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Volume 19
Main Index

Issue 1


Structure of medicinal chemistry
Corwin Hansch
pp 1 - 6; DOI:
10.1021/jm00223a001
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Synthesis and adrenoreceptor blocking action of aziridinium ions derived from phenoxybenzamine and dibenamine
James G. Henkel, Philip S. Portoghese, Jack W. Miller, and Patricia Lewis
pp 6 - 10; DOI:
10.1021/jm00223a002
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Importance of the aromatic ring in adrenergic amines. 2. Synthesis and adrenergic activity of some nonaromatic six- and eight-membered ring analogs of .beta.-phenylethanolamine
Gary L. Grunewald, Joseph M. Grindel, Popat N. Patil, and Kadhim N. Salman
pp 10 - 16; DOI:
10.1021/jm00223a003
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Relation between analgetic ED50 dose and time-course brain levels of N-alkylnormeperidine homologs
Dennis L. Larson and Philip S. Portoghese
pp 16 - 19; DOI:
10.1021/jm00223a004
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Specificity of an antibody directed against d-methamphetamine. Rigid and nonrigid analogs
Bahjat A. Faraj, Zafar H. Israili, Nancy E. Kight, Edward E. Smissman, and Thomas L. Pazdernik
pp 20 - 25; DOI:
10.1021/jm00223a005
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Aporphines. 14. Dopaminergic and antinociceptive activity of aporphine derivatives. Synthesis of 10-hydroxyaporphines and 10-hydroxy-N-propylnoraporphine
J. L. Neumeyer, J. F. Reinhard, W. P. Dafeldecker, J. Guarino, D. S. Kosersky, K. Fuxe, and L. Agnati
pp 25 - 29; DOI:
10.1021/jm00223a006
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Catechol O-methyltransferase. 7. Affinity labeling with the oxidation products of 6-aminodopamine
Ronald T. Borchardt, Edward E. Smissman, Donald Nerland, and Jack R. Reid
pp 30 - 37; DOI:
10.1021/jm00223a007
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Potential oxidative pathways of brain catecholamines
Daniel C. S. Tse, Richard L. McCreery, and Ralph N. Adams
pp 37 - 40; DOI:
10.1021/jm00223a008
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8-Chloro-(S)- and -(R)-10-[(S)- and -(R)-3'-methylethylaminopyrrolidino]-10,11-dihydrodibenzo[b,f]thiepins. Synthesis and pharmacological studies
Donald T. Witiak, Babu R. Vishnuvajjala, Tribhuwan K. Gupta, and Michael C. Gerald
pp 40 - 47; DOI:
10.1021/jm00223a009
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Novel analogs of tricyclic psychopharmacological agents
Karen E. Eichstadt, John C. Reepmeyer, Richard B. Cook, Paul G. Riley, Dwight P. Davis, and Robert A. Wiley
pp 47 - 51; DOI:
10.1021/jm00223a010
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Conformational study of .beta.-phenethanolamine receptor sites. 8. Pharmacological study of 3-isopropylamino-2-phenyl-trans-2-decalols
M. Hava, J. Bernstein, E. E. Smissman, and S. El-Antably
pp 52 - 54; DOI:
10.1021/jm00223a011
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Stereochemical studies on medicinal agents. 19. The x-ray crystal structures of two (+-)-allylprodine diastereomers. Role of the allyl group in conferring high stereoselectivity and potency at analgetic receptors
Philip S. Portoghese and Eli Shefter
pp 55 - 57; DOI:
10.1021/jm00223a012
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Chemistry and antibacterial activity of nitrobenzofurans
Larry J. Powers
pp 57 - 62; DOI:
10.1021/jm00223a013
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Correlation analysis of Baker's studies on enzyme inhibition. 1. Guanine deaminase, xanthine oxidase, dihydrofolate reductase, and complement
Carlo Silipo and Corwin Hansch
pp 62 - 71; DOI:
10.1021/jm00223a014
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Correlation analysis of Baker's studies on enzyme inhibition. 2. Chymotrypsin, trypsin, thymidine phosphorylase, uridine phosphorylase, thymidilate synthetase, cytosine nucleoside deaminase, dihydrofolate reductase, malate, glutamate, lactate, and glyceraldehyde-phosphate dehydrogenase
Masafumi Yoshimoto and Corwin Hansch
pp 71 - 98; DOI:
10.1021/jm00223a015
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Ergoline congeners as potential inhibitors of prolactin release 2
David B. Rusterholz, Charles F. Barfknecht, and James A. Clemens
pp 99 - 102; DOI:
10.1021/jm00223a016
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Improved delivery through biological membranes. 1. Synthesis and properties of 1-methyl-1,6-dihydropyridine-2-carbaldoxime, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride
Nicolae Bodor, Efraim Shek, and Takeru Higuchi
pp 102 - 107; DOI:
10.1021/jm00223a017
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Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride
Efraim Shek, Takeru Higuchi, and Nicolae Bodor
pp 108 - 112; DOI:
10.1021/jm00223a018
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Improved delivery through biological membranes. 3. Delivery of N-methylpyridinium-2-carbaldoxime chloride through the blood-brain barrier in its dihydropyridine pro-drug form
Efraim Shek, Takeru Higuchi, and Nicolae Bodor
pp 113 - 117; DOI:
10.1021/jm00223a019
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Conformationally restricted analogs of histamine H1 receptor antagonists, trans- and cis-1-benzyl-3-dimethylamino-6-phenylpiperidine
Ahmed E. Ahmed, Patrick E. Hanna, and Vernon R. Grund
pp 117 - 122; DOI:
10.1021/jm00223a020
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Synthesis and biological actions of 2-substituted quinolizidines
Thomas L. Lemke and Michael B. Cramer
pp 122 - 126; DOI:
10.1021/jm00223a021
