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Volume 24
Main Index

Issue 1


Toward more selective antiarthritic therapy
T. Y. Shen
pp 1 - 5; DOI:
10.1021/jm00133a001
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Potential organ- or tumor-imaging agents. 21. Acyl-labeled esters of cholesterol
R. E. Counsell, R. H. Seevers, N. Korn, and S. W. Schwendner
pp 5 - 6; DOI:
10.1021/jm00133a002
PDF
Importance of the aromatic ring in adrenergic amines. 5. Nonaromatic analogs of phenylethanolamine as inhibitors of phenylethanolamine N-methyltransferase: role of hydrophobic and steric interactions
William C. Vincek, Constance S. Aldrich, Ronald T. Borchardt, and Gary L. Grunewald
pp 7 - 12; DOI:
10.1021/jm00133a003
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Importance of the aromatic ring in adrenergic amines. 6. Nonaromatic analogs of phenylethanolamine as inhibitors of phenylethanolamine N-methyltransferase: role of .pi.-electronic and steric interactions
Dwight P. Davis, Ronald T. Borchardt, and Gary L. Grunewald
pp 12 - 16; DOI:
10.1021/jm00133a004
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.alpha.-Ethynyl and .alpha.-vinyl analogs of ornithine as enzyme-activated inhibitors of mammalian ornithine decarboxylase
Charles Danzin, Patrick Casara, Nicole Claverie, and Brian W. Metcalf
pp 16 - 20; DOI:
10.1021/jm00133a005
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Novel peptidoaminobenzophenones, terminal N-substituted peptidoaminobenzophenones, and N-(acylglycyl)aminobenzophenones as open-ring derivatives of benzodiazepines
Kentaro Hirai, Teruyuki Ishiba, Hirohiko Sugimoto, Toshio Fujishita, Yuji Tsukinoki, and Katsumi Hirose
pp 20 - 27; DOI:
10.1021/jm00133a006
PDF
Regiospecific attack of nitrogen and sulfur nucleophiles on quinones derived from poison oak/ivy catechols (urushiols) and analogs as models for urushiol-protein conjugate formation
Daniel J. Liberato, Vera S. Byers, Reg G. Dennick, and Neal Castagnoli
pp 28 - 33; DOI:
10.1021/jm00133a007
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Permethyl analog of the pyrrolic antibiotic distamycin A
Paul L. Gendler and Henry Rapoport
pp 33 - 38; DOI:
10.1021/jm00133a008
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Synthesis and antiinflammatory activity of metabolites of piroxicam
Joseph G. Lombardino
pp 39 - 42; DOI:
10.1021/jm00133a009
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Nonsteroidal antiinflammatroy agents. 2. Synthesis of 4',5-disubstituted 3-diphenylylacetic acids and their derivatives with antiinflammatory and analgesic activities
Yasumitsu Tamura, Yoshihiko Yoshimoto, Katsutoshi Kunimoto, Shinichi Tada, Shingo Matsumura, Masao Murayama, Yoshihisa Shibata, and Hiroshi Enomoto
pp 43 - 47; DOI:
10.1021/jm00133a010
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New antiarrhythmic agents. 4. 1'-(aminoalkyl)-1,2,3,4-tetrahydronaphthalene-1-spiro-3'-pyrrolidine-2',5'-dione derivatives
Paul A. Tenthorey, Robert A. Ronfeld, Hal S. Feldman, Rune V. Sandberg, Paul D. McMaster, and Emil R. Smith
pp 47 - 53; DOI:
10.1021/jm00133a011
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New antiarrhythmic agents. 5. .alpha.-Aminoaceto-2,6-xylidides with functionalized amide alkyl substituents
Paul D. McMaster, Eugene W. Byrnes, Alan J. Block, and Paul A. Tenthorey
pp 53 - 58; DOI:
10.1021/jm00133a012
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Synthesis and antihypertensive activity of new 6-heteroaryl-3-hydrazinopyridazine derivatives
Gerd Steiner, Josef Gries, and Dieter Lenke
pp 59 - 63; DOI:
10.1021/jm00133a013
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Tetrahydro-2-benzoxepins: a novel family of hypotensives
Ruth E. TenBrink, John M. McCall, Donald T. Pals, Robert B. McCall, John Orley, Steve J. Humphrey, and Michael G. Wendling
pp 64 - 67; DOI:
10.1021/jm00133a014
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1-(Naphthylalkyl)-1H-imidazole derivatives, a new class of anticonvulsant agents
Keith A. M. Walker, Marshall B. Wallach, and Donald R. Hirschfeld
pp 67 - 74; DOI:
10.1021/jm00133a015
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Novel tetracyclic spiropiperidines. 1. 3-Aryl-1,3-dihydrospiro[benzo[c]thiophene-1,4'-piperidines] as potential antidepressants
Helen H. Ong, James A. Profitt, V. Brian Anderson, Hansjoerg Kruse, Jeffrey C. Wilker, and Harry M. Geyer
pp 74 - 79; DOI:
10.1021/jm00133a016
PDF
Synthesis and stereochemistry of 7-phenyl-2-propionanilidobenzo[a]quinolizidine derivatives. Structural probes of fentanyl analgesics
Bruce E. Maryanoff, David F. McComsey, Russell J. Taylor, and Joseph F. Gardocki
pp 79 - 88; DOI:
10.1021/jm00133a017
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1-Oxacephalosporins: enhancement of .beta.-lactam reactivity and antibacterial activity
Kazuhisa Murakami, Mamoru Takasuka, Kiyoshi Motokawa, and Tadashi Yoshida
pp 88 - 93; DOI:
10.1021/jm00133a018
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Piperazinylquinoxalines with central serotoninmimetic activity
William C. Lumma, Richard D. Hartman, Walfred S. Saari, Edward L. Engelhardt, Victor J. Lotti, and Clement A. Stone
pp 93 - 101; DOI:
10.1021/jm00133a019
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Fluorinated retinoic acids and their analogs. 2. Synthesis and biological activity of aromatic 4-fluoro analogs
Ka-Kong Chan, Anthony C. Specian, and Beverly A. Pawson
pp 101 - 104; DOI:
10.1021/jm00133a020
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Synthesis and angiotensin-converting enzyme inhibitory activity of 3-(mercaptomethyl)-2-oxo-1-pyrrolidineacetic acids and 3-(mercaptomethyl)-2-oxo-1-piperidineacetic acids
Sylvester Klutchko, Milton L. Hoefle, Ronald D. Smith, Arnold D. Essenburg, Robert B. Parker, Vicki L. Nemeth, Michael Ryan, Deborah H. Dugan, and Harvey R. Kaplan
pp 104 - 109; DOI:
10.1021/jm00133a021
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Synthesis and antiviral activity of 1-(2-deoxy-.beta.-D-ribofuranosyl)-5-(methylmercapto)-2-pyrimidinone
Alan C. Schroeder, Thomas J. Bardos, and Yung-Chi Cheng
pp 109 - 112; DOI:
10.1021/jm00133a022
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Synthesis of 2'-deoxy-L-fucopyranosylcarminomycinone and -.epsilon.-pyrromycinone as well as 2'-deoxy-D-erythro-pentopyranosyldaunomycinone, -carminomycinone, and -.epsilon.-pyrromycinone
Hassan S. El Khadem and David L. Swartz
pp 112 - 115; DOI:
10.1021/jm00133a023
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2-(Aminomethyl)phenols, a new class of saluretic agents. 2. Synthesis and pharmacological properties of the 5-aza isostere of 2-(aminomethyl)-4-(1,1-dimethylethyl)-6-iodophenol
G. E. Stokker, R. L. Smith, E. J. Cragoe, C. T. Ludden, H. F. Russo, C. S. Sweet, and L. S. Watson
pp 115 - 117; DOI:
10.1021/jm00133a024
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Synthesis and study of the potential antiallergic activity of some pyrazole derivatives
Maria T. Di Parsia, Cecilia Suarez, Maria J. Vitolo, Victor E. Marquez, Bernardo Beyer, Cecilia Urbina, and Ines Hurtado
pp 117 - 119; DOI:
10.1021/jm00133a025
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Book Reviews

pp 120 - 120; DOI:
10.1021/jm00133a600
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Issue 2


The leukotrienes: a major step in the understanding of immediate hypersensitivity reactions
Pierre Borgeat and Pierre Sirois
pp 121 - 126; DOI:
10.1021/jm00134a001
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Synthesis and antimalarial effects of N2-aryl-N4-[(dialkylamino)alkyl]- and N4-aryl-N2-[(dialkylamino)alkyl]-2,4-quinazolinediamines
Edward F. Elslager, Carolyn Hess, Judith Johnson, Daniel Ortwine, Vera Chu, and Leslie M. Werbel
pp 127 - 140; DOI:
10.1021/jm00134a002
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Folate antagonists. 18. Synthesis and antimalarial effects of N6-(arylmethyl)-N6-methyl-2,4,6-pteridinetriamines and related N6,N6-disubstituted 2,4,6-pteridinetriamines
Edward F. Elslager, Judith L. Johnson, and Leslie M. Werbel
pp 140 - 145; DOI:
10.1021/jm00134a003
PDF
Synthesis and antidepressant activity of substituted (.omega.-aminoalkoxy)benzene derivatives
Ryoji Kikumoto, Akihiro Tobe, and Shinji Tonomura
pp 145 - 148; DOI:
10.1021/jm00134a004
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5,7-Dihydroxy-2-aminotetralin derivatives: synthesis and assessment of dopaminergic and adrenergic actions
Joseph G. Cannon, Abram N. Brubaker, John Paul Long, Jan R. Flynn, Turkiz Verimer, Peerarat Harnirattisai, Brenda Costall, Robert J. Naylor, and V. Nohria
pp 149 - 153; DOI:
10.1021/jm00134a005
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Thiophene systems. 5. Thieno[3,4-b][1,5]benzoxazepines, thieno[3,4-b][1,5]benzothiazepines, and thieno[3,4-b][1,4]benzodiazepines as potential central nervous system agents
Jeffery B. Press, Corris M. Hofmann, Nancy H. Eudy, Ivana P. Day, Eugene N. Greenblatt, and Sidney R. Safir
pp 154 - 159; DOI:
10.1021/jm00134a006
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Synthesis and antiarrhythmic activity of new benzofuran derivatives
Guy Bourgery, Philippe Dostert, Alain Lacour, Michel Langlois, Bernard Pourrias, and Jacky Tisne-Versailles
pp 159 - 167; DOI:
10.1021/jm00134a007
PDF
Synthesis of seleno- and thioguanine-platinum(II) complexes and their antitumor activity in mice
Mitsuaki Maeda, Noriko Abiko, and Takuma Sasaki
pp 167 - 169; DOI:
10.1021/jm00134a008
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Potential antitumor agents. 34. Quantitative relationships between DNA binding and molecular structure for 9-anilinoacridines substituted in the anilino ring
Bruce C. Baguley, William A. Denny, Graham J. Atwell, and Bruce F. Cain
pp 170 - 177; DOI:
10.1021/jm00134a009
PDF
New monofunctional reagents for DNA as possible agents for the photochemotherapy of psoriasis: derivatives of 4,5'-dimethylangelicin
Francesco Dall'Acqua, Daniela Vedaldi, Sergio Caffieri, Adriano Guiotto, Paolo Rodighiero, Francarosa Baccichetti, Francesco Carlassare, and Franco Bordin
pp 178 - 184; DOI:
10.1021/jm00134a010
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Potential inhibitors of nucleotide biosynthesis. 1. Nitrosoureidonucleosides. 2
John A. Montgomery, H. Jeanette Thomas, R. Wallace Brockman, and Glynn P. Wheeler
pp 184 - 189; DOI:
10.1021/jm00134a011
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Inactivation of liver alcohol dehydrogenases and inhibition of ethanol metabolism by ambivalent active-site-directed reagents
Wen-Sherng Chen, David P. Bohlken, and Bryce V. Plapp
pp 190 - 193; DOI:
10.1021/jm00134a012
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Synthesis and structure-activity relationship of spiro[isochromanpiperidine] analogs for inhibition of histamine release. 1
Masatoshi Yamato, Kuniko Hashigaki, Masao Ikeda, Hidetoshi Ohtake, and Kenji Tasaka
pp 194 - 198; DOI:
10.1021/jm00134a013
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Quantitative structure-activity relationships by distance geometry: thyroxine binding site
Gordon M. Crippen
pp 198 - 203; DOI:
10.1021/jm00134a014
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Synthetic enterobactin analogs. Carboxamido-2,3-dihydroxyterephthalate conjugates of spermine and spermidine
Frederick L. Weitl, Kenneth N. Raymond, and Patricia W. Durbin
pp 203 - 206; DOI:
10.1021/jm00134a015
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Comparison of solution conformational preferences for the hallucinogens bufotenin and psilocin using 360-MHz proton NMR spectroscopy
Gerald P. Migliaccio, Tiee-Leou N. Shieh, Stephen R. Byrn, Bruce A. Hathaway, and David E. Nichols
pp 206 - 209; DOI:
10.1021/jm00134a016
PDF
Studies on position 1 of angiotensin II: effects on affinity and duration of action from alkyl amide substitution
Paul Cordopatis, Dimitrios Theodoropoulos, Gaetan Guillemette, and Emanuel Escher
pp 209 - 211; DOI:
10.1021/jm00134a017
PDF
Some 14.beta.-substituted analogs of N-(cyclopropylmethyl)normorphine
Peter Osei-Gyimah, Sydney Archer, Maureen G. C. Gillan, and Hans W. Kosterlitz
pp 212 - 214; DOI:
10.1021/jm00134a018
PDF
Synthesis and antimalarial activity of 8-[(1-alkyl-4-aminobutyl)amino]-6-methoxy-4-methylquinolines
Shou-Jen Yan, Ping-Lu Chien, and C. C. Cheng
pp 215 - 217; DOI:
10.1021/jm00134a019
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Structure-activity studies on narcotic antagonists. 2. N-substituted ethyl3-(m- or p-hydroxyphenyl)nipecotates
Ronald L. Jacoby, Dick Boon, Leonard E. Darling, and Robert E. Willette
pp 218 - 221; DOI:
10.1021/jm00134a020
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Some analogs of luteinizing hormone-releasing hormone with substituents in position 10
Satoe H. Nakagawa, Dai Chang Yang, and George Flouret
pp 221 - 223; DOI:
10.1021/jm00134a021
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Book Reviews

