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Volume 23
Main Index

Issue 1


Congeners of the .beta. conformer of dopamine derived from cis- and trans-octahydrobenzo[f]quinoline and trans-octahydrobenzo[g]quinoline
Joseph G. Cannon, Teresa Lee, H. Duane Goldman, John Paul Long, Jan R. Flynn, Turkiz Verimer, Brenda Costall, and Robert J. Naylor
pp 1 - 5; DOI:
10.1021/jm00175a001
PDF
Use of acetylacetone to prepare a prodrug of cycloserine
N. P. Jensen, J. J. Friedman, H. Kropp, and F. M. Kahan
pp 6 - 8; DOI:
10.1021/jm00175a002
PDF
Glycerides as prodrugs. 3. Synthesis and antiinflammatory activity of [1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetyl]glycerides (indomethacin glycerides)
Gerard Y. Paris, David L. Garmaise, Denis G. Cimon, Leo Swett, George W. Carter, and Patrick Young
pp 9 - 13; DOI:
10.1021/jm00175a003
PDF
Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines
Schneur Rachlin, E. Bramm, I. Ahnfelt-Roenne, and E. Arrigoni-Martelli
pp 13 - 20; DOI:
10.1021/jm00175a004
PDF
Adaptive least-squares method applied to structure-activity correlation of hypotensive N-alkyl-N''-cyano-N'-pyridylguanidines
Ikuo Moriguchi, Katsuichiro Komatsu, and Yasuo Matsushita
pp 20 - 26; DOI:
10.1021/jm00175a005
PDF
Synthesis of analogs of the carboxyl protease inhibitor pepstatin. Effect of structure on inhibition of pepsin and renin
Daniel H. Rich, Eric T. O. Sun, and Edgar Ulm
pp 27 - 33; DOI:
10.1021/jm00175a006
PDF
Inhibitors of Bacillus subtilis DNA polymerase III. 6-Anilinouracils and 6-(alkylamino)uracils
George E. Wright and Neal C. Brown
pp 34 - 38; DOI:
10.1021/jm00175a007
PDF
Binding specificities of adenosine aminohydrolase from calf intestinal mucosa with dialdehydes derived from hexofuranosyladenine nucleosides
Alan J. Grant and Leon M. Lerner
pp 39 - 42; DOI:
10.1021/jm00175a008
PDF
Aminoglycoside antibiotics. 3. Epimino derivatives of neamine, ribostamycin, and kanamycin B
Virendra Kumar, Gerald S. Jones, Ilene Blacksberg, William A. Remers, Martin Misiek, and Theresa A. Pursiano
pp 42 - 49; DOI:
10.1021/jm00175a009
PDF
Studies of hypolipidemic agents. 1. Synthesis and hypolipidemic activities of alkoxycinnamic acid derivatives
Toshio Watanabe, Kimiaki Hayashi, Shigeki Yoshimatsu, Kazuo Sakai, Shigeyuki Takeyama, and Kohki Takashima
pp 50 - 59; DOI:
10.1021/jm00175a010
PDF
Folate analogs altered in the C9-N10 bridge region. 14. 11-Oxahomofolic acid, a potential antitumor agent
M. G. Nair, Colleen Saunders, Shiang-Yuan Chen, Roy L. Kisliuk, and Y. Gaumont
pp 59 - 65; DOI:
10.1021/jm00175a011
PDF
Heterocyclic analogs of the antihypertensive .beta.-adrenergic blocking agent (S)-2-[3-(tert-butylamino)-2-hydroxypropoxy]-3-cyanopyridine
John J. Baldwin, Edward L. Engelhardt, Ralph Hirschmann, Gerald S. Ponticello, Joseph G. Atkinson, Burton K. Wasson, Charles S. Sweet, and Alexander Scriabine
pp 65 - 70; DOI:
10.1021/jm00175a012
PDF
Synthesis and pharmacology of 8-amino-3-(cyclopropylmethyl)-1,2,3,4,5,6-hexahydro-cis-6,11-dimethyl-2,6-methano-3-benzazocine and related compounds
Mark P. Wentland, Noel F. Albertson, and Anne K. Pierson
pp 71 - 74; DOI:
10.1021/jm00175a013
PDF
Synthesis of [82Br]bromperidol and preliminary tissue distribution studies in the rat
Styliani H. Vincent, Manvendra B. Shambhu, and George A. Digenis
pp 75 - 79; DOI:
10.1021/jm00175a014
PDF
Glycerides as prodrugs. 2. 1,3-Dialkanoyl-2-(2-methyl-4-oxo-1,3-benzodioxan-2-yl)glycerides (cyclic aspirin triglycerides) as antiinflammatory agents
Gerard Y. Paris, David L. Garmaise, Denis G. Cimon, Leo Swett, George W. Carter, and Patrick Young
pp 79 - 82; DOI:
10.1021/jm00175a015
PDF
Cholecystokinin (pancreozymin). 5. Hormonally active desamino derivative of Tyr(SO3H)-Met-Gly-Trp-Met-Asp-Phe-NH2
Miklos Bodanszky, Jean Martinez, Michael Walker, Jerry D. Gardner, and Viktor Mutt
pp 82 - 85; DOI:
10.1021/jm00175a016
PDF
Potential carcinostatics. 4. Synthesis and biological properties of erythro- and threo-.beta.-fluoroaspartic acid and erythro-.beta.-fluoroasparagine
Martinus J. Wanner, Johanna J. M. Hageman, Gerrit Jan Koomen, and Upendra K. Pandit
pp 85 - 87; DOI:
10.1021/jm00175a017
PDF
Vinylogous carbinolamine tumor inhibitors. 6. Synthesis and antileukemic activity of 1-methyl-2,5-diphenyl-3,4-bis(hydroxymethyl)-, 1,2,3-triphenyl-4,5-bis(hydroxymethyl)-, and 1-methyl-2,3-diphenyl-4,5-bis(hydroxymethyl)pyrrole bis(N-methylcarbamate)
Wayne K. Anderson, Michael J. Halat, and Arvela C. Rick
pp 87 - 89; DOI:
10.1021/jm00175a018
PDF
Steroidal .alpha.-methylene .delta.-lactones as potential antitumor agents
Shangara S. Dehal, Brian A. Marples, Reginald J. Stretton, and John R. Traynor
pp 90 - 92; DOI:
10.1021/jm00175a019
PDF
Pyrido[2,1-b]quinazolinecarboxylic acids as orally active antiallergy agents
Jefferson W. Tilley, Ronald A. LeMahieu, Mathew Carson, Richard W. Kierstead, Herman W. Baruth, and Bohdan Yaremko
pp 92 - 95; DOI:
10.1021/jm00175a020
PDF
Synthesis of 8-methoxy-15,16-dinor-6,8,10-trichothecatriene 12,13.alpha.-epoxide and 12,13.beta.-epoxide as potential antineoplastic agents
Wayne K. Anderson and George E. Lee
pp 96 - 97; DOI:
10.1021/jm00175a021
PDF
Synthesis and biological activity of 5-(4-chlorobenzoyl)-4-(hydroxymethyl)-1-methyl-1H-pyrrole-2-acetic acid, a major metabolite of zomepirac sodium
Neal G. Anderson and John R. Carson
pp 98 - 100; DOI:
10.1021/jm00175a022
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Book Reviews

pp 100 - 102; DOI:
10.1021/jm00175a600
PDF

Issue 2


Perspectives on the design and biochemical pharmacology of inhibitors of thymidylate synthetase
Daniel V. Santi
pp 103 - 111; DOI:
10.1021/jm00176a001
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.beta.-Adrenergic blocking agents. 19. 1-Phenyl-2-[[(substituted-amido)alkyl]amino]ethanols
M. S. Large and L. H. Smith
pp 112 - 117; DOI:
10.1021/jm00176a002
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Cerebrovasodilatation through selective inhibition of the enzyme carbonic anhydrase. 2. Imidazo[2,1-b]thiadiazole and imidazo[2,1-b]thiazolesulfonamides
Ian T. Barnish, Peter E. Cross, Roger P. Dickinson, Brian Gadsby, Michael J. Parry, Michael J. Randall, and Ian W. Sinclair
pp 117 - 121; DOI:
10.1021/jm00176a003
PDF
Inhibitors of polyamine biosynthesis. 8. Irreversible inhibition of mammalian S-adenosyl-L-methionine decarboxylase by substrate analogs
Marvin Pankaskie and Mahmoud M. Abdel-Monem
pp 121 - 127; DOI:
10.1021/jm00176a004
PDF
Synthesis and biological activities of 5-(hydroxymethyl, azidomethyl, or aminomethyl)-2'-deoxyuridine and related 5'-substituted analogs
George T. Shiau, Raymond F. Schinazi, Ming S. Chen, and William H. Prusoff
pp 127 - 133; DOI:
10.1021/jm00176a005
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Trapping of metabolically generated electrophilic species with cyanide ion: metabolism of 1-benzylpyrrolidine
Bert Ho and Neal Castagnoli
pp 133 - 139; DOI:
10.1021/jm00176a006
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Structural requirements for the sequestration of metabolically generated acetaldehyde
Herbert T. Nagasawa, James A. Elberling, and Eugene G. DeMaster
pp 140 - 143; DOI:
10.1021/jm00176a007
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Halogenated L-fucose and D-galactose analogs: synthesis and metabolic effects
Janice R. Sufrin, Ralph J. Bernacki, Michael J. Morin, and Walter Korytnyk
pp 143 - 149; DOI:
10.1021/jm00176a008
PDF
Synthesis and psychoanaleptic properties of new compounds structurally related to diphenhydramine
Andre Buzas, Andre Champagnac, Andre Dehnel, Gilbert Lavielle, and Michele Pommier
pp 149 - 153; DOI:
10.1021/jm00176a009
PDF
Phenylalkylamines with potential psychotherapeutic utility. 2. Nuclear substituted 2-amino-1-phenylbutanes
Robert T. Standridge, Henry G. Howell, Hugh A. Tilson, John H. Chamberlain, Henry M. Holava, Jonas A. Gylys, Richard A. Partyka, and Alexander T. Shulgin
pp 154 - 162; DOI:
10.1021/jm00176a010
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Synthesis and analgesic activity of some 14.beta.-substituted analogs of morphine
Peter Osei-Gyimah and Sydney Archer
pp 162 - 166; DOI:
10.1021/jm00176a011
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Analgesic narcotic antagonists. 1. 8.beta.-Alkyl-, 8.beta.-acyl-, and 8.beta.-(tertiary alcohol)dihydrocodeinones and -dihydromorphinones
Michael P. Kotick, David L. Leland, Joseph O. Polazzi, and Robert N. Schut
pp 166 - 174; DOI:
10.1021/jm00176a012
PDF
Analgesic narcotic antagonists. 2. 8-Alkylmorphinan-6-ones
Joseph O. Polazzi, Robert N. Schut, Michael P. Kotick, John F. Howes, Patricia F. Osgood, Raj K. Razdan, and Julian E. Villarreal
pp 174 - 179; DOI:
10.1021/jm00176a013
PDF
Mono- and diaryl-2-quinuclidinylcarbinols with local anesthetic and antiarrhythmic activity
P. H. Nelson, A. M. Strosberg, and K. G. Untch
pp 180 - 184; DOI:
10.1021/jm00176a014
PDF
Quantitative structure-activity relationships for N-[(N',N'-disubstituted-amino)acetyl]arylamines for local anesthetic activity and acute toxicity
Francoise Heymans, Laurence Le Therizien, Jean Jacques Godfroid, and Pierre Bessin
pp 184 - 193; DOI:
10.1021/jm00176a015
PDF
Rm values and structure-activity relationship of benzodiazepines
G. L. Biagi, A. M. Barbaro, M. C. Guerra, M. Babbini, M. Gaiardi, M. Bartoletti, and P. A. Borea
pp 193 - 201; DOI:
10.1021/jm00176a016
PDF
Antiamebic amidines and sulfonamides of 5- and 6-amino-2,3-bis(4-alkyl-1-piperazazinyl)quinoxalines
Paul F. Fabio, S. A. Lang, Yang-I Lin, and Andrew S. Tomcufcik
pp 201 - 206; DOI:
10.1021/jm00176a017
PDF
Synthesis and antiarrhythmic properties of some 5-benzamido-2-methyl-trans-decahydroisoquinolines
Ian W. Mathison and Robert J. Pennington
pp 206 - 209; DOI:
10.1021/jm00176a018
PDF
Synthesis and biological activity of flavipucine analogs
N. N. Girotra, A. A. Patchett, S. B. Zimmerman, D. L. Achimov, and N. L. Wendler
pp 209 - 213; DOI:
10.1021/jm00176a019
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Oxytocin and lysine-vasopressin with N5,N5-dialkylglutamine in the 4 position: effect of introducing sterically hindered groups into the hydrophilic cluster of neurohypophyseal hormones
Glenn L. Stahl, Clark W. Smith, Roderich Walter, Theodor Tsegenidis, George Stavropoulos, Paul Cordopatis, and Dimitrios Theodoropoulos
pp 213 - 217; DOI:
10.1021/jm00176a020
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[5-(N4,N4-Dimethylasparagine),8-lysine]vasopressin: the first 5-position neurohypophyseal hormone analog to retain significant antidiuretic potency
Clark W. Smith, Roderich Walter, George Stavropoulos, and Dimitrios Theodoropoulos
pp 217 - 219; DOI:
10.1021/jm00176a021
PDF
Cannabidiol and phenytoin: a structural comparison
Ilana Tamir, Raphael Mechoulam, and Amatzya Y. Meyer
pp 220 - 223; DOI:
10.1021/jm00176a022
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Book Reviews