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Synthesis and biological activity of 2- and 4-substituted 6,7-dihydroxy-1,2,3,4-tetrahydroisoquinolines
Edward E. Smissman, Jack R. Reid, David A. Walsh, and Ronald T. Borchardt
pp 127 - 131; DOI:
10.1021/jm00223a022
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Comparative analysis of the cytotoxicity of substituted [phenylglyoxal bis(4-methyl-3-thiosemicarbazone]copper(II) chelates
Eugene A. Coats, Stanley R. Milstein, Gary Holbein, Joh McDonald, Ronald Reed, and Harold G. Petering
pp 131 - 135; DOI:
10.1021/jm00223a023
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Copper chelates as possible active forms of the antiarthritic agents
John R. J. Sorenson
pp 135 - 148; DOI:
10.1021/jm00223a024
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Podophyllotoxin analogs. 1. Synthesis and biological evaluation of certain trans-2-aryl-trans-6-hydroxymethyl-3-cyclohexenecarboxylic acid .gamma.-lactones as antimitotic agents
Edward E. Smissman, Robert J. Murray, James D. McChesney, L. L. Houston, and Thomas L. Pazdernik
pp 148 - 153; DOI:
10.1021/jm00223a025
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Stereochemical analogs of a muscarinic, ganglionic stimulant. 2. The cis and trans olefinic, epoxide, and cyclopropane analogs related to 4-[N-(3-chlorophenyl)carbamoyloxy]-2-butynyltrimethylammonium chloride
W. L. Nelson, D. S. Freeman, and F. F. Vincenzi
pp 153 - 158; DOI:
10.1021/jm00223a026
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Stereochemical analogs of a muscarinic, ganglionic stimulant. 3. 2,3-Substituted bicyclo[2.2.1]hept-5-enes and -heptanes related to 4-[N-(3-chlorophenyl)carbamoyloxy]-2-butynyltrimethylammonium chloride
W. L. Nelson, D. S. Freeman, and F. F. Vincenzi
pp 159 - 160; DOI:
10.1021/jm00223a027
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Specificity in enzyme inhibition. 3. Synthesis of 5-substituted-2,2-dimethyl-4-imidazolidinones as inhibitors of tyrosine decarboxylase and histidine decarboxylase
Edward E. Smissman, Roger L. Inloes, Samir El-Antably, and Phyllis J. Shaffer
pp 161 - 163; DOI:
10.1021/jm00223a028
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Synthesis and evaluation of brain catecholamine depletion by N-alkyl derivatives of 6-aminodopamine
Donald E. Nerland and Edward E. Smissman
pp 163 - 164; DOI:
10.1021/jm00223a029
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Synthesis of inhibitors of bacterial cell wall biogenesis. Analogs of D-alanyl-D-alanine
Edward E. Smissman, Atsusuke Terada, and Samir El-Antably
pp 165 - 167; DOI:
10.1021/jm00223a030
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Synthesis and in vitro evaluation of 8-hydroxyquinoline analogs as inhibitors of dental plaque
Victor D. Warner, Jayant N. Sane, Dale B. Mirth, Samuel S. Turesky, and Barbara Soloway
pp 167 - 169; DOI:
10.1021/jm00223a031
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Difference in antimalarial activity between certain amino alcohol diastereomers
Ping-Lu Chien and C. C. Cheng
pp 170 - 172; DOI:
10.1021/jm00223a032
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Synthesis and antiinflammatory properties of N-substituted 4,5-dioxopyrrolidine-3-carboxanilides
Saul B. Kadin
pp 172 - 173; DOI:
10.1021/jm00223a033
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Effect of aromatic nitro compounds on oxidative metabolism by cytochrome P-450 dependent enzymes
Larry A. Sternson and Richard E. Gammans
pp 174 - 177; DOI:
10.1021/jm00223a034
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Intracyclization rates of 6-hydroxydopamine and 6-aminodopamine analogs under physiological conditions
C. L. Blank, Richard L. McCreery, R. M. Wightman, W. Chey, Ralph N. Adams, J. R. Reid, and Edward E. Smissman
pp 178 - 180; DOI:
10.1021/jm00223a035
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Stereochemical studies of adrenergic drugs. Diastereomeric 2-amino-1-phenylcyclobutanols
Duane D. Miller, Fu-Lian Hsu, Kadhim N. Salman, and Popat N. Patil
pp 180 - 184; DOI:
10.1021/jm00223a036
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7-Aza analogs of the analgetic agent azabicyclane. Synthesis and pharmacologic analysis
Edward E. Smissman and Peter C. Ruenitz
pp 184 - 186; DOI:
10.1021/jm00223a037
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Adamantanamine derivatives. Antimicrobial activities of certain Mannich bases
Robert A. Magarian and William G. Sorenson
pp 186 - 189; DOI:
10.1021/jm00223a038
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2,3-Dihydroxyphenethanolamine as an adrenergic agent
R. Martin Bartholow and Edward J. Walaszek
pp 189 - 190; DOI:
10.1021/jm00223a039
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Amino acids. 1. .alpha.-Hydroxymethylphenylalanines
Richard A. Schnettler, John T. Suh, and Richard C. Dage
pp 191 - 192; DOI:
10.1021/jm00223a040
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Central nervous system depressants. 13. s-Triazolo-1,5-benzodiazepin-5-ones
Robert B. Moffett, Bharat V. Kamdar, and P. F. Von Voigtlander
pp 192 - 193; DOI:
10.1021/jm00223a041
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Synthesis of 5-substituted uracil derivatives
Eric C. Ressner, Phillip Fraher, Marshall S. Edelman, and Mathias P. Mertes
pp 194 - 196; DOI:
10.1021/jm00223a042
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S-aristeromycinyl-L-homocysteine, a potent inhibitor of S-adenosylmethionine-dependent transmethylations
Ronald T. Borchardt and Yih-Shiong Wu
pp 197 - 198; DOI:
10.1021/jm00223a043
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Issue 2