pp 224 - 228; DOI:
10.1021/jm00134a600
PDF

Issue 3


A practitioner's perspective of the role of quantitative structure-activity analysis in medicinal chemistry
Yvonne C. Martin
pp 229 - 237; DOI:
10.1021/jm00135a001
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Proposed dopaminergic pharmacophore of lergotrile, pergolide, and related ergot alkaloid derivatives
Joseph G. Cannon, Basil J. Demopoulos, John Paul Long, Jan R. Flynn, and Fouad M. Sharabi
pp 238 - 240; DOI:
10.1021/jm00135a002
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Computer-assisted structure-activity studies of chemical carcinogens. Aromatic amines
Kohtaro Yuta and Peter C. Jurs
pp 241 - 251; DOI:
10.1021/jm00135a003
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Quantitative structure-activity relationships of colchicines against P388 leukemia in mice
Frank R. Quinn and John A. Beisler
pp 251 - 256; DOI:
10.1021/jm00135a004
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Biological effects of modified colchicines. Improved preparation of 2-demethylcolchicine, 3-demethylcolchicine, and (+)-colchicine and reassignment of the position of the double bond in dehydro-7-deacetamidocolchicines
Manfred Roesner, Hans-Georg Capraro, Arthur E. Jacobson, Louise Atwell, Arnold Brossi, Maria A. Iorio, Thomas H. Williams, Robert H. Sik, and Colin F. Chignell
pp 257 - 261; DOI:
10.1021/jm00135a005
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Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity
Stefan H. Unger and Grace H. Chiang
pp 262 - 270; DOI:
10.1021/jm00135a006
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Mechanism of action of (2-haloethyl)nitrosoureas on DNA. Isolation and reactions of postulated 2-(alkylimino)-3-nitrosooxazolidine intermediates in the decomposition of 1,3-bis(2-chloroethyl)-, 1-(2-chloroethyl)-3-cyclohexyl-, and 1-(2-chloroethyl)-3-(4'-trans-methylcyclohexyl)-1-nitrosourea
J. William Lown and Shive M. S. Chauhan
pp 270 - 279; DOI:
10.1021/jm00135a007
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Synthesis and DNA binding of [3-[2'-(2-acetamidoethyl)-2,4'-bithiazole-4-carboxamido]propyl]dimethylsulfonium chloride, a fragment of bleomycin A2
Ted T. Sakai, James M. Riordan, Thomas E. Booth, and Jerry D. Glickson
pp 279 - 285; DOI:
10.1021/jm00135a008
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Esters of isoguvacine as potential prodrugs
Erik Falch, Povl Krogsgaard-Larsen, and Anne Vibeke Christensen
pp 285 - 289; DOI:
10.1021/jm00135a009
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Bioactivation of the antitumor drugs 9-hydroxyellipticine and derivatives by a peroxidase-hydrogen peroxide system
Christian Auclair and Claude Paoletti
pp 289 - 295; DOI:
10.1021/jm00135a010
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In vitro activity of 2-alkyl-3-hydroxy-1,4-naphthoquinones against Theileria parva
Peter Boehm, Kelvin Cooper, Alan T. Hudson, Jane P. Elphick, and Nicholas McHardy
pp 295 - 299; DOI:
10.1021/jm00135a011
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Studies on chiral interactions of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane and the corresponding n-hydroxy metabolites with cytochrome P-450
N. Peter McGraw and N. Castagnoli
pp 299 - 304; DOI:
10.1021/jm00135a012
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Puromycin analogs. Effect of aryl-substituted puromycin analogs on the ribosomal peptidyltransferase reaction
Heejoo Lee, Kei-Lai Fong, and Robert Vince
pp 304 - 308; DOI:
10.1021/jm00135a013
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Ring-hydroxylated propranolol: synthesis and .beta.-receptor antagonist and vasodilating activities of the seven isomers
J. E. Oatis, M. P. Russell, D. R. Knapp, and T. Walle
pp 309 - 314; DOI:
10.1021/jm00135a014
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.beta.-Adrenoceptor stimulant properties of amidoalkylamino-substituted 1-aryl-2-ethanols and 1-(aryloxy)-2-propanols
Jeffrey J. Barlow, Brian G. Main, and H. Michael Snow
pp 315 - 322; DOI:
10.1021/jm00135a015
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Fibrin polymerization. 1. Alkylating peptide inhibitors of fibrin polymerization
Kun-hwa Hsieh, M. Susan Mudd, and George D. Wilner
pp 322 - 327; DOI:
10.1021/jm00135a016
PDF
Salicylamide derivatives related to medroxalol with .alpha.- and .beta.-adrenergic antagonist and antihypertensive activity
J. Martin Grisar, George P. Claxton, Thomas M. Bare, Richard C. Dage, Hsien C. Cheng, and James K. Woodward
pp 327 - 336; DOI:
10.1021/jm00135a017
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Imine analogs of tricyclic antidepressants
Engelbert Ciganek, Roy T. Uyeda, Marvin Cohen, and Dewey H. Smith
pp 336 - 341; DOI:
10.1021/jm00135a018
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4-Aryl-4-aminocyclohexanones and their derivatives, a novel class of analgesics. 3. m-Hydroxyphenyl derivatives
Daniel Lednicer, Philip F. Von Voigtlander, and D. Edward Emmert
pp 341 - 346; DOI:
10.1021/jm00135a019
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Cognition-activating properties of 3-(aryloxy)pyridines
Donald E. Butler, B. P. H. Poschel, and John G. Marriott
pp 346 - 350; DOI:
10.1021/jm00135a020
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Nucleosides containing chemically reactive groups
Robert D. Elliott, R. Wallace Brockman, and John A. Montgomery
pp 350 - 352; DOI:
10.1021/jm00135a021
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Book Reviews

pp 353 - 354; DOI:
10.1021/jm00135a600
PDF

Issue 4


Inhibition of the renin-angiotensin system. A new approach to the therapy of hypertension
Miguel A. Ondetti and David W. Cushman
pp 355 - 361; DOI:
10.1021/jm00136a001
PDF
Photochemical inactivation of the angiotensin receptor of rabbit aorta by N.alpha.-(2-Nitro-5-azidobenzoyl)-[1-aspartic acid,5-isoleucine]angiotensin II
Richard E. Galardy and Kathleen A. LaVorgna
pp 362 - 366; DOI:
10.1021/jm00136a002
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Potential thyroliberin affinity labels. 1. Chloroacetyl-substituted phenylalanylpyrrolidines
Richard J. Goebel, Bruce L. Currie, and Cyril Y. Bowers
pp 366 - 370; DOI:
10.1021/jm00136a003
PDF
Synthesis of peptides by the solid-phase method. 6. Neurotensin, fragments, and analogs
S. St-Pierre, J. M. Lalonde, M. Gendreau, R. Quirion, D. Regoli, and F. Rioux
pp 370 - 376; DOI:
10.1021/jm00136a004
PDF
Cyclic guanidines. 14. Imidazo[1,2-a]thienopyrimidin-2-one derivatives as blood platelet aggregation inhibitors
Fumiyoshi Ishikawa, Akira Kosasayama, Hitoshi Yamaguchi, Yoshifumi Watanabe, Junji Saegusa, Seiichi Shibamura, Kyoko Sakuma, Shinichiro Ashida, and Yasushi Abiko
pp 376 - 382; DOI:
10.1021/jm00136a005
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Antihypertensive activity of 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives
Lawrence R. Bennett, C. John Blankley, Robert W. Fleming, Ronald D. Smith, and Deirdre K. Tessman
pp 382 - 389; DOI:
10.1021/jm00136a006
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Synthesis and antiviral activity of 5-[(cyanomethylene)oxy]-2'-deoxyuridine
Guang-Fu Huang, Masashi Okada, Erik De Clercq, and Paul F. Torrence
pp 390 - 393; DOI:
10.1021/jm00136a007
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Synthesis and biological evaluation of certain 2'-deoxy-.beta.-D-ribo-and 2.beta.-D-arabinofuranosyl nucleosides of purine-6-carboxamide and 4,8-diaminopyrimido[5,4-d]pyrimidine
Prem C. Srivastava, Ganapathi R. Revankar, Roland K. Robins, and Robert J. Rousseau
pp 393 - 398; DOI:
10.1021/jm00136a008
PDF
Promotion of carbohydrate oxidation in the heart by some phenylglyoxylic acids
Ian T. Barnish, Peter E. Cross, John C. Danilewicz, Roger P. Dickinson, and David A. Stopher
pp 399 - 404; DOI:
10.1021/jm00136a009
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4-Amino-4-arylcyclohexanones and their derivatives: a novel class of analgesics. 2. Modification of the carbonyl function
Daniel Lednicer, Philip F. VonVoigtlander, and D. Edward Emmert
pp 404 - 408; DOI:
10.1021/jm00136a010
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Dihydrochalcone sweeteners. A study of the atypical temporal phenomena
Grant E. DuBois, Guy A. Crosby, and Rebecca A. Stephenson
pp 408 - 428; DOI:
10.1021/jm00136a011
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Monophenolic 2-(dipropylamino)indans and related compounds: central dopamine-receptor stimulating activity
Uli Hacksell, Lars Erik Arvidsson, Uno Svensson, J. Lars G. Nilsson, Haakan Wikstroem, Per Lindberg, Domingo Sanchez, Stephan Hjorth, Arvid Carlsson, and Lennart Paalzow
pp 429 - 434; DOI:
10.1021/jm00136a012
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Chemically reactive estrogens: synthesis and estrogen receptor interactions of hexestrol ether derivatives and 4-substituted deoxyhexestrol derivatives bearing alkylating functions
John A. Katzenellenbogen, Robert J. McGorrin, Tochiro Tatee, Robert J. Kempton, Kathryn E. Carlson, and David H. Kinder
pp 435 - 450; DOI:
10.1021/jm00136a013
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Adrenoceptor blocking agents. Compounds related to metoprolol
Kurt Loevgren, Anders Hedberg, and J. Lars G. Nilsson
pp 451 - 454; DOI:
10.1021/jm00136a014
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Structure-activity relationships in dihydropteroate synthase inhibition by sulfanilamides. Comparison with the antibacterial activity
Pier G. De Benedetti, Augusto Rastelli, Chiara Frassineti, and Carlo Cennamo
pp 454 - 457; DOI:
10.1021/jm00136a015
PDF
Synthesis and pharmacological properties of 1,2,3,4,5,6-hexahydro-1,6-methano-2-benzazocines
Paul H. Mazzocchi and Barbara C. Stahly
pp 457 - 462; DOI:
10.1021/jm00136a016
PDF
Some reactions of 1,4-dihydropyridines with organic azides. Synthesis of 2,7-diazabicyclo[4.1.0]hept-3-enes with analgesic and antiprotozoal activity
Brent K. Warren and Edward E. Knaus
pp 462 - 464; DOI:
10.1021/jm00136a017
PDF
Potential anticonvulsants. 1. 5-Benzylhydantoins
Nariman B. Mehta, Cheryl A. Risinger Diuguid, and Francis E. Soroko
pp 465 - 468; DOI:
10.1021/jm00136a018
PDF
Synthesis and antitumor activity of simple vinyl and .alpha.-methylene-.gamma.-butyrolactone sulfonate esters and silyl enol ethers
Peter J. Stang and Warren L. Treptow
pp 468 - 472; DOI:
10.1021/jm00136a019
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Pyrimidine acyclic nucleosides. 5-Substituted 1-[(2-aminoethoxy)methyl]uracils as candidate antivirals
James L. Kelley, Mark P. Krochmal, and Howard J. Schaeffer
pp 472 - 474; DOI:
10.1021/jm00136a020
PDF
Sulfonate analogs of adenosine nucleotides as inhibitors of nucleotide-binding enzymes
Paul H. C. Mundill, Richard W. Fries, Christoph Woenckhaus, and Bryce V. Plapp
pp 474 - 477; DOI:
10.1021/jm00136a021
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Book Reviews

