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Volume 22
Main Index

Issue 1


The benzodiazepine story
Leo H. Sternbach
pp 1 - 7; DOI:
10.1021/jm00187a001
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[1-Penicillamine,2-leucine]oxytocin. Synthesis and pharmacological and conformational studies of a potent peptide hormone inhibitor
Victor J. Hruby, K. K. Deb, Diane M. Yamamoto, Mac E. Hadley, and W. Y. Chan
pp 7 - 12; DOI:
10.1021/jm00187a002
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Molecular orbital study on the reaction mechanism of irreversible enzyme inhibitors
Chikayoshi Nagata and Tamie Yamaguchi
pp 13 - 17; DOI:
10.1021/jm00187a003
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Structure-activity relationship in a new series of atropine analogs. 1. N,N'-Disubstituted 6,7-diazabicyclo[3.2.2]nonane derivatives
Stephan Cherkez, Haim Yellin, Yoel Kashman, Bella Yaavetz, and Mordechai Sokolovsky
pp 18 - 21; DOI:
10.1021/jm00187a004
PDF
Nucleosides. 110. Synthesis and antiherpes virus activity of some 2'-fluoro-2'-deoxyarabinofuranosylpyrimidine nucleosides
Kyoichi A. Watanabe, Uri Reichman, Kosaku Hirota, Carlos Lopez, and Jack J. Fox
pp 21 - 24; DOI:
10.1021/jm00187a005
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Preparation of the enantiomeric forms of 9-(5-deoxy-.alpha.-threo-pent-4-enofuranosyl)adenine and 9-(3,5-dideoxy-.beta.-D-glycero-pent-4-enofuranosyl)adenine and in vitro antileukemic screening
Vinai K. Srivastava and Leon M. Lerner
pp 24 - 28; DOI:
10.1021/jm00187a006
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Antileukemic activity of substituted ureidothiazoles, ureidothiadiazoles, and related compounds
Robert K. Y. Zee-Cheng and C. C. Cheng
pp 28 - 32; DOI:
10.1021/jm00187a007
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Ergot alkaloids. Synthesis of nitrosourea derivatives of ergolines as potential anticancer agents
A. Michael Crider, Catherine K. L. Lu, Heinz G. Floss, John M. Cassady, and James A. Clemens
pp 32 - 35; DOI:
10.1021/jm00187a008
PDF
5-Iminodaunorubicin. Reduced cardiotoxic properties in an antitumor anthracycline
George L. Tong, David W. Henry, and Edward M. Acton
pp 36 - 39; DOI:
10.1021/jm00187a009
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Synthesis of daunorubicin analogs with novel 9-acyl substituents
Thomas H. Smith, Allan N. Fujiwara, and David W. Henry
pp 40 - 44; DOI:
10.1021/jm00187a010
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Development of ethyl 3,4-dihydro-4-oxopyrimido[4,5-b]quinoline-2-carboxylate, a new prototype with oral antiallergy activity
T. H. Althuis, P. F. Moore, and H. J. Hess
pp 44 - 48; DOI:
10.1021/jm00187a011
PDF
Syntheses and antiinflammatory actions of 4,5,6,7-tetrahydroindazole-5-carboxylic acids
Masahiko Nagakura, Tomio Ota, Noboru Shimidzu, Kiyoshi Kawamura, Yoshinori Eto, and Yasushi Wada
pp 48 - 52; DOI:
10.1021/jm00187a012
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A new nonsteroidal analgesic-antiinflammatory agent. Synthesis and activity of 4-ethoxy-2-methyl-5-morpholino-3(2H)-pyridazinone and related compounds
M. Takaya, M. Sato, K. Terashima, H. Tanizawa, and Y. Maki
pp 53 - 58; DOI:
10.1021/jm00187a013
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Studies on analgesic agents. 1. Preparation of 1,2-diphenyl-2-(4-substituted 1-piperazinyl)ethanol derivatives and structure-activity relationships
Noriaki Shimokawa, Hideo Nakamura, Keiko Shimakawa, Hideo Minami, and Haruki Nishimura
pp 58 - 63; DOI:
10.1021/jm00187a014
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Synthesis and evaluation of the antiovulatory activity of a variety of melatonin analogs
Michael E. Flaugh, Thomas A. Crowell, James A. Clemens, and Barry D. Sawyer
pp 63 - 69; DOI:
10.1021/jm00187a015
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Hypobetalipoproteinemic agents. 2. Compounds related to 4-(1-adamantyloxy)aniline
Daniel Lednicer, William E. Heyd, D. Edward Emmert, Ruth E. TenBrink, Paul E. Schurr, and Charles E. Day
pp 69 - 77; DOI:
10.1021/jm00187a016
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2-Indanpropionic acids: structural leads for prostaglandin F2.alpha. antagonist development
Donald T. Witiak, Sunil V. Kadodkar, Timothy P. Johnson, John R. Baldwin, and Ralf G. Rahwan
pp 77 - 81; DOI:
10.1021/jm00187a017
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Relationship of nonspecific antiarrhythmic and negative inotropic activity with physicochemical parameters of propranolol analogs
David O. Rauls and John K. Baker
pp 81 - 86; DOI:
10.1021/jm00187a018
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Antimalarials. 4. Trichloronaphthalene amino alcohols
Dwight A. Shamblee and J. Samuel Gillespie
pp 86 - 89; DOI:
10.1021/jm00187a019
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Discriminant-analytical investigation on the structural dependence of hyperglycemic and hypoglycemic activity in a series of substituted o-toluenesulfonylthioureas and o-toluenesulfonylureas
S. Dove, R. Franke, O. L. Mndshojan, W. A. Schkuljev, and L. W. Chashakjan
pp 90 - 95; DOI:
10.1021/jm00187a020
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Studies on biologically active halogenated compounds. 1. Synthesis and central nervous system depressant activity of 2-(fluoromethyl)-3-aryl-4(3H)-quinazolinone derivatives
Junichi Tani, Yoshihisa Yamada, Toyonari Oine, Takashi Ochiai, Ryuichi Ishida, and Ichizo Inoue
pp 95 - 99; DOI:
10.1021/jm00187a021
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Kojic amine - a novel .gamma.-aminobutyric acid analog
Joseph G. Atkinson, Yves Girard, J. Rokach, C. S. Rooney, C. S. McFarlane, A. Rackham, and N. N. Share
pp 99 - 106; DOI:
10.1021/jm00187a022
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Synthesis and evaluation for diuretic activity of 1-substituted 6-chloro-5-sulfamylindolines
Edward J. Glamkowski and Philip A. Reitano
pp 106 - 109; DOI:
10.1021/jm00187a023
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Phosphonate analog of 2'-deoxy-5-fluorouridylic acid
John A. Montgomery, H. Jeanette Thomas, Roy L. Kisliuk, and Yvette Gaumont
pp 109 - 111; DOI:
10.1021/jm00187a024
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Correlation of carbonic anhydrase inhibitory activities of benzenesulfonamides with the data obtained by use of nitrogen-14 nuclear quadrupole resonance
S. N. Subbarao and P. J. Bray
pp 111 - 114; DOI:
10.1021/jm00187a025
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11-Oxo-11H-pyrido[2,1-b]quinazoline-8-carboxylic acid, an orally active antiallergy agent
Charles F. Schwender, Brooks R. Sunday, and David J. Herzig
pp 114 - 116; DOI:
10.1021/jm00187a026
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Actions of two dopamine derivatives at adreno- and cholinoceptors
I. W. Rodger, A. S. Hersom, and R. D. Waigh
pp 117 - 119; DOI:
10.1021/jm00187a027
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Apparent bioisosteric replacement of -S- by NCN: synthesis of N-cyano-2-aza-A-nor-5.alpha.-androstan-17.beta.-ol acetate, an aza steroid androgen
Wen-Hsiung Chiu, Thomas H. Klein, and Manfred E. Wolff
pp 119 - 120; DOI:
10.1021/jm00187a028
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Issue 2


Synthesis and antitumor activity of 4'-O-methyldaunorubicin, 4'-O-methyladriamycin, and their 4'-epi analogs
G. Cassinelli, D. Ruggieri, and F. Arcamone
pp 121 - 123; DOI:
10.1021/jm00188a001
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1,3,5-Tris(N,N',N"-2,3-dihydroxybenzoyl)aminomethylbenzene, a synthetic iron chelator related to enterobactin
Michael C. Venuti, William H. Rastetter, and J. B. Neilands
pp 123 - 124; DOI:
10.1021/jm00188a002
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3-Substituted adenines. In vitro enzyme inhibition and antiviral activity
Tozo Fujii, Graham C. Walker, Nelson J. Leonard, Donald C. DeLong, and Koert Gerzon
pp 125 - 129; DOI:
10.1021/jm00188a003
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Structural requirements for progestational activity. Synthesis and properties of rac-8.alpha.,9.beta.,10.alpha.14.beta.-progesterone
A. J. Solo, Virendra Kumar, Vitauts Alks, and William L. Duax
pp 129 - 133; DOI:
10.1021/jm00188a004
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Potential antitumor agents. 29. Quantitative structure-activity relationships for the antileukemic bisquaternary ammonium heterocycles
William A. Denny, Graham J. Atwell, Bruce C. Baguley, and Bruce F. Cain
pp 134 - 150; DOI:
10.1021/jm00188a005
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Synthesis and antitumor activity of cyclophosphamide analogs. 2. Preparation, hydrolytic studies, and anticancer screening of 5-bromocyclophosphamide, 3,5-dehydrocyclophosphamide, and related systems
Susan Marie Ludeman, Gerald Zon, and William Egan
pp 151 - 158; DOI:
10.1021/jm00188a006
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Aryloxyalkyloxy- and aralkyloxy-4-hydroxy-3-nitrocoumarins which inhibit histamine release in the rat and also antagonize the effects of a slow reacting substance of anaphylaxis
Derek R. Buckle, D. James Outred, Janet W. Ross, Harry Smith, Raymond J. Smith, Barbara A. Spicer, and Brian C. Gasson
pp 158 - 168; DOI:
10.1021/jm00188a007
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Synthesis and pharmacologic characterization of an alkylating analog chlornaltrexamine, of naltrexone with ultralong-lasting narcotic antagonist properties
P. S. Portoghese, D. L. Larson, J. B. Jiang, T. P. Caruso, and A. E. Takemori
pp 168 - 173; DOI:
10.1021/jm00188a008
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Optically pure (+)-nicotine from (.+-.)-nicotine and biological comparisons with (-)-nicotine
Mario D. Aceto, Billy R. Martin, Ibrahim M. Uwaydah, Everette L. May, Louis S. Harris, Consuelo Izazola-Conde, William L. Dewey, Thomas J. Bradshaw, and W. C. Vincek
pp 174 - 177; DOI:
10.1021/jm00188a009
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Synthesis of pyridinium analogs of acetylcholine and their interactions with intestinal muscarinic receptors
Dida Kuhnen-Clausen, Ilse Hagedorn, and Rudolf Bill
pp 177 - 180; DOI:
10.1021/jm00188a010
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Studies on 3-substituted 1,2-benzisoxazole derivatives. 6. Syntheses of 3-(sulfamoylmethyl)-1,2-benzisoxazole derivatives and their anticonvulsant activities
Hitoshi Uno, Mikio Kurokawa, Yoshinobu Masuda, and Haruki Nishimura
pp 180 - 183; DOI:
10.1021/jm00188a011
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Azetidine derivatives of tricyclic antidepressant agents
Piero Melloni, Arturo Della Torre, Maurizio Meroni, Anna Ambrosini, and Alessandro C. Rossi
pp 183 - 191; DOI:
10.1021/jm00188a012
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Easily hydrolyzable, water-soluble derivatives of (.+-.)-.alpha.-5-[1-(indol-3-yl)ethyl]-2-methylamino-.DELTA.2-thiazolin-4-one, a novel antiviral compound
Michael R. Harnden, Stuart Bailey, Malcolm R. Boyd, J. Bruce Wilkinson, and Nicholas D. Wright
pp 191 - 195; DOI:
10.1021/jm00188a013
PDF
Electrochemical oxidation of hydroxylated phenothiazine and imipramine derivatives
Marilyn Neptune, Richard L. McCreery, and Albert A. Manian
pp 196 - 199; DOI:
10.1021/jm00188a014
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Synthesis of steroidal nitrosoureas with antitumor activity
Hing-Yat P. Lam, Asher Begleiter, Gerald J. Goldenberg, and Chiu-Ming Wong
pp 200 - 202; DOI:
10.1021/jm00188a015
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Phototoxicity of chlorpromazine
Nigel J. Bunce, Yogesh Kumar, and Luis Ravanal
pp 202 - 204; DOI:
10.1021/jm00188a016
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Aminotetralins as narcotic antagonists. Synthesis and opiate-related activity of 1-phenyl-1-aminotetralin derivatives
William G. Reifenrath and David S. Fries
pp 204 - 206; DOI:
10.1021/jm00188a017
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Bicyclic pyrazolines, potential central nervous system depressants and antiinflammatory agents
John Krapcho and Chester F. Turk
pp 207 - 210; DOI:
10.1021/jm00188a018
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Synthesis and preliminary biological studies of 4- and 5-[2-hydroxy-3-(isopropylamino)propoxy]benzimidazoles: selective β2 adrenergic blocking agents
C. Richard Crooks, Jeremy Wright, Patrick S. Callery, and J. Edward Moreton
pp 210 - 214; DOI:
10.1021/jm00188a019
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Book Reviews