pp 223 - 224; DOI:
10.1021/jm00176a600
PDF

Issue 3


Reminiscences and musings of a classical medicinal chemist
Everette L. May
pp 225 - 232; DOI:
10.1021/jm00177a001
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A novel opioid receptor site directed alkylating agent with irreversible narcotic antagonistic and reversible agonistic activities
Philip S. Portoghese, Dennis L. Larson, Lawrence M. Sayre, David S. Fries, and A. E. Takemori
pp 233 - 234; DOI:
10.1021/jm00177a002
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10,10-Difluoro-13-dehydroprostacyclin: a chemically and metabolically stabilized potent prostacyclin
Josef Fried, D. K. Mitra, M. Nagarajan, and M. M. Mehrotra
pp 234 - 237; DOI:
10.1021/jm00177a003
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5-Substituted 2-amino-6-phenyl-4(3H)-pyrimidinones. Antiviral- and interferon-inducing agents
Wendell Wierenga, Harvey I. Skulnick, Dale A. Stringfellow, Sheldon D. Weed, Harold E. Renis, and Emerson E. Eidson
pp 237 - 239; DOI:
10.1021/jm00177a004
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Biomimetic synthesis of catechol estrogens: potentially mutagenic arene oxide intermediates in estrogen metabolism
Philip W. Le Quesne, Adhyam V. Durga, Vinayakam Subramanyam, Albert H. Soloway, Ronald W. Hart, and Robert H. Purdy
pp 239 - 240; DOI:
10.1021/jm00177a005
PDF
Synthetic modulators of the complement system. 1. Synthesis and biological activity of 5,5',5"-[1,3,6-naphthalenetriyltris(sulfonylimino)]tris[1,3-benzenedisulfonate] hexasodium salt
R. B. Conrow, N. Bauman, J. A. Brockman, and S. Bernstein
pp 240 - 242; DOI:
10.1021/jm00177a006
PDF
Synthesis and enzymic and ionotropic activity of some new 8-substituted and 6,8-disubstituted derivatives of adenosine cyclic 3',5'-monophosphate
Jon P. Miller, Kay H. Boswell, Rich B. Meyer, Leon F. Christensen, and Roland K. Robins
pp 242 - 251; DOI:
10.1021/jm00177a007
PDF
Synthesis of 5-[(methylthio)methyl]-2'-deoxyuridine, the corresponding sulfoxide and sulfone, and their 5'-phosphates: antiviral effects and thymidylate synthetase inhibition
Charles L. Schmidt, Charles T. C. Chang, Erik De Clercq, Johan Descamps, and Mathias P. Mertes
pp 252 - 256; DOI:
10.1021/jm00177a008
PDF
Quantitative structure-activity correlations of rifamycins as inhibitors of viral RNA-directed DNA polymerase and mammalian .alpha. and .beta. DNA polymerases
Roy S. Wu, Mary K. Wolpert DeFilippes, and Frank R. Quinn
pp 256 - 261; DOI:
10.1021/jm00177a009
PDF
Structure-activity relationships in a series of novel 3,4-dihydro-4-oxopyrimido[4,5-b]quinoline-2-carboxylic acid antiallergy agents
T. H. Althuis, S. B. Kadin, L. J. Czuba, P. F. Moore, and H. J. Hess
pp 262 - 269; DOI:
10.1021/jm00177a010
PDF
Potential antitumor agents. 33. Quantitative structure-activity relationships for mutagenic activity and antitumor activity of substituted 4'-(9-acridinylamino)methanesulfonanilide derivatives
Lynnette R. Ferguson and William A. Denny
pp 269 - 274; DOI:
10.1021/jm00177a011
PDF
Antitumor agents: diazomethyl ketone and chloromethyl ketone analogs prepared from N-tosyl amino acids
Z. Sajadi, M. Kashani, L. J. Loeffler, and I. H. Hall
pp 275 - 278; DOI:
10.1021/jm00177a012
PDF
Synthesis and mutagenicity of A-ring reduced analogs of 7,12-dimethylbenz[a]anthracene
Muthiah N. Inbasekaran, Donald T. Witiak, Karen Barone, and John C. Loper
pp 278 - 281; DOI:
10.1021/jm00177a013
PDF
Synthesis and study of conformationally defined enantiomers of local anesthetics and conformationally defined enantiomers of fluorescent dyes designed to label electrically excitable membranes
Henry G. Mautner, Carol Lorenc, Paul Quain, Judith K. Marquis, and Ichiji Tasaki
pp 282 - 285; DOI:
10.1021/jm00177a014
PDF
Antihypertensive indole derivatives of phenoxypropanolamines with .beta.-adrenergic receptor antagonist and vasodilating activity
William E. Kreighbaum, W. Lesley Matier, Ronald D. Dennis, Joseph L. Minielli, David Deitchman, James L. Perhach, and William T. Comer
pp 285 - 289; DOI:
10.1021/jm00177a015
PDF
Synthesis, in vitro opiate activity, and intramolecular tyrosine-tryptophan distances of (4-tryptophan)enkephalin analogs. A reassessment of conformational models of enkephalin in solution
Peter W. Schiller and Johanne St.-Hilaire
pp 290 - 294; DOI:
10.1021/jm00177a016
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Serotonin receptor affinities of psychoactive phenalkylamine analogs
Richard A. Glennon, Stephen M. Liebowitz, and George M. Anderson
pp 294 - 299; DOI:
10.1021/jm00177a017
PDF
Cyclophosphamide potentiation and aldehyde oxidase inhibition by phosphorylated aldehydes and acetals
Lindley A. Cates, Gerald S. Jones, Daniel J. Good, Helen Y. L. Tsai, Ven-Shun Li, Norman Caron, Shiao-Chun Tu, and Aubrey P. Kimball
pp 300 - 304; DOI:
10.1021/jm00177a018
PDF
Mechanism of decomposition of N-hydroxyacetaminophen, a postulated toxic metabolite of acetaminophen
Mark W. Gemborys, Gilbert H. Mudge, and Gordon W. Gribble
pp 304 - 308; DOI:
10.1021/jm00177a019
PDF
Structure-taste relationship of perillartine and nitro- and cyanoaniline derivatives
Hajime Iwamura
pp 308 - 312; DOI:
10.1021/jm00177a020
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Modification of the 5' position of purine nucleosides. 2. Synthesis and some cardiovascular properties of adenosine-5'-(N-substituted)carboxamides
Raj Nandan Prasad, Dilbagh S. Bariana, Anthony Fung, Milica Savic, Karin Tietje, Herman H. Stein, Harold Brondyk, and Richard S. Egan
pp 313 - 319; DOI:
10.1021/jm00177a021
PDF
Convenient synthesis of 10-deazaaminopterin via a pteridine ylide
James R. Piper and John A. Montgomery
pp 320 - 321; DOI:
10.1021/jm00177a022
PDF
Synthesis of isomeric thienobenzothiazines and their effect on dopamine metabolism in rat brain
Cor J. Grol, Hans Rollema, Durk Dijkstra, and Ben H. C. Westerink
pp 322 - 324; DOI:
10.1021/jm00177a023
PDF
Synthesis and anticancer activity of nitrosourea derivatives of phensuximide
A. Michael Crider, Thomas M. Kolczynski, and Kathleen M. Yates
pp 324 - 326; DOI:
10.1021/jm00177a024
PDF
Synthesis and antitumor activity of 2,4-diamino-6-(2,5-dimethoxybenzyl)-5-methylpyrido[2,3-d]pyrimidine
Eugene M. Grivsky, Shuliang Lee, Carl W. Sigel, David S. Duch, and Charles A. Nichol
pp 327 - 329; DOI:
10.1021/jm00177a025
PDF
Synthesis and biological activity of some 15-oxaestranes
Perry Rosen, Alfred Boris, and Gloria Oliva
pp 329 - 330; DOI:
10.1021/jm00177a026
PDF
Synthesis, .beta.-adrenergic activity, and platelet antiaggregatory activity of a positional isomer of trimetoquinol: 1-(2',4',5'-trimethoxybenzyl)-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline
Duane D. Miller, Josef F. Bossart, Joseph R. Mayo, and Dennis R. Feller
pp 331 - 333; DOI:
10.1021/jm00177a027
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Central nervous system activity of 7-substituted 1-azaphenoxathiin analogs and their oxidation products
Arthur J. Elliott, Norman Eisenstein, and Louis C. Iorio
pp 333 - 335; DOI:
10.1021/jm00177a028
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Inhibition of histamine-induced gastric secretion by flavone-6-carboxylic acids
Juerg R. Pfister, Walter E. Wymann, Margery E. Schuler, and Adolph P. Roszkowski
pp 335 - 338; DOI:
10.1021/jm00177a029
PDF
Conformational energy differences between side chain alkylated analogs of the hallucinogen 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane
Herschel J. R. Weintraub, David E. Nichols, Alexandros Makriyannis, and Stephen W. Fesik
pp 339 - 341; DOI:
10.1021/jm00177a030
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Book Reviews