pp 477 - 478; DOI:
10.1021/jm00136a600
PDF

Issue 5


A novel connector linkage applicable in prodrug design
Philip L. Carl, Prasun K. Chakravarty, and John A. Katzenellenbogen
pp 479 - 480; DOI:
10.1021/jm00137a001
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1-Aryl-3-azabicyclo[3.1.0]hexanes, a new series of nonnarcotic analgesic agents
Joseph W. Epstein, Herbert J. Brabander, William J. Fanshawe, Corris M. Hofmann, Thomas C. McKenzie, Sidney R. Safir, Arnold C. Osterberg, D. B. Cosulich, and F. M. Lovell
pp 481 - 490; DOI:
10.1021/jm00137a002
PDF
A potent, new, sedative-hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide
G. B. Bennett, R. G. Babington, M. A. Deacon, P. L. Eden, S. P. Kerestan, G. H. Leslie, E. A. Ryan, R. B. Mason, and H. E. Minor
pp 490 - 496; DOI:
10.1021/jm00137a003
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New analgesic drugs derived from phencyclidine
Yossef Itzhak, Asher Kalir, Ben Avi Weissman, and Sasson Cohen
pp 496 - 499; DOI:
10.1021/jm00137a004
PDF
Oxazepam esters. 3. Intrinsic activity, selectivity, and prodrug effect
Gabor Maksay, Eva Palosi, Zsuzsanna Tegyey, and Laszlo Otvos
pp 499 - 502; DOI:
10.1021/jm00137a005
PDF
Characterization of .alpha.-adrenoceptor populations. Quantitative relationships between cardiovascular effects initiated at central and peripheral .alpha.-adrenoceptors
Pieter B. M. W. M. Timmermans, Adriaan De Jonge, Jacques C. A. Van Meel, Frieda P. Slothorst-Grisdijk, Egbert Lam, and Pieter A. Van Zwieten
pp 502 - 507; DOI:
10.1021/jm00137a006
PDF
Relation of conformation to antitumor activity of platinum(II) complexes of 1,2-cyclohexanediamine and 2-(aminomethyl)cyclohexylamine isomers against leukemia P388
Masahide Noji, Koji Okamoto, Yoshinori Kidani, and Tazuko Tashiro
pp 508 - 515; DOI:
10.1021/jm00137a007
PDF
Showdomycin analogs: synthesis and antitumor evaluation
Naganori Numao, Hiromichi Hemmi, Saulius A. Naujokaitis, Marco Rabinovitz, and John A. Beisler
pp 515 - 520; DOI:
10.1021/jm00137a008
PDF
Potential antitumor agents. 35. Quantitative relationships between antitumor (L1210) potency and DNA binding for 4'-(9-acridinylamino)methanesulfon-m-anisidide (m-AMSA) analogs
B. C. Baguley, W. A. Denny, G. J. Atwell, and B. F. Cain
pp 520 - 525; DOI:
10.1021/jm00137a009
PDF
Structure-activity relationship in cinnamamides. 3. Synthesis and anticonvulsant activity evaluation of some derivatives of (E)- and (Z)-m-(trifluoromethyl)cinnamamide
A. Balsamo, P. Crotti, A. Lapucci, B. Macchia, F. Macchia, A. Cuttica, and N. Passerini
pp 525 - 532; DOI:
10.1021/jm00137a010
PDF
Structure-activity relationships in a broad-spectrum anthelmintic series. Acid chloride phenylhydrazones. I. Aryl substitutions and chloride variations
Douglas L. Rector, S. D. Folz, R. D. Conklin, L. H. Nowakowski, and Girts Kaugars
pp 532 - 538; DOI:
10.1021/jm00137a011
PDF
Quantitative structure-selectivity relationships. Comparison of the inhibition of Escherichia coli and bovine liver dihydrofolate reductase by 5-(substituted-benzyl)-2,4-diaminopyrimidines
Ren-Li Li, Stephen W. Dietrich, and Corwin Hansch
pp 538 - 544; DOI:
10.1021/jm00137a012
PDF
Inhibition of bovine and rat liver dihydrofolate reductase by 4,6-diamino-1,2-dihydro-2,2-dimethyl-1-(4-substituted-phenyl)-s-triazines
Corwin Hansch, Stephen W. Dietrich, and James Y. Fukunaga
pp 544 - 549; DOI:
10.1021/jm00137a013
PDF
Inhibitors of polyamine biosynthesis. 9. Effects of S-adenosyl-L-methionine analogs on mammalian aminopropyltransferases in vitro and polyamine biosynthesis in transformed lymphocytes
Marvin C. Pankaskie, Mahmoud M. Abdel-Monem, Aarne Raina, Tinchung Wang, and John E. Foker
pp 549 - 553; DOI:
10.1021/jm00137a014
PDF
Potential inhibitors of L-asparagine biosynthesis. 5. Electrophilic amide analogs of (S)-2,3-diaminopropionic acid
Michael Mokotoff and Lawrence W. Logue
pp 554 - 559; DOI:
10.1021/jm00137a015
PDF
Methotrexate analogs. 13. Chemical and pharmacological studies on amide, hydrazide, and hydroxamic acid derivatives of the glutamate side chain
Andre Rosowsky, Cheng-Sein Yu, Jack Uren, Herbert Lazarus, and Michael Wick
pp 559 - 567; DOI:
10.1021/jm00137a016
PDF
Analogs of the cytostatic cyclic tetrapeptide chlamydocin. Synthesis of N.beta.-(N-maleoylglycyl) and N.beta.-(tert-butyloxycarbonyl) derivatives of cyclo(Gly-L-Phe-D-Pro-L-Dap)
Daniel H. Rich, Ronald D. Jasensky, Gerald C. Mueller, and Kristin E. Anderson
pp 567 - 572; DOI:
10.1021/jm00137a017
PDF
Structure-sweetness relationship of L-aspartyl dipeptide analogs. A receptor site topology
Hajime Iwamura
pp 572 - 583; DOI:
10.1021/jm00137a018
PDF
Aromatic retinoic acid analogs. Synthesis and pharmacological activity
Marcia I. Dawson, Peter D. Hobbs, Rebecca L. Chan, Wan-Ru Chao, and Victor A. Fung
pp 583 - 592; DOI:
10.1021/jm00137a019
PDF
Synthesis and anxiolytic activity of 6-(substituted-phenyl)-1,2,4-triazolo[4,3-b]pyridazines
J. D. Albright, D. B. Moran, W. B. Wright, J. B. Collins, B. Beer, A. S. Lippa, and E. N. Greenblatt
pp 592 - 600; DOI:
10.1021/jm00137a020
PDF
Potential radiosensitizing agents. 2. Synthesis and biological activity of derivatives of dinitroimidazole with oxiranes
Raj K. Sehgal, Matthew W. Webb, and Krishna C. Agrawal
pp 601 - 604; DOI:
10.1021/jm00137a021
PDF
Effect of structural change on acute toxicity and antiinflammatory activity in a series of imidazothiazoles and thiazolobenzimidazoles
Larry J. Powers, S. W. Fogt, Z. S. Ariyan, D. J. Rippin, R. D. Heilman, and Richard J. Matthews
pp 604 - 609; DOI:
10.1021/jm00137a022
PDF
Synthesis and antischistosomal activity of certain pyrazolo[1,5-a]pyrimidines
Keitaro Senga, Thomas Novinson, Henry R. Wilson, and Roland K. Robins
pp 610 - 613; DOI:
10.1021/jm00137a023
PDF
Synthesis and anticholinergic properties of the enantiomers of 4-(isopropylamino)-2-(2-pyridyl)-2-phenylbutyramide, the mono-N-dealkylated metabolite of disopyramide
Wendel L. Nelson, Cherilyn K. Sneed, Kathleen M. Giacomini, John C. Giacomini, John Stauss, Terrence F. Blaschke, and Brian M. Cox
pp 614 - 617; DOI:
10.1021/jm00137a024
PDF
Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines] as potential central nervous system agents. 6. Synthesis, carbon-13 NMR, and biological evaluation of cis- and trans-4-amino-3'-arylspiro[cyclohexane-1,1'(3'H)-isobenzofuran] derivatives
Lawrence L. Martin, Manfred Worm, Marc N. Agnew, Hansjoerg Kruse, Jeffrey C. Wilker, and Harry M. Geyer
pp 617 - 621; DOI:
10.1021/jm00137a025
PDF
Synthesis and pharmacological evaluation of poly(oxyethylene) derivatives of 4-isobutylphenyl-2-propionic acid (ibuprofen)
R. Cecchi, L. Rusconi, M. C. Tanzi, F. Danusso, and P. Ferruti
pp 622 - 625; DOI:
10.1021/jm00137a026
PDF
Azaprostaglandin analogs. Synthesis and biological properties of 11-azaprostaglandin derivatives
Achille Barco, Simonetta Benetti, Gian Piero Pollini, Pier Giovanni Baraldi, Mario Guarneri, Carmelo Gandolfi, Roberto Ceserani, and Daniela Longiave
pp 625 - 628; DOI:
10.1021/jm00137a027
PDF
Approaches to vasodilating/.beta.-adrenergic blocking agents: examples of the dihydrolutidine type
John J. Baldwin, R. Hirschmann, Edward L. Engelhardt, Gerald S. Ponticello, Charles S. Sweet, and A. Scriabine
pp 628 - 631; DOI:
10.1021/jm00137a028
PDF
Synthesis and antiinflammatory activity of 2,2'-diaminobiphenyl derivatives
Romano Calcinari, Nadia Case, Alfredo Guerrato, Roberto Milanino, Elda Passarella, Michele Perchinunno, Bruno Tamburini, and Fabio Sparatore
pp 632 - 634; DOI:
10.1021/jm00137a029
PDF
Erythro-5-[1-hydroxy-2-(isopropylamino)butyl]-7-hydroxycarbostyril, a terbutaline-type derivative of the bronchodilator procaterol
Yasumitsu Tamura, Shiro Yoshizaki, and Kouzo Watanabe
pp 634 - 636; DOI:
10.1021/jm00137a030
PDF
Toxicity and quantitative structure-activity relationships of colchicines
Frank R. Quinn, Zohar Neiman, and John A. Beisler
pp 636 - 639; DOI:
10.1021/jm00137a031
PDF
Preparation and antibacterial activity of .DELTA.1-thienamycin
David H. Shih and Ronald W. Ratcliffe
pp 639 - 643; DOI:
10.1021/jm00137a032
PDF
Book Reviews

