibenz[b,c]oxepinalkanoic acids as nonsteroidal antiinflammatory agents. 4. Synthesis and evaluation of 4-(4,10-dihydro-10-oxothieno[3,2-c][1]benzoxepin-8-yl)butanol and -butyric acid and related derivatives
Lawrence L. Martin, Linda L. Setescak, Theodore C. Spaulding, and Grover C. Helsley
pp 372 - 376; DOI:
10.1021/jm00369a023
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Synthesis and antifolate properties of 10-alkyl-8,10-dideazaminopterins
J. I. DeGraw, P. H. Christie, E. G. Brown, L. F. Kelly, R. L. Kisliuk, Y. Gaumont, and F. M. Sirotnak
pp 376 - 380; DOI:
10.1021/jm00369a024
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(Imidazolylphenyl)formamidines. A structurally novel class of potent histamine H2 receptor antagonists
Arturo Donetti, Enzo Cereda, Elio Bellora, Alberto Gallazzi, Cesare Bazzano, Piercarlo Vanoni, Piero Del Soldato, Rosamaria Micheletti, Ferdinando Pagani, and Antonio Giachetti
pp 380 - 386; DOI:
10.1021/jm00369a025
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6-Hydroxy-4-[2-di-n-propylaminoethyl]indole: synthesis and dopaminergic actions
Joseph G. Cannon, Teresa Lee, Mustafa Ilhan, Jay Koons, and John Paul Long
pp 386 - 389; DOI:
10.1021/jm00369a026
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Synthesis and evaluation of radioiodinated terminal para-iodophenyl-substituted .alpha.- and .beta.-methyl-branched fatty acids
M. M. Goodman, G. Kirsch, and F. F. Knapp
pp 390 - 397; DOI:
10.1021/jm00369a027
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Phosphorus-nitrogen compounds. 24. Phosphoramide mustard carrier derivatives
Lindley A. Cates, Ven Shun Li, Douglas R. Powell, and Dick Van der Helm
pp 397 - 401; DOI:
10.1021/jm00369a028
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(.+-.)-4-Aryl-4,5-dihydro-3H-1,3-benzodiazepines. 3. 2-Phenyl and 2-amino analogs as potential antihypertensive agents
Linda L. Setescak, Frederick W. Dekow, Jan M. Kitzen, and Lawrence L. Martin
pp 401 - 404; DOI:
10.1021/jm00369a029
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A cyclic angiotensin antagonist: [1,8-cysteine)angiotensin II
John M. Matsoukas, Martin N. Scanlon, and Graham J. Moore
pp 404 - 406; DOI:
10.1021/jm00369a030
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Synthesis of certain hydroxy analogs of the antimalarial drug primaquine and their in vitro methemoglobin-producing and glutathione-depleting activity in human erythrocytes
Reza Allahyari, Allen Strother, Ian M. Fraser, and Anthony J. Verbiscar
pp 407 - 410; DOI:
10.1021/jm00369a031
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Acetylenic nucleosides. Synthesis and biological activities of some 5-ethynylpyrimidine nucleosides
Ram A. Sharma, Ivan Kavai, Robert G. Hughes, and Miroslav Bobek
pp 410 - 412; DOI:
10.1021/jm00369a032
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Nonsteroidal antiinflammatory agents. 14. Synthesis and pharmacological profile of 6-chloro-5-(cyclopentylmethyl)indan-1-carboxylic acid
Irmgard Boettcher, Walter Elger, Gerald Kirsch, Fred Siegmund, and Helmut Wachtel
pp 413 - 414; DOI:
10.1021/jm00369a033
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Book Reviews

pp 415 - 416; DOI:
10.1021/jm00369a600
PDF

Issue 4


Inhibition of aminopeptidases by amastatin and bestatin derivatives. Effect of inhibitor structure on slow-binding processes
Daniel H. Rich, Byung Jo Moon, and Scott Harbeson
pp 417 - 422; DOI:
10.1021/jm00370a001
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Potent and selective antagonists of the antidiuretic responses to arginine-vasopressin based on modifications of [1-(.beta.-mercapto-.beta.,.beta.-pentamethylenepropionic acid), 2-D-isoleucine, 4-valine]arginine-vasopressin at position 4
Maurice Manning, Eleonora Nawrocka, Aleksandra Misicka, Aleksandra Olma, Wieslaw A. Klis, Janny Seto, and Wilbur H. Sawyer
pp 423 - 429; DOI:
10.1021/jm00370a002
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Inhibitors of inosinic acid dehydrogenase. 2-Substituted inosinic acids
Corinne G. Wong and Rich B. Meyer
pp 429 - 432; DOI:
10.1021/jm00370a003
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2,3,4,4a,5,9b-Hexahydro-1H-indeno[1,2-b]pyridines: potential antidepressants
Rudolf Kunstmann, Ulrich Lerch, Hermann Gerhards, Margret Leven, and Ulrich Schacht
pp 432 - 439; DOI:
10.1021/jm00370a004
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Synthesis and biological properties of some cyclic phosphotriesters derived from 2'-deoxy-5-fluorouridine
Roger N. Hunston, A. Stanley Jones, Christopher McGuigan, Richard T. Walker, Jan Balzarini, and Erik De Clercq
pp 440 - 444; DOI:
10.1021/jm00370a005
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Synthesis and antitumor activity of cis-dichloroplatinum(II)-N-aminated nucleoside
Mitsuaki Maeda, Noriko Abiko, Hiroyuki Uchida, and Takuma Sasaki
pp 444 - 449; DOI:
10.1021/jm00370a006
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Interactions of antitumor drugs with natural DNA: proton NMR study of binding mode and kinetics
Juli Feigon, William A. Denny, Werner Leupin, and David R. Kearns
pp 450 - 465; DOI:
10.1021/jm00370a007
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NMR spectroscopic studies of intermediary metabolites of cyclophosphamide. A comprehensive kinetic analysis of the interconversion of cis- and trans-4-hydroxycyclophosphamide with aldophosphamide and the concomitant partitioning of aldophosphamide between irreversible fragmentation and reversible conjugation pathways
Gerald Zon, Susan Marie Ludeman, Joan A. Brandt, Victoria L. Boyd, Gunay Ozkan, William Egan, and Kai Liu Shao
pp 466 - 485; DOI:
10.1021/jm00370a008
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Base-catalyzed hydrolysis of 4-hydroperoxycyclophosphamide: evidence for iminocyclophosphamide as an intermediate
Richard F. Borch and Kathleen M. Getman
pp 485 - 490; DOI:
10.1021/jm00370a009
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In situ preparation and fate of cis-4-hydroxycyclophosphamide and aldophosphamide: proton and phosphorus-31 NMR evidence for equilibration of cis- and trans-4-hydroxycyclophosphamide with aldophosphamide and its hydrate in aqueous solution
Richard F. Borch, Thomas R. Hoye, and Todd A. Swanson
pp 490 - 494; DOI:
10.1021/jm00370a010
PDF
Quantitative relationships between .alpha.-adrenergic activity and binding affinity of .alpha.-adrenoceptor agonists and antagonists
Pieter B. M. W. M. Timmermans, Adriaan De Jonge, Martin J. M. C. Thoolen, Bob Wilffert, Harry Batink, and Pieter A. Van Zwieten
pp 495 - 503; DOI:
10.1021/jm00370a011
PDF
.beta.1-Selective adrenoceptor antagonists. 3. 4-Azolyl linked phenoxypropanolamines
Peter J. Machin, David N. Hurst, Rachel M. Bradshaw, Leslie C. Blaber, David T. Burden, and Rosemary A. Melarange
pp 503 - 509; DOI:
10.1021/jm00370a012
PDF
Synthesis, receptor binding, and target-tissue uptake of carbon-11 labeled carbamate derivatives of estradiol and hexestrol
Rene Ouellet, Jacques Rousseau, Nicole Brasseur, Johan E. Van Lier, Mirko Diksic, and Gerrit Westera
pp 509 - 513; DOI:
10.1021/jm00370a013
PDF
Synthesis and physicochemical and neurotoxicity studies of 1-(4-substituted-2,5-dihydroxyphenyl)-2-aminoethane analogs of 6-hydroxydopamine
Alice C. Cheng and Neal Castagnoli
pp 513 - 520; DOI:
10.1021/jm00370a014
PDF
Analgesics of the orvinol type. 19-Deoxy and 6,20-epoxy derivatives
Charles W. Hutchins and Henry Rapoport
pp 521 - 527; DOI:
10.1021/jm00370a015
PDF
Synthesis and antiallergy activity of 10-oxo-10H-pyrido[1,2-a]thieno[3,2-d]pyrimidines and 10-oxo-10H-pyrido[1,2-a]thieno[3,4-d]pyrimidines
David T. Connor, Roderick J. Sorenson, Wiaczeslaw A. Cetenko, Joseph J. Kerbleski, and Francis J. Tinney
pp 528 - 530; DOI:
10.1021/jm00370a016
PDF
8-Methoxypsoralen-nucleic acid photoreaction. Effect of methyl substitution on pyrone vs. furan photoaddition
David Kanne, Henry Rapoport, and John E. Hearst
pp 531 - 534; DOI:
10.1021/jm00370a017
PDF
(.+-.)-3-(4-Amino-1H-pyrrolo[2,3-d]pyrimidin-1-yl)-5-(hydroxymethyl)-(1.alpha.,2.alpha.,3.beta.,5.beta.)-1,2-cyclopentanediol, the carbocyclic analog of tubercidin
John A. Secrist, Sarah Jo Clayton, and John A. Montgomery
pp 534 - 536; DOI:
10.1021/jm00370a018
PDF
Racemic and optically active 2,9-dimethyl-5-(m-hydroxyphenyl)morphans and pharmacological comparison with the 9-demethyl homologs
Hiroyoshi Awaya, Everette L. May, Mario D. Aceto, Herbert Merz, Michael E. Rogers, and Louis S. Harris
pp 536 - 539; DOI:
10.1021/jm00370a019
PDF
Studies on heterocyclic compounds. 6. Synthesis and analgesic and antiinflammatory activities of 3,4-dimethylpyrano[2,3-c]pyrazol-6-one derivatives
Sheng Chu Kuo, Li Jiau Huang, and Hideo Nakamura
pp 539 - 544; DOI:
10.1021/jm00370a020
PDF
Synthesis and biological activity of structural analogs of the anticancer benzophenanthridine alkaloid nitidine chloride
Mark Cushman, Prem Mohan, and Edward C. R. Smith
pp 544 - 547; DOI:
10.1021/jm00370a021
PDF
Synthesis and antitumor activity of some aromatic selenolactones
W. C. Groutas, M. C. Theodorakis, W. A. F. Tomkins, G. Herro, and T. Gaynor
pp 548 - 550; DOI:
10.1021/jm00370a022
PDF
Synthesis and pharmacological activity of some 9-substituted .DELTA.8-tetrahydrocannabinol (THC) analogs
Lauri R. Robertson, Richard P. Duffley, Raj K. Razdan, Billy R. Martin, Louis S. Harris, and William L. Dewey
pp 550 - 552; DOI:
10.1021/jm00370a023
PDF
Book Reviews