pp 342 - 346; DOI:
10.1021/jm00177a600
PDF

Issue 4


S-Adenosyl-L-methionine-dependent macromolecule methyltransferases: potential targets for the design of chemotherapeutic agents
Ronald T. Borchardt
pp 347 - 357; DOI:
10.1021/jm00178a001
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Synthesis of potential inhibitors of hypoxanthine-guanine phosphoribosyltransferase for testing as antiprotozoal agents. 1. 7-Substituted 6-oxopurines
James R. Piper, Anne G. Laseter, and John A. Montgomery
pp 357 - 364; DOI:
10.1021/jm00178a002
PDF
[1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid),2-(O-methyl)tyrosine]arginine-vasopressin and [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)]arginine-vasopressin, two highly potent antagonists of the vasopressor response to arginine-vasopressin
Marian Kruszynski, Bernard Lammek, Maurice Manning, Janny Seto, Jaya Haldar, and Wilbur H. Sawyer
pp 364 - 368; DOI:
10.1021/jm00178a003
PDF
Synthesis of syn and anti isomers of 6-[[(hydroxyimino)phenyl]methyl]-1-[(1-methylethyl)sulfonyl]-1H-benzimidazol-2-amine. Inhibitors of rhinovirus multiplication
J. H. Wikel, C. J. Paget, D. C. DeLong, J. D. Nelson, C. Y. E. Wu, J. W. Paschal, A. Dinner, R. J. Templeton, M. O. Chaney, and et al.
pp 368 - 372; DOI:
10.1021/jm00178a004
PDF
Synthesis and antitumor activity of cyclophosphamide analogs. 3. Preparation, molecular structure determination, and anticancer screening of racemic cis- and trans-4-phenylcyclophosphamide
Victoria L. Boyd, Gerald Zon, Vicky L. Himes, Judith K. Stalick, Alan D. Mighell, and Henry V. Secor
pp 372 - 375; DOI:
10.1021/jm00178a005
PDF
Preparation and antitumor activity of olivomycin A analogs
Virendra Kumar, William A. Remers, and William T. Bradner
pp 376 - 379; DOI:
10.1021/jm00178a006
PDF
2,4-Diamino-5-benzylpyrimidines and analogs as antibacterial agents. 2. C-Alkylation of pyrimidines with Mannich bases and application to the synthesis of trimethoprim and analogs
Barbara Roth, Justina Z. Strelitz, and Barbara S. Rauckman
pp 379 - 384; DOI:
10.1021/jm00178a007
PDF
2,4-Diamino-5-benzylpyrimidines and analogs as antibacterial agents. 3. C-Benzylation of aminopyridines with phenolic Mannich bases. Synthesis of 1- and 3-deaza analogs of trimethoprim
Barbara S. Rauckman and Barbara Roth
pp 384 - 391; DOI:
10.1021/jm00178a008
PDF
1-(Aminoalkyl)-6-aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines with antianxiety and antidepressant activity
Jackson B. Hester, Allan D. Rudzik, and Philip F. Von Voigtlander
pp 392 - 402; DOI:
10.1021/jm00178a009
PDF
2,4-Dihydro-6-phenyl-1H-s-triazolo[4,3-a][1,4]benzodiazepin-1-ones with antianxiety and antidepressant activity
Jackson B. Hester, Allan D. Rudzik, and Philip Von Voigtlander
pp 402 - 405; DOI:
10.1021/jm00178a010
PDF
Orally active cephalosporins and penicillins
E. H. W. Boehme, R. E. Bambury, R. J. Baumann, R. C. Erickson, B. L. Harrison, P. F. Hoffman, F. J. McCarty, R. A. Schnettler, M. J. Vaal, and D. L. Wenstrup
pp 405 - 412; DOI:
10.1021/jm00178a011
PDF
Peptide sweeteners. 3. Effect of modifying the peptide bond on the sweet taste of L-aspartyl-L-phenylalanine methyl ester and its analogs
Scott A. MacDonald, C. Grant Willson, Michael Chorev, Fred S. Vernacchia, and Murray Goodman
pp 413 - 420; DOI:
10.1021/jm00178a012
PDF
Peptide sweeteners. 4. Hydroxy and methoxy substitution of the aromatic ring in L-aspartyl-L-phenylalanine methyl ester. Structure-taste relationships
Masao Kawai, Michael Chorev, Janine Marin-Rose, and Murray Goodman
pp 420 - 424; DOI:
10.1021/jm00178a013
PDF
4-Amino-4-arylcyclohexanones and their derivatives, a novel class of analgesics. 1. Modification of the aryl ring
Daniel Lednicer, Philip F. Von Voigtlander, and D. Edward Emmert
pp 424 - 430; DOI:
10.1021/jm00178a014
PDF
Synthesis and structure-activity studies in a series of 7.alpha.-halogeno corticosteroids
Ho-Jane Shue, Michael J. Green, Joseph Berkenkoph, Margaret Monahan, Xiomara Fernandez, and Barry N. Lutsky
pp 430 - 437; DOI:
10.1021/jm00178a015
PDF
Structure-activity study of antiulcerous and antiinflammatory drugs by discriminant analysis
Akio Ogino, Shingo Matsumura, and Toshio Fujita
pp 437 - 444; DOI:
10.1021/jm00178a016
PDF
Convulsant and anticonvulsant barbiturates. 1. Molecular conformations from classical potential-energy calculations
G. P. Jones and P. R. Andrews
pp 444 - 448; DOI:
10.1021/jm00178a017
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Decomposition of pharmacological activity indices into mutually independent components using principal component analysis
Istvan Lukovits and Antal Lopata
pp 449 - 459; DOI:
10.1021/jm00178a018
PDF
Mutagenicity of substituted (o-phenylenediamine)platinum dichloride in the Ames test. A quantitative structure-activity analysis
Corwin Hansch, Benjamin H. Venger, and Augustine Panthananickal
pp 459 - 461; DOI:
10.1021/jm00178a019
PDF
Derivatives of 11-(1-piperazinyl)-5H-pyrrolo[2,1-c][1,4]benzodiazepine as central nervous system agents
William B. Wright, Eugene N. Greenblatt, Ivana P. Day, Nicanor Q. Quinones, and Robert A. Hardy
pp 462 - 465; DOI:
10.1021/jm00178a020
PDF
Book Reviews

pp 466 - 468; DOI:
10.1021/jm00178a600
PDF

Issue 5


Soft drugs. 1. Labile quaternary ammonium salts as soft antimicrobials
Nicholas Bodor, James J. Kaminski, and Sally Selk
pp 469 - 474; DOI:
10.1021/jm00179a001
PDF
Soft drugs. 3. A new class of anticholinergic agents
Nicholas Bodor, Ross Woods, Colin Raper, Pauline Kearney, and James J. Kaminski
pp 474 - 480; DOI:
10.1021/jm00179a002
PDF
Bicyclic and tricyclic ergoline partial structures. Rigid 3-(2-aminoethyl)pyrroles and 3- and 4-(2-aminoethyl)pyrazoles as dopamine agonists
Nicholas J. Bach, Edmund C. Kornfeld, Noel D. Jones, Michael O. Chaney, Douglas E. Dorman, Jonathan W. Paschal, James A. Clemens, and E. Barry Smalstig
pp 481 - 491; DOI:
10.1021/jm00179a003
PDF
Preparation and biological evaluation of 2-azaergolines
Nicholas J. Bach, Edmund C. Kornfeld, James A. Clemens, E. Barry Smalstig, and Robert C. A. Frederickson
pp 492 - 494; DOI:
10.1021/jm00179a004
PDF
Tricyclics with analgesic and antidepressant activity. 1. [[(Alkylamino)ethyl]thio]dibenz[b,f]oxepins and 10,11-dihydro derivatives
Helen H. Ong, James A. Profitt, V. Brian Anderson, Theodore C. Spaulding, Jeffrey C. Wilker, Harry M. Geyer, and Hansjoerg Kruse
pp 494 - 501; DOI:
10.1021/jm00179a005
PDF
Congeners of the .alpha. conformer of dopamine derived from octahydrobenz[h]isoquinoline
Joseph G. Cannon, Teresa Lee, Fu-Lian Hsu, John Paul Long, and Jan R. Flynn
pp 502 - 505; DOI:
10.1021/jm00179a006
PDF
Inhibitors of phenylethanolamine N-methyltransferase and epinephrine biosynthesis. 1. Chloro-Substituted 1,2,3,4-tetrahydroisoquinolines
William E. Bondinell, Frederic W. Chapin, Gerald R. Girard, Carl Kaiser, Arnold J. Krog, Alex M. Pavloff, Mark S. Schwartz, Joanne S. Silvestri, Praful D. Vaidya, and et al.
pp 506 - 511; DOI:
10.1021/jm00179a007
PDF
New cyclopenta[a]naphthalene derivatives. Synthesis of 2-(carbamylmethyl)-8-hydroxy-3H-cyclopenta[a]naphthalene as a possible deoxyribonucleic acid binding agent
Nitya G. Kundu
pp 512 - 516; DOI:
10.1021/jm00179a008
PDF
4-[(Aminoalkyl)amino]-1,2-dimethoxynaphthalenes as antimalarial agents
Sydney Archer, Peter Osei-Gyimah, and Stephen Silbering
pp 516 - 519; DOI:
10.1021/jm00179a009
PDF
Prostaglandin analogs possessing antinidatory effects. 1. Modification of the .omega. chain
Masaki Hayashi, Hajimu Miyake, Seiji Kori, Tadao Tanouchi, Hirohisa Wakatsuka, Yoshinobu Arai, Takashi Yamato, Ikuo Kajiwara, Yoshitaka Konishi, and et al.
pp 519 - 524; DOI:
10.1021/jm00179a010
PDF
Prostaglandin analogs possessing antinidatory effects. 2. Modification of the .alpha. chain
Masaki Hayashi, Yoshinobu Arai, Hirohisa Wakatsuka, Masanori Kawamura, Yoshitaka Konishi, Takeshi Tsuda, and Kimiichiro Matsumoto
pp 525 - 535; DOI:
10.1021/jm00179a011
PDF
2,4-Diamino-5-benzylpyrimidines as antibacterial agents. 4. 6-Substituted trimethoprim derivatives from phenolic Mannich intermediates. Application to the synthesis of trimethoprim and 3,5-dialkylbenzyl analogs
Barbara Roth, Edward Aig, Kenneth Lane, and Barbara S. Rauckman
pp 535 - 541; DOI:
10.1021/jm00179a012
PDF
Synthesis, biological activity, and structure-activity/toxicity relationships of a series of terphenyl analogs of hemicholinium-3 and acetyl-seco-hemicholinium-3. 3
Floyd R. Domer, David M. Chihal, H. Cecil Charles, and Richard C. Koch
pp 541 - 545; DOI:
10.1021/jm00179a013
PDF
Structure-antitubulin activity relationships in steganacin congeners and analogs. Inhibition of tubulin polymerization in vitro by (.+-.)-isodeoxypodophyllotoxin
Flora Zavala, Daniel Guenard, Jean Pierre Robin, and Eric Brown
pp 546 - 549; DOI:
10.1021/jm00179a014
PDF
Synthesis and antitumor activity of analogs of the antitumor antibiotic chartreusin
Makoto Takai, Yoshimasa Uehara, and John A. Beisler
pp 549 - 553; DOI:
10.1021/jm00179a015
PDF
Plant antitumor agents. 18. Synthesis and biological activity of camptothecin analogs
Mansukh C. Wani, Peter E. Ronman, James T. Lindley, and Monroe E. Wall
pp 554 - 560; DOI:
10.1021/jm00179a016
PDF
Accumulation of drugs by guinea pig isolated atria. Quantitative correlations
Heinz Luellmann, Pieter B. M. W. M. Timmermans, Gerhard M. Weikert, and Albrecht Ziegler
pp 560 - 565; DOI:
10.1021/jm00179a017
PDF
Soft drugs. 2. Soft alkylating compounds as potential antitumor agents
Nicholas Bodor and James J. Kaminski
pp 566 - 569; DOI:
10.1021/jm00179a018
PDF
Synthesis of some new S-alkylated derivatives of 5-mercapto-2'-deoxyuridine as potential antiviral agents
Frank J. Dinan and Thomas J. Bardos
pp 569 - 572; DOI:
10.1021/jm00179a019
PDF
A direct method for the preparation of 2-hydroxyethoxymethyl derivatives of guanine, adenine, and cytosine
Jorge R. Barrio, Jerry D. Bryant, and Gene E. Keyser
pp 572 - 574; DOI:
10.1021/jm00179a020
PDF
Synthesis and properties of the sulfonyl analogs of 4(5)-aminoimidazole-5(4)-carboxamide, 4(5)-(formylamino)imidazole-5(4)-carboxamide, guanine, and xanthine
Bao-Shan Huang, Paul L. Chello, Lily Yip, and James C. Parham
pp 575 - 577; DOI:
10.1021/jm00179a021
PDF
Synthesis and antitrypanosomal activity of some bis(4-guanylphenyl) five- and six-membered ring heterocycles
Bijan P. Das, Rebecca A. Wallace, and David Withers Boykin
pp 578 - 581; DOI:
10.1021/jm00179a022
PDF
Synthesis of 2,4-disubstituted 6-methoxy-8-aminoquinoline analogs as potential antiparasitics
F. Ivy Carroll, Bertold D. Berrang, and C. Preston Linn
pp 581 - 584; DOI:
10.1021/jm00179a023
PDF
Role of iodine in thyroid hormones: molecular conformation of a halogen-free hormone analog
Vivian Cody
pp 584 - 587; DOI:
10.1021/jm00179a024
PDF
Book Reviews