pp 643 - 650; DOI:
10.1021/jm00137a600
PDF

Issue 6


Perspectives for the use of collagen synthesis inhibitors as antifibrotic agents
George C. Fuller
pp 651 - 658; DOI:
10.1021/jm00138a001
PDF
Mesoionic xanthine analogs: phosphodiesterase inhibitory and hypotensive activity
Richard A. Glennon, Michael E. Rogers, J. Doyle Smith, M. K. El-Said, and John L. Egle
pp 658 - 661; DOI:
10.1021/jm00138a002
PDF
Cyclic urea nucleosides. Cytidine deaminase activity as a function of aglycon ring size
Paul S. Liu, Victor E. Marquez, John S. Driscoll, Richard W. Fuller, and John J. McCormack
pp 662 - 666; DOI:
10.1021/jm00138a003
PDF
Mammalian metabolism of phencyclidine
John K. Baker, James G. Wohlford, Barton J. Bradbury, and Philip W. Wirth
pp 666 - 669; DOI:
10.1021/jm00138a004
PDF
Synthesis and preliminary antitumor evaluation of 5-iminodoxorubicin
Edward M. Acton and George L. Tong
pp 669 - 673; DOI:
10.1021/jm00138a005
PDF
Synthesis and antitumor activity of cysteinyl-3,4-dihydroxyphenylalonines and related compounds
Shosuke Ito, Shigeki Inoue, Yoshinobu Yamamoto, and Keisuke Fujita
pp 673 - 677; DOI:
10.1021/jm00138a006
PDF
Synthesis and evaluation of novel alkylpiperazines as potential dopamine antagonists
Richard A. Glennon, John J. Salley, Odd S. Steinsland, and Sharon Nelson
pp 678 - 683; DOI:
10.1021/jm00138a007
PDF
Synthesis and pharmacological evaluation of sulfonium analogs of dopamine: nonclassical dopamine agonists
Karen Anderson, Alice Kuruvilla, Norman Uretsky, and Duane D. Miller
pp 683 - 687; DOI:
10.1021/jm00138a008
PDF
An approach to the elucidation of metabolic breakdown products of the luteinizing hormone-releasing hormone
Mary Alice Stetler-Stevenson, Dai Chang Yang, Andrew Lipkowski, Linda McCartney, Darryl Peterson, and George Flouret
pp 688 - 692; DOI:
10.1021/jm00138a009
PDF
Synthesis of thyrotropin-releasing hormone analogs with selective central nervous system effects
Ruth F. Nutt, Frederick W. Holly, Carl Homnick, Ralph Hirschmann, Daniel F. Veber, and Byron H. Arison
pp 692 - 698; DOI:
10.1021/jm00138a010
PDF
Inactivation of trypsin-like proteases by depsipeptides of p-guanidinobenzoic acid
Vishwas S. Ganu and Elliott Shaw
pp 698 - 700; DOI:
10.1021/jm00138a011
PDF
Synthetic antagonists of in vivo antidiuretic and vasopressor responses to arginine-vasopressin
Maurice Manning, Bernard Lammek, Alexander M. Kolodziejczyk, J. Seto, and W. H. Sawyer
pp 701 - 706; DOI:
10.1021/jm00138a012
PDF
Synthesis of peptide analogs of prothrombin precursor sequence 5-9. Substrate specificity of vitamin K dependent carboxylase
Daniel H. Rich, S. Russ Lehrman, Megumi Kawai, Hedda L. Goodman, and John W. Suttie
pp 706 - 711; DOI:
10.1021/jm00138a013
PDF
Synthesis and preliminary pharmacological evaluation of asymmetric chloroquine analogs
Donald T. Witiak, David A. Grattan, Richard J. Heaslip, and Ralf G. Rahwan
pp 712 - 717; DOI:
10.1021/jm00138a014
PDF
Analgesic narcotic antagonists. 5. 7,7-Dimethyldihydrocodeinones and 7,7-dimethyldihydromorphinones
David L. Leland and Michael P. Kotick
pp 717 - 721; DOI:
10.1021/jm00138a015
PDF
Analgesic narcotic antagonists. 6. 7.beta.,8.beta.-Methano- and 7.beta.,8.beta.-epoxydihydrocodeinone
Michael P. Kotick
pp 722 - 726; DOI:
10.1021/jm00138a016
PDF
Synthesis and anticonvulsant activity of N-(benzoylalkyl)imidazoles and N-(.omega.-phenyl-.omega.-hydroxyalkyl)imidazoles
Dante Nardi, Alberto Tajana, Amedeo Leonardi, Renzo Pennini, Ferruccio Portioli, Maria Jose Magistretti, and Alessandro Subissi
pp 727 - 731; DOI:
10.1021/jm00138a017
PDF
Synthesis and antiherpetic activity of some 4-[(aryloxy)alkyl]pyrazoles
Guy D. Diana, Philip M. Carabateas, Gordon L. Williams, Francis Pancic, and Bernard A. Steinberg
pp 731 - 735; DOI:
10.1021/jm00138a018
PDF
Pyrazolo[5,1-b]quinazolin-9-ones: a new series of antiallergic agents
Jagadish C. Sircar, Thomas Capiris, Stephen J. Kesten, and David J. Herzig
pp 735 - 742; DOI:
10.1021/jm00138a019
PDF
N-(Aminophenyl)oxamic acids and esters as potent, orally active antiallergy agents
Dieter H. Klaubert, John H. Sellstedt, Charles J. Guinosso, Robert J. Capetola, and Stanley C. Bell
pp 742 - 748; DOI:
10.1021/jm00138a020
PDF
5-Tetrazolecarboxamides and their salts: new orally active antiallergy agents
Dieter H. Klaubert, John H. Sellstedt, Charles J. Guinosso, Stanley C. Bell, and Robert J. Capetola
pp 748 - 752; DOI:
10.1021/jm00138a021
PDF
Pyrimidine acyclic nucleosides. 1-[(2-Hydroxyethoxy)methyl]pyrimidines as candidate antivirals
James L. Kelley, John E. Kelsey, William R. Hall, Mark P. Krochmal, and Howard J. Schaeffer
pp 753 - 756; DOI:
10.1021/jm00138a022
PDF
Inhibitors of phenylethanolamine N-methyltransferase and epinephrine biosynthesis. 3. Bis[tetrahydroisoquinoline]s
R. M. DeMarinis, W. M. Bryan, L. M. Hillegass, D. McDermott, and R. G. Pendleton
pp 756 - 759; DOI:
10.1021/jm00138a023
PDF
Synthesis and antiviral properties of (Z)-5-(2-bromovinyl)-2'-deoxyuridine
A. Stanley Jones, S. George Rahim, Richard T. Walker, and Erik De Clercq
pp 759 - 760; DOI:
10.1021/jm00138a024
PDF
Metabolism of 1,3-bis(2-chloroethyl)-1-nitrosourea by rat hepatic microsomes
Huey-Shin Lin and Robert J. Weinkam
pp 761 - 763; DOI:
10.1021/jm00138a025
PDF
Nitrogen-13-labeled L-amino acids for in vivo assessment of local myocardial metabolism
Fritz J. Baumgartner, Jorge R. Barrio, Eberhard Henze, Heinrich R. Schelbert, Norman S. MacDonald, Michael E. Phelps, and David E. Kuhl
pp 764 - 766; DOI:
10.1021/jm00138a026
PDF
Benz-fused mesoionic xanthine analogs as inhibitors of cyclic-AMP phosphodiesterase
Richard A. Glennon, Judith J. Gaines, and Michael E. Rogers
pp 766 - 769; DOI:
10.1021/jm00138a027
PDF
Book Reviews