pp 214 - 214; DOI:
10.1021/jm00188a600
PDF

Issue 3


Conformational analysis of podophyllotoxin and its congeners. Structure-activity relationship in microtubule assembly
C. Fred Brewer, John D. Loike, Susan B. Horwitz, Himan Sternlicht, and Walter J. Gensler
pp 215 - 221; DOI:
10.1021/jm00189a001
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A model for thyroid hormone-receptor interactions
Tariq A. Andrea, Stephen W. Dietrich, Wallace J. Murray, Peter A. Kollman, Eugene C. Jorgensen, and Steve Rothenberg
pp 221 - 232; DOI:
10.1021/jm00189a002
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Coenzyme-substrate adducts as inhibitors of mouse liver 3,4-dihydroxyphenylalanine decarboxylase
E. A. Rudd, W. C. Cunningham, and J. W. Thanassi
pp 233 - 237; DOI:
10.1021/jm00189a003
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Cyclic amidine inhibitors of indolamine N-methyltransferase
Joshua Rokach, Pierre Hamel, Norman R. Hunter, Grant Reader, Clarence S. Rooney, Paul S. Anderson, Edward J. Cragoe, and Lewis R. Mandel
pp 237 - 247; DOI:
10.1021/jm00189a004
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Synthesis and activities of antitumor agents
Tetsuo Suami, Tomoya Machinami, and Takashi Hisamatsu
pp 247 - 250; DOI:
10.1021/jm00189a005
PDF
Potential antitumor agents. 30. Mutagenic activity of some 9-anilinoacridines: relationships between structure, mutagenic potential, and antileukemic activity
Lynnette R. Ferguson and William A. Denny
pp 251 - 255; DOI:
10.1021/jm00189a006
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Deoxymorphines: role of the phenolic hydroxyl in antinociception and opiate receptor interactions
Juergen Reden, Marvin F. Reich, Kenner C. Rice, Arthur E. Jacobson, Arnold Brossi, Richard A. Streaty, and Werner A. Klee
pp 256 - 259; DOI:
10.1021/jm00189a007
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Metabolic oxidation of nicotine to chemically reactive intermediates
Trong Lang Nguyen, Larry D. Gruenke, and Neal Castagnoli Jr.
pp 259 - 263; DOI:
10.1021/jm00189a008
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Antiallergy agents. 1. 1,6-Dihydro-6-oxo-2-phenylpyrimidine-5-carboxylic acids and esters
Peter F. Juby, Thomas W. Hudyma, Myron Brown, John M. Essery, and Richard A. Partyka
pp 263 - 269; DOI:
10.1021/jm00189a009
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Synthesis and some pharmacological properties of 8-L-methionine-oxytocin
Miklos Bodanszky, Nagarajan Chandramouli, Jean Martinez, and Roderich Walter
pp 270 - 273; DOI:
10.1021/jm00189a010
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Prodrugs of 9-(.beta.-D-arabinofuranosyl)adenine. 2. Synthesis and evaluation of a number of 2',3'- and 3',5'-di-O-acyl derivatives
David C. Baker, Theodore H. Haskell, Sterling R. Putt, and Bernard J. Sloan
pp 273 - 279; DOI:
10.1021/jm00189a011
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New bronchodilators. Synthesis and bronchodilating activity of some 3-(alkoxymethyl)-.alpha.-(N-substituted aminomethyl)-4-hydroxybenzyl alcohols
Shigeru Sohda, Masatoshi Fujimoto, Tomozo Tamegai, and Noriyasu Hirose
pp 279 - 286; DOI:
10.1021/jm00189a012
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Cardenolide analogs. 9. Synthesis and biological activity of 17.beta.-carbomethoxyethylene and 17.beta.-cyanoethylene 14.alpha.-H steroids
Alex Gelbart, John Boutagy, and Richard Thomas
pp 287 - 290; DOI:
10.1021/jm00189a013
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Studies on antianaphylactic agents. 6. Synthesis of some metabolites of 6-ethyl-3-(1H-tetrazol-5-yl)chromone and their analogs
Akira Nohara, Hisashi Kuriki, Toshihiro Ishiguro, Taketoshi Saijo, Kiyoshi Ukawa, Yoshitaka Maki, and Yasushi Sanno
pp 290 - 295; DOI:
10.1021/jm00189a014
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2-Mercaptoacetamidines as gastric antisecretory agents
William A. Bolhofer, Charles N. Habecker, Adolph M. Pietruszkiewicz, Mary Lou Torchiana, Henry I. Jacoby, and Clement A. Stone
pp 295 - 301; DOI:
10.1021/jm00189a015
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Inhibition of gastric acid secretion by 1,8-naphthyridin-2(1H)-ones
William A. Bolhofer, Jacob M. Hoffman, Charles N. Habecker, Adolph M. Pietruszkiewicz, Edward J. Cragoe, and Mary Lou Torchiana
pp 301 - 306; DOI:
10.1021/jm00189a016
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An attempt to apply lethal synthesis to the design of chemotherapeutic agents. Fluorinated 5.beta.-(hydroxyethyl)-4-methylthiazoles
Sydney Archer and Cecily Perianayagam
pp 306 - 309; DOI:
10.1021/jm00189a017
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Prodrug analogs of the antitumor alkaloid camptothecin
John A. Adamovics and C. Richard Hutchinson
pp 310 - 314; DOI:
10.1021/jm00189a018
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Synthesis and antitumor activity of water-soluble (2-chloroethyl)nitrosoureas
Tetsuo Suami, Kinichi Tadano, and William T. Bradner
pp 314 - 316; DOI:
10.1021/jm00189a019
PDF
5-Substituted uracil arabinonucleosides as potential antiviral agents
P. F. Torrence, G. F. Huang, M. W. Edwards, B. Bhooshan, J. Descamps, and E. De Clercq
pp 316 - 319; DOI:
10.1021/jm00189a020
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Enzyme affinity of the 5,6-dihydro derivatives of the substrate and product of thymidylate synthetase catalysis
Joon Sup Park, Charles T. C. Chang, and Mathias P. Mertes
pp 319 - 321; DOI:
10.1021/jm00189a021
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Preparation and antidiabetic activity of some sulfonylurea derivatives of 3,5-disubstituted pyrazoles
Raafat Soliman
pp 321 - 325; DOI:
10.1021/jm00189a022
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Differential solubilities in subregions of the membrane: a nonsteric mechanism of drug specificity
Emmanuel M. Landau, Jacob Richter, and Sasson Cohen
pp 325 - 327; DOI:
10.1021/jm00189a023
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Paradoxical effects of N-cyanoalkyl substituents upon the activities of several classes of opioids
Arthur E. Jacobson, Kenner C. Rice, Juergen Reden, Lillian Lupinacci, Arnold Brossi, Richard A. Streaty, and Werner A. Klee
pp 328 - 331; DOI:
10.1021/jm00189a024
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Conformations, DNA binding parameters, and antileukemic activity of certain cytotoxic protoberberine alkaloids
Mark Cushman, Frederick W. Dekow, and Linda B. Jacobsen
pp 331 - 333; DOI:
10.1021/jm00189a025
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Synthesis and pharmacological properties of [5-isoleucine]-, [8-isoleucine]-, and [5,8-diisoleucine]bradykinin
Andrew T. Chiu, Alan R. Day, Jeffrey A. Radding, and Richard J. Freer
pp 334 - 335; DOI:
10.1021/jm00189a026
PDF
Book Reviews

pp 336 - 338; DOI:
10.1021/jm00189a600
PDF

Issue 4


Trans-5-(3,3,3-trifluoro-1-propenyl)-2'-deoxyuridylate: a mechanism-based inhibitor of thymidylate synthetase
Yusuke Wataya, Akira Matsuda, Daniel V. Santi, Donald E. Bergstrom, and Jerry L. Ruth
pp 339 - 340; DOI:
10.1021/jm00190a001
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Rigid congeners of dopamine based on octahydrobenzo[f]quinoline: peripheral and central effects
Joseph G. Cannon, Cecilia Suarez-Gutierrez, Teresa Lee, John Paul Long, Brenda Costall, David H. Fortune, and Robert J. Naylor
pp 341 - 347; DOI:
10.1021/jm00190a002
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Drug-induced modifications of the immune response. 1. Substituted 1-phenylisoquinolines
V. S. Georgiev, Richard P. Carlson, Richard G. Van Inwegen, and Atul Khandwala
pp 348 - 352; DOI:
10.1021/jm00190a003
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Inhibition of uptake of catecholamines by benzylamine derivatives
R. Craig Kammerer, Bahman Amiri, and Arthur K. Cho
pp 352 - 355; DOI:
10.1021/jm00190a004
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3-Substituted pyrazole derivatives as inhibitors and inactivators of liver alcohol dehydrogenase
Richard W. Fries, David P. Bohlken, and Bryce V. Plapp
pp 356 - 359; DOI:
10.1021/jm00190a005
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Quantitative structure-activity relationships for biguanides, carbamimidates, and bisbiguanides as inhibitors of Streptococcus mutans No. 6715
Victor D. Warner, Donald M. Lynch, Ki Hwan Kim, and Gary L. Grunewald
pp 359 - 366; DOI:
10.1021/jm00190a006
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Quantitative structure-activity relationships in 1-aryl-2-(alkylamino)ethanol antimalarials
Ki Hwan Kim, Corwin Hansch, James Y. Fukunaga, Edward E. Steller, Priscilla Y. C. Jow, Paul N. Craig, and June Page
pp 366 - 391; DOI:
10.1021/jm00190a007
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Structure-activity relationships of dimeric Catharanthus alkaloids. 2. Experimental antitumor activities of N-substituted deacetylvinblastine amide (vindesine) sulfates
Robert A. Conrad, George J. Cullinan, Koert Gerzon, and Gerald A. Poore
pp 391 - 400; DOI:
10.1021/jm00190a008
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Use of the butaclamol template in a search for antipsychotic agents with lessened side effects
Michael J. Kukla, James L. Bloss, and Linda R. Brougham
pp 401 - 406; DOI:
10.1021/jm00190a009
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Synthesis and antitumor activity of sugar-ring hydroxyl analogs of daunorubicin
Ernst F. Fuchs, Derek Horton, Wolfgang Weckerle, and Eva Winter-Mihaly
pp 406 - 411; DOI:
10.1021/jm00190a010
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Antianaphylactic agents. 1. 2-(Acylamino)oxazoles
W. J. Ross, R. G. Harrison, M. R. J. Jolley, M. C. Neville, A. Todd, J. P. Verge, W. Dawson, and W. J. F. Sweatman
pp 412 - 417; DOI:
10.1021/jm00190a011
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Pharmacologically active sulfoximides: 5-hexyl-7-(S-methylsulfonimidoyl)xanthone-2-carboxylic acid, a potent antiallergic agent
Alan C. Barnes, Peter W. Hairsine, Saroop S. Matharu, Peter J. Ramm, and John B. Taylor
pp 418 - 424; DOI:
10.1021/jm00190a012
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Biological properties of transition-metal organometallic compounds. 3. .beta.-Ferrocenylalanine
Robert P. Hanzlik, Phyllis Soine, and William H. Soine
pp 424 - 428; DOI:
10.1021/jm00190a013
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Serotonin receptor binding affinities of tryptamine analogs
Richard A. Glennon and Peter K. Gessner
pp 428 - 432; DOI:
10.1021/jm00190a014
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Aminoglycoside antibiotics. 2. N, N-Dialkylkanamycins
Virendra Kumar and William A. Remers
pp 432 - 436; DOI:
10.1021/jm00190a015
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Novel application of proton nuclear magnetic resonance spectroscopy in the identification of 2'-chloronordiazepam metabolites in the dog
Thomas H. Williams, Gino J. Sasso, John J. Ryan, and Morton A. Schwartz
pp 436 - 440; DOI:
10.1021/jm00190a016
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.beta.-Adrenoceptor studies. 5. Proton NMR and IR spectroscopic analysis of the conformation of the hydrohalide salts of .beta.-adrenoceptor-blocking aryloxypropanolamines. Evidence for a seven-membered ring structure with participation of two hydrogen bonds
Johan Zaagsma
pp 441 - 449; DOI:
10.1021/jm00190a017
PDF
Potential organ- or tumor-imaging agents. 18. Radioiodinated diamines and bisquaternaries
C. C. Huang, N. Korn, and R. E. Counsell
pp 449 - 452; DOI:
10.1021/jm00190a018
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A new chemical series active against African trypanosomes: benzyltriphenylphosphonium salts
Kenneth E. Kinnamon, Edgar A. Steck, and Dora S. Rane
pp 452 - 455; DOI:
10.1021/jm00190a019
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Synthesis and pharmacological activity of 2,3,4,5-tetrahydro-1,5-methano-1H-3-benzazepines
Paul H. Mazzocchi and Barbara C. Stahly
pp 455 - 457; DOI:
10.1021/jm00190a020
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Resolution and absolute configuration of trans-2-(2,5-dimethoxy-4-methylphenyl)cyclopropylamine, a potent hallucinogen analog
David E. Nichols, Ronald Woodard, Bruce A. Hathaway, Martin T. Lowy, and George K. W. Yim
pp 458 - 460; DOI:
10.1021/jm00190a021
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Book Reviews