pp 553 - 556; DOI:
10.1021/jm00370a600
PDF

Issue 5


Drug design by the method of receptor fit
Peter J. Goodford
pp 557 - 564; DOI:
10.1021/jm00371a001
PDF
Biomimetic approach to potential benzodiazepine receptor agonists and antagonists
Filadelfo Guzman, Michael Cain, Paul Larscheid, Tim Hagen, James M. Cook, Margaret Schweri, Phil Skolnick, and Steven M. Paul
pp 564 - 570; DOI:
10.1021/jm00371a002
PDF
.alpha.-Adrenoceptor reagents. 2. Effects of modification of the 1,4-benzodioxan ring system on .alpha.-adrenoreceptor activity
Christopher B. Chapleo, Peter L. Myers, Richard C. M. Butler, John A. Davis, John C. Doxey, Stanley D. Higgins, Malcolm Myers, Alan G. Roach, Colin F. C. Smith, and et al.
pp 570 - 576; DOI:
10.1021/jm00371a003
PDF
Ring-substituted 1,2-dialkylated 1,2-bis(hydroxyphenyl)ethanes. 2. Synthesis and estrogen receptor binding affinity of 4,4'-, 5,5'-, and 6,6'-disubstituted metahexestrols
Rolf W. Hartmann, Aledander Heindl, and Helmut Schoenenberger
pp 577 - 585; DOI:
10.1021/jm00371a004
PDF
Ibotenic acid analogs. Synthesis and biological and in vitro activity of conformationally restricted agonists at central excitatory amino acid receptors
Povl Krogsgaard-Larsen, Elsebet O. Nielsen, and David R. Curtis
pp 585 - 591; DOI:
10.1021/jm00371a005
PDF
2-Substituted thiazolidine-4(R)-carboxylic acids as prodrugs of L-cysteine. Protection of mice against acetaminophen hepatotoxicity
Herbert T. Nagasawa, David J. W. Goon, William P. Muldoon, and Richard T. Zera
pp 591 - 596; DOI:
10.1021/jm00371a006
PDF
Synthesis of pyridine derivatives of L-phenylalanine as antisickling reagents
Janina Altman, Marian Gorecki, Meir Wilchek, Joseph R. Votano, and Alexander Rich
pp 596 - 600; DOI:
10.1021/jm00371a007
PDF
Methotrexate analogs. 19. Replacement of the glutamate side-chain in classical antifolates by L-homocysteic acid and L-cysteic acid: effect on enzyme inhibition and antitumor activity
Andre Rosowsky, Ronald A. Forsch, James H. Freisheim, Richard G. Moran, and Michael Wick
pp 600 - 604; DOI:
10.1021/jm00371a008
PDF
Methotrexate analogs. 21. Divergent influence of alkyl chain length on the dihydrofolate reductase affinity and cytotoxicity of methotrexate monoesters
Andre Rosowsky, Ronald A. Forsch, Cheng Sein Yu, Herbert Lazarus, and G. Peter Beardsley
pp 605 - 609; DOI:
10.1021/jm00371a009
PDF
3-Alkyl-2-aryl-3H-naphth[1,2-d]imidazoles, a novel class of nonacidic antiinflammatory agents
Emilio Toja, Domenica Selva, and Pierfranco Schiatti
pp 610 - 616; DOI:
10.1021/jm00371a010
PDF
Synthesis and central nervous system properties of 2-[(alkoxycarbonyl)amino]-4(5)-phenyl-2-imidazolines
Klaus Weinhardt, Colin C. Beard, Charles Dvorak, Michael Marx, John Patterson, Adolph Roszkowski, Margery Schuler, Stefan H. Unger, Paul J. Wagner, and Marshall B. Wallach
pp 616 - 627; DOI:
10.1021/jm00371a011
PDF
5-Aryl-3-azabicyclo[3.2.0]heptan-5-one ketals, compounds with morphine-like analgesic activity
Thomas C. McKenzie, Joseph W. Epstein, William J. Fanshawe, J. Scott Dixon, Arnold C. Osterberg, Lawrence P. Wennogle, Barbara A. Regan, Marc S. Abel, and Laurence R. Meyerson
pp 628 - 632; DOI:
10.1021/jm00371a012
PDF
Novel opiates and antagonists. 6. 7-Alkyl-6,7-didehydromorphinans
James Quick, Patricia Herlihy, and John F. Howes
pp 632 - 637; DOI:
10.1021/jm00371a013
PDF
Intensely potent morpholinyl anthracyclines
Edward M. Acton, George L. Tong, Carol W. Mosher, and Richard L. Wolgemuth
pp 638 - 645; DOI:
10.1021/jm00371a014
PDF
Substituted (.omega.-aminoalkoxy)stilbene derivatives as a new class of anticonvulsants
Ryoji Kikumoto, Akihiro Tobe, Harukazu Fukami, Kunihiro Ninomiya, and Mitsuo Egawa
pp 645 - 649; DOI:
10.1021/jm00371a015
PDF
Cyheptamide and 3-hydroxy-3-phenacyloxindole structural similarity to diphenylhydantoin as the basis for anticonvulsant activity
Penelope W. Codding, Tamara A. Lee, and John F. Richardson
pp 649 - 654; DOI:
10.1021/jm00371a016
PDF
Phosphorus analogs of .gamma.-aminobutyric acid, a new class of anticonvulsants
Lindley A. Cates, Ven Shun Li, Chriss C. Yakshe, Michael O. Fadeyi, Terrance H. Andree, Edward W. Karbon, and Salvatore J. Enna
pp 654 - 659; DOI:
10.1021/jm00371a017
PDF
.gamma.-Aminobutyric acid esters. I. Synthesis, brain uptake, and pharmacological studies of aliphatic and steroid esters of .gamma.-aminobutyric acid
Victor E. Shashoua, James N. Jacob, Richard Ridge, Alexander Campbell, and Ross J. Baldessarini
pp 659 - 664; DOI:
10.1021/jm00371a018
PDF
2-Chloroethyl (methylsulfonyl)methanesulfonate and related (methylsulfonyl)methanesulfonates. Antineoplastic activity in vivo
Y. Fulmer Shealy, Charles A. Krauth, and W. Russell Laster
pp 664 - 670; DOI:
10.1021/jm00371a019
PDF
Synthesis and antiviral evaluation of carbocyclic analogs of ribofuranosides of 2-amino-6-substituted-purines and of 2-amino-6-substituted-8-azapurines
Y. Fulmer Shealy, Joe D. Clayton, Gussie Arnett, and William M. Shannon
pp 670 - 674; DOI:
10.1021/jm00371a020
PDF
Dopaminergic agonists: comparative actions of amine and sulfonium analogs of dopamine
Akihiko Hamada, Yu An Chang, Norman Uretsky, and Duane D. Miller
pp 675 - 680; DOI:
10.1021/jm00371a021
PDF
Potential inhibitors of nucleotide biosynthesis. 2. Halomethyl ketone derivatives of pyrimidine nucleosides
John A. Montgomery, H. Jeanette Thomas, R. Wallace Brockman, and Robert D. Elliott
pp 680 - 684; DOI:
10.1021/jm00371a022
PDF
Amnesia-reversal activity of a series of N-[(disubstituted-amino)alkyl]-2-oxo-1-pyrrolidineacetamides, including pramiracetam
Donald E. Butler, Ivan C. Nordin, Yvon J. L'Italien, Lynette Zweisler, Paul H. Poschel, and John G. Marriott
pp 684 - 691; DOI:
10.1021/jm00371a023
PDF
Synthesis of some phosphonates with antiherpetic activity
G. D. Diana, E. S. Zalay, U. J. Salvador, F. Pancic, and B. Steinberg
pp 691 - 694; DOI:
10.1021/jm00371a024
PDF
Substituent effects on reactivity and spectral parameters of cephalosporins
Bernard Coene, Andre Schanck, Jean Marie Dereppe, and Maurice Van Meerssche
pp 694 - 700; DOI:
10.1021/jm00371a025
PDF
Mitomycin C analogs with aryl substituents on the 7-amino group
Salah M. Sami, Bhashyam S. Iyengar, Shirley E. Tarnow, William A. Remers, William T. Bradner, and John E. Schurig
pp 701 - 708; DOI:
10.1021/jm00371a026
PDF
Book Reviews