pp 769 - 772; DOI:
10.1021/jm00138a600
PDF

Issue 7


6-Demethoxythebaine and its conversion to analgesics of the 6,14-ethenomorphinan type
Charles W. Hutchins, Geoffrey K. Cooper, Serge Puerro, and Henry Rapoport
pp 773 - 777; DOI:
10.1021/jm00139a002
PDF
Opiate receptor interaction of compounds derived from or structurally related to fentanyl
Marinus W. Lobbezoo, Willem Soudijn, and Ineke Van Wijngaarden
pp 777 - 782; DOI:
10.1021/jm00139a003
PDF
Allylprodine analogs as receptor probes. Evidence that phenolic and nonphenolic ligands interact with different subsites on identical opioid receptors
Philip S. Portoghese, Bipin D. Alreja, and Dennis L. Larson
pp 782 - 787; DOI:
10.1021/jm00139a004
PDF
Epimeric cis-decahydroquinoline-5-carboxylic acids: effects on .gamma.-aminobutyric acid uptake and receptor binding in vitro
Donald T. Witiak, Kuniyuki Tomita, Raymond J. Patch, and S. J. Enna
pp 788 - 794; DOI:
10.1021/jm00139a005
PDF
Potential pancreatic imaging agents. Tellurium-123m labeled-DL-.alpha.-amino-.gamma.-(phenyltelluro)butyric acid
Furn F. Knapp, Kathleen R. Ambrose, and Alvin P. Callahan
pp 794 - 797; DOI:
10.1021/jm00139a006
PDF
New antiarrhythmic agents. 6. Quantitative structure-activity relationships of aminoxylidides
Paul A. Tenthorey, Alan J. Block, Robert A. Ronfeld, Paul D. McMaster, and Eugene W. Byrnes
pp 798 - 806; DOI:
10.1021/jm00139a007
PDF
Methylangelicins: new potential agents for the photochemotherapy of psoriasis. Structure-activity study on the dark and photochemical interactions with DNA
Francesco Dall'Acqua, Daniela Vedaldi, Adriano Guiotto, Paolo Rodighiero, Francesco Carlassare, Francarosa Baccichetti, and Franco Bordin
pp 806 - 811; DOI:
10.1021/jm00139a008
PDF
Inhibition of dihydrofolate reductase: structure-activity correlations of quinazolines based upon molecular shape analysis
Carol Battershell, D. Malhotra, and A. J. Hopfinger
pp 812 - 818; DOI:
10.1021/jm00139a009
PDF
Inhibition of dihydrofolate reductase: structure-activity correlations of 2,4-diamino-5-benzylpyrimidines based upon molecular shape analysis
A. J. Hopfinger
pp 818 - 822; DOI:
10.1021/jm00139a010
PDF
Effects of 1-arylpyrroles and naphthoflavones upon cytochrome P-450 dependent monooxygenase activities
Tito Viswanathan and W. L. Alworth
pp 822 - 830; DOI:
10.1021/jm00139a011
PDF
Novel immunosuppressive agents. Potent immunological activity of some benzothiopyrano[4,3-c]pyrazol-3-ones
Joseph G. Lombardino and Ivan G. Otterness
pp 830 - 834; DOI:
10.1021/jm00139a012
PDF
N-Aralkyl substitution of 2-amino-5,6- and -6,7-dihydroxy-1,2,3,4-tetrahydronaphthalenes. 1. Cardiac and pressor/depressor activities
Richard J. Gorczynski, William G. Anderson, and David M. Stout
pp 835 - 839; DOI:
10.1021/jm00139a013
PDF
Synthesis and biological evaluation of the methyl esters of (+)-12-fluoro-13,14-dihydroprostaglandin F2.alpha. and (+)-15-epi-12-fluoro-13,14-dihydroprostaglandin F2.alpha.
Paul A. Grieco and Tetsuo Takigawa
pp 839 - 843; DOI:
10.1021/jm00139a014
PDF
A nonmetabolized analog of phenytoin
James D. Henderson, Peter G. Dayton, Zafar H. Israili, and Leon Mandell
pp 843 - 847; DOI:
10.1021/jm00139a015
PDF
Haloacetamido analogs of 2-amino-2-deoxy-D-mannose. Syntheses and effects on tumor-bearing mice
Thomas P. Fondy and Cheryl A. Emlich
pp 848 - 852; DOI:
10.1021/jm00139a016
PDF
Synthesis and antitumor activity of a series of sulfone analogs of 1,4-naphthoquinone
Mark H. Holshouser, Larry J. Loeffler, and Iris H. Hall
pp 853 - 858; DOI:
10.1021/jm00139a017
PDF
Comparison of mutagenic and carcinogenic activities of aniline mustards
Albert Leo, Augustine Panthananickal, Corwin Hansch, Jeffrey Theiss, Michael Shimkin, and A. W. Andrews
pp 859 - 864; DOI:
10.1021/jm00139a018
PDF
(Acylaryloxy)acetic acid diuretics. 3. 2,3-Dihydro-5-acyl-2-benzofurancarboxylic acids, a new class of uricosuric diuretics
William F. Hoffman, Otto W. Woltersdorf, Frederick C. Novello, Edward J. Cragoe, James P. Springer, L. Sherman Watson, and George M. Fanelli
pp 865 - 873; DOI:
10.1021/jm00139a019
PDF
(Acylaryloxy)acetic acid diuretics. 4. Indeno[5,4-b]furan-2-carboxylic acids
Otto W. Woltersdorf, S. Jane deSolms, and Edward J. Cragoe
pp 874 - 878; DOI:
10.1021/jm00139a020
PDF
Synthesis and antiallergy activity of 4-oxo-4H-pyrido[1,2-a]thieno[2,3-d]pyrimidines
Francis J. Tinney, Wiaczeslaw A. Cetenko, Joseph J. Kerbleski, David T. Connor, Roderick J. Sorenson, and David J. Herzig
pp 878 - 882; DOI:
10.1021/jm00139a021
PDF
Synthesis and serotonin-like activity of 2-amino-5,8-dimethoxy-6-methyl-1,2-dihydronaphthalene
Paresh J. Kothari, Bruce A. Hathaway, David E. Nichols, and George K. W. Yim
pp 882 - 884; DOI:
10.1021/jm00139a022
PDF
Synthesis of Ala-Pro-Gly-[Ile3,Val5]angiotensin II isolated from the skin of the Australian frog Crinia georgiana
M. C. Khosla, F. M. Bumpus, T. Yasuhara, and T. Nakajima
pp 885 - 887; DOI:
10.1021/jm00139a023
PDF
Synthesis of 5'-thymidinyl bis(1-aziridinyl)phosphinates as antineoplastic agents
Luke Y. Hsiao and Thomas J. Bardos
pp 887 - 889; DOI:
10.1021/jm00139a024
PDF
(Phenylthio)phenylamine derivatives as potential antiinflammatory compounds
A. Marcincal-Lefebvre, J. C. Gesquiere, C. Lemer, and B. Dupuis
pp 889 - 893; DOI:
10.1021/jm00139a025
PDF
Nucleosides. 114. 5'-O-Glucuronides of 5-fluorouridine and 5-fluorocytidine. Masked precursors of anticancer nucleosides
K. A. Watanabe, A. Matsuda, M. J. Halat, D. H. Hollenberg, J. S. Nisselbaum, and J. J. Fox
pp 893 - 897; DOI:
10.1021/jm00139a026
PDF
Aporphines. 34. (-)-2,10,11-Trihydroxy-N-n-propylnoraporphine, a novel dopaminergic aporphine alkaloid with anticonvulsant activity
J. L. Neumeyer, S. J. Law, B. Meldrum, G. Anlezark, and K. J. Watling
pp 898 - 899; DOI:
10.1021/jm00139a027
PDF
Compatibility of the Free-Wilson and Hansch quantitative structure-activity relations
L. J. Schaad, B. A. Hess, W. P. Purcell, A. Cammarata, R. Franke, and H. Kubinyi
pp 900 - 901; DOI:
10.1021/jm00139a028
PDF
Synthesis and evaluation of the male antifertility properties of a series of N-unsubstituted sulfamates
Allen F. Hirsch, Charles Kasulanis, Larry Kraft, Robert A. Mallory, Gregory Powell, and Benny Wong
pp 901 - 903; DOI:
10.1021/jm00139a029
PDF
Synthesis of analogs of acetylmethadol and methadol as potential narcotic antagonists
Danny L. Lattin, Bill Caviness, Rick G. Hudson, David L. Greene, Pamela K. Raible, and J. Blake Richardson
pp 903 - 906; DOI:
10.1021/jm00139a030
PDF
Studies on phenethylamine hallucinogens. 2. Conformations of arylmethoxyl groups by carbon-13 NMR
James J. Knittel and Alexandros Makriyannis
pp 906 - 909; DOI:
10.1021/jm00139a031
PDF
Book Reviews

pp 909 - 912; DOI:
10.1021/jm00139a600
PDF

Issue 8


1980 Award in medicinal chemistry. Medicinal chemistry and dynamic structure-activity analysis in the discovery of drugs acting at histamine H2 receptors
Robin Ganellin
pp 913 - 920; DOI:
10.1021/jm00140a001
PDF
8-Hydroxy-2-(dipropylamino)tetralin, a new centrally acting 5-hydroxytryptamine receptor agonist
Lars Erik Arvidsson, Uli Hacksell, J. Lars G. Nilsson, Stephan Hjorth, Arvid Carlsson, Per Lindberg, Domingo Sanchez, and Haakan Wikstroem
pp 921 - 923; DOI:
10.1021/jm00140a002
PDF
Antitumor agents. 44. Bis(helenalinyl) esters and related derivatives as novel potent antileukemic agents
Kuo-Hsiung Lee, Toshiro Ibuka, Donald Sims, Osamu Muraoka, Hiroshi Kiyokawa, Iris H. Hall, and Hyeong L. Kim
pp 924 - 927; DOI:
10.1021/jm00140a003
PDF
Gastric antisecretory agents. 1. Antisecretory and antiulcer activity of 5H-[1]benzopyrano[2,3-b]pyridin-5-ylureas and 5H-[1]benzothiopyrano[2,3-b]pyridin-5-ylureas
James A. Bristol, Elijah H. Gold, Raymond G. Lovey, and James F. Long
pp 927 - 932; DOI:
10.1021/jm00140a004
PDF
2,4-Diamino-5-benzylpyrimidines and analogs as antibacterial agents. 5. 3',5'-Dimethoxy-4'-substituted-benzyl analogs of trimethoprim
Barbara Roth, Edward Aig, Barbara S. Rauckman, Justina Z. Strelitz, Arthur P. Phillips, Robert Ferone, S. R. M. Bushby, and Carl W. Sigel
pp 933 - 941; DOI:
10.1021/jm00140a005
PDF
Synthesis and antiviral activity of certain 9-.beta.-D-ribofuranosylpurine-6-carboxamides
James D. Westover, Ganapathi R. Revankar, Roland K. Robins, Randall D. Madsen, John R. Ogden, James A. North, Robert W. Mancuso, Robert J. Rousseau, and Edward L. Stephen
pp 941 - 946; DOI:
10.1021/jm00140a006
PDF
Synthesis and pharmacological evaluation of a series of analogs of 1-methylisoguanosine
Robert T. Bartlett, Alan F. Cook, Michael J. Holman, Warren W. McComas, Eugene F. Nowoswait, Mohindar S. Poonian, Judy A. Baird-Lambert, Brian A. Baldo, and John F. Marwood
pp 947 - 954; DOI:
10.1021/jm00140a007
PDF
Inhibition of separated forms of cyclic nucleotide phosphodiesterase from pig coronary arteries by 1,3-disubstituted and 1,3,8-trisubstituted xanthines
Jack N. Wells, John E. Garst, and George L. Kramer
pp 954 - 958; DOI:
10.1021/jm00140a008
PDF
Cerebrovasodilatation through selective inhibition of the enzyme carbonic anhydrase. 3. 5-(Arylthio)-, 5-(arylsulfinyl)-, and 5-(arylsulfonyl)thiophene-2-sulfonamides
Ian T. Barnish, Peter E. Cross, Roger P. Dickinson, Michael J. Parry, and Michael J. Randall
pp 959 - 964; DOI:
10.1021/jm00140a009
PDF
Novel synthesis of (S)-1-[5-(benzoylamino)-1,4-dioxo-6-phenylhexyl]-L-proline and analogs: potent angiotensin converting enzyme inhibitors
Robert F. Meyer, Ernest D. Nicolaides, Francis G. Tinney, Elizabeth A. Lunney, Ann Holmes, Milton L. Hoefle, Ronald D. Smith, Arnold D. Essenburg, Harvey R. Kaplan, and Ronald G. Almquist
pp 964 - 969; DOI:
10.1021/jm00140a010
PDF
Selective and potent .beta.2-adrenoceptor agents within the tetrahydroisoquinoline class: effect of methyl substitution at the benzylic carbon of the 1-(3,4,5-trimethoxybenzyl) group of trimetoquinol
Douglas J. Sober, Jane Chang, Edward H. Fairchild, John W. Fowble, Asoke Mukhopadhyay, Dennis R. Feller, and Duane D. Miller
pp 970 - 974; DOI:
10.1021/jm00140a011
PDF
Development of new mitomycin C and porfiromycin analogs
Bhashyam S. Iyengar, Horng-Jau Lin, Leung Cheng, William A. Remers, and William T. Bradner
pp 975 - 981; DOI:
10.1021/jm00140a012
PDF
Pyrazolodiazepines. III. 4-Aryl-1,6,7,8-tetrahydro-1,3-dialkylpyrazolo[3,4-e][1,4]diazepines as antidepressant agents
H. A. DeWald, S. Lobbestael, and B. P. H. Poschel
pp 982 - 987; DOI:
10.1021/jm00140a013
PDF
N-Hydroxyacetaminophen: a postulated toxic metabolite of acetaminophen
Ian C. Calder, Sandra J. Hart, Kevin Healey, and Kathryn N. Ham
pp 988 - 993; DOI:
10.1021/jm00140a014
PDF
2-Benzodioxinylaminoethanol: a new class of .beta.-adrenergic blocking and antihypertensive agents
Lucien Lalloz, Vincent Loppinet, Gerard Coudert, Gerald Guillaumet, Bernard Loubinoux, Claude Labrid, Michele Beaughard, Georges Dureng, and Jean Claude Lamar
pp 994 - 998; DOI:
10.1021/jm00140a015
PDF
2-(Arylmethyl)arylacetic acids as potential antiinflammatory agents
Giovanni Brancaccio, Angelo Larizza, Guglielmo Lettieri, and Pietro Monforte
pp 998 - 1000; DOI:
10.1021/jm00140a016
PDF
Antimalarial drugs. 50. Folate antagonists. 19. Synthesis and antimalarial effects of 6-(arylthio)-2,4-pteridinediamines
Edward F. Elslager, Judith L. Johnson, and Leslie M. Werbel
pp 1001 - 1003; DOI:
10.1021/jm00140a017
PDF
Diuretic agents related to indapamide. 1. Synthesis and activity of 1-substituted 2-(4-chloro-3-sulfamoylbenzamido)isoindolines
Giorgio Cignarella, Paolo Sanna, Egidio Miele, Vittorio Anania, and Maria S. Desole
pp 1003 - 1006; DOI:
10.1021/jm00140a018
PDF
Nonsteroidal antiinflammatory agents. 3. Synthesis of the positional isomers of 4'-chloro-5-methoxy-3-biphenylylacetic acid and their antiinflammatory and analgesic activities
Yasumitsu Tamura, Yoshihiko Yoshimoto, Shinichi Tada, Katsutoshi Kunimoto, Shingo Matsumura, Masao Murayama, Yoshihisa Shibata, and Hiroshi Enomoto
pp 1006 - 1010; DOI:
10.1021/jm00140a019
PDF
Gastric antisecretory agents. 2. Antisecretory activity of 9-[(aminoalkyl)thio]-9H-xanthenes and 5-[(aminoalkyl)thio]-5H-[1]benzopyrano[2,3-b]pyridines
James A. Bristol, Elijah H. Gold, Irwin Gross, Raymond G. Lovey, and James F. Long
pp 1010 - 1013; DOI:
10.1021/jm00140a020
PDF
Dopamine agonist properties of N-alkyl-4-(3,4-dihydroxyphenyl)-1,2,3,4-tetrahydroisoquinolines
James N. Jacob, David E. Nichols, Jai D. Kohli, and Dana Glock
pp 1013 - 1015; DOI:
10.1021/jm00140a021
PDF
Syntheses of 9-acridine- and 2-phenanthridinemethanols as potential antimalarials
Chester W. Muth, Howard L. Minigh, Suchart Chookruvong, Larry A. Hall, and Hung-Tai Chao
pp 1016 - 1018; DOI:
10.1021/jm00140a022
PDF
Book Reviews