pp 461 - 462; DOI:
10.1021/jm00190a600
PDF

Issue 5


Propiolaldehyde, a pargyline metabolite that irreversibly inhibits aldehyde dehydrogenase. Isolation from a hepatic microsomal system
Frances N. Shirota, Eugene G. DeMaster, and Herbert T. Nagasawa
pp 463 - 464; DOI:
10.1021/jm00191a001
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Classification of drugs by discriminant analysis using fragment molecular connectivity values
Douglas R. Henry and John H. Block
pp 465 - 472; DOI:
10.1021/jm00191a002
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Ames test of 1-(X-phenyl)-3,3-dialkyltriazenes. A quantitative structure-activity study
Benjamin H. Venger, Corwin Hansch, Gerard J. Hatheway, and Yost U. Amrein
pp 473 - 476; DOI:
10.1021/jm00191a003
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Computer-assisted structure-activity studies of chemical carcinogens. A heterogeneous data set
Peter C. Jurs, J. T. Chou, and M. Yuan
pp 476 - 483; DOI:
10.1021/jm00191a004
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Multivariate analysis and quantitative structure-activity relationships. Inhibition of dihydrofolate reductase and thymidylate synthetase by quinazolines
Bor-Kuan Chen, Csaba Horvath, and Joseph R. Bertino
pp 483 - 491; DOI:
10.1021/jm00191a005
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Quantitative structure-activity relationships in 2,5-bis(1-aziridinyl)-p-benzoquinone derivatives against leukemia L-1210
Masafumi Yoshimoto, Hachio Miyazawa, Hideo Nakao, Kenkichi Shinkai, and Masao Arakawa
pp 491 - 496; DOI:
10.1021/jm00191a006
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Alkylating nucleosides. 1. Synthesis and cytostatic activity of N-glycosyl(halomethyl)-1,2,3-triazoles. A new type of alkylating agent
Federico G. De las Heras, Rosario Alonso, and Gregorio Alonso
pp 496 - 501; DOI:
10.1021/jm00191a007
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Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity
Robert K. Y. Zee-Cheng, Eugene G. Podrebarac, C. S. Menon, and C. C. Cheng
pp 501 - 505; DOI:
10.1021/jm00191a008
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Synthesis of 3,4-dihydro-4-oxothieno[2,3-d]pyrimidine-2-carboxylates, a new series of orally active antiallergy agents
D. L. Temple, J. P. Yevich, R. R. Covington, C. A. Hanning, R. J. Seidehamel, H. K. Mackey, and M. J. Bartek
pp 505 - 510; DOI:
10.1021/jm00191a009
PDF
Antiviral activity of aliphatic nucleoside analogs: structure-function relationship
E. De Clercq and A. Holy
pp 510 - 513; DOI:
10.1021/jm00191a010
PDF
Synthesis and antitumor and antiviral activities of 1-.beta.-D-arabinofuranosyl-2-amino-1,4(2H)-iminopyrimidine, and its derivatives
A. Mohsin Mian, Robert A. Long, Lois B. Allen, Robert W. Sidwell, Roland K. Robins, and Tasneem A. Khwaja
pp 514 - 518; DOI:
10.1021/jm00191a011
PDF
Improved antitumor effects in 3'-branched homologs of 2'-deoxythioguanine. Synthesis and evaluation of thioguanine nucleosides of 2,3-dideoxy-3-(hydroxymethyl)-D-erythro-pentofuranose
Edward M. Acton, Richard N. Goerner, Hong S. Uh, Kenneth J. Ryan, David W. Henry, Carol E. Cass, and Gerald A. LePage
pp 518 - 525; DOI:
10.1021/jm00191a012
PDF
Synthesis and platelet aggregation inhibitory activity of 6-isobutyl-.alpha.-methyl-3-pyridineacetic acid
Ronald H. Rynbrandt, Burris D. Tiffany, Doris P. Balgoyen, Edward E. Nishizawa, and A. Rene Mendoza
pp 525 - 528; DOI:
10.1021/jm00191a013
PDF
Cardenolide analogs. 4. (20R)- and (20S)-cardanolides: on the roles of the 20(22)-ene and 14.beta.-hydroxyl in genin activity
Dwight S. Fullerton, Kouichi Yoshioka, Douglas C. Rohrer, Arthur H. L. From, and Khalil Ahmed
pp 529 - 533; DOI:
10.1021/jm00191a014
PDF
Conformational analogy between .beta.-lactam antibiotics and tetrahedral transition states of dipeptide
Donald B. Boyd
pp 533 - 537; DOI:
10.1021/jm00191a015
PDF
Syntheses, analgetic activity and physical dependence capacity of 5-phenyl-6,7-benzomorphan derivatives
Naokata Yokoyama, Prabodh I. Almaula, Fred B. Block, Frank R. Granat, Norman Gottfried, Ronald T. Hill, Elihu H. McMahon, Walter F. Munch, Howard Rachlin, and et al.
pp 537 - 553; DOI:
10.1021/jm00191a016
PDF
Synthesis and analgesic activities of some (4-substituted phenyl-1-piperazinyl)alkyl 2-aminobenzoates and 2-aminonicotinates
Philippe M. Manoury, Andre P. Dumas, Henry Najer, Dan Branceni, Monique Prouteau, and Francoise M. Lefevre-Borg
pp 554 - 559; DOI:
10.1021/jm00191a017
PDF
Synthesis and antibacterial activity of 2'-substituted chelocardin analogs
David L. Garmaise, Daniel T. W. Chu, Edith Bernstein, and Makoto Inaba
pp 559 - 564; DOI:
10.1021/jm00191a018
PDF
Synthetic antagonists of in vivo responses by the rat uterus to oxytocin
John Lowbridge, Maurice Manning, Jenny Seto, Jaya Haldar, and Wilbur H. Sawyer
pp 565 - 569; DOI:
10.1021/jm00191a019
PDF
Synthesis and chemical carcinogen inhibitory activity of 2-tert-butyl-4-hydroxyanisole
Luke K. T. Lam, Ramdas P. Pai, and Lee W. Wattenberg
pp 569 - 571; DOI:
10.1021/jm00191a020
PDF
Biomolecules bearing the S- or SeAsMe2 function: amino acid and steroid derivatives
Catherine H. Banks, James R. Daniel, and Ralph A. Zingaro
pp 572 - 575; DOI:
10.1021/jm00191a021
PDF
Platinum and palladium derivatives for chemotherapy studies
Carl Tabb Bahner, Truett C. Patterson, Lydia M. Rives, and Harry D. Harmon
pp 575 - 577; DOI:
10.1021/jm00191a022
PDF
Synthesis of all the stereoisomers of statine (4-amino-3-hydroxy-6-methylheptanoic acid). Inhibition of pepsin activity by N-carbobenzoxy-L-valyl-L-valyl-statine derived from the four stereoisomers
W. S. Liu, S. C. Smith, and G. I. Glover
pp 577 - 579; DOI:
10.1021/jm00191a023
PDF
Synthesis and biologic distribution of mercapto derivatives of palmitic acid
Eli Livni, Michael A. Davis, and Victor D. Warner
pp 580 - 583; DOI:
10.1021/jm00191a024
PDF
Potential radiosensitizing agents. Dinitroimidazoles
Krishna C. Agrawal, Kathleen B. Bears, Raj K. Sehgal, Joe N. Brown, Patricia E. Rist, and W. D. Rupp
pp 583 - 586; DOI:
10.1021/jm00191a025
PDF
Synthesis of a proposed thymic factor
Robert G. Strachan, William J. Paleveda, Susan J. Bergstrand, Ruth F. Nutt, Frederick W. Holly, and Daniel F. Veber
pp 586 - 588; DOI:
10.1021/jm00191a026
PDF
Synthesis of hydroxy- and amino-substituted benzohydroxamic acids: inhibition of ribonucleotide reductase and antitumor activity
Bart Van't Riet, Galen L. Wampler, and Howard L. Elford
pp 589 - 592; DOI:
10.1021/jm00191a027
PDF
Synthesis and biological activity of 5-fluoro- and 5-methyl-1,3-oxazine-2,6(3H)-dione
M. Bobek, S. Kuhar, and A. Bloch
pp 592 - 594; DOI:
10.1021/jm00191a028
PDF
A structural modification study of procarbazine
Louis T. Weinstock and C. C. Cheng
pp 594 - 597; DOI:
10.1021/jm00191a029
PDF
L-Chlorozotocin
Thomas P. Johnston, George S. McCaleb, Tom Anderson, and Donald S. Murinson
pp 597 - 599; DOI:
10.1021/jm00191a030
PDF
1-(Dichloroacetyl)-1,2,3,4-tetrahydro-6-quinolinol esters. New potent antiamebic agents
Denis M. Bailey, Eldridge M. Mount, James Siggins, John A. Carlson, Allen Yarinsky, and Ralph G. Slighter
pp 599 - 601; DOI:
10.1021/jm00191a031
PDF
Book Reviews