Inhibitors of the luteinizing hormone-releasing hormone based upon modifications in the 2, 3, and 6 positions
Yieh-Ping Wan, John Humphries, George Fisher, Karl Folkers, and Cyril Y. Bowers
pp 199 - 202; DOI:
10.1021/jm00224a001
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Synthesis and evaluation of 1,.omega.-diaryl-1,.omega.-alkanediamines related to the fibrinolytic bis(tetrahydroisoquinolines) and bis(benzylamines)
Leonard J. Fliedner, Melvyn J. Myers, Joseph M. Schor, and Irwin J. Pachter
pp 202 - 208; DOI:
10.1021/jm00224a002
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Basic derivatives of 6,7-dihydroindolo[1,7-ab][1]benzazepine and 6H-indolo[7,1-cd][1,5]benzoxazepine as potential antidepressant agents
Luciano Toscano, Giampiero Grisanti, Giuseppe Fioriello, Ennio Seghetti, Alberto Bianchetti, Giuseppe Bossoni, and Mario Riva
pp 208 - 213; DOI:
10.1021/jm00224a003
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Preparation and in vitro antifungal activities of some quinolizidine derived hemiaminals and .beta.-tert-amino sulfides
Robert T. LaLonde, Amy I. M. Tsai, Chun Juan Wang, Chunfook Wong, and Gigi Lee
pp 214 - 219; DOI:
10.1021/jm00224a004
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Cycloalkanones. 8. Hypocholesterolemic activity of long-chain ketones related to pentadecanone
Steven D. Wyrick, Iris H. Hall, Claude Piantadosi, and Charles R. Fenske
pp 219 - 222; DOI:
10.1021/jm00224a005
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Hypocholesterolemic activity of 1,3-bis(substituted phenoxy)-2-propanones
Claude Piantadosi, Iris H. Hall, Steven D. Wyrick, and Khalid S. Ishaq
pp 222 - 229; DOI:
10.1021/jm00224a006
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Novel pyrazolo, isoxazolo, and thiazolo steroidal systems and model analogs containing dimethoxylaryl (or dihydroxylaryl) groups and derivatives. Synthesis, spectral properties, and biological activity
M. M. Hashem, K. D. Berlin, R. W. Chesnut, and N. N. Durham
pp 229 - 239; DOI:
10.1021/jm00224a007
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Synthesis and structure-activity relations of heterocyclic compounds containing a trimethoxyarene function
E. A. Mawdsley, K. D. Berlin, R. W. Chesnut, and N. N. Durham
pp 239 - 243; DOI:
10.1021/jm00224a008
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Synthesis of angiotensin II antagonists containing N- and O-methylated and other amino acid residues
M. C. Khosla, H. Munoz-Ramirez, M. M. Hall, R. R. Smeby, P. A. Khairallah, F. M. Bumpus, and M. J. Peach
pp 244 - 250; DOI:
10.1021/jm00224a009
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Synthesis and some pharmacological properties of five analogs of oxytocin having L-homocysteine in position 6
Clark W. Smith and Martha F. Ferger
pp 250 - 254; DOI:
10.1021/jm00224a010
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Synthesis and biological inactivity of some 4.alpha.,6-cyclo steroids
F. Thomas Bond, Walter Weyler, Bernard Brunner, and Jeffrey E. Stemke
pp 255 - 259; DOI:
10.1021/jm00224a011
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Synthesis and pharmacology of 2,9.alpha.-dimethyl-2'-hydroxy-6,7-benzomorphan
Hirozumi Inoue and Everette L. May
pp 259 - 262; DOI:
10.1021/jm00224a012
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Interferon inducing activities of derivatives of 1,3-dimethyl-4-(3-dimethylaminopropylamino)-1H-pyrazolo[3,4-b]quinoline and related compounds
R. R. Crenshaw, George M. Luke, and Paul Siminoff
pp 262 - 275; DOI:
10.1021/jm00224a013
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Antifertility agents. 12. Structure-activity relation of 3,4-diphenylchromenes and -chromans
Suprabhat Ray, Payara K. Grover, Ved P. Kamboj, B. S. Setty, Amiya B. Kar, and Nitya Anand
pp 276 - 279; DOI:
10.1021/jm00224a014
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Relation of molecular structure to in vivo scintigraphic distribution patterns of carbon-11-labeled compounds. 3. Carbon-11-labeled hydantoins
Meldrum B. Winstead, Shelley J. Parr, Michael J. Rogal, Paul S. Brockman, Ronald Lubcher, Archie Khentigan, Tz-Hong Lin, James F. Lamb, and H. Saul Winchell
pp 279 - 286; DOI:
10.1021/jm00224a015
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Synthesis of tetrazole ribonucleosides and their evaluation as antiviral agents
Mohindar S. Poonian, Eugene F. Nowoswiat, John F. Blount, Thomas H. Williams, Ross G. Pitcher, and Michael J. Kramer
pp 286 - 290; DOI:
10.1021/jm00224a016
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Synthesis and enzymic activity of some novel xanthine oxidase inhibitors. 3-Substituted 5,7-dihydroxypyrazolo[1,5-a]pyrimidines
Robert H. Springer, Mary K. Dimmitt, Thomas Novinson, Darrell E. O'Brien, Roland K. Robins, Lionel N. Simon, and Jon P. Miller
pp 291 - 296; DOI:
10.1021/jm00224a017
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Immobilized glucuronosyltransferase for the synthesis of conjugates
Indu Parikh, Donald W. MacGlashan, and Catherine Fenselau
pp 296 - 299; DOI:
10.1021/jm00224a018
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Chemistry and biological activities of N,N-dimethylaminoethyl acrylate, a choline acetyltransferase inhibitor
Peter P. Rowell and C. Y. Chiou
pp 300 - 303; DOI:
10.1021/jm00224a019
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Antiinflammatory activity of some 2,3-dihydrobenzofuran-5-acetic acids and related compounds
Noriyasu Hirose, Shizuo Kuriyama, Yoshinori Kato, and Shoji Toyoshima
pp 303 - 308; DOI:
10.1021/jm00224a020
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Potential antitumor agents. Synthesis of bifunctional .alpha.-methylene-.gamma.-butyrolactones
Gary A. Howie, Ioannis K. Stamos, and John M. Cassady
pp 309 - 313; DOI:
10.1021/jm00224a021
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Potential central nervous system antitumor agents. Aziridinylbenzoquinones. 1
A. Hameed Khan and John S. Driscoll
pp 313 - 317; DOI:
10.1021/jm00224a022
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Carboxyarylindoles as nonsteroidal antiinflammatory agents
V. Brian Anderson, Marc N. Agnew, Richard C. Allen, Jeffrey C. Wilker, Howard B. Lassman, and William J. Novick
pp 318 - 325; DOI:
10.1021/jm00224a023
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Hypothalamic hormones. 71. Synthesis and some biological activities of the tyrosine-8 analog of substance P
George H. Fisher, Karl Folkers, Bengt Pernow, and Cyril Y. Bowers
pp 325 - 328; DOI:
10.1021/jm00224a024
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Synthetic metabolites of neurohypophyseal hormones. [Des-9-glycinamide]oxytocin and [des-9-glycinamide,des-8-leucine]oxytocin
Roderich Walter, Robert T. Havran, and I. L. Schwartz
pp 328 - 330; DOI:
10.1021/jm00224a025
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.beta.-Lactam antibiotics with N-oxide side chains. 1. Quinoxaline N-oxides
M. L. Edwards, R. E. Bambury, and H. W. Ritter
pp 330 - 333; DOI:
10.1021/jm00224a026
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Synthesis and pharmacological evaluation of some 3-substituted octahydropyrido[2,1-c][1,4]oxazines
Thomas N. Riley and Gary O. Rankin
pp 334 - 336; DOI:
10.1021/jm00224a027
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Synthesis of N-hydroxythiourea
Masayuki Sato and Charles H. Stammer
pp 336 - 337; DOI:
10.1021/jm00224a028
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Substituted naphthazarins as potential anticancer agents
Kenneth D. Paull, Robert K. Y. Zee-Cheng, and C. C. Cheng
pp 337 - 339; DOI:
10.1021/jm00224a029
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Inhibition of tumor cell transplantability by iron and copper complexes of 5-substituted 2-formylpyridine thiosemicarbazones
William E. Antholine, Judith M. Knight, and David H. Petering
pp 339 - 341; DOI:
10.1021/jm00224a030
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Racemic diastereoisomers of 1-amino-2-hydroxycyclopentanecarboxylic acid
Dimitri E. Gaitanopoulos, James Nash, Danny L. Dunn, and Charles G. Skinner
pp 342 - 344; DOI:
10.1021/jm00224a031
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Synthesis of 5-substituted aminomethyluracils via the Mannich reaction
Thomas J. Delia, John P. Scovill, William D. Munslow, and Joseph H. Burckhalter
pp 344 - 346; DOI:
10.1021/jm00224a032
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Products from furans. 1. Synthesis and anticoccidial and antimicrobial activity of 5-amino-5,6-dihydro-6-methoxy-2-methyl-2-(4'-biphenylyl)-2H-pyran-3(4H)-ones and related compounds
Minas P. Georgiadis
pp 346 - 349; DOI:
10.1021/jm00224a033
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Anthelmintic 1-cinnamamido-2,4-imidazolidinediones
Robert J. Alaimo and Christopher J. Hatton
pp 349 - 350; DOI:
10.1021/jm00224a034
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Book Reviews