pp 1018 - 1020; DOI:
10.1021/jm00140a600
PDF

Issue 9


Synthesis of clozapine analogs and their affinity for clozapine and spiroperidol binding sites in rat brain
Tomas De Paulis, C. Ross Betts, Howard E. Smith, Philip L. Mobley, D. Hal Manier, and Fridolin Sulser
pp 1021 - 1026; DOI:
10.1021/jm00141a001
PDF
Dopamine receptor model and its application in the design of a new class of rigid pyrrolo[2,3-g]isoquinoline antipsychotics
Gary L. Olson, Ho-Chuen Cheung, Keith D. Morgan, John F. Blount, Louis Todaro, Leo Berger, Arnold B. Davidson, and Edward Boff
pp 1026 - 1034; DOI:
10.1021/jm00141a002
PDF
Inhibition of cholesterol side-chain cleavage. 3. 22-Azacholesterol analogs bearing aryl-substituted side chains
Norma G. Delaney and Matthias C. Lu
pp 1034 - 1038; DOI:
10.1021/jm00141a003
PDF
Inhibition of cholesterol side-chain cleavage. 4. Synthesis of A or B ring-modified azacholesterols
Matthias C. Lu, Norma G. Delaney, and Raymond E. Counsell
pp 1038 - 1042; DOI:
10.1021/jm00141a004
PDF
Synthesis of fluorine-containing peptides. Analogs of angiotensin II containing hexafluorovaline
William H. Vine, Kun-Hwa Hsieh, and Garland R. Marshall
pp 1043 - 1047; DOI:
10.1021/jm00141a005
PDF
Phencyclidine metabolism: resolution, structure, and biological activity of the isomers of the hydroxymetabolite, 4-phenyl-4-(1-piperidinyl)cyclohexanol
F. Ivy Carroll, George A. Brine, Karl G. Boldt, Edward J. Cone, David Yousefnejad, D. Bruce Vaupel, and William F. Buchwald
pp 1047 - 1051; DOI:
10.1021/jm00141a006
PDF
N2- and C-7-Substituted actinomycin D analogs: synthesis, DNA-binding affinity, and biochemical and biological properties. Structure-activity relationship
Sisir K. Sengupta, Jerome E. Anderson, Yury Kogan, Dorothy H. Trites, William R. Beltz, and Madulla S. Madhavarao
pp 1052 - 1059; DOI:
10.1021/jm00141a007
PDF
New antiarrhythmic agents. 7. 2,3-Diaminopropionanilides
Paul A. Tenthorey, H. Jack Adams, George H. Kronberg, and Bertil H. Takman
pp 1059 - 1063; DOI:
10.1021/jm00141a008
PDF
2-(Aminomethyl)phenols, a new class of saluretic agents. 3. Effects of functional group reorientation and modification
G. E. Stokker, A. A. Deana, S. J. DeSolms, E. M. Schultz, R. L. Smith, E. J. Cragoe, J. E. Baer, H. F. Russo, and L. S. Watson
pp 1063 - 1067; DOI:
10.1021/jm00141a009
PDF
Folate analogs altered in the C9-N10 bridge region. 18. Synthesis and antitumor evaluation of 11-oxahomoaminopterin and related compounds
M. G. Nair, Timothy W. Bridges, Timothy J. Henkel, Roy L. Kisliuk, Y. Gaumont, and F. M. Sirotnak
pp 1068 - 1073; DOI:
10.1021/jm00141a010
PDF
Antimicrobial 3-methylene flavanones
Frederick E. Ward, David L. Garling, Robert T. Buckler, David M. Lawler, and Dennis P. Cummings
pp 1073 - 1077; DOI:
10.1021/jm00141a011
PDF
Synthesis and biological effects of acyclic pyrimidine nucleoside analogs
Alan C. Schroeder, Robert G. Hughes, and Alexander Bloch
pp 1078 - 1083; DOI:
10.1021/jm00141a012
PDF
Carbocyclic analogs of 5-fluorouracil nucleosides
Y. Fulmer Shealy, Jerry L. Frye, Nancy F. DuBois, Sue C. Shaddix, and R. Wallace Brockman
pp 1083 - 1086; DOI:
10.1021/jm00141a013
PDF
Synthesis of 5,11-methenyltetrahydrohomofolate and its antifolate activity in vitro
Carol A. Caperelli, Paul Domanico, and Stephen J. Benkovic
pp 1086 - 1088; DOI:
10.1021/jm00141a014
PDF
Cyclic urea and thiourea derivatives as inducers of murine erythroleukemia differentiation
Chau-Der Li, Sharon L. Mella, and Alan C. Sartorelli
pp 1089 - 1092; DOI:
10.1021/jm00141a015
PDF
Induction of differentiation of leukemia cells in vitro by N-substituted amides, lactams, and 2-pyridones
Chau-Der Li, Edward L. Schwartz, Sharon L. Mella, Lana S. Rittmann, and Alan C. Sartorelli
pp 1092 - 1094; DOI:
10.1021/jm00141a016
PDF
Potential histamine H2-receptor blockers. 3- and 2-Indole derivatives as immobile analogs of tautomeric forms of cimetidine
Haile Tecle, Lillian Robichaud, and Charles F. Schwender
pp 1095 - 1097; DOI:
10.1021/jm00141a017
PDF
Antiinflammatory 5,6-dihydro-11-oxodibenz[b,e]azepine-3-acetic acids
James P. Dunn, Joseph M. Muchowski, and Peter H. Nelson
pp 1097 - 1099; DOI:
10.1021/jm00141a018
PDF
Inhibition of liver alanine aminotransferase activity by some benzophenanthridine alkaloids
Daniela Walterova, Jitka Ulrichova, Vladimir Preininger, Vilim Simanek, Jiri Lenfeld, and Jan Lasovsky
pp 1100 - 1103; DOI:
10.1021/jm00141a019
PDF
Structure-activity relationship study of spirolactones. Contribution of the cyclopropane ring to antimineralocorticoid activity
Leland J. Chinn, Karlene W. Salamon, and Bipin N. Desai
pp 1103 - 1107; DOI:
10.1021/jm00141a020
PDF
Synthesis and evaluation of 1,2,3,4-tetrahydro[1]benzothieno[2,3-h]isoquinolines as dopamine antagonists
Charles R. Ellefson and Kathleen A. Prodan
pp 1107 - 1110; DOI:
10.1021/jm00141a021
PDF
Book Reviews