pp 601 - 602; DOI:
10.1021/jm00191a600
PDF

Issue 6


Intramolecular hydrogen bonding and conformational studies of bridged thebaine and oripavine opiate narcotic agonists and antagonists
Gilda H. Loew and Donald S. Berkowitz
pp 603 - 607; DOI:
10.1021/jm00192a001
PDF
Quantitative structure-activity relationships involving the inhibition of glycolic acid oxidase by derivatives of glycolic and glyoxylic acids
William C. Randall, Kermit B. Streeter, Emlen L. Cresson, Harvey Schwam, Stuart R. Michelson, Paul S. Anderson, Edward J. Cragoe, Haydn W. R. Williams, Eva Eichler, and C. Stanley Rooney
pp 608 - 614; DOI:
10.1021/jm00192a002
PDF
Quantitative structure-activity relationship of 5-(X-benzyl)-2,4-diaminopyrimidines inhibiting bovine liver dihydrofolate reductase
Jeffrey M. Blaney, Stephen W. Dietrich, Mark A. Reynolds, and Corwin Hansch
pp 614 - 617; DOI:
10.1021/jm00192a003
PDF
Synthesis of 5-selenium-substituted uracil derivatives. Inhibition of thymidylate synthetase by 5-hydroseleno-2'-deoxyuridylate
Seyuen Choi, T. I. Kalman, and T. J. Bardos
pp 618 - 621; DOI:
10.1021/jm00192a004
PDF
Design of species- or isozyme-specific enzyme inhibitors. I. Effect of thymidine substituents on affinity for the thymidine site of hamster cytoplasmic thymidine kinase
Alexander Hampton, Francis Kappler, and Ram R. Chawla
pp 621 - 631; DOI:
10.1021/jm00192a005
PDF
S-2,.omega.-Diaminoalkyl dihydrogen phosphorothioates as antiradiation agents
James R. Piper, Lucy M. Rose, Thomas P. Johnston, and Marie M. Grenan
pp 631 - 639; DOI:
10.1021/jm00192a006
PDF
Studies on biologically active nucleosides and nucleotides. 5. Synthesis and antitumor activity of some 2,2'-anhydro-1-(3',5'-di-O-acyl-.beta.-D-arabinofuranosyl)cytosine salts and 2,2'-anhydro-1-(3'-O-acyl-.beta.-D-arabinofuranosyl)cytosine 5'-phosphates
Kazuhiko Kondo, Takeo Nagura, Yoshihisa Arai, and Ichizo Inoue
pp 639 - 646; DOI:
10.1021/jm00192a007
PDF
Synthesis and antiviral activities of arabinofuranosyl-5-ethylpyrimidine nucleosides. Selective antiherpes activity of 1-(.beta.-D-arabinofuranosyl)-5-ethyluracil
Tadeusz Kulikowski, Zbigniew Zawadzki, David Shugar, Johan Descamps, and Erik De Clercq
pp 647 - 653; DOI:
10.1021/jm00192a008
PDF
Studies on the mechanism of antiviral action of 1-(.beta.-D-ribofuranosyl)-1,2,4-triazole-3-carboxamide (ribavirin)
Alicja K. Drabikowska, Lech Dudycz, and David Shugar
pp 653 - 657; DOI:
10.1021/jm00192a009
PDF
Orally active esters of cephalosporin antibiotics. 3. Synthesis and biological properties of aminoacyloxymethyl esters of 7-[D-(-)-mandelamido]-3-[[(1-methyl-1H-tetrazol-5-yl)thio]methyl]-3-cephem-4-carboxylic acid
W. J. Wheeler, D. A. Preston, W. E. Wright, G. W. Huffman, H. E. Osborne, and D. P. Howard
pp 657 - 661; DOI:
10.1021/jm00192a010
PDF
Chemical and biological studies of 1-(2,5-dihydroxy-4-methylphenyl)-2-aminopropane, an analog of 6-hydroxydopamine
Peyton Jacob, Toni Kline, and Neal Castagnoli
pp 662 - 671; DOI:
10.1021/jm00192a011
PDF
Synthesis and antihypertensive activity of novel 3-hydrazino-5-phenyl-1,2,4-triazines
William P. Heilman, Richard D. Heilman, James A. Scozzie, Robert J. Wayner, James M. Gullo, and Zaven S. Ariyan
pp 671 - 677; DOI:
10.1021/jm00192a012
PDF
Synthesis of 2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole derivatives and their central nervous system activities
Yasutaka Nagai, Akira Irie, Yoshinobu Masuda, Makoto Oka, and Hitoshi Uno
pp 677 - 683; DOI:
10.1021/jm00192a013
PDF
Glycerides as prodrugs. 1. Synthesis and antiinflammatory activity of 1,3-bis(alkanoyl)-2-(O-acetylsalicyloyl)glycerides (aspirin triglycerides)
Gerard Y. Paris, David L. Garmaise, Denis G. Cimon, Leo Swett, George W. Carter, and Patrick Young
pp 683 - 687; DOI:
10.1021/jm00192a014
PDF
.beta.-Adrenergic blocking agents with acute antihypertensive activity
J. J. Baldwin, E. L. Engelhardt, R. Hirschmann, G. F. Lundell, G. S. Ponticello, C. T. Ludden, C. S. Sweet, A. Scriabine, N. N. Share, and R. Hall
pp 687 - 694; DOI:
10.1021/jm00192a015
PDF
Synthesis of some 4-substituted 8-amino-6-methoxyquinolines as potential antimalarials
F. Ivy Carroll, Bertold Berrang, C. P. Linn, and Charles E. Twine
pp 694 - 699; DOI:
10.1021/jm00192a016
PDF
Synthesis and pharmacological evaluation of cis-3,4,4a,9a,-tetrahydro-1H-pyrano[3,4-b]benzofuran-1-ones. Tricyclic analogs related to the antilipidemic drug clofibrate
Donald T. Witiak, William Loh, Dennis R. Feller, John R. Baldwin, Howard A. I. Newman, Christine L. Sober, and Richard C. Cavestri
pp 699 - 705; DOI:
10.1021/jm00192a017
PDF
Pyranenamines: a new series of antiallergic compounds
Kenneth M. Snader, Lawrence W. Chakrin, Richard D. Cramer, Yoshiko M. Gelernt, Clara K. Miao, Dinubai H. Shah, Joseph W. Venslavsky, Chester R. Willis, and Blaine M. Sutton
pp 706 - 714; DOI:
10.1021/jm00192a018
PDF
Application of quantitative structure-activity relationships in the development of the antiallergic pyranenamines
Richard D. Cramer, Kenneth M. Snader, Chester R. Willis, Lawrence W. Chakrin, Jean Thomas, and Blaine M. Sutton
pp 714 - 725; DOI:
10.1021/jm00192a019
PDF
10-(Alkylamino)-4H-thieno[3,4-b][1,5]benzodiazepines. A novel class of potential neuroleptic agents
Jeffrey B. Press, Corris M. Hofmann, Nancy H. Eudy, William J. Fanshawe, Ivana P. Day, Eugene N. Greenblatt, and Sidney R. Safir
pp 725 - 731; DOI:
10.1021/jm00192a020
PDF
Preparation and purification of L-(.+-.)-5-formyl-5,6,7,8-tetrahydrofolic acid
Carroll Temple, Robert D. Elliott, Jerry D. Rose, and John A. Montgomery
pp 731 - 734; DOI:
10.1021/jm00192a021
PDF
Cardioselectivity of .beta.-adrenoceptor blocking agents. 1. 1-[(4-Hydroxyphenethyl)amino]-3-(aryloxy)propan-2-ols
W. J. Rzeszotarski, R. E. Gibson, W. C. Eckelman, and R. C. Reba
pp 735 - 737; DOI:
10.1021/jm00192a022
PDF
Conformational effects on the activity of drugs. 7. Synthesis and pharmacological properties of 2-(p-nitrophenyl)-substituted morpholines
A. Balsamo, P. Crotti, A. Lapucci, B. Macchia, F. Macchia, M. Del Tacca, L. Mazzanti, and R. Ceserani
pp 738 - 741; DOI:
10.1021/jm00192a023
PDF
Synthesis and biological activity of 8-oxadihydropteridines
Shwu-Ching Lin, Gary P. Holmes, Danny L. Dunn, and Charles G. Skinner
pp 741 - 743; DOI:
10.1021/jm00192a024
PDF
Synthesis and antibacterial activity of 2-oxocephalosporins
C. U. Kim, P. F. Misco, and D. N. McGregor
pp 743 - 745; DOI:
10.1021/jm00192a025
PDF
Synthesis of imidazolidinediones and oxazolidinediones from cyclization of propargylureas and propargyl carbamates
Sai-Keung Chiu, Leonard Keifer, and Jack W. Timberlake
pp 746 - 748; DOI:
10.1021/jm00192a026
PDF
Antiallergy activity of substituted 11-oxo-11H-pyrido[2,1-b]quinazoline-8-carboxylic acids
Charles F. Schwender, Brooks R. Sunday, David J. Herzig, Edward K. Kusner, P. R. Schumann, and Daniel L. Gawlak
pp 748 - 750; DOI:
10.1021/jm00192a027
PDF
Blood glucose lowering sulfonamides with asymmetric carbon atoms. 3. Related N-substituted carbamoylbenzoic acids
Clemens Rufer and Wolfgang Losert
pp 750 - 752; DOI:
10.1021/jm00192a028
PDF
Book Reviews