pp 350 - 352; DOI:
10.1021/jm00224a600
PDF

Issue 3


Synthesis of a potential water-soluble radiographic contrast medium, 2,4,6-triiodo-3-acetamido-5-N-methylcarboxamidophenyl .beta.-D-glucopyranoside
F. L. Weitl, M. Sovak, and M. Ohno
pp 353 - 356; DOI:
10.1021/jm00225a001
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Radiopharmaceuticals. 16. Halogenated dopamine analogs. Synthesis and radiolabeling of 6-iododopamine and tissue distribution studies in animals
J. S. Fowler, R. R. MacGregor, A. P. Wolf, A. N. Ansari, and H. L. Atkins
pp 356 - 360; DOI:
10.1021/jm00225a002
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Antimalarials. 8. Synthesis of amino ethers as candidate antimalarials
M. P. LaMontagne, M. S. Ao, A. Markovac, and J. R. Menke
pp 360 - 365; DOI:
10.1021/jm00225a003
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Hypoglycemic .alpha.-cycloalkylphenylmethyl, furanalkyl, and thiophenealkyl lactamimides
J. Martin Grisar, George P. Claxton, and Norbert L. Wiech
pp 365 - 369; DOI:
10.1021/jm00225a004
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Synthesis and biological activity of new 2-substituted analogs of fluphenazine
Paul C. Bossle, C. Parker Ferguson, Walter E. Sultan, Willard J. Lennox, Gaston E. Dudley, Thomas H. Rea, and Jacob I. Miller
pp 370 - 373; DOI:
10.1021/jm00225a005
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Synthesis and biological activity of camel and bovine .beta.-melanotropins
Simon Lemaire, Donald Yamashiro, and Choh Hao Li
pp 373 - 376; DOI:
10.1021/jm00225a006
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Synthesis and some pharmacological properties of [1-(L-2-hydroxy-3-mercaptopropanoic acid),4-threonine]oxytocin (hydroxy[4-thr]oxytocin), a peptide with strikingly high oxytocic potency, and of [1-(L-2-hydroxy-3-mercaptopropanoic acid)]oxytocin (hydroxy-oxytocin)
Maurice Manning, John Lowbridge, Jaya Haldar, and Wilbur H. Sawyer
pp 376 - 380; DOI:
10.1021/jm00225a007
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Structure-activity relation of daunorubicin and its peptide derivatives
David W. Wilson, Douglas Grier, Ronald Reimer, Jeffrey D. Bauman, James F. Preston, and Edmond J. Gabbay
pp 381 - 384; DOI:
10.1021/jm00225a008
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Physicochemical and pharmacological studies of some 8-substituted decahydroisoquinolines
Ian W. Mathison, Phillip H. Morgan, Norbert J. Wojciechowski, Jack P. Bandura, and James R. Wennemark
pp 385 - 391; DOI:
10.1021/jm00225a009
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Etodolic acid and related compounds. Chemistry and antiinflammatory actions of some potent di- and trisubstituted 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acids
Christopher A. Demerson, Leslie G. Humber, Adolph H. Philipp, and Rene R. Martel
pp 391 - 395; DOI:
10.1021/jm00225a010
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Adriamycin analogs. Periodate oxidation of adriamycin
George Tong, William W. Lee, Douglas R. Black, and David W. Henry
pp 395 - 398; DOI:
10.1021/jm00225a011
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New series of cardioselective adrenergic .beta.-receptor blocking compounds. 1-(2-Acyl-4-acylaminophenoxy)-3-isopropylaminopropan-2-ols
B. Basil, J. R. Clark, E. C. J. Coffee, R. Jordan, A. H. Loveless, D. L. Pain, and K. R. H. Wooldridge
pp 399 - 402; DOI:
10.1021/jm00225a012
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Aminobenzoic acid diuretics. 8. 3,4-Disubstituted 5-methylsulfonylbenzoic acids and related compounds
Peter W. Feit and Ole B. Tvaermose Nielsen
pp 402 - 406; DOI:
10.1021/jm00225a013
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Antimalarials. 11. 2-Vinylogs of substituted 2-aryl-4-quinoline amino alcohols
Robert E. Lutz and J. Milton Sanders
pp 407 - 410; DOI:
10.1021/jm00225a014
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Conformational influence of a 19-methyl substituent in 19-oxygenated steroid structures
Douglas C. Rohrer, Charles M. Weeks, Yoshio Osawa, and William L. Duax
pp 410 - 414; DOI:
10.1021/jm00225a015
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Contraceptive agents from cycloaddition reactions of diarylcyclopropenones and diarylthiirene 1,1-dioxides
Melvin H. Rosen, Ingrid Fengler, Georgina Bonet, Thomas Giannina, Margaret C. Butler, Fred R. Popick, and Bernard G. Steinetz
pp 414 - 419; DOI:
10.1021/jm00225a016
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Synthesis of some 1,8- and 2,8-disubstituted derivatives of adenosine cyclic 3',5'-phosphate and their interaction with some enzymes of cAMP metabolism
Hitoshi Uno, Rich B. Meyer, Dennis A. Shuman, Roland K. Robins, Lionel N. Simon, and Jon P. Miller
pp 419 - 422; DOI:
10.1021/jm00225a017
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Analogs of luteinizing hormone-releasing hormone with increased biological activity produced by D-amino acid substitutions in position 6
David H. Coy, Jesus A. Vilchez-Martinez, Esther J. Coy, and Andrew V. Schally
pp 423 - 425; DOI:
10.1021/jm00225a018
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Synthesis of the antileukemic compound N,N''-[5-[bis(2-chloroethyl)amino]-1,3-phenylene]bisurea
George H. Denny, Malcolm A. Ryder, Anthony M. De Marco, and Robert D. Babson
pp 426 - 428; DOI:
10.1021/jm00225a019
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Synthesis and microbiological activities of .beta.-(1-chloro-2-naphthyl)alanine and .beta.-(1-bromo-2-naphthyl)alanine
Tommy J. McCord, Richard N. Watson, Clifton E. DuBose, Karen L. Hulme, and Alvie L. Davis
pp 429 - 430; DOI:
10.1021/jm00225a020
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Optical resolution of (+-)-2,5-dimethyl-2'-hydroxy-9.alpha.- and -9.beta.-propyl-6,7-benzomorphans and their pharmacological properties
Kenner C. Rice and Arthur E. Jacobson
pp 430 - 432; DOI:
10.1021/jm00225a021
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Structure and antitumor activity relation of 2-arylidene-4-cyclopentene-1,3-diones and 2-arylideneindan-1,3-diones
Seiichi Inayama, Katsuhiro Mamoto, Tetsuichi Shibata, and Tadaaki Hirose
pp 433 - 436; DOI:
10.1021/jm00225a022
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Synthesis and central nervous system depressant activity of some bicyclic amides
Paul Aeberli, John H. Gogerty, William J. Houlihan, and Louis C. Iorio
pp 436 - 438; DOI:
10.1021/jm00225a023
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Potentiation of the estrogenic activity of stilbestrol by spiro(cyclohexane-1,2'-indan)-1',4-dione
David J. Bailey, Neil S. Doggett, Lai Yin Ng, and Tariq Qazi
pp 438 - 439; DOI:
10.1021/jm00225a024
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Book Reviews