pp 1110 - 1112; DOI:
10.1021/jm00141a600
PDF

Issue 10


Future directions in dopaminergic nervous system and dopaminergic agonists
Joseph G. Cannon, John Paul Long, and Ranbir Bhatnagar
pp 1113 - 1118; DOI:
10.1021/jm00142a001
PDF
Evidence of the preferential involvement of .mu.-receptors in analgesia using enkephalins highly selective for peripheral .mu. or .delta. receptors
Gilles Gacel, Marie Claude Fournie-Zaluski, Etienne Fellion, and Bernard P. Roques
pp 1119 - 1124; DOI:
10.1021/jm00142a002
PDF
Nonquaternary cholinesterase reactivators. Dialkylaminoalkyl thioesters of .alpha.-ketothiohydroximic acids as reactivators of diisopropyl phosphorofluoridate-inhibited acetylcholinesterase
Richard A. Kenley, Robert A. Howd, Carol W. Mosher, and John S. Winterle
pp 1124 - 1133; DOI:
10.1021/jm00142a003
PDF
Trapping of metabolically generated electrophilic species with cyanide ion: metabolism of methapyrilene
R. Ziegler, Bert Ho, and N. Castagnoli
pp 1133 - 1138; DOI:
10.1021/jm00142a004
PDF
Highly selective inhibitors of thromboxane synthetase. 1. Imidazole derivatives
Kinji Iizuka, Kenji Akahane, Denichi Momose, Masayuki Nakazawa, Tadao Tanouchi, Masanori Kawamura, Isao Ohyama, Ikuo Kajiwara, Yohichi Iguchi, and et al.
pp 1139 - 1148; DOI:
10.1021/jm00142a005
PDF
Highly selective inhibitors of thromboxane synthetase. 2. Pyridine derivatives
Tadao Tanouchi, Masamori Kawamura, Isao Ohyama, Ikuo Kajiwara, Yohichi Iguchi, Takanori Okada, Tsumoru Miyamoto, Ken Taniguchi, Masaki Hayashi, and et al.
pp 1149 - 1155; DOI:
10.1021/jm00142a006
PDF
Inhibition of inosinic acid dehydrogenase by 8-substituted purine nucleotides
Edward B. Skibo and Rich B. Meyer
pp 1155 - 1161; DOI:
10.1021/jm00142a007
PDF
Interaction of 1-(5-phospho-.beta.-D-arabinofuranosyl)-5-substituted-uracils with thymidylate synthetase: mechanism-based inhibition by 1-(5-phospho-.beta.-D-arabinofurosyl)-5-fluorouracil
Chikao Nakayama, Yusuke Wataya, Daniel V. Santi, Mineo Saneyoshi, and Tohru Ueda
pp 1161 - 1165; DOI:
10.1021/jm00142a008
PDF
Pyrazolopyrimidine nucleosides. 12. Synthesis and biological activity of certain pyrazolo[3,4-d]pyrimidine nucleosides related to adenosine
Ganapati A. Bhat, Jean Louis G. Montero, Raymond P. Panzica, Linda L. Wotring, and Leroy B. Townsend
pp 1165 - 1172; DOI:
10.1021/jm00142a009
PDF
Synthesis and biological activity of certain derivatives of oxazinomycin and related oxadiazole nucleosides
Prem C. Srivastava and Roland K. Robins
pp 1172 - 1177; DOI:
10.1021/jm00142a010
PDF
Synthesis and antitumor activity of an acyclonucleoside derivative of 5-fluorouracil
Andre Rosowsky, Sun-Hyuk Kim, and Michael Wick
pp 1177 - 1181; DOI:
10.1021/jm00142a011
PDF
N*-N*-S* Tridentate ligand system as potential antitumor agents
Ippolito Antonini, Francesco Claudi, Gloria Cristalli, Palmarisa Franchetti, Mario Grifantini, and Sante Martelli
pp 1181 - 1184; DOI:
10.1021/jm00142a012
PDF
Synthesis and antineoplastic activity of mitosene analogs of the mitomycins
John C. Hodges, William A. Remers, and William T. Bradner
pp 1184 - 1191; DOI:
10.1021/jm00142a013
PDF
Potential antiestrogens. Synthesis and evaluation of mammary tumor inhibiting activity of 1,2-dialkyl-1,2-bis(3'-hydroxyphenyl)ethanes
Rolf W. Hartmann, Helga Buchborn, Gerhard Kranzfelder, Helmut Schoenenberger, and Arthur E. Bogden
pp 1192 - 1197; DOI:
10.1021/jm00142a014
PDF
Membrane effects of antiinflammatory agents. 1. Interaction of sulindac and its metabolites with phospholipid membrane, a magnetic resonance study
Sophie S. Fan and T. Y. Shen
pp 1197 - 1202; DOI:
10.1021/jm00142a015
PDF
Membrane effects of antiinflammatory agents. 2. Interaction of nonsteroidal antiinflammatory drugs with liposome and purple membranes
San-Bao Hwang and T. Y. Shen
pp 1202 - 1211; DOI:
10.1021/jm00142a016
PDF
.beta.-Adrenergic blocking agents. .alpha.- and .gamma.-Methyl(aryloxy)propanolamines
Thomas L. Lemke, Michael B. Cramer, Stanley W. Adamski, Carolyn A. Pedone, and Gary Brooker
pp 1211 - 1214; DOI:
10.1021/jm00142a017
PDF
Retinoic acid analogs with ring modifications. Synthesis and pharmacological activity
Marcia I. Dawson, Peter D. Hobbs, Rebecca L. S. Chan, and Wan-Ru Chao
pp 1214 - 1223; DOI:
10.1021/jm00142a018
PDF
Synthesis and neuroleptic activity of benzamides. cis-N-(1-Benzyl-2-methylpyrrolidin-3-yl)-5-chloro-2-methoxy-4-(methylamino)benzamide and related compounds
Sumio Iwanami, Mutsuo Takashima, Yasufumi Hirata, Osamu Hasegawa, and Shinji Usuda
pp 1224 - 1230; DOI:
10.1021/jm00142a019
PDF
A new nontricyclic antidepressant agent. Synthesis and activity of N-[trans-2-dimethylaminocyclopentyl]-N-(3,4-dichlorophenyl)propanamide and related compounds
J. Szmuszkovicz, P. F. VonVoigtlander, and M. P. Kane
pp 1230 - 1236; DOI:
10.1021/jm00142a020
PDF
Synthesis and pharmacology of hydroxylated metabolites of methyl phenidate
Kennerly S. Patrick, Clinton D. Kilts, and George R. Breese
pp 1237 - 1240; DOI:
10.1021/jm00142a021
PDF
Synthesis and pharmacological activity of thiohexital enantiomers
F. Ivy Carroll, Abraham Philip, D. Mark Naylor, H. Dix Christensen, and W. C. Goad
pp 1241 - 1244; DOI:
10.1021/jm00142a022
PDF
Potential salicylamide antiplaque agents: in vitro antibacterial activity against Actinomyces viscosus
Robert A. Coburn, Armando J. Batista, Richard T. Evans, and Robert J. Genco
pp 1245 - 1249; DOI:
10.1021/jm00142a023
PDF
Synthesis and evaluation of ureido and vinylureidopenicillins as inhibitors of intraruminal lactic acid production
Robin D. Clark, Joan M. Caroon, Ian T. Harrison, Arthur F. Kluge, Stefan H. Unger, Howard R. Spires, and Thomas R. Mathews
pp 1250 - 1253; DOI:
10.1021/jm00142a024
PDF
New synthesis of N-[4-[[(2-amino-4(3H)-oxopyrido[3,2-d]pyrimidin-6-yl)methyl]amino]benzoyl]-L-glutamic acid (8-deazafolic acid) and the preparation of some 5,6,7,8-tetrahydro derivatives
Carroll Temple, C. L. Kussner, J. D. Rose, D. L. Smithers, L. L. Bennett, and J. A. Montgomery
pp 1254 - 1258; DOI:
10.1021/jm00142a025
PDF
Synthesis and adrenoceptor affinity of some highly polar .beta.-substituted catecholamines
James G. Henkel, Neil Sikand, Alexandros Makriyannis, and Gerald Gianutsos
pp 1258 - 1260; DOI:
10.1021/jm00142a026
PDF
(.alpha.S)-erythro-.alpha.-Methylepinephrine: preparation and stereoselective binding to adrenergic receptors in rat forebrain
Clinton A. Taylor, Howard E. Smith, Michael R. Goldberg, and David Robertson
pp 1261 - 1263; DOI:
10.1021/jm00142a027
PDF
A novel approach for heavy metal poisoning treatment, a model. Mercury poisoning by means of chelating microspheres: hemoperfusion and oral administration
Shlomo Margel
pp 1263 - 1266; DOI:
10.1021/jm00142a028
PDF
Book Reviews

pp 1267 - 1268; DOI:
10.1021/jm00142a600
PDF

Issue 11


Diterpenoid sweeteners. Synthesis and sensory evaluation of stevioside analogs nondegradable to steviol
Grant E. DuBois, Paul S. Dietrich, Janice F. Lee, Geoff V. McGarraugh, and Rebecca A. Stephenson
pp 1269 - 1271; DOI:
10.1021/jm00143a001
PDF
Synthesis and evaluation of some stable multisubstrate adducts as inhibitors of catechol O-methyltransferase
Gary L. Anderson, Donald L. Bussolotti, and James K. Coward
pp 1271 - 1277; DOI:
10.1021/jm00143a002
PDF
Synthesis and evaluation of some stable multisubstrate adducts as specific inhibitors of spermidine synthase
Kuo-Chang Tang, Roy Mariuzza, and James K. Coward
pp 1277 - 1284; DOI:
10.1021/jm00143a003
PDF
Mesoionic purinone analogs as inhibitors of cyclic-AMP phosphodiesterase: comparison of several ring systems
Michael E. Rogers, Richard A. Glennon, J. Doyle Smith, Marvin R. Boots, Nitin Nanavati, Julie E. Maconaughey, Debbie Aub, Sheree Thomas, R. G. Bass, and Godwin Mbagwu
pp 1284 - 1287; DOI:
10.1021/jm00143a004
PDF
Inhibition of human acrosin by monosaccharides and related compounds: structure-activity relationships
Robert A. Anderson, Christine Oswald, and Lourens J. D. Zaneveld
pp 1288 - 1291; DOI:
10.1021/jm00143a005
PDF
2-L-Rhamnopyranosyl[1,2,4]triazolo[1,5-a]pyridine. 4' and 3' Oxidation products. Synthesis and structure-activity relationships
Patrice Allard, Tam Huynh Dinh, Catherine Gouyette, Jean Igolen, Jean-Claude Chermann, and Francoise Barre-Sinoussi
pp 1291 - 1297; DOI:
10.1021/jm00143a006
PDF
Preparation and analgesic properties of amino acid derivatives of (-)-5,9.alpha.-diethyl-2'-hydroxybenzomorphan
Patrice C. Belanger, John Scheigetz, Robert N. Young, Stella E. Charleson, Roger L. Hudgin, and Edward L. Engelhardt
pp 1297 - 1299; DOI:
10.1021/jm00143a007
PDF
Acidic epinephrine analogs derived from 1H,3H-2,1,3-benzothiadiazole 2,2-dioxide and from trifluoromethanesulfonanilide. New synthesis of 1H,3H-2,1,3-benzothiadiazole 2,2-dioxide
R. Morrin Acheson, Maris G. Bite, and John E. G. Kemp
pp 1300 - 1304; DOI:
10.1021/jm00143a008
PDF
Alkylating angiotensin II analogs: Synthesis, analysis, and biological activity of angiotensin II analogs containing the nitrogen mustard melphalan in position 8
Kun-Hwa Hsieh and Garland R. Marshall
pp 1304 - 1310; DOI:
10.1021/jm00143a009
PDF
Synthesis and antibacterial activity of some esters, amides, and hydrazides of 3-carboxyrifamycin S. Relationship between structure and activity of ansamycins
Piero Bellomo, Egidio Marchi, Giuseppe Mascellani, and Mario Brufani
pp 1310 - 1314; DOI:
10.1021/jm00143a010
PDF
Synthesis and antibacterial activity of 1-(arylamino)-1H-pyrroles and 4-(1H-pyrrol-1-ylimino)-2,5-cyclohexadienes
Robert E. Johnson, Albert E. Soria, John R. O'Connor, and Richard A. Dobson
pp 1314 - 1319; DOI:
10.1021/jm00143a011
PDF
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones
Joan M. Caroon, Robin D. Clark, Arthur F. Kluge, Janis T. Nelson, Arthur M. Strosberg, Stefan H. Unger, Anton D. Michel, and Roger L. Whiting
pp 1320 - 1328; DOI:
10.1021/jm00143a012
PDF
Synthesis and antimetastatic properties of stereoisomeric tricyclic bis(dioxopiperazine) analogs in a B16 melanoma model
Donald T. Witiak, Bharat K. Trivedi, Laura B. Campolito, Bruce S. Zwilling, and Nancy A. Reiches
pp 1329 - 1332; DOI:
10.1021/jm00143a013
PDF
New dimeric analogs of ethidium: synthesis, interaction with DNA, and antitumor activity
Karl F. Kuhlmann and Carol W. Mosher
pp 1333 - 1337; DOI:
10.1021/jm00143a014
PDF
Anticoccidial derivatives of 6-azauracil. 4. A 1000-fold enhancement of potency by phenyl sulfide and phenyl sulfone side chains
Max W. Miller, Banavara L. Mylari, Harold L. Howes, Sanford K. Figdor, Martin J. Lynch, John E. Lynch, Shyam K. Gupta, Larry R. Chappel, and Richard C. Koch
pp 1337 - 1342; DOI:
10.1021/jm00143a015
PDF
Side-chain effects on phenothiazine cation radical reactions
Patricia Holt Sackett, J. S. Mayausky, Theresa Smith, Susan Kalus, and Richard L. McCreery
pp 1342 - 1347; DOI:
10.1021/jm00143a016
PDF
Sulfur analogues of psychotomimetic agents. Monothio analogs of mescaline and isomescaline
Peyton Jacob and Alexander T. Shulgin
pp 1348 - 1353; DOI:
10.1021/jm00143a017
PDF
N-(Methanesulfonyl)-16-phenoxyprostaglandin carboxamides: tissue-selective, uterine stimulants
Thomas K. Schaaf, Jasjit S. Bindra, James F. Eggler, Jacob J. Plattner, A. James Nelson, M. Ross Johnson, Jay W. Constantine, Hans-Juergen Hess, and Walter Elger
pp 1353 - 1359; DOI:
10.1021/jm00143a018
PDF
Antimycotic imidazoles. 5. Synthesis and antimycotic properties of 1-[[2-aryl-4-(arylalkyl)-1,3-dioxolan-2-yl]methyl]-1H-imidazoles
J. Heeres and J. Van Cutsem
pp 1360 - 1364; DOI:
10.1021/jm00143a019
PDF
.beta.-Adrenergic blocking agents. 21. Threo-1-(aryloxy)-3-(alkylamino)butan-2-ols
Howard Tucker
pp 1364 - 1368; DOI:
10.1021/jm00143a020
PDF
Structure of a copper-isoniazid complex
Jonathan C. Hanson, Norman Camerman, and Arthur Camerman
pp 1369 - 1371; DOI:
10.1021/jm00143a021
PDF
Book Reviews