pp 708 - 710; DOI:
10.1021/jm00371a600
PDF

Issue 6


Vinylogous amino acid esters: a new class of inactivators for thiol proteases
Robert P. Hanzlik and Stewart A. Thompson
pp 711 - 712; DOI:
10.1021/jm00372a001
PDF
3-Hydroxy-.alpha.-methyltyrosine progenitors, synthesis and evaluation of some (2-oxo-1,3-dioxol-4-yl)methyl esters
Walfred S. Saari, Wasyl Halczenko, David W. Cochran, Michael R. Dobrinska, William C. Vincek, David C. Titus, S. Lee Gaul, and Charles S. Sweet
pp 713 - 717; DOI:
10.1021/jm00372a002
PDF
Inhibition of arabinose 5-phosphate isomerase. An approach to the inhibition of bacterial lipopolysaccharide biosynthesis
Eric C. Bigham, Charles E. Gragg, William R. Hall, John E. Kelsey, William R. Mallory, Drew C. Richardson, Charles Benedict, and Paul H. Ray
pp 717 - 726; DOI:
10.1021/jm00372a003
PDF
Oligonucleotide structural parameters that influence binding of 5'-O-triphosphoadenylyl-(2' .fwdarw. 5')-adenylyl-(2' .fwdarw. 5')-adenosine to the 5'-O-triphosphoadenylyl-(2' .fwdarw. 5')-adenylyl-(2' .fwdarw. 5')-adenosine dependent endoribonuclease: chain length, phosphorylation state, and heterocyclic base
Paul F. Torrence, Jiro Imai, Krystyna Lesiak, Jean Claude Jamoulle, and Hiroaki Sawai
pp 726 - 733; DOI:
10.1021/jm00372a004
PDF
Synthesis and evaluation of 19-aza- and 19-aminoandrostenedione analogs as potential aromatase inhibitors
Jane A. Lovett, Michael V. Darby, and Raymond E. Counsell
pp 734 - 740; DOI:
10.1021/jm00372a005
PDF
Synthesis of thyrotropin-releasing hormone analogs. 1. Complete dissociation of central nervous system effects from thyrotropin-releasing activity
Tamas Szirtes, Lajos Kisfaludy, Eva Palosi, and Laszlo Szporny
pp 741 - 745; DOI:
10.1021/jm00372a006
PDF
Bile acids with a cyclopropyl-containing side chain. 1. Preparation and properties of 3.alpha.,7.beta.-dihydroxy-22,23-methylene-5.beta.-cholan-24-oic acid
Roberto Pellicciari, Sergio Cecchetti, Benedetto Natalini, Aldo Roda, Brunella Grigolo, and Adamo Fini
pp 746 - 749; DOI:
10.1021/jm00372a007
PDF
Formation of a reactive iminium derivative by enzymatic and chemical oxidations of 16-O-acetylvindoline
F. Sima Sariaslani, Frances M. Eckenrode, John M. Beale, and John P. Rosazza
pp 749 - 754; DOI:
10.1021/jm00372a008
PDF
Acetylation of some novel hemicholinium compounds by soluble choline acetyltransferase: structure-activity relationships
S. Martin Shreeve, G. B. A. Veitch, and Brian A. Hemsworth
pp 754 - 757; DOI:
10.1021/jm00372a009
PDF
Synthesis, conformational analysis, and antiarrhythmic properties of 7-benzyl-3-thia-7-azabicyclo[3.3.1]nonan-9-one, 7-benzyl-3-thia-7-azabicyclo[3.3.1]nonane hydroperchlorate, and 7-benzyl-9-phenyl-3-thia-7-azabicyclo[3.3.1]nonan-9-ol hydroperchlorate and derivatives. Single-crystal x-ray diffraction analysis and evidence for chair-chair and chair-boat conformers in the solid state
Bruce R. Bailey, K. Darrell Berlin, Elizabeth M. Holt, Benjamin J. Scherlag, Ralph Lazzara, Johannes Brachmann, Dick Van der Helm, Douglas R. Powell, Nantelle S. Pantaleo, and Peter C. Ruenitz
pp 758 - 767; DOI:
10.1021/jm00372a010
PDF
Hypolipidemic activity of phthalimide derivatives. 7. Structure-activity studies of indazolone analogs
Steven D. Wyrick, P. Josee Voorstad, George Cocolas, and Iris H. Hall
pp 768 - 772; DOI:
10.1021/jm00372a011
PDF
Synthesis of previously inaccessible quinazolines and 1,4-benzodiazepines as potential anticonvulsants
Aqeel A. Fatmi, Niteen A. Vaidya, W. B. Iturrian, and C. DeWitt Blanton
pp 772 - 778; DOI:
10.1021/jm00372a012
PDF
Anticonvulsant activity of some 4-aminobenzamides
C. Randall Clark, Martha J. M. Wells, Ricky T. Sansom, George N. Norris, Randy C. Dockens, and William R. Ravis
pp 779 - 782; DOI:
10.1021/jm00372a013
PDF
In the search for new anticancer drugs. 9. Synthesis and anticancer activity of spin-labeled analogs of N,N:N',N':N",N"-tris(1,2-ethanediyl)phosphoric triamide and N,N:N',N':N",N"-tris(1,2-ethanediyl)phosphorothioic triamide
George Sosnovsky and Buddha D. Paul
pp 782 - 788; DOI:
10.1021/jm00372a014
PDF
Substituent branching in phenethylamine-type hallucinogens: a comparison of 1-[2,5-dimethoxy-4-(2-butyl)phenyl]-2-aminopropane and 1-[2,5-dimethoxy-4-(2-methylpropyl)phenyl]-2-aminopropane
Robert A. Oberlender, Paresh J. Kothari, David E. Nichols, and Joseph E. Zabik
pp 788 - 792; DOI:
10.1021/jm00372a015
PDF
Synthesis of a novel series of (aryloxy)propanolamines: new selective .beta.2-blocking agents
Marie Christiane Carre, Alphonse Youlassani, and Paul Caubere
pp 792 - 799; DOI:
10.1021/jm00372a016
PDF
Improved synthesis and antitumor activity of 2-bromo-2'-deoxyadenosine
Minchi Huang, Thomas L. Avery, Raymond L. Blakeley, John A. Secrist, and John A. Montgomery
pp 800 - 802; DOI:
10.1021/jm00372a017
PDF
Synthesis and biological evaluation of radiolabeled .beta.-ruthenocenylalanine
William H. Soine, Clarence E. Guyer, and Furn F. Knapp
pp 803 - 806; DOI:
10.1021/jm00372a018
PDF
Aporphines. 58. N-(2-Chloroethyl)[8,9-2H]norapomorphine, an irreversible ligand for dopamine receptors: synthesis and application
Ji Hua Guan, John L. Neumeyer, Crist N. Filer, David G. Ahern, Leslie Lilly, Masayuki Watanabe, Dimitri Grigoriadis, and Philip Seeman
pp 806 - 810; DOI:
10.1021/jm00372a019
PDF
Topical carbonic anhydrase inhibitors
Ronald D. Schoenwald, Mark G. Eller, John A. Dixson, and Charles F. Barfknecht
pp 810 - 812; DOI:
10.1021/jm00372a020
PDF
2,3-Dimethyl-1,4-naphthoquinone derivatives as bioreductive alkylating agents with crosslinking potential
Tai Shun Lin, Ippolito Antonini, Lucille A. Cosby, and Alan C. Sartorelli
pp 813 - 815; DOI:
10.1021/jm00372a021
PDF
Bicyclic lactam inhibitors of angiotensin converting enzyme
Jeffrey W. H. Watthey, Terrence Gavin, and Mahesh Desai
pp 816 - 818; DOI:
10.1021/jm00372a022
PDF
Book Reviews

pp 818 - 818; DOI:
10.1021/jm00372a600
PDF

Issue 7


Ring-substituted 1,2-dialkylated 1,2-bis(hydroxyphenyl)ethanes. 3. Synthesis, estrogen receptor binding affinity, and evaluation of antiestrogenic and mammary tumor inhibiting activity of 2,2'-disubstituted butestrols and 6,6'-disubstituted metabutestrols
Rolf W. Hartmann, Alexander Heindl, Walter Schwarz, and Helmut Schoenenberger
pp 819 - 824; DOI:
10.1021/jm00373a001
PDF
Structural correlations of choline acetyltransferase inhibitors: trans-N-(carboxymethyl)-4-(.beta.-1-naphthylvinyl)pyridinium bromide and cis-N-(2-aminoethyl)-4-(.beta.-1-naphthylvinyl)-3-methylpyridinium bromide hydrobromide
Andrew Y. Chweh, John F. DeBernardis, Jerome F. Siuda, Nelson G. Rondan, Jaime E. Abola, and Donald J. Abraham
pp 825 - 830; DOI:
10.1021/jm00373a002
PDF
.beta.-Adrenergic blocking agents: substituted phenylalkanolamines. Effect of side-chain length on .beta.-blocking potency in vitro
Walter Fuhrer, Franz Ostermayer, Markus Zimmermann, Max Meier, and Hedi Mueller
pp 831 - 836; DOI:
10.1021/jm00373a003
PDF
A photoaffinity reagent to label the opiate receptors of guinea pig ileum and mouse vas deferens
Toshiyuki Fujioka, Tohru Matsunaga, Hitoshi Nakayama, Yuichi Kanaoka, Yujiro Hayashi, Kenji Kangawa, and Hisayuki Matsuo
pp 836 - 840; DOI:
10.1021/jm00373a004
PDF
(Acylaryloxy)acetic acid diuretics. 5. [(2-Alkyl- and 2,2-disubstituted-1,3-dioxo-5-indanyl)oxy]acetic acids
O. W. Woltersdorf, S. J. DeSolms, G. E. Stokker, and E. J. Cragoe
pp 840 - 845; DOI:
10.1021/jm00373a005
PDF
Synthesis of potent heptapeptide analogs of cholecystokinin
Botond Penke, Ferenc Hajnal, Janos Lonovics, Gabor Holzinger, Tibor Kadar, Gyula Telegdy, and Jean Rivier
pp 845 - 849; DOI:
10.1021/jm00373a006
PDF
Histamine H2 receptor antagonists. 1. Synthesis of N-cyano and N-carbamoyl amidine derivatives and their biological activities
Isao Yanagisawa, Yasufumi Hirata, and Yoshio Ishii
pp 849 - 857; DOI:
10.1021/jm00373a007
PDF
3,4-Catechol derivative of propranolol, a minor dihydroxylated metabolite
Wendel L. Nelson, Michael J. Bartels, Patrick J. Bednarski, Shoufang Zhang, Karen Messick, J. S. Horng, and Robert R. Ruffolo
pp 857 - 861; DOI:
10.1021/jm00373a008
PDF
Synthesis, characterization, and properties, of a group of platinum(IV) complexes
Robert J. Brandon and James C. Dabrowiak
pp 861 - 865; DOI:
10.1021/jm00373a009
PDF
Identification of an acridine photoaffinity probe for trypanocidal action
William J. Firth, Andrew Messa, Robert Reid, Rung Chou Wang, Charles L. Watkins, and Lerena W. Yielding
pp 865 - 870; DOI:
10.1021/jm00373a010
PDF
Tumor inhibitory triazenes. 3. Dealkylation within an homologous series and its relation to antitumor activity
Derry E. V. Wilman, Peter J. Cox, Phyllis M. Goddard, Leigh I. Hart, Kanti Merai, and David R. Newell
pp 870 - 874; DOI:
10.1021/jm00373a011
PDF
Troponoids. 6. Troponylpiperazines: a new class of dopamine agonists
Jehan Bagli, T. Bogri, and Katherine Voith
pp 875 - 881; DOI:
10.1021/jm00373a012
PDF
Sulfur analogs of psychotomimetic agents. 30. Ethyl homologs of mescaline and their monothioanalogs
Peyton Jacob and Alexander T. Shulgin
pp 881 - 888; DOI:
10.1021/jm00373a013
PDF
Methotrexate analogs. 22. Synthesis, dihydrofolate reductase affinity, cytotoxicity, and in vivo antitumor activity of some putative degradation products of methotrexate-poly(L-lysine) conjugates
Andre Rosowsky, Ronald A. Forsch, James H. Freisheim, John Galivan, and Michael Wick
pp 888 - 893; DOI:
10.1021/jm00373a014
PDF
Antimycotic azoles. 7. Synthesis and antifungal properties of a series of novel triazol-3-ones
J. Heeres, L. J. J. Backx, and J. Van Cutsem
pp 894 - 900; DOI:
10.1021/jm00373a015
PDF
A general distance-geometry three-dimensional receptor model for diverse dihydrofolate reductase inhibitors
Arup K. Ghose and Gordon M. Crippen
pp 901 - 914; DOI:
10.1021/jm00373a016
PDF
Synthesis of potential antifilarial agents. 1. 1-(5-Benzoylbenzimidazol-2-yl)-3-alkyl and aryl ureas
Siya Ram, Mike Skinner, Doug Kalvin, Dean S. Wise, Leroy B. Townsend, John W. McCall, Don Worth, Don Ortwine, and Leslie M. Werbel
pp 914 - 917; DOI:
10.1021/jm00373a017
PDF
Development of an affinity ligand for purification of .alpha.2-adrenoceptors from human platelet membranes
R. M. DeMarinis, A. J. Krog, D. H. Shah, J. Lafferty, K. G. Holden, J. P. Hieble, W. D. Matthews, J. W. Regan, R. J. Lefkowitz, and M. G. Caron
pp 918 - 921; DOI:
10.1021/jm00373a018
PDF
Catechol derivatives of 6-aminobenzocycloheptene: assessment of dopaminergic effects
Joseph G. Cannon, Jonathan P. Pease, John Paul Long, and Jan Flynn
pp 922 - 923; DOI:
10.1021/jm00373a019
PDF
Biological activity and a modified synthesis of 8-amino-3-.beta.-D-ribofuranosyl-1,2,4-triazolo[4,3-.alpha.]pyrazine, an isomer of formycin
Stewart W. Schneller, Robert D. Thompson, Joseph G. Cory, Ray A. Olsson, Erik De Clercq, In Kyung Kim, and Peter K. Chiang
pp 924 - 928; DOI:
10.1021/jm00373a020
PDF
Steroidogenesis inhibitors. 1. Adrenal inhibitory and interceptive activity of trilostane and related compounds
Rokbert G. Christiansen, Helmut C. Neumann, U. Joseph Salvador, Malcolm R. Bell, H. Philip Schane, John E. Creange, Gordon O. Potts, and A. J. Anzalone
pp 928 - 931; DOI:
10.1021/jm00373a021
PDF
Book Reviews