pp 439 - 444; DOI:
10.1021/jm00225a600
PDF

Issue 4


Drugs derived from cannabinoids. 1. Nitrogen analogs, benzopyranopyridines and benzopyranopyrroles
Harry G. Pars, Felix E. Granchelli, Raj K. Razdan, Jacqueline K. Keller, David G. Teiger, Franklin J. Rosenberg, and Louis S. Harris
pp 445 - 454; DOI:
10.1021/jm00226a001
PDF
Drugs derived from cannabinoids. 2. Basic esters of nitrogen and carbocyclic analogs
Raj K. Razdan, B. Zitko Terris, Harry G. Pars, Nicholas P. Plotnikoff, Patrick W. Dodge, Anthony T. Dren, Jaroslav Kyncl, and Peter Somani
pp 454 - 461; DOI:
10.1021/jm00226a002
PDF
Drugs derived from cannabinoids. 5. .DELTA.6a,10a,-Tetrahydrocannabinol and heterocyclic analogs containing aromatic side chains
Martin Winn, David Arendsen, Patrick W. Dodge, Anthony Dren, Daniel Dunnigan, Robert Hallas, Kao Hwang, Jaroslav Kyncl, Yien-Hwei Lee, and et al.
pp 461 - 471; DOI:
10.1021/jm00226a003
PDF
Monoquaternary neuromuscular blocking agents based on 1-tetralone and 1-indanone
D. F. Biggs, A. F. Casy, Ih Chu, and R. T. Coutts
pp 472 - 475; DOI:
10.1021/jm00226a004
PDF
Analgesic agents. 3. New bridged aminotetralins
Meier E. Freed, John R. Potoski, Elisabeth H. Freed, George L. Conklin, and Stanley C. Bell
pp 476 - 480; DOI:
10.1021/jm00226a005
PDF
Azaparacyclophanes. Novel class of conformationally rigid analogs of phenylethylamine and phenylpropylamine
Kent E. Opheim, Adolph P. Roszkowski, Marshall B. Wallach, and Ian T. Harrison
pp 480 - 483; DOI:
10.1021/jm00226a006
PDF
Mode of action and quantitative structure-activity correlations of tuberculostatic drugs of the isonicotinic acid hydrazide type
Joachim K. Seydel, Klaus J. Schaper, Ellen Wempe, and Hans P. Cordes
pp 483 - 492; DOI:
10.1021/jm00226a007
PDF
Structure-activity relationships in luteinizing hormone-releasing hormone
Kari U. Prasad, Roger W. Roeske, Frederick L. Weitl, Jesus A. Vilchez-Martinez, and Andrew V. Schally
pp 492 - 495; DOI:
10.1021/jm00226a008
PDF
Synthesis and antiviral activity of 5- and 5'-substituted thymidine analogs
Tai-Shun Lin, John P. Neenan, Yung-Chi Cheng, William H. Prusoff, and David C. Ward
pp 495 - 498; DOI:
10.1021/jm00226a009
PDF
Inhibition of separated forms of phosphodiesterases from pig coronary arteries by uracils and by 7-substituted derivatives of 1-methyl-3-isobutylxanthine
J. E. Garst, G. L. Kramer, Y. J. Wu, and J. N. Wells
pp 499 - 503; DOI:
10.1021/jm00226a010
PDF
Substituted .alpha.-methylbenzyl and tricyclic arylalkyl lactamimides as inhibitors of blood platelet aggregation
J. Martin Grisar, George P. Claxton, and Robert D. MacKenzie
pp 503 - 508; DOI:
10.1021/jm00226a011
PDF
Central nervous system active 5-oxo-1,4,5,6,7,8-hexahydrocinnolines
Kuppuswamy Nagarajan, Joy David, and Rashmi K. Shah
pp 508 - 511; DOI:
10.1021/jm00226a012
PDF
Novel heterocyclic nitrofurfural hydrazones. In vivo antitrypanosomal activity
Thomas Novinson, Bharat Bhooshan, Takayuki Okabe, Ganapathi R. Revankar, Roland K. Robins, Keitaro Senga, and H. Robert Wilson
pp 512 - 516; DOI:
10.1021/jm00226a013
PDF
Synthesis and antimicrobial activity of some novel heterocycles. Azolo-as-triazines
Thomas Novinson, Takayuki Okabe, Roland K. Robins, and Thomas R. Matthews
pp 517 - 520; DOI:
10.1021/jm00226a014
PDF
Circular dichroism and carbon-13 nuclear magnetic resonance spectra of (S)-5-alkyl-5-(2'-pentyl)-2-thiobarbituric acids
Frank I. Carroll, Abraham Philip, and Charles G. Moreland
pp 521 - 524; DOI:
10.1021/jm00226a015
PDF
Syntheses of heterocyclic fused thiazole acetic acids. 2
Stanley C. Bell and Peter H. L. Wei
pp 524 - 530; DOI:
10.1021/jm00226a016
PDF
(Vinylaryloxy)acetic acids. A new class of diuretic agents. 1. (Diacylvinylaryloxy)acetic acids
John B. Bicking, Wilbur J. Holtz, L. Sherman Watson, and Edward J. Cragoe
pp 530 - 535; DOI:
10.1021/jm00226a017
PDF
Biologically active polycycloalkanes. 2. Antiviral 4-homoisotwistane derivatives
Koji Aigami, Yoshiaki Inamoto, Naotake Takaishi, Yoshiaki Fujikura, Akira Takatsuki, and Gakuzo Tamura
pp 536 - 540; DOI:
10.1021/jm00226a018
PDF
Local anesthetics. 2-Diethylamino-2',6'-acylxylidides
Sigmund M. Waraszkiewicz, William O. Foye, H. Jack Adams, and Bertil H. Takman
pp 541 - 544; DOI:
10.1021/jm00226a019
PDF
(Vinylaryloxy)acetic acids. A new class of diuretic agents. 2. [4-(3-Oxo-1-alkenyl)phenoxy]acetic acids
John B. Bicking, Charles M. Robb, L. Sherman Watson, and Edward J. Cragoe
pp 544 - 547; DOI:
10.1021/jm00226a020
PDF
Synthesis and dopaminergic activity of (+-)-, (+)-, and (-)-2-dipropylamino-5-hydroxy-1,2,3,4-tetrahydronaphthalene
John D. McDermed, Gerald M. McKenzie, and Harold S. Freeman
pp 547 - 549; DOI:
10.1021/jm00226a021
PDF
Drugs derived from cannabinoids. 3. Sulfur analogs, thiopyranobenzopyrans and thienobenzopyrans
Raj K. Razdan, B. Zitko Terris, G. R. Handrick, Haldean C. Dalzell, H. G. Pars, J. F. Howes, Nicholas P. Plotnikoff, Patrick W. Dodge, Anthony T. Dren, and et al.
pp 549 - 551; DOI:
10.1021/jm00226a022
PDF
Drugs derived from cannabinoids. 4. Effect of alkyl substitution in sulfur and carbocyclic analogs
Raj K. Razdan, G. R. Handrick, Haldean C. Dalzell, J. F. Howes, Martin Winn, Nicholas P. Plotnikoff, Patrick W. Dodge, and Anthony T. Dren
pp 552 - 554; DOI:
10.1021/jm00226a023
PDF
Synthesis and biological activities of some N4-substituted 4-aminopyrazolo[3,4-d]pyrimidines
C. I. Hong, N. C. De, G. L. Tritsch, and G. B. Chheda
pp 555 - 558; DOI:
10.1021/jm00226a024
PDF
Catechol O-methyltransferase. 8. Structure-activity relationships for inhibition by 8-hydroxyquinolines
Ronald T. Borchardt, Dhiren R. Thakker, Victor D. Warner, Dale B. Mirth, and Jayant N. Sane
pp 558 - 560; DOI:
10.1021/jm00226a025
PDF
Bridged aminotetralins. 4. Resolution of potent analgesics of the bridged aminotetralin type
Meier E. Freed, John R. Potoski, George L. Conklin, and Stanley C. Bell
pp 560 - 562; DOI:
10.1021/jm00226a026
PDF
3-Cyanocephems and carbon-13 heterocyclic-substituted cephems via 1,3-dipolar cycloadditions
John L. Fahey, Raymond A. Firestone, and B. G. Christensen
pp 562 - 565; DOI:
10.1021/jm00226a027
PDF
Book Reviews

pp 565 - 568; DOI:
10.1021/jm00226a600
PDF
Correction - Ergoline Congeners as Potential Inhibitors of Prolactin Release. 2.
D. B. Rusterholz, C. F .Barfknecht, and J. A. Clemens
pp 568 - 568; DOI:
10.1021/jm00226a601
PDF