pp 587 - 590; DOI:
10.1021/jm00179a600
PDF

Issue 6


Biological significance and therapeutic potential of prostacyclin
S. Moncada and J. R. Vane
pp 591 - 593; DOI:
10.1021/jm00180a001
PDF
Aporphines. 30. (-)-N-(2-Chloroethyl)-10,11-dihydroxynoraporphine (chloroethylnorapomorphine), novel irreversible dopamine receptor antagonist
J. L. Neumeyer, S. J. Law, R. J. Baldessarini, and N. S. Kula
pp 594 - 595; DOI:
10.1021/jm00180a002
PDF
Structure-activity analyzed by pattern recognition: the asymmetric case
W. J. Dunn and Svante Wold
pp 595 - 599; DOI:
10.1021/jm00180a003
PDF
Quantitative structure-activity relationships by distance geometry: systematic analysis of dihydrofolate reductase inhibitors
Gordon M. Crippen
pp 599 - 606; DOI:
10.1021/jm00180a004
PDF
Quantitative structure-pharmacokinetic relationships derived on antibacterial sulfonamides in rats and its comparison to quantitative structure-activity relationships
J. K. Seydel, D. Trettin, H. P. Cordes, O. Wassermann, and M. Malyusz
pp 607 - 613; DOI:
10.1021/jm00180a005
PDF
Pronounced pharmacological differences arising from minor structural changes in conformationally defined amphetamine analogs. Comparative evaluation of endo- and exo-2-amino- and endo- and exo-2-(methylamino)benzobicyclo[2.2.1]heptene and -benzobicyclo[2.2.2]octene analogs. Conformationally defined adrenergic agents. 4
Gary L. Grunewald, Thomas J. Reitz, Augusta Hallett, Charles O. Rutledge, Sheila Vollmer, James M. Archuleta, and James A. Ruth
pp 614 - 620; DOI:
10.1021/jm00180a006
PDF
Synthesis and .beta.-adrenergic blocking activity of new aliphatic oxime ethers
Gerard Leclerc, Nicole Bieth, and Jean Schwartz
pp 620 - 624; DOI:
10.1021/jm00180a007
PDF
Adrenergic receptor agonists
Kurt Loevgren, Anders Hedberg, and J. Lars G. Nilsson
pp 624 - 627; DOI:
10.1021/jm00180a008
PDF
Synthesis and antineoplastic activity of hydroquinone dialdehydes
Edward M. Newman, Ai Jeng Lin, and Alan C. Sartorelli
pp 627 - 631; DOI:
10.1021/jm00180a009
PDF
Synthesis and antineoplastic activity of phenyl-substituted phenylsulfonylhydrazones of 1-pyridinecarboxaldehyde 1-oxide
William Loh, Lucille A. Cosby, and Alan C. Sartorelli
pp 631 - 634; DOI:
10.1021/jm00180a010
PDF
Neuroleptic activity in 5-aryltetrahydro-.gamma.-carbolines
Charles A. Harbert, Jacob J. Plattner, Willard M. Welch, Albert Weissman, and B. Kenneth Koe
pp 635 - 643; DOI:
10.1021/jm00180a011
PDF
8-Chloro-1-methyl-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines with substituents at C-4
Jackson B. Hester, Allan D. Rudzik, and Philip F. VonVoigtlander
pp 643 - 647; DOI:
10.1021/jm00180a012
PDF
Mammalian alkaloids. 8. Synthesis and biological effects of tetrahydropapaveroline related 1-benzyltetrahydroisoquinolines
Arnold Brossi, Kenner C. Rice, Ching-Pong Mak, Juergen Reden, Arthur E. Jacobson, Yuthasak Nimitkitpaisan, Phil Skolnick, and John Daly
pp 648 - 652; DOI:
10.1021/jm00180a013
PDF
Acylthioxanthenes: agents which selectively reduce decerebrate rigidity in the cat
Michael J. Ashton, Robert F. Chapman, and Anthony H. Loveless
pp 653 - 657; DOI:
10.1021/jm00180a014
PDF
Alkylating nucleosides. 4. Synthesis and cytostatic activity of chloro- and iodomethylpyrazole nucleosides
M. Teresa Garcia Lopez, M. Jose Dominguez, Rosario Herranz, Rosa M. Sanchez-Perez, Antonio Contreras, and Gregorio Alonso
pp 657 - 660; DOI:
10.1021/jm00180a015
PDF
Oxime and dithiolane derivatives of 5-formyl-2'-deoxyuridine and their 5'-phosphates: antivirial effects and thymidylate synthetase inhibition
Joon Sup Park, Charles T. C. Chang, Charles L. Schmidt, Yechiel Golander, Erik De Clercq, Johan Descamps, and Mathias P. Mertes
pp 661 - 665; DOI:
10.1021/jm00180a016
PDF
N-(.alpha.-hydroxyalkanoyl) derivatives of Leu-Val-Phe-OCH3 as inhibitors of renin
Rodney L. Johnson
pp 666 - 669; DOI:
10.1021/jm00180a017
PDF
Metabolic depropargylation and its relationship to aldehyde dehydrogenase inhibition in vivo
Frances N. Shirota, Eugene G. DeMaster, James A. Elberling, and Herbert T. Nagasawa
pp 669 - 673; DOI:
10.1021/jm00180a018
PDF
Long-acting opiate agonists and antagonists: 14-hydroxydihydromorphinone hydrazones
Gavril W. Pasternak and Elliot F. Hahn
pp 674 - 676; DOI:
10.1021/jm00180a019
PDF
Benzenesulfenamides as antihypertensive agents. Substituted piperidine and 1-arylpiperazine derivatives
Sol S. Klioze, Richard C. Allen, Jeffrey C. Wilker, and David L. Woodward
pp 677 - 679; DOI:
10.1021/jm00180a020
PDF
Synthesis and analgesic properties of some conformationally restricted analogs of profadol
Peter A. Crooks and Richard Szyndler
pp 679 - 682; DOI:
10.1021/jm00180a021
PDF
Relationship of octanol/water partition coefficient and molecular weight to rat brain capillary permeability
Victor A. Levin
pp 682 - 684; DOI:
10.1021/jm00180a022
PDF
Effects of platinum complexes on chymotrypsin
P. Melius, Laura A. Andersson, and Y. Y. Lee
pp 685 - 687; DOI:
10.1021/jm00180a023
PDF
Some spiro analogs of the potent analgesic ketobemidone
M. E. Rogers, D. S. Wilkinson, J. R. Thweatt, and S. P. Halenda
pp 688 - 690; DOI:
10.1021/jm00180a024
PDF
Synthesis and diuretic profile of 3-(3-amino-1,2,4-oxadiazol-5-yl)-5-chloro-2,6-pyrazinediamine, an amiloride-type diuretic
Jeffrey W. H. Watthey, Mahesh Desai, Richard Rutledge, and Ronald Dotson
pp 690 - 692; DOI:
10.1021/jm00180a025
PDF
Effect of changing the COOH-terminal amide group present in the hydrophilic cluster of oxytocin to dimethylamide
Yuan Fen Ting, Clark W. Smith, Glenn L. Stahl, Roderich Walter, Paul Cordopatis, and Dimitrios Theodoropoulos
pp 693 - 695; DOI:
10.1021/jm00180a026
PDF
N-Acetyl-[2-(O-methyl)tyrosine]arginine-vasopressin, an interesting antagonist of the vasopressor response to vasopressin
David A. Jones and Wilbur H. Sawyer
pp 696 - 698; DOI:
10.1021/jm00180a027
PDF
14-(Arylhydroxyamino)codeinones and derivatives as analgetics and antagonists
Linda S. Schwab
pp 698 - 702; DOI:
10.1021/jm00180a028
PDF
New anticonvulsants: Schiff bases of .gamma.-aminobutyric acid and .gamma.-aminobutyramide
Jean Pierre Kaplan, Bernard M. Raizon, Michel Desarmenien, Paul Feltz, P. Max Headley, Paul Worms, Kenneth G. Lloyd, and Giuseppe Bartholini
pp 702 - 704; DOI:
10.1021/jm00180a029
PDF
Neuroleptic 4-aryltetrahydropyrrolo[3,4-b]indoles
Willard M. Welch, Charles A. Harbert, and Albert Weissman
pp 704 - 707; DOI:
10.1021/jm00180a030
PDF
Book Reviews