pp 1371 - 1376; DOI:
10.1021/jm00143a600
PDF

Issue 12


.gamma.-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects
Povl Krogsgaard-Larsen
pp 1377 - 1383; DOI:
10.1021/jm00144a001
PDF
Adenosine deaminase inhibitors. Conversion of a single chiral synthon into erythro- and threo-9-(2-hydroxy-3-nonyl)adenines
Gerard Bastian, Michel Bessodes, Raymond P. Panzica, Elie Abushanab, Shih Fong Chen, Johanna D. Stoeckler, and Robert E. Parks
pp 1383 - 1385; DOI:
10.1021/jm00144a002
PDF
Inhibition of thymidylate synthetase by 5-alkynyl-2'-deoxyuridylates
Philip J. Barr, Patricia A. Nolan, Daniel V. Santi, and Morris J. Robins
pp 1385 - 1388; DOI:
10.1021/jm00144a003
PDF
Cell-specific ligands for selective drug delivery to tissues and organs
Mitree M. Ponpipom, Robert L. Bugianesi, James C. Robbins, T. W. Doebber, and T. Y. Shen
pp 1388 - 1395; DOI:
10.1021/jm00144a004
PDF
Influence of fluorine substitution on the site of enzymic O-methylation of fluorinated norepinephrines
Cyrus R. Creveling, Elizabeth T. McNeal, Daniele Cantacuzene, and Kenneth L. Kirk
pp 1395 - 1399; DOI:
10.1021/jm00144a005
PDF
5-Fluoro- and 5-chlorocyclophosphamide: synthesis, metabolism, and antitumor activity of the cis and trans isomers
Allan B. Foster, Michael Jarman, Ryszard W. Kinas, Johannes M. S. Van Maanen, Grahame N. Taylor, John L. Gaston, Ann Parkin, and Anthony C. Richardson
pp 1399 - 1403; DOI:
10.1021/jm00144a006
PDF
Synthesis of 3-hydroxycyclophosphamide and studies related to its possible role in the metabolism of cyclophosphamide
Joan A. Brandt, Susan Marie Ludeman, Gerald Zon, William Egan, John A. Todhunter, and Ruth Dickerson
pp 1404 - 1408; DOI:
10.1021/jm00144a007
PDF
Biological activities of photoaffinity labeling analogs of kinins and their irreversible effects on kinin receptors
Emanuel Escher, Endre Laczko, Gaetan Guillemette, and Domenico Regoli
pp 1409 - 1413; DOI:
10.1021/jm00144a008
PDF
Photoelectron spectra of psychotropic drugs. 6. Relationships between physical properties and pharmacological actions of amphetamine analogs
L. N. Domelsmith, Thomas A. Eaton, K. N. Houk, G. M. Anderson, R. A. Glennon, A. T. Shulgin, N. Castagnoli, and P. A. Kollman
pp 1414 - 1421; DOI:
10.1021/jm00144a009
PDF
Comparison of the inhibition of methotrexate-sensitive and -resistant Lactobacillus casei cell cultures with purified Lactobacillus casei dihydrofolate reductase by 4,6-diamino-1,2-dihydro-2,2-dimethyl-1-(3-substituted-phenyl)-s-triazines. Use of quantitative structure-activity relationships in making inferences about the mechanism of resistance and the structure of the enzyme in situ compared with the enzyme in vitro
Eugene A. Coats, Clara S. Genther, Stephen W. Dietrich, Zong Ru Guo, and Corwin Hansch
pp 1422 - 1429; DOI:
10.1021/jm00144a010
PDF
Structure-activity relationships of the cycloalkyl ring of phencyclidine
Roy L. McQuinn, Edward J. Cone, Harlan E. Shannon, and Tsung-Ping Su
pp 1429 - 1432; DOI:
10.1021/jm00144a011
PDF
.alpha.-Adrenergic agents. 1. Direct-acting .alpha.1 agonists related to methoxamine
R. M. DeMarinis, W. M. Bryan, D. H. Shah, J. P. Hieble, and R. G. Pendleton
pp 1432 - 1437; DOI:
10.1021/jm00144a012
PDF
(-)-4-Hydroxymorphinanones: their synthesis and analgesic activity
Awinash Manmade, Haldean C. Dalzell, John F. Howes, and Raj K. Razdan
pp 1437 - 1440; DOI:
10.1021/jm00144a013
PDF
Aporphines. 36. Dopamine receptor interactions of trihydroxyaporphines. Synthesis, radioreceptor binding, and striatal adenylate cyclase stimulation of 2,10,11-trihydroxyaporphines in comparison with other hydroxylated aporphines
John L. Neumeyer, George W. Arana, Say Jong Law, Jeffrey S. Lamont, Nora S. Kula, and Ross J. Baldessarini
pp 1440 - 1445; DOI:
10.1021/jm00144a014
PDF
Analgesic narcotic antagonists. 8. 7.alpha.-Alkyl-4,5.alpha.-epoxymorphinan-6-ones
Michael P. Kotick, David L. Leland, Joseph O. Polazzi, John F. Howes, and Ann R. Bousquet
pp 1445 - 1450; DOI:
10.1021/jm00144a015
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Methotrexate analogs. 14. Synthesis of new .gamma.-substituted derivatives as dihydrofolate reductase inhibitors and potential anticancer agents
Andre Rosowsky, Ronald Forsch, Jack Uren, and Michael Wick
pp 1450 - 1455; DOI:
10.1021/jm00144a016
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Antihypertensive pyrrolo[1,2-c]quinazolines and pyrrolo[1,2-c]quinazolinones
Victor T. Bandurco, Elizabeth Malloy Wong, Seymour D. Levine, and Zoltan G. Hajos
pp 1455 - 1460; DOI:
10.1021/jm00144a017
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2-(Isoxazolylethenyl)phenoxypropanolamines: a new class of .beta.-receptor antagonists with antihypertensive activity
Albrecht Franke, Fritz F. Frickel, Josef Gries, Dieter Lenke, Rainer Schlecker, and Peter D. Thieme
pp 1460 - 1464; DOI:
10.1021/jm00144a018
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2,3-Dihydrobenzofuran-2-ones: a new class of highly potent antiinflammatory agents
Annemarie Closse, Walter Haefliger, Daniel Hauser, Hans Ulrich Gubler, Beatrice Dewald, and Marco Baggiolini
pp 1465 - 1471; DOI:
10.1021/jm00144a019
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Synthesis of some novel amodiaquine analogs as potential antimalarial and antifilarial compounds
Meilin Go, Tonglan Ngiam, and Alfred S. C. Wan
pp 1471 - 1475; DOI:
10.1021/jm00144a020
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3-Phenylpiperidines. Central dopamine-autoreceptor stimulating activity
Uli Hacksell, Lars Erik Arvidsson, Uno Svensson, J. Lars G. Nilsson, Domingo Sanchez, Hakan Wikstroem, Per Lindberg, Stephan Hjorth, and Arvid Carlsson
pp 1475 - 1482; DOI:
10.1021/jm00144a021
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Isomeric phenylthioimidazo[1,2-a]pyridines as anthelmintics
Richard J. Bochis, Leonard E. Olen, M. H. Fisher, Robert A. Reamer, George Wilks, Joyce E. Taylor, and George Olson
pp 1483 - 1487; DOI:
10.1021/jm00144a022
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Chemical modification of aminoglycosides. 3. Synthesis of 2"-deoxykanamycins from neamine
R. J. Reid, S. A. Mizsak, L. M. Reineke, G. E. Zurenko, K. F. Stern, and B. J. Magerlein
pp 1487 - 1492; DOI:
10.1021/jm00144a023
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Synthesis and in vitro antimicrobial property of o-carborane derivatives
Tetsushi Totani, Katsutoshi Aono, Kiyoe Yamamoto, and Katsuya Tawara
pp 1492 - 1499; DOI:
10.1021/jm00144a024
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Synthesis of pyridylallylamines related to zimelidine and their inhibition of neuronal monoamine uptake
Thomas Hoegberg, Bengt Ulff, Anna L. Renyi, and Svante B. Ross
pp 1499 - 1507; DOI:
10.1021/jm00144a025
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Synthesis and platelet aggregation inhibitory activity of 4,5-bis(aryl)-2-substituted-thiazoles
Ronald H. Rynbrandt, Edward E. Nishizawa, Doris P. Balgoyen, A. Rene Mendoza, and Kathleen A. Annis
pp 1507 - 1510; DOI:
10.1021/jm00144a026
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5'-Chloropuromycin. Inhibition of protein synthesis and antitrypanosomal activity
Robert Vince, Heejoo Lee, A. S. Narang, and Frances N. Shirota
pp 1511 - 1514; DOI:
10.1021/jm00144a027
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Synthesis of S-(3-deazaadenosyl)-L-homocysteine
J. A. Montgomery, H. J. Thomas, M. C. Thorpe, and P. K. Chiang
pp 1514 - 1516; DOI:
10.1021/jm00144a028
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Analgesic narcotic antagonists. 9. 6-Methylene-8.beta.-alkyl-N-(cycloalkylmethyl)-3-hydroxy- or -methoxymorphinans
Joseph O. Polazzi, Michael P. Kotick, John F. Howes, and Ann R. Bousquet
pp 1516 - 1518; DOI:
10.1021/jm00144a029
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Substituted imidazo[1,2-a]pyridine-2-carbamate anthelmintics
Richard J. Bochis, Leonard E. Olen, Frank S. Waksmunski, Helmut Mrozik, Philip Eskola, Peter Kulsa, George Wilks, Joyce E. Taylor, John R. Egerton, and et al.
pp 1518 - 1521; DOI:
10.1021/jm00144a030
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Chemistry and hypoglycemic activity of benzimidoylpyrazoles
James R. Shroff, Victor Bandurco, Rohit Desai, Sidney Kobrin, and Peter Cervoni
pp 1521 - 1525; DOI:
10.1021/jm00144a031
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Efficient synthesis of 14-hydroxymorphinans from codeine
Martin A. Schwartz and Rebecca A. Wallace
pp 1525 - 1528; DOI:
10.1021/jm00144a032
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Purine acyclic nucleosides. Nitrogen isosteres of 9-[(2-hydroxyethoxy)methyl] guanine as candidate antivirals
James L. Kelley, Mark P. Krochmal, and Howard J. Schaeffer
pp 1528 - 1531; DOI:
10.1021/jm00144a033
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Synthesis and .beta.-lactamase inhibitory properties of 2.beta.-(chloromethyl)-2.alpha.-methylpenam-3.alpha.-carboxylic acid 1,1-dioxide
William J. Gottstein, Leonard B. Crast, Robert G. Graham, Ute J. Haynes, and Donald N. McGregor
pp 1531 - 1534; DOI:
10.1021/jm00144a034
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Interaction of aromatic dyes with the coenzyme A binding site of choline acetyltransferase
Henry G. Mautner, Robert E. Merrill, Stephen F. Currier, and Gregory Harvey
pp 1534 - 1537; DOI:
10.1021/jm00144a035
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Interaction of 5-ethynyl-2'-deoxyuridylate with thymidylate synthetase
Peter V. Danenberg, Ram S. Bhatt, Nitya G. Kundu, Kathleen Danenberg, and Charles Heidelberger
pp 1537 - 1540; DOI:
10.1021/jm00144a036
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Book Reviews

pp 1541 - 1546; DOI:
10.1021/jm00144a600
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Additions and Corrections - Estrogen Receptor Based Imaging Agents. 1. Synthesis and Receptor Binding Affinity of Some Aromatic and D-Ring Halogenated Estrogens.
Daniel F. Heiman, Stephen G. Senderoff, John A. Katzenellenbogen, and Richard J. Neeley
pp 1540 - 1540; DOI:
10.1021/jm00144a601
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Additions and Corrections - Some Short-Chain N6-Substituted Adenosine Analogues with Antitumor Properties.
M. H .Fleysher, R. J. Bernacki, and G. A. Bullard
pp 1540 - 1540; DOI:
10.1021/jm00144a602
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Additions and Corrections - In Vitro Activity of 2-Alkyl-3-hydroxy-1,4-naphthoquinones against Theileria parva
Peter Boehm, Kelvin Cooper, Alan T. Hudson, Jane P. Elphick, and Nicholas McHardy
pp 1540 - 1540; DOI:
10.1021/jm00144a603
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