pp 931 - 942; DOI:
10.1021/jm00373a600
PDF

Issue 8


Pyrroloisoquinoline antidepressants. Potent, enantioselective inhibition of tetrabenazine-induced ptosis and neuronal uptake of norepinephrine, dopamine, and serotonin
Bruce E. Maryanoff, David F. McComsey, Michael J. Costanzo, Paulette E. Setler, Joseph F. Gardocki, Richard P. Shank, and Craig R. Schneider
pp 943 - 946; DOI:
10.1021/jm00374a001
PDF
Synthetic CNS agents. 1. (.+-.)-1,2,3,4,4a,5,10,10a-Octahydro-5,10[1',2']-benzenobenz[g]isoquinoline hydrochloride. A new, highly potent, potential antidepressant
P. Rajagopalan
pp 946 - 947; DOI:
10.1021/jm00374a002
PDF
Preparation and antibacterial activities of new 1,2,3-diazaborine derivatives and analogs
Maximilian A. Grassberger, Friederike Turnowsky, and Johannes Hildebrandt
pp 947 - 953; DOI:
10.1021/jm00374a003
PDF
Synthesis and biological activity of a new class of cytotoxic agents: N-(3-oxoprop-1-enyl)-substituted pyrimidines and purines
Francis Johnson, K. M. R. Pillai, Arthur P. Grollman, Lucy Tseng, and Masaru Takeshita
pp 954 - 958; DOI:
10.1021/jm00374a004
PDF
6-Methylangelicins: a new series of potential photochemotherapeutic agents for the treatment of psoriasis
A. Guiotto, P. Rodighiero, P. Manzini, G. Pastorini, F. Bordin, F. Baccichetti, F. Carlassare, D. Vedaldi, and F. Dall'Acqua
pp 959 - 967; DOI:
10.1021/jm00374a005
PDF
Design, synthesis, and testing of potential antisickling agents. 4. Structure-activity relationships of benzyloxy and phenoxy acids
D. J. Abraham, P. E. Kennedy, A. S. Mehanna, D. C. Patwa, and F. L. Williams
pp 967 - 978; DOI:
10.1021/jm00374a006
PDF
[(E)-1-[123I]Iodo-1-penten-5-yl]triphenylphosphonium iodide: convenient preparation of a potentially useful myocardial perfusion agent
P. C. Srivastava and F. F. Knapp
pp 978 - 981; DOI:
10.1021/jm00374a007
PDF
Isomeric N-methyl-7-deazaguanines: synthesis, structural assignment, and inhibitory activity on xanthine oxidase
Frank Seela, Werner Bussmann, Andreas Goetze, and Helmut Rosemeyer
pp 981 - 985; DOI:
10.1021/jm00374a008
PDF
Pyrazolo[4,3-d]pyrimidine nucleosides. Synthesis and antiviral activity of 1-.beta.-D-ribofuranosyl-3-methyl-6-substituted-7H-pyrazolo[4,3-d]pyrimidin-7-ones
Pier Giovanni Baraldi, Daniele Simoni, Vittorio Periotto, Stefano Manfredini, Mario Guarneri, Roberto Manservigi, and Enzo Cassai
pp 986 - 990; DOI:
10.1021/jm00374a009
PDF
.beta.-Lapachone: synthesis of derivatives and activities in tumor models
Karl Schaffner-Sabba, Karl H. Schmidt-Ruppin, Walter Wehrli, Alfred R. Schuerch, and Jan W. F. Wasley
pp 990 - 994; DOI:
10.1021/jm00374a010
PDF
cis-1,3,4,6,7,11b-Hexahydro-2-methyl-7-phenyl-2H-pyrazino[2,1-a]isoquinoline: a new atypical antidepressant
Ronald C. Griffith, Robert J. Gentile, Roger C. Robichaud, and Jerry Frankenheim
pp 995 - 1003; DOI:
10.1021/jm00374a011
PDF
C1-Methylated 5-hydroxy-2-(dipropylamino)tetralins: central dopamine-receptor stimulating activity
Uli Hacksell, Anette M. Johansson, Lars Erik Arvidsson, J. Lars G. Nilsson, Stephan Hjorth, Arvid Carlsson, Hakan Wikstroem, Domingo Sanchez, and Per Lindberg
pp 1003 - 1007; DOI:
10.1021/jm00374a012
PDF
[(Arylcarbonyl)oxy]propanolamines. 1. Novel .beta.-blockers with ultrashort duration of action
Sheung Tsam Kam, William L. Matier, Khuong X. Mai, Cynthia Barcelon-Yang, Robert J. Borgman, John P. O'Donnell, Herman F. Stampfli, Check Y. Sum, William G. Anderson, and et al.
pp 1007 - 1016; DOI:
10.1021/jm00374a013
PDF
Substituted 5,6-dihydrofuro[3,2-f]-1,2-benzisoxazole-6-carboxylic acids: high-ceiling diuretics with uricosuric activity
Jacob J. Plattner, Anthony K. L. Fung, James A. Parks, Richard J. Pariza, Steven R. Crowley, Andre G. Pernet, Paul R. Bunnell, and Patrick W. Dodge
pp 1016 - 1026; DOI:
10.1021/jm00374a014
PDF
Synthesis and antiviral/antitumor activities of certain pyrazolo[3,4-d]pyrimidine-4(5H)-selone nucleosides and related compounds
Bheemarao G. Ugarkar, Howard B. Cottam, Patricia A. McKernan, Roland K. Robins, and Ganapathi R. Revankar
pp 1026 - 1030; DOI:
10.1021/jm00374a015
PDF
Resolved 3-(3-Hydroxyphenyl)-N-n-propylpiperidine and its analogs: central dopamine receptor activity
Haakan Wikstroem, Domingo Sanchez, Per Lindberg, Uli Hacksell, Lars Erik Arvidsson, Anette M. Johnsson, Seth Olof Thorberg, J. Lars G. Nilsson, and Kjell Svensson
pp 1030 - 1036; DOI:
10.1021/jm00374a016
PDF
Selective delivery of cytotoxic compounds to cells by the LDL pathway
Raymond A. Firestone, Judith M. Pisano, J. R. Falck, Michael M. McPhaul, and Monty Krieger
pp 1037 - 1043; DOI:
10.1021/jm00374a017
PDF
A reappraisal of the effect upon thymidine kinase of thymidine derivatives carrying large groups at the 5'-position
S. Elaine Barrie, Lawrence C. Davies, John A. Stock, and Kenneth R. Harrap
pp 1044 - 1047; DOI:
10.1021/jm00374a018
PDF
Structure-activity, theoretical, and x-ray studies on the intramolecular interactions in a series of novel histamine H2 receptor antagonists
William C. Lumma Jr., John J. Baldwin, John B. Bicking, William A. Bolhofer, Jacob M. Hoffman, Brian T. Phillips, Charles M. Robb, Mary Lou Torchiana, H. B. Schlegel, and et al.
pp 1047 - 1052; DOI:
10.1021/jm00374a019
PDF
Potential antitumor agents. 42. Structure-activity relationships for acridine-substituted dimethyl phosphoramidate derivatives of 9-anilinoacridine
Gordon W. Rewcastle, Graham J. Atwell, Bruce C. Baguley, and William A. Denny
pp 1053 - 1056; DOI:
10.1021/jm00374a020
PDF
Antiestrogens. 2. Structure-activity studies in a series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl]-[4-[2-(1-piperidinyl)ethoxy]phenyl]methanone hydrochloride (LY 156758), a remarkably effective estrogen antagonist with only minimal intrinsic estrogenicity
Charles D. Jones, Mary G. Jevnikar, Andrew J. Pike, Mary K. Peters, Larry J. Black, Allen R. Thompson, Julie F. Falcone, and James A. Clemens
pp 1057 - 1066; DOI:
10.1021/jm00374a021
PDF
Structure-activity studies on antidepressant 2,2-diarylethylamines
Bruce E. Maryanoff, Samuel O. Nortey, and Joseph F. Gardocki
pp 1067 - 1071; DOI:
10.1021/jm00374a022
PDF
Radiohalogen-labeled imaging agents. 3. Compounds for measurement of brain blood flow by emission tomography
Thornton Sargent, Alexander T. Shulgin, and Chester A. Mathis
pp 1071 - 1077; DOI:
10.1021/jm00374a023
PDF
Antihypertensives. N-1H-Pyrrol-1-yl-3-pyridazinamines
Elvio Bellasio, Ambrogio Campi, Nunzio Di Mola, and Emiliana Baldoli
pp 1077 - 1083; DOI:
10.1021/jm00374a024
PDF
Syntheses and anthelmintic activity of alkyl 5(6)-(substituted carbamoyl)- and 5(6)-(disubstituted carbamoyl)benzimidazole-2-carbamates and related compounds
Shiv Kumar, Manju Seth, Amiya P. Bhaduri, Pradeep K. S. Visen, Anuradha Misra, Suman Gupta, Nigar Fatima, Jagdish C. Katiyar, Ranjeet K. Chatterjee, and Amiya B. Sen
pp 1083 - 1089; DOI:
10.1021/jm00374a025
PDF
Synthesis and pharmacological evaluation of an 8.beta.-bis(2-chloroethyl)amino opiate as a nonequilibrium opioid receptor probe
Sunan Fang, K. H. Bell, and P. S. Portoghese
pp 1090 - 1092; DOI:
10.1021/jm00374a026
PDF
The preferred solution conformation of warfarin at the active site of cytochrome P-450 based on the CD spectra in octanol/water model system
Larry D. Heimark and William F. Trager
pp 1092 - 1095; DOI:
10.1021/jm00374a027
PDF
2,5-Anhydro-1-deoxy-1-phosphono-D-altritol, an isosteric analog of .alpha.-D-ribofuranose 1-phosphate
Rich B. Meyer, Thomas E. Stone, and Pradipta K. Jesthi
pp 1095 - 1098; DOI:
10.1021/jm00374a028
PDF