Issue 5


Application of SCAP to drug design. 1. Prediction of octanol-water partition coefficients using solvent-dependent conformational analyses
Anton J. Hopfinger and Robert D. Battershell
pp 569 - 573; DOI:
10.1021/jm00227a001
PDF
Molecular connectivity. 6. Examination of the parabolic relationship between molecular connectivity and biological activity
Wallace J. Murray, Lemont B. Kier, and Lowell H. Hall
pp 573 - 578; DOI:
10.1021/jm00227a002
PDF
Quantitative structure-activity relationships. 1. The modified Free-Wilson approach
Hugo Kubinyi and Ott H. Kehrhahn
pp 578 - 586; DOI:
10.1021/jm00227a003
PDF
Quantitative structure-activity relationships. 2. A mixed approach, based on Hansch and Free-Wilson analysis
Hugo Kubinyi
pp 587 - 600; DOI:
10.1021/jm00227a004
PDF
Quantitative structure-activity studies on monoamine oxidase inhibitors
Carl Lynn Johnson
pp 600 - 605; DOI:
10.1021/jm00227a005
PDF
Inhibition of dihydrofolate reductase. Structure-activity correlations of quinazolines
James Y. Fukunaga, Corwin Hansch, and Edward E. Steller
pp 605 - 611; DOI:
10.1021/jm00227a006
PDF
Dependence of hydrophobicity of apolar molecules on their molecular volume
A. Leo, Corwin Hansch, and Priscilla Y. C. Jow
pp 611 - 615; DOI:
10.1021/jm00227a007
PDF
Direct measurement of octanol-water partition coefficients by high-pressure liquid chromatography
Margaret S. Mirrlees, Stuart J Moulton, Christopher T. Murphy, and Peter J. Taylor
pp 615 - 619; DOI:
10.1021/jm00227a008
PDF
Use of high-pressure liquid chromatography for quantitative structure-activity relationship studies of sulfonamides and barbiturates
Doug Henry, John H. Block, John L. Anderson, and Garnet R. Carlson
pp 619 - 626; DOI:
10.1021/jm00227a009
PDF
Adrenergic sulfonanilides. 4. Centrally active .beta.-adrenergic agonists
D. L. Temple, W. T. Comer, H. C. Ferguson, and L. E. Allen
pp 626 - 633; DOI:
10.1021/jm00227a010
PDF
Novel bis(benzamidino) compounds with an aromatic central link. Inhibitors of thrombin, pancreatic kallikrein, trypsin, and complement
J. D. Geratz, M. C. F. Cheng, and R. R. Tidwell
pp 634 - 639; DOI:
10.1021/jm00227a011
PDF
Synthesis and anticancer activity of 5-diethylaminomethyl derivatives and nitrogen mustards of uracil and 2-thiouracils
Silvio Fabrissin, Marilena De Nardo, Carlo Nisi, Ersilia Dolfini, Giuseppe Franchi, and Luciano Morasca
pp 639 - 642; DOI:
10.1021/jm00227a012
PDF
Synthesis and biological studies of 3-(.beta.-D-ribofuranosyl)-2,3-dihydro-6H-1,3-oxazine-2,6-dione, a new pyrimidine nucleoside analog related to uridine
Tek-Ling Chwang, William F. Wood, J. Rodney Parkhurst, Stephen Nesnow, Peter V. Danenberg, and Charles Heidelberger
pp 643 - 647; DOI:
10.1021/jm00227a013
PDF
Metabolic formation and synthesis of 1-(3-chlorophenyl)-2-(4-hydroxyphenyl)-1-methyl-2-(2-pyridine)ethanol. A potential hypocholesteremic agent
J. E. Sinsheimer, E. Van den Eeckhout, L. E. Hewitt, Y. Kido, D. R. Wade, D. W. Hansen, J. C. Drach, and J. H. Burckhalter
pp 647 - 650; DOI:
10.1021/jm00227a014
PDF
Cellular pharmacodynamics of several anthracycline antibiotics
Nicholas R. Bachur, Malcolm Steele, W. Delano Meriwether, and Robert C. Hildebrand
pp 651 - 654; DOI:
10.1021/jm00227a015
PDF
Reactions of 2-acyloxyisobutyryl halides with nucleosides. 6. Synthesis and biological evaluation of some 3'-acyl derivatives of 2,2'-anhydro-1-(.beta.-D-arabinofuranosyl)cytosine hydrochloride
Ernest K. Hamamura, Miroslav Prystasz, Julien P. H. Verheyden, John G. Moffatt, Kenji Yamaguchi, Naomi Uchida, Kosaburo Sato, Akio Nomura, Osamu Shiratori, and et al.
pp 654 - 662; DOI:
10.1021/jm00227a016
PDF
Reactions of 2-acyloxyisobutyryl halides with nucleosides. 7. Synthesis and biological evaluation of some 2,2'-anhydro-1-(3',5'-di-O-acyl-.beta.-D-arabinofuranosyl)cytosine hydrochlorides
Ernest K. Hamamura, Miroslav Prystasz, Julien P. H. Verheyden, John G. Moffatt, Kenji Yamaguchi, Naomi Uchida, Kosaburo Sato, Akio Nomura, Osamu Shiratori, and et al.
pp 663 - 667; DOI:
10.1021/jm00227a017
PDF
Reactions of 2-acyloxyisobutyryl halides with nucleosides. 8. Synthesis and biological evaluation of some 3'-acyl and 3',5'-diacyl derivatives of 1-.beta.-D-arabinofuranosylcytosine
Ernest K. Hamamura, Miroslav Prystasz, Julien P. H. Verheyden, John G. Moffatt, Kenji Yamaguchi, Naomi Uchida, Kosaburo Sato, Akio Nomura, Osamu Shiratori, and et al.
pp 667 - 674; DOI:
10.1021/jm00227a018
PDF
Experiments on the synthesis of dl-camptothecin. 4. Synthesis and antileukemic activity of dl-camptothecin analogues
Tsutomu Sugasawa, Tatsuo Toyoda, Naomi Uchida, and Kenji Yamaguchi
pp 675 - 679; DOI:
10.1021/jm00227a019
PDF
Solid-phase synthesis and drug glucuronides by immobilized glucuronosyltransferase
Catherine Fenselau, Sharon Pallante, and Indu Parikh
pp 679 - 683; DOI:
10.1021/jm00227a020
PDF
Analogues of S-adenosylhomocysteine as potential inhibitors of biological transmethylation. Synthesis of analogues with modifications at the 5'-thioether linkage
Chi-Deu Chang and James K. Coward
pp 684 - 691; DOI:
10.1021/jm00227a021
PDF
Conformations and "nicotinic" activities of cyclic analogues of choline aryl ether
E. R. Clark, I. E. Hughes, and C. F. C. Smith
pp 692 - 695; DOI:
10.1021/jm00227a022
PDF
Sulfamylurea hypoglycemic agents. 6. High-potency derivatives
Reinhard Sarges, Donald E. Kuhla, Hans E. Wiedermann, and Dale A. Mayhew
pp 695 - 709; DOI:
10.1021/jm00227a023
PDF
Synthesis and biological evaluation of substituted 2,2'-oxybis(propionic acid) derivatives and related compounds
Gregory B. Bennett, William J. Houlihan, Robert B. Mason, and Robert G. Engstrom
pp 709 - 714; DOI:
10.1021/jm00227a024
PDF
Synthesis and biological activity of a series of 1-aryl-3-pyrazolidinones
Gregory B. Bennett, William J. Houlihan, Robert B. Mason, and J. B. Roach
pp 715 - 717; DOI:
10.1021/jm00227a025
PDF
Diester derivatives as apomorphine prodrugs
Robert J. Borgman, Ross J. Baldessarini, and Kenneth G. Walton
pp 717 - 719; DOI:
10.1021/jm00227a026
PDF
Drugs derived from cannabinoids. 6. Synthesis of cyclic analogues of dimethylheptylpyran
Raj K. Razdan and Haldean C. Dalzell
pp 719 - 721; DOI:
10.1021/jm00227a027
PDF
Preparation of 16.alpha.-alkoxy and 16.alpha.-acyloxy derivatives of 21-chloro-17-acyloxycorticosteroids and determination of their vasoconstrictor activities in humans
Christopher M. Cimarusti, Sam T. Chao, and Leo J. Brannick
pp 721 - 723; DOI:
10.1021/jm00227a028
PDF
Antimalarial activity of some novel derivatives of 2,4-diamino-5-(p-chlorophenyl)-6-ethylpyrimidine (Pyrimethamine)
Richard W. A. Rees, Sie Yearl Chai, Michael W. Winkley, and Peter B. Russell
pp 723 - 725; DOI:
10.1021/jm00227a029
PDF
Conformationally rigid amphetamine analogs as inhibitors of monoamine uptake by brain synaptosomes
Jouko Tuomisto, Leena Tuomisto, and Thomas L. Pazdernik
pp 725 - 727; DOI:
10.1021/jm00227a030
PDF
Partition coefficients and surface areas of some alkylbenzenes
S. H. Yalkowsky and S. C. Valvani
pp 727 - 728; DOI:
10.1021/jm00227a031
PDF
Metabolic and photochemical hydroxylation of 5-nitro-2-furancarboxaldehyde derivatives
Joanne Olivard, Gordon M. Rose, George M. Klein, and James P. Heotis
pp 729 - 731; DOI:
10.1021/jm00227a032
PDF
Stereocontrolled glycosidation of daunomycinone. Synthesis and biological evaluation of 6-hydroxy-L-arabino analogues of antitumor anthracyclines
F. Arcamone, A. Bargiotti, G. Cassinelli, S. Redaelli, S. Hanessian, A. Di Marco, A. M. Casazza, T. Dasdia, A. Necco, and et al.
pp 733 - 734; DOI:
10.1021/jm00227a033
PDF
Antidepressant and Anticonvulsant Activity of 1-(5-Phenyl-4-oxo-2-oxazolin-2-yl)-4-substituted Piperazines
Cheuk-Man Lee, and Nicholas P. Plotnikoff
pp 731 - 733; DOI:
10.1021/jm00227a600
PDF
Book Reviews