pp 752 - 756; DOI:
10.1021/jm00192a600
PDF

Issue 7


Synthetic studies on β-lactam antibiotics. Part 10. Synthesis of 7β-[2-carboxy-2-(4-hydroxyphenyl)acetamido]-7.alpha.-methoxy-3-[[(1-methyl-1H-tetrazol-5-yl)thio]methyl]-1-oxa-1-dethia-3-cephem-4-carboxylic acid disodium salt (6059-S) and its related 1-oxacephems
Masayuki Narisada, Tadashi Yoshida, Hiroshi Onoue, Mitsuaki Ohtani, Tetsuo Okada, Teruji Tsuji, Ikuo Kikkawa, Nobuhiro Haga, Hisashi Satoh, and et al.
pp 757 - 759; DOI:
10.1021/jm00193a001
PDF
Cyclopropylamines as suicide substrates for cytochromes P-450
Robert P. Hanzlik, Vimal Kishore, and Robert Tullman
pp 759 - 761; DOI:
10.1021/jm00193a002
PDF
Mapping the dopamine receptor. 1. Features derived from modifications in ring E of the neuroleptic butaclamol
Leslie G. Humber, Francois T. Bruderlein, Adolf H. Philipp, Manfred Goetz, and Katherine Voith
pp 761 - 767; DOI:
10.1021/jm00193a003
PDF
Mapping the dopamine receptor. 2. Features derived from modifications in the rings A/B region of the neuroleptic butaclamol
Adolf H. Philipp, Leslie G. Humber, and Katherine Voith
pp 768 - 773; DOI:
10.1021/jm00193a004
PDF
Peptide hormones. 137. Structural requirements in positions 1, 2, 3, and 6 of the luteinizing hormone-releasing hormone (LH-RH) for antiovulatory activity
John Humphries, Yieh-Ping Wan, Tadeusz Wasiak, Karl Folkers, and Cyril Y. Bowers
pp 774 - 777; DOI:
10.1021/jm00193a005
PDF
Electronic structures of cephalosporins and penicillins. 9. Departure of a leaving group in cephalosporins
Donald B. Boyd and W. H. W. Lunn
pp 778 - 784; DOI:
10.1021/jm00193a006
PDF
Mathematical considerations in series design
Yvonne Connolly Martin and Helen Nehrich Panas
pp 784 - 791; DOI:
10.1021/jm00193a007
PDF
Computer assisted structure-activity studies of chemical carcinogens. An N-nitroso compound data set
J. T. Chou and Peter C. Jurs
pp 792 - 797; DOI:
10.1021/jm00193a008
PDF
Actinomycin D oxazinones as improved antitumor agents
Sisir K. Sengupta, Dorothy H. Trites, Maddula S. Madhavarao, and William R. Beltz
pp 797 - 802; DOI:
10.1021/jm00193a009
PDF
Synthesis, base-catalyzed hydrolytic reactivity, and anticancer evaluation of O-aryl phosphorodiamidates as a novel class of pro(phosphorodiamidic acid mustards)
Fang-Ting Chiu, Fai-Po Tsui, and Gerald Zon
pp 802 - 807; DOI:
10.1021/jm00193a010
PDF
Alkylating nucleosides. 2. Synthesis and cytostatic activity of bromomethylpyrazole and pyrazole nitrogen mustard nucleosides
M. Teresa Garcia-Lopez, Rosario Herranz, and Gregorio Alonso
pp 807 - 811; DOI:
10.1021/jm00193a011
PDF
2'-O-Acyl-6-thioinosine cyclic 3',5'-phosphates as prodrugs of thioinosinic acid
Rich B. Meyer, Thomas E. Stone, and Buddy Ullman
pp 811 - 815; DOI:
10.1021/jm00193a012
PDF
Inhibition of rat passive cutaneous anaphylaxis by 3-(tetrazol-5-yl)quinolines
Edward H. Erickson, Carol F. Hainline, Larry S. Lenon, Charles J. Matson, Thomas K. Rice, Karl F. Swingle, and Michael Van Winkle
pp 816 - 823; DOI:
10.1021/jm00193a013
PDF
Azaprostanoic acid derivatives. Inhibitors of arachidonic acid induced platelet aggregation
D. L. Venton, Steven E. Enke, and G. C. LeBreton
pp 824 - 830; DOI:
10.1021/jm00193a014
PDF
Acute effects of alkylating agents on canine renal function. 1. [4-(2-Bromoalkanoyl)phenoxy]acetic acids
Daniel A. Koechel, Gary O. Rankin, and William R. Sloan
pp 830 - 834; DOI:
10.1021/jm00193a015
PDF
Synthesis and analgesic activity of some spiro[dibenz[b,f]oxepin-10,4'-piperidine] derivatives
Helen H. Ong, James A. Profitt, Theodore C. Spaulding, and Jeffrey C. Wilker
pp 834 - 839; DOI:
10.1021/jm00193a016
PDF
Synthesis and hypoglycemic activity of pyridylalcohols
Benjamin Blank, Nicholas W. DiTullio, Arnold J. Krog, and Harry L. Saunders
pp 840 - 844; DOI:
10.1021/jm00193a017
PDF
Synthesis and biological activity of cocaine analogs. 2. 6H-[2]Benzopyrano[4,3-c]pyridin-6-ones
Edward S. Lazer, Gilbert J. Hite, Karl A. Nieforth, and Eugene S. Stratford
pp 845 - 849; DOI:
10.1021/jm00193a018
PDF
Folate analogs altered in the C9-N10 bridge region: 11-thiohomofolic acid
M. G. Nair, Shiang-Yuan Chen, Roy L. Kisliuk, Y. Gaumont, and D. Strumpf
pp 850 - 855; DOI:
10.1021/jm00193a019
PDF
2-Acetylpyridine thiosemicarbazones. 1. A new class of potential antimalarial agents
Daniel L. Klayman, Joseph F. Bartosevich, T. Scott Griffin, Carl J. Mason, and John P. Scovill
pp 855 - 862; DOI:
10.1021/jm00193a020
PDF
Analogs of methotrexate
John A. Montgomery, James R. Piper, Robert D. Elliott, Carroll Temple, Eugene C. Roberts, and Y. F. Shealy
pp 862 - 868; DOI:
10.1021/jm00193a021
PDF
Methotrexate analogs. 12. Synthesis and biological properties of some aza homologs
Jack E. Martinelli, Michael Chaykovsky, Roy L. Kisliuk, Yvette Gaumont, and Marc C. Gittelman
pp 869 - 874; DOI:
10.1021/jm00193a022
PDF
Synthesis of aza homologs of folic acid
Jack E. Martinelli, Michael Chaykovsky, Roy L. Kisliuk, and Yvette Gaumont
pp 874 - 877; DOI:
10.1021/jm00193a023
PDF
Dipeptides of O-methyl-L-threonine as potential antimalarials
Herman Gershon and Ira S. Krull
pp 877 - 879; DOI:
10.1021/jm00193a024
PDF
Some 11-substituted tetrahydrocannabinols. Synthesis and comparison with the potent cannabinoid metabolites 11-hydroxytetrahydrocannabinols
Raymond S. Wilson, B. R. Martin, and W. L. Dewey
pp 879 - 882; DOI:
10.1021/jm00193a025
PDF
2',3'-Bis(2-chloroethyl)aminophosphoryl-3'-amino-3'-deoxyadenosine: a cyclic nucleotide with antitumor activity
A. Okruszek and J. G. Verkade
pp 882 - 885; DOI:
10.1021/jm00193a026
PDF
Some 9-hydroxycannabinoid-like compounds. Synthesis and evaluation of analgesic and behavioral properties
Raymond S. Wilson, Everett L. May, and W. L. Dewey
pp 886 - 888; DOI:
10.1021/jm00193a027
PDF
N-(2-Cyanoethyl) derivatives of meperidine, ketobemidone, and a potent 6,7-benzomorphan
Ibrahim M. Uwaydah, M. Kathleen Waddle, and Michael E. Rogers
pp 889 - 890; DOI:
10.1021/jm00193a028
PDF
Active-site studies of neurohypophyseal hormones: synthesis and pharmacological properties of [5-(N4,N4-dimethylasparagine)]oxytocin
Roderich Walter, Glenn L. Stahl, Themistoeles Caplaneris, Paul Cordopatis, and Dimitrios Theodoropoulos
pp 890 - 893; DOI:
10.1021/jm00193a029
PDF
Book Reviews

pp 893 - 896; DOI:
10.1021/jm00193a600
PDF

Issue 8


Phosphorus-31 NMR investigations of phosphoramide mustard: evaluation of pH control over the rate of intramolecular cyclization to an aziridinium ion and the hydrolysis of this reactive alkylator
Thomas W. Engle, Gerald Zon, and William Egan
pp 897 - 899; DOI:
10.1021/jm00194a001
PDF
(+)-Isobutaclamol: a crystallographic, pharmacological, and biochemical study
L. G. Humber, A. H. Philipp, K. Voith, T. Pugsley, W. Lippmann, F. R. Ahmed, and M. Przybylska
pp 899 - 901; DOI:
10.1021/jm00194a002
PDF
N-Alkyl derivatives of (.+-.)-.alpha.-methyldopamine
Joseph G. Cannon, Zurilma Perez, John Paul Long, David B. Rusterholz, Jan R. Flynn, Brenda Costall, David H. Fortune, and Robert J. Naylor
pp 901 - 907; DOI:
10.1021/jm00194a003
PDF
Conformational analogs of dopamine. Synthesis and pharmacological activity of (E)- and (Z)-2-(3,4-dihydroxyphenyl)cyclopropylamine hydrochlorides
Paul W. Erhardt, Richard J. Gorczynski, and William G. Anderson
pp 907 - 911; DOI:
10.1021/jm00194a004
PDF
Adriamycin analogs. 3. Synthesis of N-alkylated anthracyclines with enhanced efficacy and reduced cardiotoxicity
George L. Tong, Helen Y. Wu, Thomas H. Smith, and David W. Henry
pp 912 - 918; DOI:
10.1021/jm00194a005
PDF
A phenazine analog of actinomycin D
Carol W. Mosher, Daw-Yuan Lee, Rudyard M. Enanoza, Priscilla A. Sturm, and Karl F. Kuhlmann
pp 918 - 922; DOI:
10.1021/jm00194a006
PDF
7-(Aminoethyl) ether and thioether of daunomycinone
Edward M. Acton, George L. Tong, Carol W. Mosher, Thomas H. Smith, and David W. Henry
pp 922 - 926; DOI:
10.1021/jm00194a007
PDF
Synthesis and biological activities of arginine-vasopressin analogs designed from a conformation-activity approach
Christopher R. Botos, Clark W. Smith, Yun-Lai Chan, and Roderich Walter
pp 926 - 931; DOI:
10.1021/jm00194a008
PDF
Tripeptide analogs of melanocyte-stimulating hormone release-inhibiting hormone (Pro-Leu-Gly-NH2) as inhibitors of oxotremorine-induced tremor
Sven Bjoerkman, Staffan Castensson, and Hans Sievertsson
pp 931 - 935; DOI:
10.1021/jm00194a009
PDF
Synthesis and biological activity of peptide antagonists of luliberin (luteinizing hormone-releasing hormone)
G. W. Moersch, M. C. Rebstock, E. L. Wittle, F. J. Tinney, E. D. Nicolaides, M. P. Hutt, T. F. Mich, J. M. Vandenbelt, R. E. Edgren, and et al.
pp 935 - 943; DOI:
10.1021/jm00194a010
PDF
Synthesis of fused [1,2,6]thiadiazine 1,1-dioxides as potential transition-state analog inhibitors of xanthine oxidase and guanase
Rich B. Meyer and Edward B. Skibo
pp 944 - 948; DOI:
10.1021/jm00194a011
PDF
3-Phenyl-5-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]indole-2-carbonitrile, a potent inhibitor of prostaglandin synthetase and of platelet aggregation
Kenneth E. Fahrenholtz, Mary Z. Silverzweig, Nicholas Germane, Herman J. Crowley, Beverly A. Simko, and Colin Dalton
pp 948 - 953; DOI:
10.1021/jm00194a012
PDF
5-Fluoro-2'-deoxyuridine 5'-(p-azidophenyl phosphate), a potential photoaffinity label of thymidylate synthetase
Lawrence G. Stephanson and John M. Whiteley
pp 953 - 957; DOI:
10.1021/jm00194a013
PDF
Synthesis of arabinofuranosyl derivatives of 3-deazaguanine
Mohindar S. Poonian, Warren W. McComas, and Michael J. Kramer
pp 958 - 962; DOI:
10.1021/jm00194a014
PDF
Synthesis and antiestrogenic activity of [3,4-dihydro-2-(4-methoxyphenyl)-1-naphthalenyl][4-[2-(1-pyrrolidinyl)ethoxy]phenyl]methanone, methanesulfonic acid salt
Charles D. Jones, Tulio Suarez, Eddie H. Massey, Larry J. Black, and Frank C. Tinsley
pp 962 - 966; DOI:
10.1021/jm00194a015
PDF
Synthesis of 11.beta.,13.beta.- and 13.beta.,16.beta.-propano steroids: probes of hormonal activity
Colin G. Pitt, Douglas H. Rector, Clarence E. Cook, and Mansukh C. Wani
pp 966 - 970; DOI:
10.1021/jm00194a016
PDF
Synthesis and biological activity of potential antimetabolites of L-fucose
Jesse A. May and Alan C. Sartorelli
pp 971 - 976; DOI:
10.1021/jm00194a017
PDF
Vinylogous carbinolamine tumor inhibitors. 4. Antileukemic activity of derivatives of 1,2-dimethyl-3,4-bis(hydroxymethyl)-5-phenylpyrrole bis(N-methylcarbamate)
Wayne K. Anderson and Michael J. Halat
pp 977 - 980; DOI:
10.1021/jm00194a018
PDF
Structure-mutagenicity relationships of N-oxidized derivatives of aniline, o-toluidine, 2'-methyl-4-aminobiphenyl, and 3,2'-dimethyl-4-aminobiphenyl
Stephen S. Hecht, Karam El-Bayoumy, Lorraine Tulley, and Edmond LaVoie
pp 981 - 987; DOI:
10.1021/jm00194a019
PDF
Distance geometry approach to rationalizing binding data
Gordon M. Crippen
pp 988 - 997; DOI:
10.1021/jm00194a020
PDF
Synthesis of benzo-15-crown-5 polyethers, anticoccidial ionophore analogs
George R. Brown and Alan J. Foubister
pp 997 - 999; DOI:
10.1021/jm00194a021
PDF
Alkenylidene bisphenols, a new class of bisphenol bactericide
Robert A. Conradi, James C. Vander Wyk, and Stephen B. Bowlus
pp 1000 - 1002; DOI:
10.1021/jm00194a022
PDF
Antimycotic imidazoles. Part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent
J. Heeres, L. J. J. Backx, J. H. Mostmans, and J. Van Cutsem
pp 1003 - 1005; DOI:
10.1021/jm00194a023
PDF
Antimalarials. 11. Synthesis of 3- and 5-aminoquinolines as potential antimalarials
M. Sami Khan and M. P. LaMontagne
pp 1005 - 1008; DOI:
10.1021/jm00194a024
PDF
Adamantylthiourea derivatives as antiviral agents
Jefferson W. Tilley, Paul Levitan, and Michael J. Kramer
pp 1009 - 1010; DOI:
10.1021/jm00194a025
PDF
Nicotinamide adenine dinucleotide phosphate-decanaldehyde adduct as an inhibitor of beef brain NADP-linked aldehyde reductase
John F. Towell, V. Gene Erwin, and Richard A. Deitrich
pp 1011 - 1014; DOI:
10.1021/jm00194a026
PDF
Partial synthesis of 6'-hydroxycinchonine and its antiarrhythmic activity in mice
LaVerne D. Small, Harry Rosenberg, Peter U. Nwangwu, Terry L. Holcslaw, and Sidney J. Stohs
pp 1014 - 1016; DOI:
10.1021/jm00194a027
PDF
Hexofuranosyladenine nucleosides as substrates and inhibitors of calf intestional adenosine deaminase
Alan J. Grant and Leon M. Lerner
pp 1016 - 1018; DOI:
10.1021/jm00194a028
PDF