Issue 9


Cardiotonic agents. 1. 4,5-Dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3(2H)-pyridazinones: novel positive inotropic agents for the treatment of congestive heart failure
James A. Bristol, Ila Sircar, Walter H. Moos, Dale B. Evans, and Ronald E. Weishaar
pp 1099 - 1101; DOI:
10.1021/jm00375a001
PDF
Oxidation of sparteines by cytochrome P-450: evidence against the formation of N-oxides
F. Peter Guengerich
pp 1101 - 1103; DOI:
10.1021/jm00375a002
PDF
Novel amino-substituted 3-quinolinecarboxylic acid antibacterial agents: synthesis and structure-activity relationships
Mark P. Wentland, Denis M. Bailey, James B. Cornett, Richard A. Dobson, Ronald G. Powles, and Roland B. Wagner
pp 1103 - 1108; DOI:
10.1021/jm00375a003
PDF
Synthesis and evaluation of substituted 2-phenylcyclobutylamines as analogs of hallucinogenic phenethylamines: lack of LSD-like biological activity
David E. Nichols, Kiran P. Jadhav, Robert A. Oberlender, Joseph E. Zabik, Josef F. Bossart, Akihiko Hamada, and Duane D. Miller
pp 1108 - 1111; DOI:
10.1021/jm00375a004
PDF
Benzylamines: synthesis and evaluation of antimycobacterial properties
Wolfgang R. Meindl, Erwin Von Angerer, Helmut Schoenenberger, and Gotthard Ruckdeschel
pp 1111 - 1118; DOI:
10.1021/jm00375a005
PDF
Synthesis and biological activity of certain 3,4-disubstituted pyrazolo[3,4-d]pyrimidine nucleosides
Howard B. Cottam, Charles R. Petrie, Patricia A. McKernan, Richard J. Goebel, N. Kent Dalley, Richard B. Davidson, Roland K. Robins, and Ganapathi R. Revankar
pp 1119 - 1127; DOI:
10.1021/jm00375a006
PDF
Synthesis and antihypertensive activity of 6,7-disubstituted trans-4-amino-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-3-ols
John M. Evans, Charles S. Fake, Thomas C. Hamilton, Robert H. Poyser, and Graham A. Showell
pp 1127 - 1131; DOI:
10.1021/jm00375a007
PDF
Steroids. 2. Synthesis of C-18 functionalized steroids via the Smith-Hughes route
K. M. R. Pillai, W. V. Murray, I. Shooshani, D. L. Williams, D. Gordon, S. Y. Wang, and Francis Johnson
pp 1131 - 1137; DOI:
10.1021/jm00375a008
PDF
Synthesis and neuroleptic activity of N-[(1-ethyl-2-pyrrolidinyl)methyl]-2-methoxy-5-sulfonamidobenzamides
Masaru Ogata, Hiroshi Matsumoto, Shiro Kida, Teruo Shiomi, Masami Eigyo, and Katsumi Hirose
pp 1137 - 1141; DOI:
10.1021/jm00375a009
PDF
Synthesis and antiarrhythmic activity of new 1-[1-[2-[3-{alkylamino}-2-hydroxypropoxy]phenyl]vinyl]-1H-imidazoles and related compounds
Masaru Ogata, Hiroshi Matsumoto, Kimio Takahashi, Sumio Shimizu, Shiro Kida, Motohiko Ueda, Sadatoshi Kimoto, and Masao Haruna
pp 1142 - 1149; DOI:
10.1021/jm00375a010
PDF
Synthesis and antidepressant activity of 4-aryltetrahydrothieno[2,3-c]pyridine derivatives
Claus S. Schneider, Karl H. Weber, Helmut Daniel, Wolf D. Bechtel, and Karin Boeke-Kuhn
pp 1150 - 1155; DOI:
10.1021/jm00375a011
PDF
Synthesis, spectral analysis, and mutagenicity of 1-, 3-, and 6-nitrobenzo[a]pyrene
M. W. Chou, R. H. Heflich, D. A. Casciano, D. W. Miller, J. P. Freeman, F. E. Evans, and P. P. Fu
pp 1156 - 1161; DOI:
10.1021/jm00375a012
PDF
Potential antitumor agents: synthesis and biological properties of aliphatic amino acid 9-hydroxyellipticinium derivatives
Christian Auclair, Emmanuelle Voisin, Helene Banoun, Claude Paoletti, Jean Bernadou, and Bernard Meunier
pp 1161 - 1166; DOI:
10.1021/jm00375a013
PDF
Synthesis and kinetic studies of protease substrates containing the 1-methyl-6-aminoquinolinium ion as a fluorogenic leaving group
Patricia Andrade-Gordon, David Gordon, Paul J. Brynes, and Cheng Wen Wu
pp 1166 - 1170; DOI:
10.1021/jm00375a014
PDF
Luteinizing hormone-releasing hormone antagonists containing very hydrophobic amino acids
John J. Nestor, Ram Tahilramani, Teresa L. Ho, Georgia I. McRae, and Brian H. Vickery
pp 1170 - 1174; DOI:
10.1021/jm00375a015
PDF
Analogs of platelet activating factor (PAF). 1. Some modifications of the alkoxy chain
A. Wissner, P. E. Sum, R. E. Schaub, C. A. Kohler, and B. M. Goldstein
pp 1174 - 1181; DOI:
10.1021/jm00375a016
PDF
Adrenoceptor and tetrabenazine antagonism activities of some pyridinyltetrahydropyridines
Walfred S. Saari, Wasyl Halczenko, Joel R. Huff, James P. Guare, Cecilia A. Hunt, William C. Randall, Victor J. Lotti, and George G. Yarbrough
pp 1182 - 1185; DOI:
10.1021/jm00375a017
PDF
Cyclic melanotropins. 5. Importance of the C-terminal tripeptide (Lys-Pro-Val)
Wayne L. Cody, Brian C. Wilkes, Brian J. Muska, Victor J. Hruby, Ana Maria de L. Castrucci, and Mac E. Hadley
pp 1186 - 1190; DOI:
10.1021/jm00375a018
PDF
Solution conformations of barbituric acid derivatives: a 3J(13C,1H) NMR study
F. Ivy Carroll, Anita H. Lewin, Emily E. Williams, Jack A. Berdasco, and Charles G. Moreland
pp 1191 - 1195; DOI:
10.1021/jm00375a019
PDF
Derivatives of 2-methyl-1,4-naphthoquinone as substrates and inhibitors of the vitamin K-dependent carboxylase
Madhup K. Dhaon, S. R. Lehrman, D. H. Rich, J. A. Engelke, and J. W. Suttie
pp 1196 - 1201; DOI:
10.1021/jm00375a020
PDF
Nonquaternary cholinesterase reactivators. 2. .alpha.-Heteroaromatic aldoximes and thiohydroximates as reactivators of ethyl methylphosphonyl-acetylcholinesterase in vitro
Richard A. Kenley, Clifford D. Bedford, Oliver D. Dailey, Robert A. Howd, and Alexi Miller
pp 1201 - 1211; DOI:
10.1021/jm00375a021
PDF
Benzisoxazolones: antimicrobial and antileukemic activity
W. Wierenga, B. R. Evans, and G. E. Zurenko
pp 1212 - 1215; DOI:
10.1021/jm00375a022
PDF
Synthesis and pharmacological evaluation of indanpropionic acids as uterine relaxants
Donald T. Witiak, Ahmed M. Hassan, Franziska R. Del Vecchio, Richard J. Brumbaugh, and Ralf G. Rahwan
pp 1215 - 1219; DOI:
10.1021/jm00375a023
PDF
Potential synthetic codeine substitutes: (-)-3-O-aryl-N-methylmorphinans
Erno Mohacsi, Tom Hayes, and Jerry Sepinwall
pp 1219 - 1222; DOI:
10.1021/jm00375a024
PDF
Synthesis and antitumor evaluation of some nitrosourea and nitrogen mustard amino acid derivatives
Marc Rodriguez, Jean Louis Imbach, and Jean Martinez
pp 1222 - 1225; DOI:
10.1021/jm00375a025
PDF
Synthesis and antibacterial activity of 2-[(methoxycarbonyl)methylene]cephalosporins
C. U. Kim, P. F. Misco, U. J. Haynes, and D. N. McGregor
pp 1225 - 1229; DOI:
10.1021/jm00375a026
PDF
Vitamin K dependent carboxylation: synthesis and biological properties of tetrazolyl analogs of pentapeptidic substrates
Joelle Dubois, Sonia Bory, Michel Gaudry, and Andree Marquet
pp 1230 - 1233; DOI:
10.1021/jm00375a027
PDF
Preferred conformers for the pharmacologically typical and atypical antipodes of phenylmorphan opiates
Mark Froimowitz
pp 1234 - 1237; DOI:
10.1021/jm00375a028
PDF
Book Reviews