pp 707 - 712; DOI:
10.1021/jm00180a600
PDF

Issue 7


Synthesis of 1,3-diazepin-2-one nucleosides as transition-state inhibitors of cytidine deaminase
Victor E. Marquez, Paul S. Liu, James A. Kelley, John S. Driscoll, and John J. McCormack
pp 713 - 715; DOI:
10.1021/jm00181a001
PDF
Prostaglandins and congeners. 25. Inhibition of gastric acid secretion. Replacement of the carboxylate moiety of a prostaglandin with a hydroxymethylketo functional group
Allan Wissner, Jay E. Birnbaum, and Donald E. Wilson
pp 715 - 717; DOI:
10.1021/jm00181a002
PDF
Synthesis and blood pressure lowering activity of 3-(substituted-amino)-1,2,4-benzothiadiazine 1-oxide derivatives
Robert D. Dillard, Terence T. Yen, Paul Stark, and Donald E. Pavey
pp 717 - 722; DOI:
10.1021/jm00181a003
PDF
Synthesis and biochemical screening of phenylselenium-substituted steroid hormones
Joseph P. Konopelski, Carl Djerassi, and J. P. Raynaud
pp 722 - 726; DOI:
10.1021/jm00181a004
PDF
Synthesis and analgesic activity of some 5-(4-hydroxyphenyl)-2-azabicyclo[3.2.1]octanes
Helen H. Ong, V. Brian Anderson, Jeffrey C. Wilker, Theodore C. Spaulding, and Laurence R. Meyerson
pp 726 - 729; DOI:
10.1021/jm00181a005
PDF
Antiinflammatory effects of some copper complexes
D. H. Brown, W. E. Smith, J. W. Teape, and A. J. Lewis
pp 729 - 734; DOI:
10.1021/jm00181a006
PDF
2-Substituted azole derivatives. 1. Synthesis and antiinflammatory activity of some 2-(substituted-pyridinyl)benzimidazoles
Goro Tsukamoto, Koichiro Yoshino, Toshihiko Kohno, Hiroshi Ohtaka, Hajime Kagaya, and Keizo Ito
pp 734 - 738; DOI:
10.1021/jm00181a007
PDF
Synthesis and structure-activity relationships among .alpha.-adrenergic receptor agonists of the phenylethanolamine type
Gerard Leclerc, Jean Claude Bizec, Nicole Bieth, and Jean Schwartz
pp 738 - 744; DOI:
10.1021/jm00181a008
PDF
Comparison of biological effects of N-alkylated congeners of .beta.-phenethylamine derived from 2-aminotetralin, 2-aminoindan, and 6-aminobenzocycloheptene
Joseph G. Cannon, Julio A. Perez, Jonathan P. Pease, John Paul Long, Jan R. Flynn, David B. Rusterholz, and Stuart E. Dryer
pp 745 - 749; DOI:
10.1021/jm00181a009
PDF
Derivatives of 5-hydroxy-6-methyl-2-aminotetralin
Joseph G. Cannon, Dale L. Koble, John Paul Long, and Turkiz Verimer
pp 750 - 754; DOI:
10.1021/jm00181a010
PDF
Conformationally defined aromatic amino acids. Synthesis and stereochemistry of 2-endo- and 2-exo-amino-1,2,3,4-tetrahydro-1,4-ethanonaphthalene-2-carboxylic acids (2-endo- and 2-exo-aminobenzobicyclo[2.2.2]octene-2-carboxylic acids)
Gary L. Grunewald, Simon H. Kuttab, Michael A. Pleiss, James B. Mangold, and Phyllis Soine
pp 754 - 758; DOI:
10.1021/jm00181a011
PDF
Bradykinin analogs containing N.alpha.-methyl amino acids
Robert H. Mazur, Patricia A. James, David A. Tyner, E. Ann Hallinan, John H. Sanner, and Renata Schulze
pp 758 - 763; DOI:
10.1021/jm00181a012
PDF
Peptidoaminobenzophenones, a novel class of ring-opened derivatives of 1,4-benzodiazepines
Kentaro Hirai, Teruyuki Ishiba, Hirohiko Sugimoto, Kazuyuki Sasakura, Toshio Fujishita, Tatsuro Toyoda, Yuji Tsukinoki, Hirokuni Joyama, Hisao Hatakeyama, and Katsumi Hirose
pp 764 - 773; DOI:
10.1021/jm00181a013
PDF
Inhibitors of indoleethylamine N-methyltransferase. Derivatives of 3-methyl-2-thiazolidinimine. In vitro, in vivo, and metabolic studies
Joshua Rokach, Yves Girard, Pierre Hamel, Grant Reader, C. Stanley Rooney, Lewis R. Mandel, Edward J. Cragoe, and Anthony G. Zacchei
pp 773 - 780; DOI:
10.1021/jm00181a014
PDF
Inhibition of ribosomal peptidyltransferase with 2'(3')-O-acetyl-2"(3")-O-glycyl-1,2-di(adenosin-N6-yl)ethane and -1,4-di(adenosin-N6-yl)butane. Effect of alkyl chain length
Masayoshi Murata, Prakash Bhuta, James Owens, and Jiri Zemlicka
pp 781 - 786; DOI:
10.1021/jm00181a015
PDF
Diaryl amidine derivatives as oncornaviral DNA polymerase inhibitors
E. De Clercq and O. Dann
pp 787 - 795; DOI:
10.1021/jm00181a016
PDF
Heat-induced formation of .alpha.,.beta.-unsaturated nucleoside dialdehydes and their activity with adenosine deaminase
Alan J. Grant and Leon M. Lerner
pp 795 - 798; DOI:
10.1021/jm00181a017
PDF
Novel antitumor nitrosoureas and related compounds and their reactions with DNA
J. William Lown, Alummoottil V. Joshua, and Larry W. McLaughlin
pp 798 - 805; DOI:
10.1021/jm00181a018
PDF
Potential prophylactic antitumor activity of retinylidene 1,3-diketones
Nancy Acton, Arnold Brossi, Dianne L. Newton, and Michael B. Sporn
pp 805 - 809; DOI:
10.1021/jm00181a019
PDF
Simple .beta.-lactam compounds derived from 6-aminopenicillanic acid
John C. Sheehan, Seiji Shibahara, and Elsie Chacko
pp 809 - 811; DOI:
10.1021/jm00181a020
PDF
Conversion of ergolines to hexahydro- and octahydrobenzo[f]quinolines (depyrroloergolines)
Nicholas J. Bach, Edmund C. Kornfeld, James A. Clemens, and E. Barry Smalstig
pp 812 - 814; DOI:
10.1021/jm00181a021
PDF
Book Reviews

pp 815 - 818; DOI:
10.1021/jm00181a600
PDF

Issue 8


Synthetic immunostimulants derived from the bacterial cell wall
Edgar Lederer
pp 819 - 825; DOI:
10.1021/jm00182a001
PDF
Prevention of Ames test mutagenicity by chemical modification in a series of monoamine oxidase inhibitors
M. Harfenist
pp 825 - 827; DOI:
10.1021/jm00182a002
PDF
Thrombin inhibitors. 1. Ester derivatives of N.alpha.-(arylsulfonyl)-L-arginine
Shosuke Okamoto, Kiyokatsu Kinjo, Akiko Hijikata, Ryoji Kikumoto, Yoshikuni Tamao, Kazuo Ohkubo, and Shinji Tonomura
pp 827 - 830; DOI:
10.1021/jm00182a003
PDF
Thrombin inhibitors. 2. Amide derivatives of N.alpha.-substituted L-arginine
Ryoji Kikumoto, Yoshikuni Tamao, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura, Shosuke Okamoto, Yoshinori Funahara, and Akiko Hijikata
pp 830 - 836; DOI:
10.1021/jm00182a004
PDF
Inhibitors of phenylethanolamine N-methyltransferase and epinephrine biosynthesis. 2. 1,2,3,4-Tetrahydroisoquinoline-7-sulfonanilides
Benjamin Blank, Arnold J. Krog, Gilbert Weiner, and Robert G. Pendleton
pp 837 - 840; DOI:
10.1021/jm00182a005
PDF
Antiestrogens. Synthesis and evaluation of mammary tumor inhibiting activity of 1,1,2,2-tetraalkyl-1,2-diphenylethanes
Rolf W. Hartmann, Gerhard Kranzfelder, Erwin Von Angerer, and Helmut Schoenenberger
pp 841 - 848; DOI:
10.1021/jm00182a006
PDF
Synthesis of nitrosourea derivatives of pyridine and piperidine as potential anticancer agents
A. Michael Crider, Randall Lamey, Heinz G. Floss, John M. Cassady, and William J. Bradner
pp 848 - 851; DOI:
10.1021/jm00182a007
PDF
Fluorinated pyrimidine nucleosides. 4. Synthesis and antitumor testing of a series of 2',5'-dideoxy- and 2',3',5'-trideoxynucleosides of 5-fluorouracil
A. F. Cook, M. J. Holman, and M. J. Kramer
pp 852 - 857; DOI:
10.1021/jm00182a008
PDF
Antihypertensive ureidopiperidines
J. L. Archibald, D. R. Beardsley, G. M. F. Bisset, P. Fairbrother, J. L. Jackson, A. Opalko, and T. J. Ward
pp 857 - 861; DOI:
10.1021/jm00182a009
PDF
Effects of phosphonium compounds on Schistosoma mansoni
Patrick R. McAllister, Mary J. Dotson, Samuel O. Grim, and Gilbert R. Hillman
pp 862 - 865; DOI:
10.1021/jm00182a010
PDF
Conformationally restricted tricyclic antidepressants. 1. Octahydrodibenzazepinonaphthyridines as rigid imipramine analogs
Arnold R. Martin, Vidyadhar M. Paradkar, Geoffrey W. Peng, Robert C. Speth, Henry I. Yamamura, and Alan S. Horn
pp 865 - 873; DOI:
10.1021/jm00182a011
PDF
6-(Substituted-amino)-4H-s-triazolo[4,3-a][1,4]benzodiazepines and 4-(substituted-amino)-6H-s-triazolo[4,3-a][1,4]benzodiazepines with potential antianxiety activity
Jackson B. Hester, Philip VonVoigtlander, and Gerald N. Evenson
pp 873 - 877; DOI:
10.1021/jm00182a012
PDF
Heteroarenobenzodiazepines. 3. 4-Piperazinyl-10H-thieno[2,3-b][1,5]benzodiazepines as potential neuroleptics
Jiban K. Chakrabarti, Linda Horsman, Terrence M. Hotten, Ian A. Pullar, David E. Tupper, and Francesca C. Wright
pp 878 - 884; DOI:
10.1021/jm00182a013
PDF
Heteroarenobenzodiazepines. 4. 10-Piperazinyl-4H-thieno[3,2-b][1,5]- and -[3,4-b][1,5]benzodiazepines as potential neuroleptics
Jiban K. Chakrabarti, John Fairhurst, Norman J. A. Gutteridge, Linda Horsman, Ian A. Pullar, Colin W. Smith, David J. Steggles, David E. Tupper, and Francesca C. Wright
pp 884 - 889; DOI:
10.1021/jm00182a014
PDF
Ultraviolet photoelectron spectroscopy of cyclic amidines. 2. Electronic structure of clonidine and some related 2-(phenylimino)imidazolidines with .alpha.-adrenergic activity
A. P. De Jong and H. Van Dam
pp 889 - 895; DOI:
10.1021/jm00182a015
PDF
4-Anilidopiperidine analgesics. 3. 1-Substituted 4-(propananilido)perhydroazepines as ring-expanded analogs
Z. Gail Finney and Thomas N. Riley
pp 895 - 899; DOI:
10.1021/jm00182a016
PDF
Folate analogs altered in the C9-N10 bridge region. 16. Synthesis and antifolate activity of 11-thiohomoaminopterin
M. G. Nair, Shiang-Yuan Chen, Roy L. Kisliuk, Y. Gaumont, and D. Strumpf
pp 899 - 903; DOI:
10.1021/jm00182a017
PDF
Prostaglandins and congeners. 22. Synthesis of 11-substituted derivatives of 11-deoxyprostaglandins E1 and E2. Potential bronchodilators
M. Brawner Floyd, Robert E. Schaub, Gerald J. Siuta, Jerauld S. Skotnicki, Charles V. Grudzinskas, Martin J. Weiss, Franz Dessy, and L. VanHumbeeck
pp 903 - 913; DOI:
10.1021/jm00182a018
PDF
Anticandidal activity of pyrimidine-peptide conjugates
Jen-Shing Ti, Alvin S. Steinfeld, Fred Naider, Ali Gulumoglu, Sam V. Lewis, and Jeffrey M. Becker
pp 913 - 918; DOI:
10.1021/jm00182a019
PDF
Metabolism of 6-substituted benzo[a]pyrene derivatives: O-dealkylation and regiospecificity in aromatic hydroxylation
Andrew J. Alpert and Ercole L. Cavalieri
pp 919 - 927; DOI:
10.1021/jm00182a020
PDF
Studies on cardiovascular agents. 6. Synthesis and coronary vasodilating and antihypertensive activities of 1,2,4-triazolo[1,5-a]pyrimidines fused to heterocyclic systems
Yasunobu Sato, Yasuo Shimoji, Hiroshi Fujita, Hiroshi Nishino, Hiroshi Mizuno, Shinsaku Kobayashi, and Seiji Kumakura
pp 927 - 937; DOI:
10.1021/jm00182a021
PDF
Conformationally restricted phenothiazine neuroleptics. 1. 3-(Dimethylamino)-1,2,3,4-tetrahydroazepino[3,2,1-kl]phenothiazine
Arnold R. Martin, Sun H. Kim, Henry I. Yamamura, and Alan S. Horn
pp 938 - 941; DOI:
10.1021/jm00182a022
PDF
Crystal and molecular structure of nafoxidine and stereochemical features of anticancer antiestrogens
Norman Camerman, Lilian Y. Y. Chan, and Arthur Camerman
pp 941 - 945; DOI:
10.1021/jm00182a023
PDF
Experimental antiulcer drugs. 4. 1,3-Disubstituted 2,4,5,6-tetrahydro-4,6,6-trimethyl-2-phenylcyclopenta[c]pyrrole-4-carboxamides
Rudolf Oesterlin, Malcolm R. Bell, Allan G. Hlavac, Ruthann H. McGarry, Karl O. Gelotte, James C. Bradford, and Janis Rozitis
pp 945 - 948; DOI:
10.1021/jm00182a024
PDF
4a,9b-trans-8-Fluoro-5-(4-fluorophenyl)-2-[4-(4-fluorophenyl)-4-hydroxybutyl]-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole hydrochloride, a new potent neuroleptic
Willard M. Welch, Frank E. Ewing, Charles A. Harbert, Albert Weissman, and B. Kenneth Koe
pp 949 - 952; DOI:
10.1021/jm00182a025
PDF
Synthesis and anxiolytic activity of a series of pyrazino[1,2-a][1,4]benzodiazepine derivatives
R. G. Smith, R. A. Lucas, and J. W. F. Wasley
pp 952 - 955; DOI:
10.1021/jm00182a026
PDF
Nitrobenzyl halides and carbamates as prototype bioreductive alkylating agents
Beverly A. Teicher and Alan C. Sartorelli
pp 955 - 960; DOI:
10.1021/jm00182a027
PDF
Synthesis and preliminary binding studies of 4,4-ditritio-(-)-nicotine of high specific activity
William C. Vincek, Billy R. Martin, Mario D. Aceto, and E. R. Bowman
pp 960 - 962; DOI:
10.1021/jm00182a028
PDF
Thymidine phosphorylase. Substrate specificity for 5-substituted 2'-deoxyuridines
Chikao Nakayama, Yusuke Wataya, Rich B. Meyer, Daniel V. Santi, Mineo Saneyoshi, and Tohru Ueda
pp 962 - 964; DOI:
10.1021/jm00182a029
PDF
Antiallergy activity of 10-oxo-10H-pyridazino[6,1-b]quinazoline-2-carboxylic acids
Charles F. Schwender, Brooks R. Sunday, Joseph J. Kerbleski, and David J. Herzig
pp 964 - 966; DOI:
10.1021/jm00182a030
PDF
Book Reviews