Issue 9


BLEDTA: tumor localization by a bleomycin analog containing a metal-chelating group
Leslie H. DeRiemer, Claude F. Meares, David A. Goodwin, and Carol I. Diamanti
pp 1019 - 1023; DOI:
10.1021/jm00195a001
PDF
Antitumor agents. 1. 1,4-Bis[(aminoalkyl)amino]-9,10-anthracenediones
K. C. Murdock, R. G. Child, P. F. Fabio, Robert D. Angier, Roslyn E. Wallace, Frederick E. Durr, and R. V. Citarella
pp 1024 - 1030; DOI:
10.1021/jm00195a002
PDF
Synthesis and biological evaluation of tetramisole analogs as inhibitors of alkaline phosphatase of the 6-thiopurine-resistant tumor sarcoma 180/TG
Chauder Li, Men Hui Lee, and Alan C. Sartorelli
pp 1030 - 1033; DOI:
10.1021/jm00195a003
PDF
Structural analogs of L-glutamic acid .gamma.-(4-hydroxyanilide) and .gamma.-(3,4-dihydroxyanilide) as potential agents against melanoma
A. Rosowsky, M. M. Wick, and S. H. Kim
pp 1034 - 1037; DOI:
10.1021/jm00195a004
PDF
Angiotensin II analogs. 12. Role of the aromatic ring of position 8 phenylalanine in pressor activity
Kun-Hwa Hsieh, Eugene C. Jorgensen, and Thomas C. Lee
pp 1038 - 1044; DOI:
10.1021/jm00195a005
PDF
Angiotensin II analogs. 13. Role of the hydroxyl group of position 4 tyrosine in pressor activity
Kun-Hwa Hsieh, Ilona C. Kiraly-Olah, Eugene C. Jorgensen, and Thomas C. Lee
pp 1044 - 1047; DOI:
10.1021/jm00195a006
PDF
Photoaffinity labeling of the angiotensin II receptor. 3. Receptor inactivation with photolabile hormone analogs
Emanuel H. F. Escher and Gaetan Guillemette
pp 1047 - 1050; DOI:
10.1021/jm00195a007
PDF
Synthesis and biological properties of N2-substituted spin-labeled analogs of actinomycin D
Birandra K. Sinha, Michael G. Cox, Colin F. Chignell, and Richard L. Cysyk
pp 1051 - 1055; DOI:
10.1021/jm00195a008
PDF
Antifungal agents. 5. Chemical modification of antibiotics from Polyangium cellulosum var fulvum. Alcohol, ketone, aldehyde and oxime analogs of ambruticin
David T. Connor and Maximillian Von Strandtmann
pp 1055 - 1059; DOI:
10.1021/jm00195a009
PDF
Fluorinated retinoic acids and their analogs. 1. Synthesis and biological activity of (4-methoxy-2,3,6-trimethylphenyl)nonatetraenoic acid analogs
Beverly A. Pawson, Ka-Kong Chan, James DeNoble, Ru Jen L. Han, Virginia Piermattie, Anthony C. Specian, Srisamorn Srisethnil, Patrick W. Trown, Oksana Bohoslawec, and et al.
pp 1059 - 1067; DOI:
10.1021/jm00195a010
PDF
(Aryloxy)[p-(aryloxy)phenyl]- and (aryloxy)[p-(arylthio)phenyl]acetic acids and esters as hypolipidemic agents
Ronald I. Trust, Francis J. McEvoy, and J. Donald Albright
pp 1068 - 1074; DOI:
10.1021/jm00195a011
PDF
Antiinflammatory agents. 1. Synthesis and antiinflammatory activity of 2-amino-3-benzoylphenylacetic acid
William J. Welstead, H. Wayne Moran, Harold F. Stauffer, Lennox B. Turnbull, and Lawrence F. Sancilio
pp 1074 - 1079; DOI:
10.1021/jm00195a012
PDF
Syntheses of N-substituted 2(3,4)-pyridylcarboxylic acid hydrazides with analgesic and antiinflammatory activity
Kinfe Redda, Linda A. Corleto, and Edward E. Knaus
pp 1079 - 1082; DOI:
10.1021/jm00195a013
PDF
Aromatic hydroxylation of .beta.-adrenergic antagonists. Formation of 4'- and 5'-hydroxy-1-(isopropylamino)-3-[2'-(allyloxy)phenoxy]-2-propanol from oxprenolol
Wendel L. Nelson and Terrence R. Burke
pp 1082 - 1088; DOI:
10.1021/jm00195a014
PDF
Metabolism of .beta.-adrenergic antagonists. Evidence for an arene oxide-NIH shift pathway in the aromatic hydroxylation of oxprenolol
Wendel L. Nelson and Terrence R. Burke
pp 1088 - 1092; DOI:
10.1021/jm00195a015
PDF
Synthesis of some carbon-3 substituted 1,4-benzodiazepin-2-ones and their central effects
Tomislav Kovac, Franjo Kajfez, Vitomir Sunjic, Nikola Blazevic, and Dragutin Kolbah
pp 1093 - 1096; DOI:
10.1021/jm00195a016
PDF
Synthesis and biological activities of ftorafur metabolites. 3'- and 4'-Hydroxyftorafur
Ai Jeng Lin, Robert S. Benjamin, Potu N. Rao, and Ti li Loo
pp 1096 - 1100; DOI:
10.1021/jm00195a017
PDF
Mechanism of the dealkylation of tertiary amines by hepatic oxygenases. Stable isotope studies with 1-benzyl-4-cyano-4-phenylpiperidine
Robert E. McMahon, Hilman W. Culp, J. Cymerman Craig, and Nnochiri Ekwuribe
pp 1100 - 1103; DOI:
10.1021/jm00195a018
PDF
Anticandidal activity of 5-fluorocytosine-peptide conjugates
Alvin S. Steinfeld, Fred Naider, and Jeffrey M. Becker
pp 1104 - 1109; DOI:
10.1021/jm00195a019
PDF
Nitrosoureidonucleosides
J. A. Montgomery and H. J. Thomas
pp 1109 - 1113; DOI:
10.1021/jm00195a020
PDF
Antiparasitic agents. 3. Synthesis and anthelmintic activities of novel 2-pyridinyl-5-isothiocyanatobenzimidazoles
R. D. Haugwitz, B. V. Maurer, G. A. Jacobs, V. L. Narayanan, L. Cruthers, and J. Szanto
pp 1113 - 1118; DOI:
10.1021/jm00195a021
PDF
Synthesis and antibacterial activity of 1-hydroxy-1-methyl-1,3-dihydrofuro[3,4-b]quinoxaline 4,9-dioxide and related compounds
John P. Dirlam, Leonard J. Czuba, Beryl W. Dominy, Richard B. James, Richard M. Pezzullo, Joseph E. Presslitz, and Wendell W. Windisch
pp 1118 - 1121; DOI:
10.1021/jm00195a022
PDF
Absolute configuration of acenocoumarin
Conrad R. Wheeler and William F. Trager
pp 1122 - 1124; DOI:
10.1021/jm00195a023
PDF
Absolute configuration of glycerol derivatives. 7. Enantiomers of 2-[[[2-(2,6-dimethoxyphenoxy)ethyl]amino]ethyl]-1,4-benzodioxane (WB-4101), a potent competitive .alpha.-adrenergic antagonist
Wendel L. Nelson, Mark L. Powell, and Donald C. Dyer
pp 1125 - 1127; DOI:
10.1021/jm00195a024
PDF
Synthesis of angiotensin II analogs by incorporating .beta.-homotyrosine or .beta.-homoisoleucine residues
K. Stachowiak, M. C. Khosla, K. Plucinska, P. A. Khairallah, and F. M. Bumpus
pp 1128 - 1130; DOI:
10.1021/jm00195a025
PDF
Lysosomotropic agents. 1. Synthesis and cytotoxic action of lysosomotropic detergents
Raymond A. Firestone, Judith M. Pisano, and Robert J. Bonney
pp 1130 - 1133; DOI:
10.1021/jm00195a026
PDF
5-[(4-Methyl-1,2,3,4-tetrahydroquinoxalyl)methyl]-2'-deoxyuridine 5'-phosphate: an analogue of a proposed intermediate in thymidylate synthetase catalysis
Joon Sup Park, Charles T. C. Chang, and Mathias P. Mertes
pp 1134 - 1137; DOI:
10.1021/jm00195a027
PDF
5-Cyano-2'-deoxyuridine 5'-phosphate: a potent competitive inhibitor of thymidylate synthetase
Charles T. C. Chang, Michael W. Edwards, Paul F. Torrence, and Mathias P. Mertes
pp 1137 - 1139; DOI:
10.1021/jm00195a028
PDF
Stereochemical aspects of the metabolism of 5-(4'-fluorophenyl)-5-phenylhydantoin in the rat
Jacques H. Poupaert, Jacques Adline, Michel H. Claesen, Pierre De Laey, and Pierre A. Dumont
pp 1140 - 1142; DOI:
10.1021/jm00195a029
PDF
Antiarrhythmic activity of some N-alkylbispidinebenzamides
Peter C. Ruenitz and Corwin M. Mokler
pp 1142 - 1144; DOI:
10.1021/jm00195a030
PDF
Antifungal agents. 4. Chemical modification of antibiotics from Polyangium cellulosum var fulvum. Ester and amide analogues of ambruticin
David T. Connor and Maximillian Von Strandtmann
pp 1144 - 1147; DOI:
10.1021/jm00195a031
PDF
Synthesis of angiotensin II antagonists containing sarcosine in position 7
Graham J. Moore, Evelyn M. Oudeman, David Ko, and Diana M. Nystrom
pp 1147 - 1149; DOI:
10.1021/jm00195a032
PDF
Book Reviews