pp 1237 - 1238; DOI:
10.1021/jm00375a600
PDF

Issue 10


New perspectives on gut peptides
Richard J. Miller
pp 1239 - 1245; DOI:
10.1021/jm00376a001
PDF
Heterocyclic analogs of chlorcyclizine with potent hypolipidemic activity
Michael J. Ashton, Alan Ashford, Anthony H. Loveless, David Riddell, John Salmon, and Gregory V. W. Stevenson
pp 1245 - 1253; DOI:
10.1021/jm00376a002
PDF
Nitrogen bridgehead compounds. 44. New antiallergic 4H-pyrido[1,2-a]pyrimidin-4-ones. 4
Istvan Hermecz, Agnes Horvath, Zoltan Meszaros, Christine De Vos, and Ludovic Rodriguez
pp 1253 - 1259; DOI:
10.1021/jm00376a003
PDF
Interaction of N4-hydroxy-2'-deoxycytidylic acid with thymidylate synthetase
Sanford Goldstein, Alfonso L. Pogolotti, Edward P. Garvey, and Daniel V. Santi
pp 1259 - 1262; DOI:
10.1021/jm00376a004
PDF
A mechanism for the addition of multiple moles of glutamate by folylpolyglutamate synthetase
Richard G. Moran, Paul D. Colman, Ronald A. Forsch, and Andre Rosowsky
pp 1263 - 1267; DOI:
10.1021/jm00376a005
PDF
N-Allyl analogs of phencyclidine: chemical synthesis and pharmacological properties
Asher Kalir, Shoshana Teomy, Adina Amir, P. Fuchs, Sung A. Lee, Elzbieta J. Holsztynska, Wieslaw Rocki, and Edward F. Domino
pp 1267 - 1271; DOI:
10.1021/jm00376a006
PDF
Conformationally restrained fentanyl analogs. 2. Synthesis and analgetic evaluation of perhydro-1,6-naphthyridin-2-ones
Ronald F. Borne, E. Kim Fifer, and I. W. Waters
pp 1271 - 1275; DOI:
10.1021/jm00376a007
PDF
Preparation of 7-(1,3,4-oxadiazolyl)-6,14-endo-etheno-6,7,8,14-tetrahydrothebaines and related compounds as potential analgesics
Kenneth W. Bentley, Michael Burton, and Barrie C. Uff
pp 1276 - 1280; DOI:
10.1021/jm00376a008
PDF
Dichloro[1,2-bis(4-hydroxyphenyl)ethylenediamine]platinum(II) complexes: an approach to develop compounds with a specific effect on the hormone-dependent mammary carcinoma
Beate Wappes, Margaretha Jennerwein, Erwin Von Angerer, Helmut Schoenenberger, Juergen Engel, Martin Berger, and Karl Heinz Wrobel
pp 1280 - 1286; DOI:
10.1021/jm00376a009
PDF
Synthesis and evaluation of (17.alpha.,20E)-21-[125I]iodo-19-norpregna-1,3,5(10),20-tetraene-3,17-diol and (17.alpha.,20E)-21-[125I]iodo-11.beta.-methoxy-19-norpregna-1,3,5(10),20-tetraene-3,17-diol [17.alpha.-iodovinyl)estradiol derivatives] as high specific activity potential radiopharmaceuticals
Iwao Nakatsuka, Nelson L. Ferreira, W. C. Eckelman, B. E. Francis, W. J. Rzeszotarski, R. E. Gibson, E. M. Jagoda, and R. C. Reba
pp 1287 - 1291; DOI:
10.1021/jm00376a010
PDF
Synthesis and .beta.-adrenergic blocking activity of new aliphatic and alicyclic oxime ethers
Mohamed Bouzoubaa, Gerard Leclerc, Nicole Decker, Jean Schwartz, and Guy Andermann
pp 1291 - 1294; DOI:
10.1021/jm00376a011
PDF
Synthesis and in vitro biological evaluation of L-alanosinyl-5-aminoimidazole-4-carboxylic acid ribonucleoside
Paolo Strazzolini, Adriano Malabarba, Pietro Ferrari, Maria Grandi, and Bruno Cavalleri
pp 1295 - 1299; DOI:
10.1021/jm00376a012
PDF
7-(Ethoxycarbonyl)-6,8-dimethyl-2-phenyl-1(2H)-phthalazinone derivatives: synthesis and inhibitory effects on platelet aggregation
Akiko Sugimoto, Hiromichi Tanaka, Yukuo Eguchi, Shigeru Ito, Yoshimi Takashima, and Masayuki Ishikawa
pp 1300 - 1305; DOI:
10.1021/jm00376a013
PDF
A water-soluble cholesteryl-containing Tris-galactoside: synthesis, properties, and use in directing lipid-containing particles to the liver
H. J. M. Kempen, C. Hoes, J. H. Van Boom, H. H. Spanjer, J. De Lange, A. Langendoen, and T. J. C. Van Berkel
pp 1306 - 1312; DOI:
10.1021/jm00376a014
PDF
Molecular analysis of hexahydro-1H-indeno[1,2-b]pyridines: potential antidepressants
Rudolf Kunstmann and Gabriele Fischer
pp 1312 - 1316; DOI:
10.1021/jm00376a015
PDF
Antiinflammatory activity of N-(2-benzoylphenyl)alanine derivatives
David A. Walsh, Mark C. Sleevi, and Lawrence F. Sancilio
pp 1317 - 1321; DOI:
10.1021/jm00376a016
PDF
Synthesis and murine antineoplastic activity of bis[carbamoyloxymethyl] derivatives of pyrrolo[2,1-a]isoquinoline
Wayne K. Anderson, Howard L. McPherson, James S. New, and Arvela C. Rick
pp 1321 - 1325; DOI:
10.1021/jm00376a017
PDF
Design and synthesis of naltrexone-derived affinity labels with nonequilibrium opioid agonist and antagonist activities. Evidence for the existence of different .mu. receptor subtypes in different tissues
L. M. Sayre, D. L. Larson, A. E. Takemori, and P. S. Portoghese
pp 1325 - 1335; DOI:
10.1021/jm00376a018
PDF
Latent inhibitors of aldehyde dehydrogenase as alcohol deterrent agents
Herbert T. Nagasawa, James A. Elberling, and Eugene G. DeMaster
pp 1335 - 1339; DOI:
10.1021/jm00376a019
PDF
6,7-Dihydroxy-3-chromanamine: synthesis and pharmacological activity of an oxygen isostere of the dopamine agonist
Alan S. Horn, B. Kaptein, T. B. A. Mulder, J. B. de Vries, and H. Wynberg
pp 1340 - 1343; DOI:
10.1021/jm00376a020
PDF
Total chemical synthesis and antitumor evaluation of 4-demethoxy-10,10-dimethyldaunomycin
Jose Alexander, Ish Khanna, Daniel Lednicer, Lester A. Mitscher, Tarik Veysoglu, Zbigniew Wielogorski, and Richard L. Wolgemuth
pp 1343 - 1347; DOI:
10.1021/jm00376a021
PDF
Synthesis and antiarrhythmic and parasympatholytic properties of substituted phenols. 2. Amides
David M. Stout, W. L. Matier, Cynthia Barcelon-Yang, Robert D. Reynolds, and Barry S. Brown
pp 1347 - 1350; DOI:
10.1021/jm00376a022
PDF
Inhibition of renin by substrate analog inhibitors containing the olefinic amino acid 5(S)-amino-7-methyl-3(E)-octenoic acid
Rodney L. Johnson
pp 1351 - 1354; DOI:
10.1021/jm00376a023
PDF
Antihypertensive activities of phenyl aminoethyl sulfides, a class of synthetic substrates for dopamine .beta.-hydroxylase
Stephen R. Padgette, Heath H. Herman, Jin Hee Han, Stanley H. Pollock, and Sheldon W. May
pp 1354 - 1357; DOI:
10.1021/jm00376a024
PDF
Carbocyclic analogs of xylofuranosylpurine nucleosides. Synthesis and antitumor activity
Robert Vince, Jay Brownell, and Susan Daluge
pp 1358 - 1360; DOI:
10.1021/jm00376a025
PDF
Activities of morphinone and N-(cyclopropylmethyl)normorphinone at opioid receptors
Sunan Fang, A. E. Takemori, and P. S. Portoghese
pp 1361 - 1363; DOI:
10.1021/jm00376a026
PDF
Mesoionic xanthine analogs: antagonists of adenosine receptors
Richard A. Glennon, Shanaz M. Tejani-Butt, William Padgett, and John W. Daly
pp 1364 - 1367; DOI:
10.1021/jm00376a027
PDF
Synthesis of a tricyclic aphidicolin analog which inhibits DNA synthesis in vitro
John E. McMurry and Thomas R. Webb
pp 1367 - 1369; DOI:
10.1021/jm00376a028
PDF
Activity of novel aminocannabinoids in baboons
H. Edery, G. Porath, R. Mechoulam, N. Lander, M. Srebnik, and N. Lewis
pp 1370 - 1373; DOI:
10.1021/jm00376a029
PDF
Book Reviews