pp 966 - 972; DOI:
10.1021/jm00182a600
PDF

Issue 9


Separation of potent central and renal dopamine agonist activity in substituted 6-chloro-2,3,4,5-tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepines
Joseph Weinstock, James W. Wilson, David L. Ladd, Charles K. Brush, Francis R. Pfeiffer, George Y. Kuo, Kenneth G. Holden, Nelson C. F. Yim, Richard A. Hahn, and et al.
pp 973 - 975; DOI:
10.1021/jm00183a001
PDF
6-(Phenylthio)-substituted 2,3,4,5-tetrahydro-1H-3-benzazepines, a novel class of dopamine receptor antagonists and neuroleptics
Carl Kaiser, Fadia E. Ali, William E. Bondinell, Martin Brenner, Kenneth G. Holden, Thomas W. Ku, Hye-Ja Oh, Stephen T. Ross, Nelson C. F. Yim, and et al.
pp 975 - 976; DOI:
10.1021/jm00183a002
PDF
Synthesis of 8-aryltetrahydroisoquinolines as dopamine antagonists and evaluation for potential neuroleptic activity
Charles R. Ellefson, Kathleen A. Prodan, Linda R. Brougham, and Arni Miller
pp 977 - 980; DOI:
10.1021/jm00183a003
PDF
Analogs of 8-[[6-(diethylamino)hexyl]amino]-6-methoxy-4-methylquinoline as candidate antileishmanial agents
Maurice P. LaMontagne, Dinesh Dagli, M. Sami Khan, and Peter Blumbergs
pp 981 - 985; DOI:
10.1021/jm00183a004
PDF
Synthesis and biological activity of fluoroalkylamine derivatives of narcotic analgesics
William G. Reifenrath, Edward B. Roche, Walid A. Al-Turk, and Howard L. Johnson
pp 985 - 990; DOI:
10.1021/jm00183a005
PDF
Demethyl analogs of psychoactive methoxyphenalkylamines: synthesis and serotonin receptor affinities
Richard A. Glennon, Stephen M. Liebowitz, Dianne Leming-Doot, and John A. Rosecrans
pp 990 - 994; DOI:
10.1021/jm00183a006
PDF
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 994 - 1002; DOI:
10.1021/jm00183a007
PDF
Estrogen receptor based imaging agents. 2. Synthesis and receptor binding affinity of side-chain halogenated hexestrol derivatives
Ramanuj Goswami, Stephen G. Harsy, Daniel F. Heiman, and John A. Katzenellenbogen
pp 1002 - 1008; DOI:
10.1021/jm00183a008
PDF
Aporphines. 31. Synthesis and antitumor activity of aporphine nitrogen mustards
John L. Neumeyer, Felix E. Granchelli, Crist N. Filer, Albert H. Soloway, and Say-Jong Law
pp 1008 - 1013; DOI:
10.1021/jm00183a009
PDF
Retinoic acid analogs. Synthesis and potential as cancer chemopreventive agents
Marcia I. Dawson, Peter D. Hobbs, Karl Kuhlmann, Victor A. Fung, C. Tucker Helmes, and Wan-Ru Chao
pp 1013 - 1022; DOI:
10.1021/jm00183a010
PDF
Evaluation of rotenone and related compounds as antagonists of slow-reacting substance of anaphylaxis
Richard J. Ashack, Leslie P. McCarty, Rebecca S. Malek, Frank R. Goodman, and Norton P. Peet
pp 1022 - 1026; DOI:
10.1021/jm00183a011
PDF
Bronchodilator and antiulcer phenoxypyrimidinones
C. A. Lipinski, J. G. Stam, J. N. Pereira, N. R. Ackerman, and H. J. Hess
pp 1026 - 1031; DOI:
10.1021/jm00183a012
PDF
Synthesis of .alpha.-methylene-.gamma.-butyrolactones: a structure-activity relationship study of their allergenic power
Gilbert Schlewer, Jean Luc Stampf, and Claude Benezra
pp 1031 - 1038; DOI:
10.1021/jm00183a013
PDF
Metabolic N-hydroxylation. Use of substituent variation to modulate the in vitro bioactivation of 4-acetamidostilbenes
Patrick E. Hanna, Richard E. Gammans, Russell D. Sehon, and Man-Kil Lee
pp 1038 - 1044; DOI:
10.1021/jm00183a014
PDF
Resolution, absolute configuration, and antiarrhythmic properties of the enantiomers of disopyramide, 4-(diisopropylamino)-2-(2-pyridyl)-2-phenylbutyramide
Terrence R. Burke, Wendel L. Nelson, Margaret Mangion, Gilbert J. Hite, Corwin M. Mokler, and Peter C. Ruenitz
pp 1044 - 1048; DOI:
10.1021/jm00183a015
PDF
Structure-activity relationship of diphenylthiourea antivirals
Angel S. Galabov, Boris S. Galabov, and Nadejda A. Neykova
pp 1048 - 1051; DOI:
10.1021/jm00183a016
PDF
Tumor inhibitory triazenes. 2. Variation of antitumor activity within an homologous series
Derry E. V. Wilman and Phyllis M. Goddard
pp 1052 - 1054; DOI:
10.1021/jm00183a017
PDF
Antileukemic compounds derived from the chemical modification of macrocyclic trichothecenes. 1. Derivatives of verrucarin A
Bruce B. Jarvis, G. Patrick Stahly, Gowsala Pavanasasivam, and Eugene P. Mazzola
pp 1054 - 1058; DOI:
10.1021/jm00183a018
PDF
1-[(Ethoxyamino)methyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-2-benzoxepins: a new class of antianaphylactic agents
Ruth E. TenBrink, John M. McCall, and Herbert G. Johnson
pp 1058 - 1060; DOI:
10.1021/jm00183a019
PDF
Book Reviews

pp 1061 - 1062; DOI:
10.1021/jm00183a600
PDF

Issue 10


Cancer chemotherapy: congener synthesis
John A. Montgomery
pp 1063 - 1067; DOI:
10.1021/jm00184a001
PDF
Stereochemical requirements for cannabinoid activity
R. Mechoulam, N. Lander, T. H. Varkony, I. Kimmel, O. Becker, Z. Ben-Zvi, H. Edery, and G. Porath
pp 1068 - 1072; DOI:
10.1021/jm00184a002
PDF
Fluoroprostaglandins: synthesis and biological evaluation of the methyl esters of (+)-12-fluoro-, (-)-ent-12-fluoro-, (+)-15-epi-fluoro-, and (-)-ent-15-epi-12-fluoroprostaglandin F2.alpha.
Paul A. Grieco, William Owens, C. L. J. Wang, Eric Williams, William J. Schillinger, Ken Hirotsu, and Jon Clardy
pp 1072 - 1077; DOI:
10.1021/jm00184a003
PDF
Carbon-14 fluorinated prostaglandins: synthesis and biological evaluation of the methyl esters of (+)-14-fluoro-, (+)-15-epi-14-fluoro-, (+)-13(E)-14-fluoro-, and (+)-13(E)-15-epi-14-fluoroprostaglandin F2.alpha.
Paul A. Grieco, William J. Schillinger, and Yuusaku Yokoyama
pp 1077 - 1083; DOI:
10.1021/jm00184a004
PDF
Anticoccidial derivatives of 6-azauracil. 3. Synthesis, high activity, and short plasma half-life of 1-phenyl-6-azauracils containing sulfonamide substituents
Max W. Miller, Banavara L. Mylari, Harold L. Howes, Sanford K. Figdor, Martin J. Lynch, John E. Lynch, and Richard C. Koch
pp 1083 - 1087; DOI:
10.1021/jm00184a005
PDF
Nucleosides. 116. 1-(.beta.-D-Xylofuranosyl)-5-fluorocytosines with a leaving group on the 3' position. Potential double-barreled masked precursors of anticancer nucleosides
K. A. Watanabe, U. Reichman, C. K. Chu, D. H. Hollenberg, and J. J. Fox
pp 1088 - 1094; DOI:
10.1021/jm00184a006
PDF
Antitumor structure-activity relationships. Nitrosoureas vs. L-1210 leukemia
Corwin Hansch, A. Leo, Charles Schmidt, P. Y. C. Jow, and John A. Montgomery
pp 1095 - 1101; DOI:
10.1021/jm00184a007
PDF
Synthesis and antiarrhythmic activity of .alpha.,.alpha.-bis[(dialkylamino)alkyl]phenylacetamides
Peter K. Yonan, Robert L. Novotney, Chi Min Woo, Kathleen A. Prodan, and Fred M. Hershenson
pp 1102 - 1108; DOI:
10.1021/jm00184a008
PDF
Synthesis and antibacterial activity of new 1-oxa-1-dethiacephalosporins
Daijiro Hagiwara, Hidekazu Takeno, Matsuhiko Aratani, Keiji Hemmi, and Masashi Hashimoto
pp 1108 - 1113; DOI:
10.1021/jm00184a009
PDF
Novel analogs of enkephalin: identification of functional groups required for biological activity
Fredric A. Gorin, T. M. Balasubramanian, Theodore J. Cicero, John Schwietzer, and Garland R. Marshall
pp 1113 - 1122; DOI:
10.1021/jm00184a010
PDF
.beta.-Adrenergic blocking agents. 20. (3-Hydroxyprop-1-enyl)-substituted 1-(aryloxy)-3-(alkylamino)propan-2-ols
H. Tucker
pp 1122 - 1126; DOI:
10.1021/jm00184a011
PDF
Synthesis of selenium-75 labeled tertiary diamines: new brain imaging agents
Hank Kung and Monte Blau
pp 1127 - 1130; DOI:
10.1021/jm00184a012
PDF
Synthesis, absorption, and toxicity of N1,N8-bis(2,3-dihydroxybenzoyl)spermidine, a potent iron chelator
Raymond J. Bergeron, Philip S. Burton, Kathy Ann McGovern, Erica J. St. Onge, and Richard R. Streiff
pp 1130 - 1133; DOI:
10.1021/jm00184a013
PDF
Ivermectin, a new broad-spectrum antiparasitic agent
John C. Chabala, Helmut Mrozik, Richard L. Tolman, Philip Eskola, Aino Lusi, Louis H. Peterson, Mary F. Woods, Michael H. Fisher, William C. Campbell, and et al.
pp 1134 - 1136; DOI:
10.1021/jm00184a014
PDF
Synthesis of potential inhibitors of hypoxanthine-guanine phosphoribosyltransferase for testing as antiprotozoal agents. 2. 1-Substituted hypoxanthines
James R. Piper, Anne G. Laseter, Thomas P. Johnston, and John A. Montgomery
pp 1136 - 1139; DOI:
10.1021/jm00184a015
PDF
Studies on antimicrobial agents. 1. Synthesis and relation between the antimicrobial activities and certain physicochemical properties of some N'-(pyridinioacetyl) fatty acid hydrazides
Susana M. Sicardi, Carlos M. Vega, and Eberhard B. Cimijotti
pp 1139 - 1142; DOI:
10.1021/jm00184a016
PDF
(.+-.)-trans-2-(Aminomethyl)cyclobutanecarboxylic acid hydrochloride: a rigid analog of .gamma.-aminobutyric acid
John P. O'Donnell, David A. Johnson, and Albert J. Azzaro
pp 1142 - 1144; DOI:
10.1021/jm00184a017
PDF
Structure-activity relationships of pyrrole amidine antiviral antibiotics. 2. Preparation of mono- and tripyrrole derivatives of congocidine
Meir Bialer, Boris Yagen, Raphael Mechoulam, and Yechiel Becker
pp 1144 - 1148; DOI:
10.1021/jm00184a018
PDF
Book Reviews