pp 1149 - 1156; DOI:
10.1021/jm00195a600
PDF

Issue 10


4-(p-Bromophenyl)-4-(dimethylamino)-1-phenethylcyclohexanol, an extremely potent representative of a new analgesic series
Daniel Lednicer and Philip F. VonVoigtlander
pp 1157 - 1158; DOI:
10.1021/jm00196a001
PDF
(2,6-Methano-3-benzazocin-11.beta.-yl)alkanones. 1. Alkylalkanones: a new series of N-methyl derivatives with novel opiate activity profiles
William F. Michne, Thomas R. Lewis, Stephen J. Michalec, Anne K. Pierson, and Franklin J. Rosenberg
pp 1158 - 1163; DOI:
10.1021/jm00196a002
PDF
Primaquine analogs: derivatives of 4-amino-2-methoxyacridine
John P. Scovill, Daniel L. Klayman, Thomas S. Woods, and Thomas R. Sweeney
pp 1164 - 1167; DOI:
10.1021/jm00196a003
PDF
4-Anilidopiperidine analgesics. 2. A study of the conformational aspects of the analgesic activity of the 4-anilidopiperidines utilizing isomeric N-substituted 3-(propananilido)nortropane analogs
Thomas N. Riley and Jerome R. Bagley
pp 1167 - 1171; DOI:
10.1021/jm00196a004
PDF
New antiarrhythmic agents. 1. Primary .alpha.-amino anilides
Eugene W. Byrnes, Paul D. McMaster, Emil R. Smith, Murray R. Blair, R. Nichol Boyes, Benjamin R. Duce, Hal S. Feldman, George H. Kronberg, Bertil H. Takman, and Paul A. Tenthorey
pp 1171 - 1176; DOI:
10.1021/jm00196a005
PDF
New antiarrhythmic agents. 2. Amide alkyl .alpha.-amino xylidides
Paul D. McMaster, Eugene W. Byrnes, Hal S. Feldman, Bertil H. Takman, and Paul A. Tenthorey
pp 1177 - 1182; DOI:
10.1021/jm00196a006
PDF
New antiarrhythmic agents. 3. Primary .beta.-amino anilides
Paul A. Tenthorey, Robert L. DiRubio, Hal S. Feldman, Bertil H. Takman, Eugene W. Byrnes, and Paul D. McMaster
pp 1182 - 1186; DOI:
10.1021/jm00196a007
PDF
Troponoids. 3. Synthesis and antiallergy activity of N-troponyloxamic acid esters
Jehan F. Bagli, T. Bogri, B. Palameta, R. Martel, W. Robinson, T. Pugsley, and W. Lippmann
pp 1186 - 1193; DOI:
10.1021/jm00196a008
PDF
Reactions of 1,3-bis(2-chloroethyl)-1-nitrosourea and 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea in aqueous solution
Robert J. Weinkam and Huey-Shin Lin
pp 1193 - 1198; DOI:
10.1021/jm00196a009
PDF
Angiotensin II analogs. 14. Roles of the imidazole nitrogens of position-6 histidine in pressor activity
Kun-Hwa Hsieh, Eugene C. Jorgensen, and Thomas C. Lee
pp 1199 - 1206; DOI:
10.1021/jm00196a010
PDF
Biologically active polycycloalkanes. 6. Antiviral 1-tricyclo[4.3.1.12,5]undecyl derivatives
Yoshiaki Inamoto, Koji Aigami, Naotake Takaishi, Yoshiaki Fujikura, Motoyoshi Ohsugi, Hiroshi Ikeda, Kiyoshi Tsuchihashi, Akira Takatsuki, and Gakuzo Tamura
pp 1206 - 1214; DOI:
10.1021/jm00196a011
PDF
3-[(1,2,3-Thiadiazol-5-ylthio)methyl]cephalosporins
Graham S. Lewis and Peter H. Nelson
pp 1214 - 1218; DOI:
10.1021/jm00196a012
PDF
Comparative cytotoxic and biochemical effects of ligands and metal complexes of .alpha.-N-heterocyclic carboxaldehyde thiosemicarbazones
Leon A. Saryan, Else Ankel, Chitra Krishnamurti, David H. Petering, and Howard Elford
pp 1218 - 1221; DOI:
10.1021/jm00196a013
PDF
Synthesis, assignment of absolute configuration, and receptor binding studies relevant to the neuroleptic activities of a series of chiral 3-substituted cyproheptadine atropisomers
William C. Randall, Paul S. Anderson, Emlen L. Cresson, Cecilia A. Hunt, Thomas F. Lyon, Kenneth E. Rittle, David C. Remy, James P. Springer, Jordan M. Hirshfield, and et al.
pp 1222 - 1230; DOI:
10.1021/jm00196a014
PDF
Synthesis and antitumor activity of 5-azacytosine arabinoside
John A. Beisler, Mohamed M. Abbasi, and John S. Driscoll
pp 1230 - 1234; DOI:
10.1021/jm00196a015
PDF
Potential antitumor agents. 31. Quantitative structure-activity relationships for the antileukemic bis(guanylhydrazones)
William A. Denny and Bruce F. Cain
pp 1234 - 1238; DOI:
10.1021/jm00196a016
PDF
Chance factors in studies of quantitative structure-activity relationships
John G. Topliss and Robert P. Edwards
pp 1238 - 1244; DOI:
10.1021/jm00196a017
PDF
A preliminary structure-activity study of the mixed-function oxidase inhibitor, 7,8-benzoflavone
Stephen Nesnow
pp 1244 - 1247; DOI:
10.1021/jm00196a018
PDF
Antimalarial drugs. 46. Folate antagonists. 15. 2,4-Diamino-6-(2-naphthylsulfonyl)quinazoline and related 2,4-diamino-6-[(phenyl and naphthyl)sulfinyl and sulfonyl]quinazolines, a potent new class of antimetabolites with phenomenal antimalarial activity
Edward F. Elslager, Marland P. Hutt, Patricia Jacob, Judith Johnson, Barbara Temporelli, Leslie M. Werbel, Donald F. Worth, and Leo Rane
pp 1247 - 1257; DOI:
10.1021/jm00196a019
PDF
Syntheses and biological activities of 7.beta.-methyl steroids
Wen-Hsiung Chiu and Manfred E. Wolff
pp 1257 - 1260; DOI:
10.1021/jm00196a020
PDF
In vivo inhibitors of Escherichia coli phenylalanyl-tRNA synthetase
Daniel V. Santi, Stephen O. Cunnion, Robert T. Anderson, and Robert W. Webster
pp 1260 - 1263; DOI:
10.1021/jm00196a021
PDF
Steric effects of substituents on phenethylamine hallucinogens. 3,4-(Methylenedioxy)amphetamine analogs alkylated on the dioxole ring
David E. Nichols and Linda J. Kostuba
pp 1264 - 1267; DOI:
10.1021/jm00196a022
PDF
Structure-activity relationship of aniline mustards acting against B-16 melanoma in mice
Augustine Panthananickal, Corwin Hansch, and A. Leo
pp 1267 - 1269; DOI:
10.1021/jm00196a023
PDF
Allylic esters as potential antitumor agents. Derivatives and analogs of 2,3-bis(hydroxymethyl)-7-oxabicyclo[2.2.1]hept-2-ene
Wayne K. Anderson, Richard H. Dewey, and Bipi Mulumba
pp 1270 - 1272; DOI:
10.1021/jm00196a024
PDF
Antiviral and antineoplastic activities of pyrimidine arabinosyl nucleosides and their 5'-amino derivatives
Raymond F. Schinazi, Ming S. Chen, and William H. Prusoff
pp 1273 - 1277; DOI:
10.1021/jm00196a025
PDF
Book Reviews

pp 1277 - 1280; DOI:
10.1021/jm00196a600
PDF

Issue 11


Sulfonated catecholamide analogs of enterobactin as iron sequestering agents
Frederick L. Weitl, Wesley R. Harris, and Kenneth N. Raymond
pp 1281 - 1283; DOI:
10.1021/jm00197a001
PDF
Symbiotic approach to drug design: antihypertensive .beta.-adrenergic blocking agents
John J. Baldwin, William C. Lumma, George F. Lundell, Gerald S. Ponticello, Andrew W. Raab, Edward L. Engelhardt, Ralph Hirschmann, Charles S. Sweet, and Alexander Scriabine
pp 1284 - 1290; DOI:
10.1021/jm00197a002
PDF
Ultraviolet photoelectron spectroscopy of cyclic amidines. 1. Electronic structure of some .alpha.-adrenergic benzylimidazolines
A. P. De Jong and H. Van Dam
pp 1290 - 1295; DOI:
10.1021/jm00197a003
PDF
Structure-activity relationships of pyrroleamidine antiviral antibiotics. 1. Modifications of the alkylamidine side chain
Meir Bialer, Boris Yagen, Raphael Mechoulam, and Yechiel Becker
pp 1296 - 1301; DOI:
10.1021/jm00197a004
PDF
Correlation of biological activity and high-pressure liquid chromatographic retention index for a series of propranolol, barbiturate, and anthranilic acid analogs
John K. Baker, David O. Rauls, and Ronald F. Borne
pp 1301 - 1306; DOI:
10.1021/jm00197a005
PDF
Antidotes to organophosphate poisoning. 2. Thiadiazole-5-carboxaldoximes
H. P. Benschop, G. R. Van den Berg, C. Van Hooidonk, L. P. A. De Jong, C. E. Kientz, F. Berends, L. A. Kepner, E. Meeter, and R. P. L. S. Visser
pp 1306 - 1313; DOI:
10.1021/jm00197a006
PDF
Synthesis and evaluation of the thiosemicarbazone, dithiocarbazonate, and 2'-pyrazinylhydrazone of pyrazinecarboxaldehyde as agents for the treatment of iron overload
Neil E. Spingarn and Alan C. Sartorelli
pp 1314 - 1316; DOI:
10.1021/jm00197a007
PDF
Synthesis, redox characteristics, and in vitro norepinephrine uptake inhibiting properties of 2-(2-mercapto-4,5-dihydroxyphenyl)ethylamine (6-mercaptodopamine)
Charles G. Chavdarian and Neal Castagnoli
pp 1317 - 1322; DOI:
10.1021/jm00197a008
PDF
Structure-activity relationships of N-substituted dopamine and 2-amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene analogs: behavioral effects in lesioned and reserpinized mice
James Z. Ginos, Janet M. Stevens, and David E. Nichols
pp 1323 - 1329; DOI:
10.1021/jm00197a009
PDF
Fluorinated pyrimidine nucleosides. 3. Synthesis and antitumor activity of a series of 5'-deoxy-5-fluoropyrimidine nucleosides
A. F. Cook, M. J. Holman, M. J. Kramer, and P. W. Trown
pp 1330 - 1335; DOI:
10.1021/jm00197a010
PDF
A study of chemical carcinogenesis. 19. Synthesis and mutagenicity of 5,11-dimethylchrysene and some methyl-oxidized derivatives of 5-methylchrysene
Shantilal Amin, Stephen S. Hecht, Edmond LaVoie, and Dietrich Hoffmann
pp 1336 - 1340; DOI:
10.1021/jm00197a011
PDF
Synthesis and biological activity of carboxyl-terminus modified prostaglandin analogs
Thomas K. Schaaf and Hans Juergen Hess
pp 1340 - 1346; DOI:
10.1021/jm00197a012
PDF
Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines] as potential central nervous system agents. 5. Conformationally mobile analogs derived by furan ring opening
Lawrence L. Martin, Solomon S. Klioze, Manfred Worm, Charles A. Crichlow, Harry M. Geyer, and Hansjoerg Kruse
pp 1347 - 1354; DOI:
10.1021/jm00197a013
PDF
Quinolone antimicrobial agents. 2. Methylenedioxy positional isomers of oxolinic acid
Lester A. Mitscher, Daniel L. Flynn, H. Eugene Gracey, and Steven D. Drake
pp 1354 - 1357; DOI:
10.1021/jm00197a014
PDF
Dibenzotropone- and dibenzosuberonecarboxylic acids with bronchodilator activity
James P. Dunn, Dallas M. Green, Ian T. Harrison, Peter H. Nelson, Jurg R. Pfister, Adolph P. Roszkowski, and Karl G. Untch
pp 1357 - 1363; DOI:
10.1021/jm00197a015
PDF
Synthesis of 4-alkyl- and 4-(.beta.-alkylvinyl) derivatives of primaquine as potential antimalarials
F. Ivy Carroll, Bertold D. Berrang, and C. Preston Linn
pp 1363 - 1367; DOI:
10.1021/jm00197a016
PDF
2-Acetylpyridine thiosemicarbazones. 2. N4,N4-Disubstituted derivatives as potential antimalarial agents
Daniel L. Klayman, John P. Scovill, Joseph F. Bartosevich, and Carl J. Mason
pp 1367 - 1373; DOI:
10.1021/jm00197a017
PDF
Substituted 3-amino-1,1-diaryl-2-propanols as potential antidepressant agents
Judith A. Clark, Michael S. G. Clark, Derek V. Gardner, Laramie M. Gaster, Michael S. Hadley, David Miller, and Anwer Shah
pp 1373 - 1379; DOI:
10.1021/jm00197a018
PDF
Usnic acid derivatives as potential antineoplastic agents
Makoto Takai, Yoshimasa Uehara, and John A. Beisler
pp 1380 - 1384; DOI:
10.1021/jm00197a019
PDF
Potential antiarthritic agents. 2. Benzoylacetonitriles and .beta.-aminocinnamonitriles
David N. Ridge, J. William Hanifin, Linda A. Harten, Bernard D. Johnson, Judith Menschik, Gabriela Nicolau, Adolph E. Sloboda, and Doris E. Watts
pp 1385 - 1389; DOI:
10.1021/jm00197a020
PDF
6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity
Jackson B. Hester and Philip Von Voigtlander
pp 1390 - 1398; DOI:
10.1021/jm00197a021
PDF
Hypolipidemic activity of phthalimide derivatives. 1. N-Substituted phthalimide derivatives
James M. Chapman, George H. Cocolas, and Iris H. Hall
pp 1399 - 1402; DOI:
10.1021/jm00197a022
PDF
Synthesis and biological evaluation of 9,11-azo-13-oxa-15-hydroxyprostanoic acid, a potent inhibitor of platelet aggregation
Sheung-Tsam Kam, Philip S. Portoghese, Jonathan M. Gerrard, and Earl W. Dunham
pp 1402 - 1408; DOI:
10.1021/jm00197a023
PDF
Antibacterial N-[.omega.,.omega.'-bis(alicyclic and aryl)-sec-alkyl]poly(methylenetriamine and -tetramine) hydrochloride salts
N. Grier, R. A. Dybas, R. A. Strelitz, B. E. Witzel, and E. L. Dulaney
pp 1409 - 1414; DOI:
10.1021/jm00197a024
PDF
Bufotenine esters
Richard A. Glennon, Peter K. Gessner, Domodar D. Godse, and Berry J. Kline
pp 1414 - 1416; DOI:
10.1021/jm00197a025
PDF
Cephalosporin derivatives with 2- and 4-pyridone groups at carbon-3
M. L. Edwards and R. C. Erickson
pp 1416 - 1418; DOI:
10.1021/jm00197a026
PDF
Antitumor and antiinflammatory agents: N-benzoyl-protected cyanomethyl esters of amino acids
Ziaodin Sajadi, Mohsen Almahmood, Larry J. Loeffler, and Iris H. Hall
pp 1419 - 1422; DOI:
10.1021/jm00197a027
PDF
Synthesis and antileukemic activities of furanyl, pyranyl, and ribosyl derivatives of 4-(3,3-dimethyl-1-triazeno)imidazole-5-carboxamide and 3-(3,3-dimethyl-1-triazeno)pyrazole-4-carboxamide
Robert A. Earl and Leroy B. Townsend
pp 1422 - 1425; DOI:
10.1021/jm00197a028
PDF
Synthesis and antitumor properties of 7-deoxy-7-[(cis- and trans-3-aminocyclohexane)thio]carminomycinone
John M. Essery, Terrence W. Doyle, and Richard H. Schreiber
pp 1425 - 1428; DOI:
10.1021/jm00197a029
PDF
Nucleoside conjugates as potential antitumor agents. 2. Synthesis and biological activity of 1-.beta.-D-arabinofuranosylcytosine conjugates of prednisolone and prednisone
Chung Il Hong, Alexander Nechaev, and Charles R. West
pp 1428 - 1432; DOI:
10.1021/jm00197a030
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Book Reviews