pp 735 - 738; DOI:
10.1021/jm00227a601
PDF

Issue 6


Pattern recognition. Classification of therapeutic agents according to pharmacophores
Arthur Cammarata and Govind K. Menon
pp 739 - 748; DOI:
10.1021/jm00228a001
PDF
Quantitative structure-activity relations among steroids. Investigations of the use of steric parameters
Robert A. Coburn and Alan J. Solo
pp 748 - 754; DOI:
10.1021/jm00228a002
PDF
Semisynthetic cephalosporins. Synthesis and structure-activity relations of 7-sulfonylacetamido-3-cephem-4-carboxylic acids
R. M. DeMarinis, J. R. E. Hoover, L. L. Lam, J. V. Uri, J. R. Guarini, L. Phillips, P. Actor, and J. A. Weisbach
pp 754 - 759; DOI:
10.1021/jm00228a003
PDF
Synthesis and structure-toxicity relationships of three new stable analogues of acetyl-seco-hemicholinium-3
Vernon B. Haarstad, Floyd R. Domer, David M. Chihal, Arvind B. Rege, and H. Cecil Charles
pp 760 - 763; DOI:
10.1021/jm00228a004
PDF
Synthesis and biological evaluation of fragmented derivatives of tetrahydroisoquinolines. 3. Trimetoquinol studies
Duane D. Miller, Peter F. Kador, R. Venkatraman, and Dennis R. Feller
pp 763 - 766; DOI:
10.1021/jm00228a005
PDF
Synthesis of actinomycin and analogs. 12. Synthesis and some properties and antitumor effects of the actinomycin lactam analog, [di-(1'-L-.alpha.,.beta.-diaminopropionic acid)]actinomycin D
Stanley Moore, Ravindra P. Patel, Eric Atherton, Michio Kondo, Johannes Meienhofer, Lea Blau, Robert Bittman, and Randall K. Johnson
pp 766 - 772; DOI:
10.1021/jm00228a006
PDF
Potential antitumor agents. 17. 9-Anilino-10-methylacridinium salts
Bruce F. Cain, Graham J. Atwell, and William A. Denny
pp 772 - 777; DOI:
10.1021/jm00228a007
PDF
1-Halobenzyl-1H-indazole-3-carboxylic acids. A new class of antispermatogenic agents
Giorgio Corsi, Giuseppe Palazzo, Claudio Germani, Patrizio Scorza Barcellona, and Bruno Silvestrini
pp 778 - 783; DOI:
10.1021/jm00228a008
PDF
(Vinylaryloxy)acetic acids. A new class of diuretic agents. 3. [(2-Nitro-1-alkenyl)aryloxy]acetic acids
Everett M. Schultz, John B. Bicking, Albert A. Deana, Norman P. Gould, Terence P. Strobaugh, L. Sherman Watson, and Edward J. Cragoe
pp 783 - 787; DOI:
10.1021/jm00228a009
PDF
Cycloalkanoindoles. 1. Syntheses and antiinflammatory actions of some acidic tetrahydrocarbazoles, cyclopentindoles, and cycloheptindoles
Andre A. Asselin, Leslie G. Humber, Thomas A. Dobson, Jacqueline Komlossy, and Rene R. Martel
pp 787 - 792; DOI:
10.1021/jm00228a010
PDF
Cycloalkanoindoles. 2. 1-Alkyl-1,2,3,4-tetrahydrocarbazole-1-ethanamines and related compounds. Potential antidepressants
Andre A. Asselin, Leslie G. Humber, Jacqueline Komlossy, and Marie P. Charest
pp 792 - 797; DOI:
10.1021/jm00228a011
PDF
Biologically oriented organic sulfur chemistry. 14. Antiinflammatory properties of some aryl sulfides, sulfoxides, and sulfones
Lawrence H. Brannigan, Ruth B. Hodge, and Lamar Field
pp 798 - 802; DOI:
10.1021/jm00228a012
PDF
10-Hydroxy-4-methyl-2,3,4,5,6,7-hexahydro-1,6-methano-1H-4-benzazonine derivatives (homobenzomorphans) as analgesics
Shunsaku Shiotani, Tadashi Kometani, Kemmotsu Mitsuhashi, Tsutomu Nozawa, Akira Kurobe, and Osamu Futsukaichi
pp 803 - 806; DOI:
10.1021/jm00228a013
PDF
Synthesis of aziridinyallylaminophosphine oxides and sulfides as potential adjuvant cancer chemotherapeutic agents
K. C. Tsou, D. Bender, N. Santora, L. David, S. Damle, and A. B. Borkovec
pp 806 - 810; DOI:
10.1021/jm00228a014
PDF
Imidazo[1,2-c]pyrimidine nucleosides. Synthesis and biological evaluation of certain 1-(.beta.-D-arabinofuranosyl)imidazo[1,2-c]pyrimidines
David G. Bartholomew, John H. Huffman, Thomas R. Matthews, Roland K. Robins, and Ganapathi R. Revankar
pp 814 - 816; DOI:
10.1021/jm00228a015
PDF
Benzodipyran derivatives with antiallergic activity
John R. Bantick, Hugh Cairns, Albert Chambers, Richard Hazard, John King, Thomas B. Lee, and Robert Minshull
pp 817 - 821; DOI:
10.1021/jm00228a016
PDF
Oxytocin analogues with combined high smooth muscle and negligible antidiuretic activities. Investigation of position 7 in neurohypophyseal hormones
Roderich Walter, Clark W. Smith, J. Roy, and Alice Formento
pp 822 - 825; DOI:
10.1021/jm00228a017
PDF
Folate analogues altered in the C9-N10 bridge region. 10-Oxafolic acid and 10-oxaaminopterin
M. G. Nair and Patricia T. Campbell
pp 825 - 829; DOI:
10.1021/jm00228a018
PDF
Antineoplastic and biochemical properties of arylsulfonylhydrazones of 2-formylpyridine N-oxide
Alan C. Sartorelli, Krishna C. Agrawal, Barbara A. Booth, James Pittman, David G. Bartholomew, and Arthur D. Broom
pp 830 - 833; DOI:
10.1021/jm00228a019
PDF
Esters of N-tert-butylarterenol. Long-acting new bronchodilators with reduced cardiac effects
Benjamin F. Tullar, Hiroaki Minatoya, and Roman R. Lorenz
pp 834 - 838; DOI:
10.1021/jm00228a020
PDF
Synthesis of 1- and 2-substituted indazoles as anthelmintic agents
William D. Kingsbury, Robert J. Gyurik, Vassilios J. Theodorides, Roger C. Parish, and Gregory Gallagher
pp 839 - 840; DOI:
10.1021/jm00228a021
PDF
Synthesis of 1-(4-thio-.beta.-D-ribofuranosyl)-1,2,4-triazole-3-carboxamide
Michael V. Pickering, Joseph T. Witkowski, and Roland K. Robins
pp 841 - 842; DOI:
10.1021/jm00228a022
PDF
Synthesis and some pharmacological properties of deamino[4-threonine,8-D-arginine]vasopressin and deamino[8-D-arginine]vasopressin, highly potent and specific antidiuretic peptides, and [8-D-arginine]vasopressin and deamino-arginine-vasopressin
Maurice Manning, Lajos Balaspiri, Jacqueline Moehring, Jaya Haldar, and Wilbur H. Sawyer
pp 842 - 845; DOI:
10.1021/jm00228a023
PDF
Antimalarials. 3. 1,2,4-Triazines
Louis C. March, Gurdip S. Bajwa, Jessie Lee, Khizar Wasti, and Madeleine M. Joullie
pp 845 - 848; DOI:
10.1021/jm00228a024
PDF
Effect of chain length on critical micelle formation and protein binding of quaternary ammonium compounds
Eric J. Lien and John H. Perrin
pp 849 - 850; DOI:
10.1021/jm00228a025
PDF
A potential amphetamine antagonist, adamantanamine derivative of fluphenazine
Beng T. Ho, Leo F. Englert, and Mary L. McKenna
pp 850 - 852; DOI:
10.1021/jm00228a026
PDF
2-Azabicyclo[2.2.2]octane analogues of the prodine analgetics
C. Randall Clark, John M. Holbrook, and Ronald F. Borne
pp 852 - 854; DOI:
10.1021/jm00228a027
PDF
Biological activity of carbon-terminal partial sequences of substance P
Ross W. Bury and Maurice L. Mashford
pp 854 - 856; DOI:
10.1021/jm00228a028
PDF
Stereospecific interaction of the quaternized opiate, N-methyllevorphanol, with opiate receptors
Kent E. Opheim and Brian M. Cox
pp 857 - 858; DOI:
10.1021/jm00228a029
PDF
Synthesis and Properties of 2-S-[2'-(N,N-Dialkylamino)ethyl]thio-1,3,2-dioxaphosphorinane 2-Oxide and of the Corresponding Quaternary Derivatives as Potential Nontoxic Antiglaucoma Agents
Gavriel Amitai, Yacov Ashani, Yona Grunfeld, Asher Kalir, and Sasson Cohen
pp 810 - 813; DOI:
10.1021/jm00228a600
PDF
Book Reviews