pp 1148 - 1152; DOI:
10.1021/jm00184a600
PDF

Issue 11


Studies on the mechanism of toxicity of acetaminophen. Synthesis and reactions of N-acetyl-2,6-dimethyl- and N-acetyl-3,5-dimethyl-p-benzoquinone imines
C. Roger Fernando, Ian C. Calder, and Kathryn N. Ham
pp 1153 - 1158; DOI:
10.1021/jm00185a001
PDF
Synthesis of certain [6:5:6] linear tricyclic nucleosides as potential antitumor agents
Fung-Lung Chung, Karl H. Schram, Raymond P. Panzica, Robert A. Earl, Linda L. Wotring, and Leroy B. Townsend
pp 1158 - 1166; DOI:
10.1021/jm00185a002
PDF
Amino acid and dipeptide derivatives of daunorubicin. 1. Synthesis, physicochemical properties, and lysosomal digestion
Michele Masquelier, Roger Baurain, and Andre Trouet
pp 1166 - 1170; DOI:
10.1021/jm00185a003
PDF
Amino acid and dipeptide derivatives of daunorubicin. 2. Cellular pharmacology and antitumor activity of L1210 leukemic cells in vitro and in vivo
R. Baurain, M. Masquelier, D. Deprez-De Campeneere, and A. Trouet
pp 1171 - 1174; DOI:
10.1021/jm00185a004
PDF
Metabolic .beta.-hydroxylation and N-oxidation of n'-nitrosonornicotine
Stephen S. Hecht, Chi-Hong B. Chen, and Dietrich Hoffmann
pp 1175 - 1178; DOI:
10.1021/jm00185a005
PDF
Urinary metabolites of timolol from humans and laboratory animals. Syntheses and .beta.-adrenergic blocking activities
B. K. Wasson, J. Scheigetz, C. S. Rooney, R. A. Hall, N. N. Share, W. J. A. VandenHeuvel, B. H. Arison, O. D. Hensens, R. L. Ellsworth, and D. J. Tocco
pp 1178 - 1184; DOI:
10.1021/jm00185a006
PDF
Glycolipids as potential immunologic adjuvants
Mitree M. Ponpipom, Robert L. Bugianesi, and Tsung-Ying Shen
pp 1184 - 1188; DOI:
10.1021/jm00185a007
PDF
Substituted 6,7-dihydroimidazo[1,2-a]purin-9(4H)-ones
D. L. Temple, J. P. Yevich, J. D. Catt, D. Owens, C. Hanning, R. R. Covington, R. J. Seidehamel, and K. W. Dungan
pp 1188 - 1198; DOI:
10.1021/jm00185a008
PDF
Antimalarials. 12. Preparation of carbon isosteres of selected 4-pyridinemethanols as suppressive antimalarials
Anica Markovac and Maurice P. LaMontagne
pp 1198 - 1201; DOI:
10.1021/jm00185a009
PDF
Confidence interval estimators for parameters associated with quantitative structure-activity relationships
Stephen W. Dietrich, Nicholas D. Dreyer, Corwin Hansch, and Donald L. Bentley
pp 1201 - 1205; DOI:
10.1021/jm00185a010
PDF
Quantitative structure-selectivity relationships. Comparison of the inhibition of Escherichia coli and bovine liver dihydrofolate reductase by 5-(substituted benzyl)-2,4-diaminopyrimidines
Stephen W. Dietrich, Jeffrey M. Blaney, Mark A. Reynolds, Priscilla Y. C. Jow, and Corwin Hansch
pp 1205 - 1212; DOI:
10.1021/jm00185a011
PDF
Structure-activity relationship in a series of newly synthesized 1-amino-substituted ellipticine derivatives
Claire Ducrocq, Francoise Wendling, Jean Claude Chermann, Martine Tourbez-Perrin, Christian Rivalle, Pierre Tambourin, Francois Pochon, and Emile Bisagni
pp 1212 - 1216; DOI:
10.1021/jm00185a012
PDF
Chemistry, pharmacology, and structure-activity relationships with a new type of imidazolines exerting a specific bradycardic action at a cardiac site
Helmut Staehle, Helmut Daniel, Walter Kobinger, Christian Lillie, and Ludwig Pichler
pp 1217 - 1222; DOI:
10.1021/jm00185a013
PDF
Studies on several 7-substituted N,N-dimethyltryptamines
R. A. Glennon, E. Schubert, J. M. Jacyno, and J. A. Rosecrans
pp 1222 - 1226; DOI:
10.1021/jm00185a014
PDF
Fluorinated analogs of 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea: an attempt to control metabolism
Allan B. Foster, Michael Jarman, Paul L. Coe, John Sleigh, and J. Colin Tatlow
pp 1226 - 1229; DOI:
10.1021/jm00185a015
PDF
Synthesis and biological activity of 5-fluoro-2'-deoxyuridine 5'-phosphorodiamidates
Mary E. Phelps, Peter W. Woodman, and Peter V. Danenberg
pp 1229 - 1232; DOI:
10.1021/jm00185a016
PDF
Optically active derivatives of imidazolines. .alpha.-Adrenergic blocking properties
Fu-Lian Hsu, Akihiko Hamada, Mark E. Booher, H. Fuder, P. N. Patil, and Duane D. Miller
pp 1232 - 1235; DOI:
10.1021/jm00185a017
PDF
Synthesis and antineoplastic activity of a novel series of phosphoramide mustard analogs of pyrimidine deoxyribonucleosides
Tai-Shun Lin, Paul H. Fischer, and William H. Prusoff
pp 1235 - 1237; DOI:
10.1021/jm00185a018
PDF
2-Methylanthraquinone derivatives as potential bioreductive alkylating agents
Tai-Shun Lin, Beverly A. Tiecher, and Alan C. Sartorelli
pp 1237 - 1242; DOI:
10.1021/jm00185a019
PDF
8-Hydroxyanthracyclinones from .epsilon.-rhodomycinone
Horng-Jau Lin, Virendra Kumar, and William A. Remers
pp 1242 - 1244; DOI:
10.1021/jm00185a020
PDF
Chemistry of nitrosoureas. Intermediacy of 4,5-dihydro-1,2,3-oxadiazole in 1,3-bis(2-chloroethyl)-1-nitrosourea decomposition
Robert B. Brundrett
pp 1245 - 1247; DOI:
10.1021/jm00185a021
PDF
Inhibition of dihydrofolate reductase. 3. 4,6-Diamino-1,2-dihydro-2,2-dimethyl-1-(2-substituted-phenyl)-s-triazine inhibition of bovine liver and mouse tumor enzymes
Ki Hwan Kim, Stephen W. Dietrich, Corwin Hansch, Bruce J. Dolnick, and Joseph R. Bertino
pp 1248 - 1251; DOI:
10.1021/jm00185a022
PDF
Synthesis and antiallergy activity of 4-oxopyrano[3,2-b]indoles
Paul C. Unangst, Richard E. Brown, and David J. Herzig
pp 1251 - 1255; DOI:
10.1021/jm00185a023
PDF
Antiarrhythmic activity of amitriptyline analogues in conscious dogs after myocardial infarction: cyproheptadinium methiodide
R. Douglas Wilkerson and James D. Henderson
pp 1255 - 1258; DOI:
10.1021/jm00185a024
PDF
Synthesis and some pharmacological properties of [8-L-tryptophan]oxytocin
Miklos Bodanszky, John C. Tolle, Janny Seto, and Wilbur H. Sawyer
pp 1258 - 1261; DOI:
10.1021/jm00185a025
PDF
Synthesis and adrenergic blocking effects of 2-(alkylamino)-3,4-dihydroquinazolines
John A. Grosso, David E. Nichols, Maxine B. Nichols, and George K. W. Yim
pp 1261 - 1264; DOI:
10.1021/jm00185a026
PDF
Synthesis and aldose reductase inhibitory activity of 7-sulfamoylxanthone-2-carboxylic acids
Jurg R. Pfister, Walter E. Wymann, Janette M. Mahoney, and L. David Waterbury
pp 1264 - 1267; DOI:
10.1021/jm00185a027
PDF
Synthesis of some 5-phenylhexahydroazepino[4,5-b]indoles as potential neuroleptic agents
Arthur J. Elliott, Elijah H. Gold, and Henry Guzik
pp 1268 - 1269; DOI:
10.1021/jm00185a028
PDF
Book Reviews