pp 1432 - 1434; DOI:
10.1021/jm00197a600
PDF

Issue 12


N-Acetimidoyl- and N-formimidoylthienamycin derivatives: antipseudomonal .beta.-lactam antibiotics
W. J. Leanza, K. J. Wildonger, T. W. Miller, and B. G. Christensen
pp 1435 - 1436; DOI:
10.1021/jm00198a001
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Oxazepam esters. 1. Correlation between hydrolysis rates and brain appearance of oxazepam
Gabor Maksay, Zsuzsanna Tegyey, Vera Kemeny, Istvan Lukovits, Laszlo Otvos, and Eva Palosi
pp 1436 - 1443; DOI:
10.1021/jm00198a002
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Oxazepam esters. 2. Correlation of hydrophobicity with serum binding, brain penetration, and excretion
Gabor Maksay, Zsuzsanna Tegyey, and Laszlo Otvos
pp 1443 - 1447; DOI:
10.1021/jm00198a003
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Effect of structure on phenothiazine cation radical reactions in aqueous buffers
Patricia Holt Sackett and Richard L. McCreery
pp 1447 - 1453; DOI:
10.1021/jm00198a004
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Potential antitumor agents. 32. Role of agent base strength in the quantitative structure-antitumor relationships for 4'-(9-acridinylamino)methanesulfonanilide analogs
William A. Denny, Graham J. Atwell, and Bruce F. Cain
pp 1453 - 1460; DOI:
10.1021/jm00198a005
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Potential antiinflammatory compounds. 1. Antiinflammatory phenylpiperidine derivatives
Terence A. Hicks, Christine E. Smith, W. R. Nigel Williamson, and Elaine H. Day
pp 1460 - 1464; DOI:
10.1021/jm00198a006
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Potential antiinflammatory compounds. 3. Compounds derived from acenaphthene and indan
Christine E. Smith, W. R. Nigel Williamson, Colin H. Cashin, and E. Ann Kitchen
pp 1464 - 1469; DOI:
10.1021/jm00198a007
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N-Alkylated 2-aminotetralins: central dopamine-receptor stimulating activity
Uli Hacksell, Uno Svensson, J. Lars G. Nilsson, Stephan Hjorth, Arvid Carlsson, Haakan Wikstroem, Per Lindberg, and Domingo Sanchez
pp 1469 - 1475; DOI:
10.1021/jm00198a008
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N-[(Tetrahydrofuryl)alkyl] and N-(alkoxyalkyl) derivatives of (-)-normetazocine, compounds with differentiated opioid action profiles
Herbert Merz and Klaus Stockhaus
pp 1475 - 1483; DOI:
10.1021/jm00198a009
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Anticoccidial derivatives of 6-azauracil. 2. High potency and long plasma life of N1-phenyl structures
Max W. Miller, Banavara L. Mylari, Harold L. Howes, John E. Lynch, Martin J. Lynch, and Richard C. Koch
pp 1483 - 1487; DOI:
10.1021/jm00198a010
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[3-(1,4-Cyclohexadienyl)-L-alanine,8-lysine]vasopressin synthesis and some pharmacological properties
Some Nath Banerjee, Lillian Diamond, Charlotte Ressler, and Wilbur H. Sawyer
pp 1487 - 1492; DOI:
10.1021/jm00198a011
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Synthesis and biological properties of 2-, 5-, and 6-fluoronorepinephrines
Kenneth L. Kirk, Daniele Cantacuzene, Yuthasak Nimitkitpaisan, David McCulloh, William L. Padgett, John W. Daly, and Cyrus R. Creveling
pp 1493 - 1497; DOI:
10.1021/jm00198a012
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Synthesis and antihypertensive activity of 2-benzamido-1,2,3,4,6,7,12,12b-octahydroindolo[2,3-a]quinolizines
Sol S. Klioze, Frederick J. Ehrgott, Jeffrey C. Wilker, and David L. Woodward
pp 1497 - 1504; DOI:
10.1021/jm00198a013
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Diels-Alder adducts of fulvenes and halogenated dienes. Synthesis and insecticidal activity
Neil J. Lewis, David B. Knight, and William J. Collins
pp 1505 - 1509; DOI:
10.1021/jm00198a014
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Antiestrogens and antiestrogen metabolites: preparation of tritium-labeled (.+-.)-cis-3-[p-(1,2,3,4-tetrahydro-6-methoxy-2-phenyl-1-naphthyl)phenoxy]-1,2-propanediol and characterization and synthesis of a biologically important metabolite
Tochiro Tatee, Kathryn E. Carlson, John A. Katzenellenbogen, David W. Robertson, and Benita S. Katzenellenbogen
pp 1509 - 1517; DOI:
10.1021/jm00198a015
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Electrostatic potentials of deoxydinucleoside monophosphates. 1. Deoxydinucleoside monophosphates and actinomycin chromophore interactions
Merrill E. Nuss and Peter A. Kollman
pp 1517 - 1524; DOI:
10.1021/jm00198a016
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Design of species- or isozyme-specific enzyme inhibitors. 2. Differences between a bacterial and a mammalian thymidine kinase in the effect of thymidine substituents on affinity for the thymidine site
Alexander Hampton, Francis Kappler, and Ram R. Chawla
pp 1524 - 1528; DOI:
10.1021/jm00198a017
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Design of species- or isozyme-specific enzyme inhibitors. 3. Species and isozymic differences between mammalian and bacterial adenylate kinases in substituent tolerance in an enzyme-substrate complex
Alexander Hampton and Donald Picker
pp 1529 - 1532; DOI:
10.1021/jm00198a018
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Syntheses and activities of sulfur and selenium isosteric substitution analogs of retinol
Steven C. Welch and John M. Gruber
pp 1532 - 1534; DOI:
10.1021/jm00198a019
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Synthesis of 4'- and 5'-hydroxyoxprenolol: pharmacologically active ring-hydroxylated metabolites of oxprenolol
Terrence R. Burke, Wendel L. Nelson, and Carl K. Buckner
pp 1535 - 1537; DOI:
10.1021/jm00198a020
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Synthesis and estrogenic properties of 17-epi-ethynylestradiol and its ether derivatives epimestranol and epiquinestrol
Ramesh M. Kanojia, George O. Allen, Joanne M. Killinger, and J. L. McGuire
pp 1538 - 1541; DOI:
10.1021/jm00198a021
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5-(.alpha.-Bromoacetyl)-2'-deoxyuridine 5'-phosphate: an affinity label for thymidylate synthetase
Christie B. Brouillette, Charles T. C. Chang, and Mathias P. Mertes
pp 1541 - 1544; DOI:
10.1021/jm00198a022
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Polymer-linked 6-azauridine 5'-monophosphate, a resin of high bioaffinity to orotidine-5'-phosphate decarboxylase
Helmut Rosemeyer and Frank Seela
pp 1545 - 1547; DOI:
10.1021/jm00198a023
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Derivatives of 1,3-disubstituted 2,4(1H,3H)-quinazolinediones as possible peripheral vasodilators or antihypertensive agents
Herbert J. Havera
pp 1548 - 1550; DOI:
10.1021/jm00198a024
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Dimerization of coralyne and its propyl analog and their association with DNA
Alice N. Gough, Rogert L. Jones, and W. David Wilson
pp 1551 - 1554; DOI:
10.1021/jm00198a025
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Potential antiinflammatory compounds. 2. Acidic antiinflammatory 1,2-benzisoxazoles
J. C. Saunders and W. R. N. Williamson
pp 1554 - 1558; DOI:
10.1021/jm00198a026
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Optical resolution of some homobenzomorphan derivatives and their pharmacological properties
Shunsaku Shiotani, Tadashi Kometani, Tsutomu Nozawa, Akira Kurobe, and Osamu Futsukaichi
pp 1558 - 1560; DOI:
10.1021/jm00198a027
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Book Reviews

pp 1561 - 1562; DOI:
10.1021/jm00198a600
PDF
Additions and Corrections - New Dopaminergic and Potential Anti-Parkinson Compounds, N,N-Disubstituted β-(3,4-Dihydroxyphenyl)ethylamines
James Z. Ginos, George C. Cotzias, and David Doroski
pp 1560 - 1560; DOI:
10.1021/jm00198a601
PDF
Additions and Corrections - Paradoxical Effects of N-Cyano-alkyl Substituents upon the Activities of Several Classes of Opioids
Arthur E. Jacobson, Kenner C. Rice, Jurgen Reden, Lillian Lupinacci, Arnold Brossi, Richard A. Streaty, and Werner A. Klee
pp 1560 - 1560; DOI:
10.1021/jm00198a602
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