pp 1373 - 1378; DOI:
10.1021/jm00376a600
PDF

Issue 11


Antiinflammatory agents. 3. Synthesis and pharmacological evaluation of 2-amino-3-benzoylphenylacetic acid and analogs
David A. Walsh, H. Wayne Moran, Dwight A. Shamblee, Ibrahim M. Uwaydah, William J. Welstead, Lawrence F. Sancilio, and Warren N. Dannenburg
pp 1379 - 1388; DOI:
10.1021/jm00377a001
PDF
Synthesis and antiviral/antitumor activities of certain 3-deazaguanine nucleosides and nucleotides
Ganapathi R. Revankar, Pranab K. Gupta, Alexander D. Adams, N. Kent Dalley, Patricia A. McKernan, P. Dan Cook, Peter G. Canonico, and Roland K. Robins
pp 1389 - 1396; DOI:
10.1021/jm00377a002
PDF
(1,3-Dialkyl-5-amino-1H-pyrazol-4-yl)arylmethanones. A series of novel central nervous system depressants
Donald E. Butler, Lawrence D. Wise, and Horace A. DeWald
pp 1396 - 1400; DOI:
10.1021/jm00377a003
PDF
Actinidin hydrolysis of substituted-phenyl hippurates: a quantitative structure-activity relationship and graphics comparison with hydrolysis by papain
Angelo Carotti, Corwin Hansch, Monica M. Mueller, and Jeffrey M. Blaney
pp 1401 - 1405; DOI:
10.1021/jm00377a004
PDF
Synthesis and biological actions of highly potent and prolonged acting biotin-labeled melanotropins
Dhirendra N. Chaturvedi, James J. Knittel, Victor J. Hruby, Ana Maria de L. Castrucci, and Mac E. Hadley
pp 1406 - 1410; DOI:
10.1021/jm00377a005
PDF
Investigations on the chemistry of berbanes. 10. Synthesis of raunescinone analogs with hypotensive and antihypertensive activity
Istvan Toth, Lajos Szabo, Gabriella Bozsar, Csaba Szantay, Laszlo Szekeres, and Julius G. Papp
pp 1411 - 1415; DOI:
10.1021/jm00377a006
PDF
Synthesis and antiviral activity of carbocyclic analogs of 2'-deoxyribofuranosides of 2-amino-6-substituted-purines and of 2-amino-6-substituted-8-azapurines
Y. Fulmer Shealy, C. Allen O'Dell, W. M. Shannon, and Gussie Arnett
pp 1416 - 1421; DOI:
10.1021/jm00377a007
PDF
Studies on synthesis and anticancer activity of selected N-(2-fluoroethyl)-N-nitrosoureas
Thomas P. Johnston, Conrad L. Kussner, Ronald L. Carter, Jerry L. Frye, Nancita R. Lomax, Jacqueline Plowman, and V. L. Narayanan
pp 1422 - 1426; DOI:
10.1021/jm00377a008
PDF
Structure-activity relationship of the ficin hydrolysis of phenyl hippurates. Comparison with papain, actinidin, and bromelain
Angelo Carotti, Giovanni Casini, and Corwin Hansch
pp 1427 - 1431; DOI:
10.1021/jm00377a009
PDF
Structure-activity relationships for reactivators of organophosphorus-inhibited acetylcholinesterase: quaternary salts of 2[(hydroxyimino)methyl]imidazoles
Clifford D. Bedford, Ralph N. Harris, Robert A. Howd, Alexi Miller, Harold W. Nolen, and Richard A. Kenley
pp 1431 - 1438; DOI:
10.1021/jm00377a010
PDF
2-Phenylindoles. Relationship between structure, estrogen receptor affinity, and mammary tumor inhibiting activity in the rat
Erwin Von Angerer, Jelica Prekajac, and Josef Strohmeier
pp 1439 - 1447; DOI:
10.1021/jm00377a011
PDF
A novel peptide delivery system involving peptidase activated prodrugs as antimicrobial agents. Synthesis and biological activity of peptidyl derivatives of 5-fluorouracil
William D. Kingsbury, Jeffrey C. Boehm, Rajanikant J. Mehta, Sarah F. Grappel, and Charles Gilvarg
pp 1447 - 1451; DOI:
10.1021/jm00377a012
PDF
N-Benzylpiperazino derivatives of 3-nitro-4-hydroxycoumarin with H1 antihistamine and mast cell stabilizing properties
Derek R. Buckle, D. James Outred, Harry Smith, and Barbara A. Spicer
pp 1452 - 1457; DOI:
10.1021/jm00377a013
PDF
Bispyridinamines: a new class of topical antimicrobial agents as inhibitors of dental plaque
Denis M. Bailey, C. George DeGrazia, Stephanie J. Hoff, Patsy L. Schulenberg, John R. O'Connor, Donald A. Paris, and Andrew McKenzie Slee
pp 1457 - 1464; DOI:
10.1021/jm00377a014
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Covalent binding of isomeric 7-(2,3-epoxypropoxy)actinomycin D to DNA
Sisir K. Sengupta, Joanne Blondin, and Josephine Szabo
pp 1465 - 1470; DOI:
10.1021/jm00377a015
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Trequinsin, a potent new antihypertensive vasodilator in the series of 2-(arylimino)-3-alkyl-9,10-dimethoxy-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-ones
Bansi Lal, Alihussein Nomanbhai Dohadwalla, Nandkumar Keshav Dadkar, Adolf D'Sa, and Noel John De Souza
pp 1470 - 1480; DOI:
10.1021/jm00377a016
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Potential antitumor agents. Part 43. Synthesis and biological activity of dibasic 9-aminoacridine-4-carboxamides, a new class of antitumor agent
Graham J. Atwell, Bruce F. Cain, Bruce C. Baguley, Graeme J. Finlay, and William A. Denny
pp 1481 - 1485; DOI:
10.1021/jm00377a017
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Nucleic acid related compounds. 47. Synthesis and biological activities of pyrimidine and purine "acyclic" nucleoside analogs
Morris J. Robins, Peter W. Hatfield, Jan Balzarini, and Erik De Clercq
pp 1486 - 1492; DOI:
10.1021/jm00377a018
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Quantitative structure-activity relationship of insect juvenile hormone mimetic compounds
Akira Nakayama, Hajime Iwamura, and Toshio Fujita
pp 1493 - 1502; DOI:
10.1021/jm00377a019
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Potentiation of the tolerogenicity of benzylpenicilloylated eicosa-L-lysine by conjugation with 4-methoxybenzyl 3.beta.-cholestanyl succinate
Immanuel F. Luescher
pp 1502 - 1508; DOI:
10.1021/jm00377a020
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Nontricyclic antidepressant agents derived from cis- and trans-1-amino-4-aryltetralins
Willard M. Welch, Allen R. Kraska, Reinhard Sarges, and B. Kenneth Koe
pp 1508 - 1515; DOI:
10.1021/jm00377a021
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Conformationally restricted retinoids
Marcia I. Dawson, Peter D. Hobbs, Krzysztof Derdzinski, Rebecca L. S. Chan, John Gruber, Wanru Chao, Saundra Smith, Richard W. Thies, and Leonard J. Schiff
pp 1516 - 1531; DOI:
10.1021/jm00377a022
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A theoretical investigation of histamine tautomerism
Sid Topiol, Harel Weinstein, and Roman Osman
pp 1531 - 1533; DOI:
10.1021/jm00377a023
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Book Reviews

pp 1534 - 1534; DOI:
10.1021/jm00377a600
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Issue 12