pp 1270 - 1274; DOI:
10.1021/jm00185a600
PDF

Issue 12


Prodrugs and site-specific drug delivery
Valentino J. Stella and Kenneth J. Himmelstein
pp 1275 - 1282; DOI:
10.1021/jm00186a001
PDF
A multifaceted approach to the study of the side-chain conformation in .beta.-lactamase-resistant penicillins
Patrick C. Blanpain, Janos B. Nagy, Guy H. Laurent, and Francois V. Durant
pp 1283 - 1292; DOI:
10.1021/jm00186a002
PDF
Thrombin inhibitors. 3. Carboxyl-containing amide derivatives of N.alpha.-substituted L-arginine
Ryoji Kikumoto, Yoshikuni Tamao, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura, Shosuke Okamoto, and Akiko Hijikata
pp 1293 - 1299; DOI:
10.1021/jm00186a003
PDF
Analogs of chloramphenicol: circular dichroism spectra, inhibition of ribosomal peptidyltransferase, and possible mechanism of action
Prakash Bhuta, Hsiao L. Chung, Jui-Shung Hwang, and Jiri Zemlicka
pp 1299 - 1305; DOI:
10.1021/jm00186a004
PDF
3-(4-Piperidinylalkyl)indoles, selective inhibitors of neuronal 5-hydroxytryptamine uptake
Claude Gueremy, Francois Audiau, Alain Champseix, Andre Uzan, Gerard Le Fur, and Jean Rataud
pp 1306 - 1310; DOI:
10.1021/jm00186a005
PDF
Cytotoxic and antitumor properties of bleomycin and several of its metal complexes
Eswara A. Rao, Leon A. Saryan, William E. Antholine, and David H. Petering
pp 1310 - 1318; DOI:
10.1021/jm00186a006
PDF
Synthetic and preliminary hemodynamic and whole animal toxicity studies on (R,S)-, (R)-, and (S)-2-methyl-3-(2,4,5-trihydroxyphenyl)alanine
D. G. Musson, D. Karashima, H. Rubiero, K. L. Melmon, A. Cheng, and N. Castagnoli
pp 1318 - 1323; DOI:
10.1021/jm00186a007
PDF
Studies on the syntheses of heterocyclic compounds. 845. Studies on the synthesis of chemotherapeutics. 10. Synthesis and antitumor activity of N-acyl- and N-(alkoxycarbonyl)-5-fluorouracil derivatives
Tetsuji Kametani, Kazuo Kigasawa, Mineharu Hiiragi, Kikuo Wakisaka, Seiji Haga, Yasuo Nagamatsu, Hideo Sugi, Kazunaga Fukawa, Osamu Irino, and et al.
pp 1324 - 1329; DOI:
10.1021/jm00186a008
PDF
DNA intercalating compounds as potential antitumor agents. 1. Preparation and properties of 7H-pyridocarbazoles
Didier Pelaprat, Robert Oberlin, Irene Le Guen, Jean Bernard Le Pecq, and Bernard P. Roques
pp 1330 - 1335; DOI:
10.1021/jm00186a009
PDF
DNA intercalating compounds as potential antitumor agents. 2. Preparation and properties of 7H-pyridocarbazole dimers
Didier Pelaprat, Alain Delbarre, Irene Le Guen, Jean Bernard Le Pecq, and Bernard P. Roques
pp 1336 - 1343; DOI:
10.1021/jm00186a010
PDF
Nucleoside conjugates as potential antitumor agents. 3. Synthesis and antitumor activity of 1-(.beta.-D-arabinofuranosyl)cytosine conjugates of corticosteroids
Chung Il Hong, Alexander Nechaev, Alan J. Kirisits, David J. Buchheit, and Charles R. West
pp 1343 - 1347; DOI:
10.1021/jm00186a011
PDF
N,N'-Dialkylbis(dichlorophenyl)ethylenediamines and -imidazolidines: relationship between structure and estradiol receptor affinity
Erwin Von Angerer, Gerhard Kranzfelder, Ashok K. Taneja, and Helmut Schoenenberger
pp 1347 - 1350; DOI:
10.1021/jm00186a012
PDF
Synthesis, biological evaluation, and preliminary structure-activity considerations of a series of alkylphenols as intravenous anesthetic agents
Roger James and John B. Glen
pp 1350 - 1357; DOI:
10.1021/jm00186a013
PDF
Structure-activity relationships of antibacterial 6,7- and 7,8-disubstituted 1-alkyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acids
Hiroshi Koga, Akira Itoh, Satoshi Murayama, Seigo Suzue, and Tsutomu Irikura
pp 1358 - 1363; DOI:
10.1021/jm00186a014
PDF
Synthesis and immunological activity of 5,6,6a,8,9,11a-hexahydronaphth[1',2':4,5]imidazo[2,1-b]thiazoles and 5,6,6a,9,10,11a-hexahydronaphth[2',1':4,5]imidazo[2,1-b]thiazoles
Masahiko Saito, Yasutaka Kayama, Tamaki Watanabe, Hisashi Fukushima, Takeshi Hara, Kazuo Koyano, Akio Takenaka, and Yoshio Sasada
pp 1364 - 1372; DOI:
10.1021/jm00186a015
PDF
Synthesis and antiallergic properties of some 4H,5H-pyrano[3,2-c][1]benzopyran-4-one, 4H,5H-[1]benzothiopyrano[4,3-b]pyran-4-one, and 1,4-dihydro-5H-[1]benzothiopyrano[4,3-b]pyridin-4-one derivatives
Adolf Philipp, Ivo Jirkovsky, and Rene R. Martel
pp 1372 - 1376; DOI:
10.1021/jm00186a016
PDF
Studies on anticoccidial agents. 13. Synthesis and anticoccidial activity of nitropyridine-2- and -3-sulfonamides and derivatives
Yasuhiro Morisawa, Mitsuru Kataoka, Hitoshi Nagahori, Toshiaki Sakamoto, Noritoshi Kitano, Kenichi Kusano, and Kiyoshi Sato
pp 1376 - 1380; DOI:
10.1021/jm00186a017
PDF
7-(Aminoacyl) and 7-(aminoalkyl) derivatives of 1,2,6,7-tetrahydroindolo[1,7-ab][1,5]benzodiazepines as potential antidepressant agents
Edward J. Glamkowski, James M. Fortunato, and Harry M. Geyer
pp 1380 - 1386; DOI:
10.1021/jm00186a018
PDF
Antihypertensive (2-aminoethyl)thiourea derivatives. 1
Jefferson W. Tilley, Paul Levitan, Richard W. Kierstead, and Michael Cohen
pp 1387 - 1392; DOI:
10.1021/jm00186a019
PDF
Synthesis and biological activity of a ketomethylene analog of a tripeptide inhibitor of angiotensin converting enzyme
Ronald G. Almquist, Wan-Ru Chao, Marie E. Ellis, and Howard L. Johnson
pp 1392 - 1398; DOI:
10.1021/jm00186a020
PDF
Antihypertensive 5,6-diarylpyridazin-3-ones
Russell Buchman, James A. Scozzie, Zaven S. Ariyan, Richard D. Heilman, Donna J. Rippin, W. J. Pyne, Larry J. Powers, and Richard J. Matthews
pp 1398 - 1405; DOI:
10.1021/jm00186a021
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Synthesis and antihypertensive activity of 5-amino-2-pyridinecarboxylic acid derivatives
Neville Finch, Thomas R. Campbell, Charles W. Gemenden, and Henry J. Povalski
pp 1405 - 1410; DOI:
10.1021/jm00186a022
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Synthesis and antifertility activity of 3,9-dihydroxy-5,6,6a.alpha.,6b.beta.,11,12,12a.beta.,12b.alpha.-octahydrodibenzo[a,g]biphenylene, a structural relative of diethylstilbestrol
P. H. Ruehle, C. E. Browne, E. H. Vickery, N. R. Beller, E. J. Eisenbraun, R. A. Loghry, and Dick Van der Helm
pp 1410 - 1414; DOI:
10.1021/jm00186a023
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2-(Aminomethyl)phenols, a new class of saluretic agents. 1. Effects of nuclear substitution
G. E. Stokker, A. A. Deana, S. J. DeSolms, E. M. Schultz, R. L. Smith, E. J. Cragoe Jr., J. E. Baer, C. T. Ludden, H. F. Russo, and et al.
pp 1414 - 1427; DOI:
10.1021/jm00186a024
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Analgesic narcotic antagonists. 4. 7-Methyl-N-(cycloalkylmethyl)-3-hydroxy morphinan-6-one and -isomorphinan-6-one
David L. Leland and Michael P. Kotick
pp 1427 - 1431; DOI:
10.1021/jm00186a025
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Synthesis and structure-function studies of melanocyte stimulating hormone analogs modified in the 2 and 4(7) positions: comparison of activities on frog skin melanophores and melanoma adenylate cyclase
Victor J. Hruby, Tomi K. Sawyer, Young C. S. Yang, Marvin D. Bregman, Mac E. Hadley, and Christopher B. Heward
pp 1432 - 1437; DOI:
10.1021/jm00186a026
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Antihypertensive (2-aminoethyl)thiourea derivatives. 2
Jefferson W. Tilley, H. Ramuz, F. Hefti, and M. Gerold
pp 1438 - 1439; DOI:
10.1021/jm00186a027
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Synthesis and biological activities of chloroethylurea, methylurea, and nitrosourea analogs of N-deacetylmethylthiocolchicine
Tai-Shun Lin, George T. Shiau, William H. Prusoff, and Robert E. Harmon
pp 1440 - 1442; DOI:
10.1021/jm00186a028
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Crystal structures of calcium channel antagonists: 2,6-dimethyl-3,5-dicarbomethoxy-4-[2-nitro-, 3-cyano-, 4-(dimethylamino)-, and 2,3,4,5,6-pentafluorophenyl]-1,4-dihydropyridine
A. M. Triggle, E. Shefter, and D. J. Triggle
pp 1442 - 1445; DOI:
10.1021/jm00186a029
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Lipophilic and hydrophilic esters of 4-acetyl-2-(2-hydroxyethyl)-5,6-bis(4-chlorophenyl)-2H-pyridazin-3-one as antihypertensive agents
S. W. Fogt, J. A. Scozzie, R. D. Heilman, and L. J. Powers
pp 1445 - 1448; DOI:
10.1021/jm00186a030
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Some short-chain N6-substituted adenosine analogs with antitumor properties
M. H. Fleysher, R. J. Bernacki, and G. A. Bullard
pp 1448 - 1452; DOI:
10.1021/jm00186a031
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Rational selection of test series. 1. Principal component method combined with multidimensional mapping
W. J. Streich, S. Dove, and R. Franke
pp 1452 - 1456; DOI:
10.1021/jm00186a032
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Rational selection of test series. 2. Two-dimensional mapping of intraclass correlation matrixes
S. Dove, W. J. Streich, and R. Franke
pp 1456 - 1459; DOI:
10.1021/jm00186a033
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Book Reviews

pp 1460 - 1462; DOI:
10.1021/jm00186a600
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Additions and Corrections - Basic Antiinflammatory Compounds. N,N'N''-Trisubstituted Guanidines.
Schneur Rachlin, E. Bramm, I. Ahnfelt-Rønne, and E. Arrigoni-Martelli
pp 1459 - 1459; DOI:
10.1021/jm00186a601
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Additions and Corrections - Quantitative Structure-Activity Relationships for N-[(N',N'-Disubstituted-amino)acetyl]arylamines for Local Anesthetic Activity and Acute Toxicity
Françoise Heymans, Laurence Le Thérizien, Jean-Jacques Godfroid, and Pierre Bessin
pp 1459 - 1459; DOI:
10.1021/jm00186a602
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Additions and Corrections - 10, 10-Difluoro-13-dehydroprostacyclin: A Chemically and Metabolically Stabilized Potent Prostacyclin.
Josef Fried, D. K. Mitra, M. Nagarajan, and M. M .Mehrotra
pp 1459 - 1459; DOI:
10.1021/jm00186a603
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Additions and Corrections - 2,4-Diamino-5-benzylpyrimidines and Analogues as Antibacterial Agents. 3. C-Benzylation of Aminopyridines with Phenolic Mannich Bases. Synthesis of 1- and 3-Deaza Analogues of Trimethoprom.
Barbara S. Rauckman, and Barbara Roth
pp 1459 - 1459; DOI:
10.1021/jm00186a604
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Additions and Corrections - Inhibition of Ribosomal Peptidyltransferase with 2'(3')-O-Acetyl-2''(3'')-O-glycyl-1,2-di(adenosin-N6-yl)ethane and 1,4-di(adenosin-N6-yl)butane. Effect of Alkyl Chain Length.
Masayoshi Murata, Prakash Bhuta, James Owens, and Jiri Zemlicka
pp 1459 - 1459; DOI:
10.1021/jm00186a605
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Additions and Corrections - Studies on Cardiovascular Agents. 6. Synthesis and Coronary Vasodilating and Antihypertensive Activities of 1,2,4-Triazolo[1,5-α]pyrimidines Fused to Heterocyclic Systems.
Yasunobu Sasto, Yasuo Shimoji, Hiroshi Fujita, Hiroshi Nishino, Hiroshi Mizuno, Shinsaku Kobayashi, and Seihi Kumakura
pp 1459 - 1459; DOI:
10.1021/jm00186a606
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Additions and Corrections - Annual Review of Neuroscience. Volume 3.
L. G. Abood
pp 1459 - 1459; DOI:
10.1021/jm00186a607
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