2-[[[2-(2,6-Dimethoxyphenoxy)ethyl]amino]methyl]-1,4-benzoxathian: a new antagonist with high potency and selectivity towards .alpha.1-adrenoreceptors
Carlo Melchiorre, Livio Brasili, Dario Giardina, Maria Pigini, and Giovannella Strappaghetti
pp 1535 - 1536; DOI:
10.1021/jm00378a001
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Cyclopentenyluridine and cyclopentenylcytidine analogs as inhibitors of uridine-cytidine kinase
Mu Ill Lim, James D. Moyer, Richard L. Cysyk, and Victor E. Marquez
pp 1536 - 1538; DOI:
10.1021/jm00378a002
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Synthesis and antifungal activity of (E)-N-(6,6-dimethyl-2-hepten-4-ynyl)-N-methyl-1-naphthalenemethanamine (SF 86-327) and related allylamine derivatives with enhanced oral activity
Anton Stuetz and Gabor Petranyi
pp 1539 - 1543; DOI:
10.1021/jm00378a003
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Pyridonecarboxylic acids as antibacterial agents. Synthesis and antibacterial activity of 7-(3-amino-1-pyrrolidinyl)-1-ethyl-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid and its analogs
Hiroshi Egawa, Teruyuki Miyamoto, Akira Minamida, Yoshiro Nishimura, Hidetsugu Okada, Hitoshi Uno, and Junichi Matsumoto
pp 1543 - 1548; DOI:
10.1021/jm00378a004
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Design, synthesis, and testing of potential antisickling agents. 5. Disubstituted benzoic acids designed for the donor site and proline salicylates designed for the acceptor site
Donald J. Abraham, David M. Gazze, Paul E. Kennedy, and Michael Mokotoff
pp 1549 - 1559; DOI:
10.1021/jm00378a005
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Synthesis and evaluation of furan, thiophene, and azole bis[(carbamoyloxy)methyl] derivatives as potential antineoplastic agents
Wayne K. Anderson and Allen N. Jones
pp 1559 - 1565; DOI:
10.1021/jm00378a006
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Synthesis of 5-aryl-2H-tetrazoles, 5-aryl-2H-tetrazole-2-acetic acids, and [(4-phenyl-5-aryl-4H-1,2,4-triazol-3-yl)thio]acetic acids as possible superoxide scavengers and antiinflammatory agents
James R. Maxwell, Dan A. Wasdahl, Alan C. Wolfson, and Virgil I. Stenberg
pp 1565 - 1570; DOI:
10.1021/jm00378a007
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Probes for narcotic receptor mediated phenomena. 7. Synthesis and pharmacological properties of irreversible ligands specific for .mu. or .delta. opiate receptors
Terrence R. Burke, Balbir S. Bajwa, Arthur E. Jacobson, Kenner C. Rice, R. A. Streaty, and W. A. Klee
pp 1570 - 1574; DOI:
10.1021/jm00378a008
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Synthesis and biological evaluation of 14-alkoxymorphinans. 1. Highly potent opioid agonists in the series of (-)-14-methoxy-N-methylmorphinan-6-ones
Helmut Schmidhammer, Lislott Aeppli, Louise Atwell, Florian Fritsch, Arthur E. Jacobson, Michaela Nebuchla, and Guenther Sperk
pp 1575 - 1579; DOI:
10.1021/jm00378a009
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[[(Aminomethyl)aryl]oxy]acetic acid esters. A new class of high-ceiling diuretics. 1. Effects of nitrogen and aromatic nuclear substitution
Cheuk Man Lee, Jacob J. Plattner, C. Wayne Ours, Bruce W. Horrom, Jill R. Smital, Yvonne C. Martin, Andre G. Pernet, Paul R. Bunnell, Souheir E. El Masry, and Patrick W. Dodge
pp 1579 - 1587; DOI:
10.1021/jm00378a010
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[[(Aminomethyl)aryl]oxy]acetic acid esters. A new class of high-ceiling diuretics. 2. Modifications of the oxyacetic side chain
Jacob J. Plattner, Anthony K. L. Fung, Jill R. Smital, Cheuk Man Lee, Steven R. Crowley, Andre G. Pernet, Paul R. Bunnell, Steven A. Buckner, and Lawrence T. Sennello
pp 1587 - 1596; DOI:
10.1021/jm00378a011
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Synthesis and biological activity of new peptide segments of gastrin exhibiting gastrin antagonist property
Jean Martinez, Richard Magous, Marie Francoise Lignon, Jeanine Laur, Bertrand Castro, and Jean Pierre Bali
pp 1597 - 1601; DOI:
10.1021/jm00378a012
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A novel method of conjugation of daunomycin with antibody with a poly(L-glutamic acid) derivative as intermediate drug carrier. An anti-.alpha.-fetoprotein antibody-daunomycin conjugate
Yoshinori Kato, Naoji Umemoto, Yasutaka Kayama, Hisashi Fukushima, Yumiko Takeda, Takeshi Hara, and Yutaka Tsukada
pp 1602 - 1607; DOI:
10.1021/jm00378a013
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Synthesis of 4-substituted 2H-naphth[1,2-b]-1,4-oxazines, a new class of dopamine agonists
James H. Jones, Paul S. Anderson, John J. Baldwin, Bradley V. Clineschmidt, David E. McClure, George F. Lundell, William C. Randall, Gregory E. Martin, Michael Williams, and et al.
pp 1607 - 1613; DOI:
10.1021/jm00378a014
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Mesoionic pyridazine ribonucleosides. A novel biologically active nucleoside metabolite
Ronald E. Bambury, Daniel T. Feeley, Gerald C. Lawton, John M. Weaver, and James Wemple
pp 1613 - 1621; DOI:
10.1021/jm00378a015
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Novel pyrimidine and 1,3,5-triazine hypolipemic agents
Gaetano D'Atri, Piero Gomarasca, Giuseppe Resnati, Giovanni Tronconi, Carlo Scolastico, and Cesare R. Sirtori
pp 1621 - 1629; DOI:
10.1021/jm00378a016
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Acidic furo[3,2-b]indoles. A new series of potent antiallergy agents
Paul C. Unangst, Mary E. Carethers, Kenneth Webster, Grace M. Janik, and Lillian J. Robichaud
pp 1629 - 1633; DOI:
10.1021/jm00378a017
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Synthesis and activity of novel nitropyrazines for use as hypoxic cell radiosensitizers
George D. Hartman, Richard D. Hartman, John E. Schwering, Nigel R. Jones, Peter Wardman, Margaret E. Watts, and Michael Woodcock
pp 1634 - 1639; DOI:
10.1021/jm00378a018
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Pyrido[3',2':4,5]thieno[3,2-d]-N-triazines: a new series of orally active antiallergic agents
Raymond D. Youssefyeh, Richard E. Brown, Jeffrey Wilson, Uresh Shah, Howard Jones, Bernard Loev, Atul Khandwala, Mitchell J. Leibowitz, and Paula Sonnino-Goldman
pp 1639 - 1643; DOI:
10.1021/jm00378a019
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Effects of volume and surface property in hydrolysis by acetylcholinesterase. The trimethyl site
Saul G. Cohen, Jerome L. Elkind, S. Bano Chishti, Jose L. Giner, and Heide Reese
pp 1643 - 1647; DOI:
10.1021/jm00378a020
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Functional group contributions to drug-receptor interactions
P. R. Andrews, D. J. Craik, and J. L. Martin
pp 1648 - 1657; DOI:
10.1021/jm00378a021
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3-Substituent effect and 3-methylene substituent effect on the structure-reactivity relationship of 7.beta.-(acylamino)-3-cephem-4-carboxylic acid derivatives studied by carbon-13 and IR spectroscopy
Junko Nishikawa and K. Tori
pp 1657 - 1663; DOI:
10.1021/jm00378a022
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Peptide sweeteners. 6. Structural studies on the C-terminal amino acid of L-aspartyl dipeptide sweeteners
Joseph W. Tsang, Bernhard Schmied, Rolf Nyfeler, and Murray Goodman
pp 1663 - 1668; DOI:
10.1021/jm00378a023
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Peptide sweeteners. 7. Taste relationships of trifluoroacetyl-L-aspartylanilides
Marc Rodriguez and Murray Goodman
pp 1668 - 1672; DOI:
10.1021/jm00378a024
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A proton NMR study of the interactions and conformations of rationally designed brodimoprim analogs in complexes with Lactobacillus casei dihydrofolate reductase
B. Birdsall, J. Feeney, C. Pascual, G. C. K. Roberts, I. Kompis, R. L. Then, K. Mueller, and A. Kroehn
pp 1672 - 1676; DOI:
10.1021/jm00378a025
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A substituent constant analysis of the interaction of substituted naphthalene monoimides with DNA
Karen A. Stevenson, Shau Fong Yen, Nai Chuang Yang, David W. Boykin, and W. David Wilson
pp 1677 - 1682; DOI:
10.1021/jm00378a026
PDF
Bulky amine analogs of ketoprofen: potent antiinflammatory agents
Donald C. Schlegel, Bernard L. Zenitz, Constance A. Fellows, Stanley C. Laskowski, D. Craig Behn, Donald K. Phillips, Irving Botton, and Phyllis T. Speight
pp 1682 - 1690; DOI:
10.1021/jm00378a027
PDF
Azasteroids as inhibitors of rat prostatic 5.alpha.-reductase
Gary H. Rasmusson, Glenn F. Reynolds, Torleif Utne, Ronald B. Jobson, Raymond L. Primka, Charles Berman, and Jerry R. Brooks
pp 1690 - 1701; DOI:
10.1021/jm00378a028
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C(2)-Methylation abolishes DA1 dopamine agonist activity of 2-amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene (6,7-ADTN): steric intolerance by the receptor
David E. Nichols, James N. Jacob, Andrew J. Hoffman, Jai D. Kohli, and Dana Glock
pp 1701 - 1705; DOI:
10.1021/jm00378a029
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N2-(4-Substituted-2,6-dichlorophenyl)-N1,N1-dimethylformamidines as antihypertensive and diuretic agents
Walter E. Meyer, Andrew S. Tomcufcik, Peter S. Chan, and John E. Emma
pp 1705 - 1710; DOI:
10.1021/jm00378a030
PDF
A potent multisubstrate analog inhibitor of human thymidylate synthetase
Ananthachari Srinivansan, Venkataraman Amarnath, Arthur D. Broom, F. C. Fou, and Yung Chi Cheng
pp 1710 - 1717; DOI:
10.1021/jm00378a031
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Diastereomeric 6-desoxy-6-spiro-.alpha.-methylene-.gamma.-butyrolactone derivatives of naltrexone and oxymorphone. Selective irreversible inhibition of naltrexone binding in an opioid receptor preparation by a conformationally restricted Michael acceptor ligand
Gary A. Koolpe, Wendel L. Nelson, T. L. Gioannini, Lloyd Angel, and Eric J. Simon
pp 1718 - 1723; DOI:
10.1021/jm00378a032
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1-Aryl-3,3-dimethyltriazenes: potential central nervous system active analogs of 5-(3,3-dimethyl-1-triazeno)imidazole-4-carboxamide (DTIC)
David Farquhar and John Benvenuto
pp 1723 - 1727; DOI:
10.1021/jm00378a033
PDF
Opioid agonists and antagonists. 6,6-Hydrazi and 6-oximino derivatives of 14-hydroxymorphinones
Ronald P. Ko, Sanjeev M. Gupte, and Wendel L. Nelson
pp 1727 - 1729; DOI:
10.1021/jm00378a034
PDF
Synthesis and binding to tubulin of colchicine spin probes
Padam N. Sharma, Arnold Brossi, J. V. Silverton, and Colin F. Chignell
pp 1729 - 1733; DOI:
10.1021/jm00378a035
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Bis(m-nitrophenyl) and bis(p-nitrophenyl) esters and the phosphorodiamidate of thymidine 5'-phosphate as potential sources of intracellular thymidine 5'-phosphate in mouse cells in culture
Ram R. Chawla, Jerome J. Freed, and Alexander Hampton
pp 1733 - 1736; DOI:
10.1021/jm00378a036
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Synthesis and biological evaluation of 6-amino-1H-pyrrolo[3,2-c]pyridin-4(5H)-one (3,7-dideazaguanine)
Stewart W. Schneller, Jiann Kuan Luo, Ramachandra S. Hosmane, Erik De Clercq, Johanna D. Stoeckler, Kailash C. Agarwal, Robert E. Parks, and Priscilla P. Saunders
pp 1737 - 1739; DOI:
10.1021/jm00378a037
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Folate antagonists. 22. Antimalarial and antibacterial effects of 2,4-diamino-6-quinazolinesulfonamides
Edward F. Elslager, Norman L. Colbry, John Davoll, Marland P. Hutt, Judith L. Johnson, and Leslie M. Werbel
pp 1740 - 1743; DOI:
10.1021/jm00378a038
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Tetrahydropyrrolo[1,2-a]quinoxalines and tetrahydropyrrolo[1,2-a]pyrido[3,2-a]pyrazines: vascular smooth muscle relaxants and antihypertensive agents
Magid Abou-Gharbia, Meier E. Freed, Ronald J. McCaully, Paul J. Silver, and Robert L. Wendt
pp 1743 - 1746; DOI:
10.1021/jm00378a039
PDF
Bis(3,5-diisopropylsalicylato)copper(II), a potent radioprotectant with superoxide dismutase mimetic activity
John R. J. Sorenson
pp 1747 - 1749; DOI:
10.1021/jm00378a040
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Synthesis and antitumor activity of tropolone derivatives. 1
Masatoshi Yamato, Kuniko Hashigaki, Nobuhiko Kokubu, Takashi Tsuruo, and Tazuko Tashiro
pp 1749 - 1753; DOI:
10.1021/jm00378a041
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Additions and Corrections- Chloroalanyl and Propargylglycyl Dipeptides. Suicide Substrate Containing Antibacterials
Kam-Sing Cheung, Steven A. Wasserman, Edward Dudek, A. Lerner, and Michael Johnston
pp 1753 - 1753; DOI:
10.1021/jm00378a600
PDF
Additions and Corrections-Improved Synthesis and Antitumor Evaluation of 5,8-Dideazaisofolic Acid and Closely Related Analogues
J.B. Hynes, Y.C.S. Yang, J.E. McGill, S.J. Harmon, and W.L. Washtien
pp 1753 - 1753; DOI:
10.1021/jm00378a601
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Additions and Corrections-2-Substituted Thiazolidine-4(R)-carboxylic Acids as Prodrugs of L-Cysteine. Protection of Mice Against Acetaminophen Hepatotoxicity
Herbert T. Nagasawa, David J.W. Goon, William P. Muldoon, and Richard T. Zera
pp 1753 - 1753; DOI:
10.1021/jm00378a602
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Additions and Corrections-Development of an Affinity Ligand for Purification of Adrenoceptors from Human Platelet Membranes
R.M. DeMarinis, A.J. Krog, D.H. Shah, J. Lafferty, K.G. Holdenm, J.P. Hieble, W.D. Matthews, J.W. Regan, R.J. Lefkowitz, and M.G. Caron
pp 1753 - 1753; DOI:
10.1021/jm00378a603
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Additions and Corrections-Antiextrogens. 2. Structure-Activity Studies in a Series of 3-Aroyl-2-arylbenzo[b]thiophene Derivatives Leading to [6-Hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl][4-[2-(1-piperidinyl)ethoxy]phenyl]methanone Hydrochloride (LY156758), a Remarkably Effective Estrogen Antagonist with Only Minimal Intrinsic Estrogenicity

pp 1753 - 1753; DOI:
10.1021/jm00378a604
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Book Reviews

pp 1754 - 1759; DOI:
10.1021/jm00378a605
PDF