pp 858 - 862; DOI:
10.1021/jm00228a601
PDF

Issue 7


Quantum chemical studies of methadone
Gilda H. Loew, Donald S. Berkowitz, and Richard C. Newth
pp 863 - 869; DOI:
10.1021/jm00229a001
PDF
Structure-activity studies on sulfamate sweeteners
G. Anthony Benson and William J. Spillane
pp 869 - 872; DOI:
10.1021/jm00229a002
PDF
Synthesis and some pharmacological properties of oxytocin analogues having L-thiazolidine-4-carboxylic acid in position 7
James D. Rosamond and Martha F. Ferger
pp 873 - 876; DOI:
10.1021/jm00229a003
PDF
Synthesis and antihypertensive activity of some thienylethanolamines
Jehan F. Bagli, Walter D. Mackay, Eckhardt Ferdinandi, Mitchell N. Cayen, Ivan Vavra, Thomas Pugsley, and Wilbur Lippmann
pp 876 - 882; DOI:
10.1021/jm00229a004
PDF
Tetramethoxydibenzoquinolizinium salts. Preparation and antileukemic activity of some positional and structural isomers of coralyne
Robert K. Y. Zee-Cheng and C. C. Cheng
pp 882 - 886; DOI:
10.1021/jm00229a005
PDF
Synthesis, antimalarial activity, and phototoxicity of some benzo[h]quinoline-4-methanols
Kenner C. Rice, Betty J. Boone, Alan B. Rubin, and T. J. Rauls
pp 887 - 892; DOI:
10.1021/jm00229a006
PDF
Oxindole-3-spiropyrrolidines and -piperidines. Synthesis and local anesthetic activity
Milton J. Kornet and Alan P. Thio
pp 892 - 898; DOI:
10.1021/jm00229a007
PDF
Synthesis of new cyclic nucleotides and their differential stimulatory effects on thyroid function in mice
Georges Cehovic, Monika Bayer, and Nguyen Ba Giao
pp 899 - 903; DOI:
10.1021/jm00229a008
PDF
Synthetic inhibitors of Escherichia coli, calf thymus, and Ehrlich ascites tumor thymidylate synthetase
Arieh Kampf, Roxane L. Barfknecht, Phyllis J. Shaffer, Shigemasa Osaki, and Mathias P. Mertes
pp 903 - 908; DOI:
10.1021/jm00229a009
PDF
Synthesis of 5-substituted 2'-deoxyuridines
Arieh Kampf, Conrad J. Pillar, Warren J. Woodford, and Mathias P. Mertes
pp 909 - 915; DOI:
10.1021/jm00229a010
PDF
Synthesis and biological activities of 5-trifluoromethyl-5'-azido-2',5'-dideoxyuridine and 5-trifluoromethyl-5'-amino-2',5'-dideoxyuridine
Tai-Shun Lin, Caroline Chai, and William H. Prusoff
pp 915 - 918; DOI:
10.1021/jm00229a011
PDF
Alkyl streptozotocin analogues with improved biological activities
Morio Iwasaki, Masaki Ueno, Kenji Ninomiya, Junzo Sekine, Yasuhiro Nagamatsu, and Goro Kimura
pp 918 - 923; DOI:
10.1021/jm00229a012
PDF
Potential histamine H2-receptor antagonists. 3. Methylhistamines
Graham J. Durant, John C. Emmett, C. Robin Ganellin, Anthony M. Roe, and R. Antony Slater
pp 923 - 928; DOI:
10.1021/jm00229a013
PDF
Quaternary pilocarpine derivatives as potential acetylcholine antagonists. 2. Alterations in the lactone and imidazole moieties
Avraham A. Ben-Bassat, David Lavie, Habib Edery, and Gila Porath
pp 928 - 933; DOI:
10.1021/jm00229a014
PDF
Vinyl ethers of choline and congeners
Joseph G. Cannon, Aleem Gangjee, John Paul Long, and Albert John Allen
pp 934 - 937; DOI:
10.1021/jm00229a015
PDF
Analogues of luteinizing hormone releasing factor modified at positions 2, 6, and 10
Nicholas C. Ling, Jean E. Rivier, Michael W. Monahan, and Wylie W. Vale
pp 937 - 941; DOI:
10.1021/jm00229a016
PDF
6,11-Dihydro-11-oxodibenz[b,e]oxepinacetic acids with potent antiinflammatory activity
Katsujiro Ueno, Shiro Kubo, Hiroaki Tagawa, Toshiyuki Yoshioka, Wataru Tsukada, Masao Tsubokawa, Hiroshi Kojima, and Akira Kasahara
pp 941 - 946; DOI:
10.1021/jm00229a017
PDF
Hypolipidemic alkoxybenzoic acids
Vern G. DeVries, Daniel B. Moran, George R. Allen, and Stephen J. Riggi
pp 946 - 957; DOI:
10.1021/jm00229a018
PDF
Chemistry of nitrosoureas. Decomposition of deuterated 1,3-bis(2-chloroethyl)-1-nitrosourea
Robert B. Brundrett, J. Wayne Cowens, Michael Colvin, and Ian Jardine
pp 958 - 961; DOI:
10.1021/jm00229a019
PDF
Tissue distribution of technetium-99m and carbon-14 labeled N-(2,6-dimethylphenylcarbamoylmethyl)iminodiacetic acid
Patrick S. Callery, William C. Faith, Michael D. Loberg, Anna T. Fields, Elizabeth B. Harvey, and Malcolm D. Cooper
pp 962 - 964; DOI:
10.1021/jm00229a020
PDF
Preliminary biological studies of certain amino acid analogues
C. J. Abshire and M. Ostiguy
pp 965 - 966; DOI:
10.1021/jm00229a021
PDF
Adamantane and protoadamantanealkanamines as potential anti-Parkinson agents. 10
Jiban K. Chakrabarti, Terrence M. Hotten, Susan Sutton, and David E. Tupper
pp 967 - 969; DOI:
10.1021/jm00229a022
PDF
Potential antitumor agents. 13. 4-Methyl-5-amino-1-formylisoquinoline thiosemicarbazone
Krishna C. Agrawal, Paul D. Mooney, and Alan C. Sartorelli
pp 970 - 972; DOI:
10.1021/jm00229a023
PDF
(Vinylaryloxy)acetic acids. A new class of diuretic agents. 4. Various [(2-substituted and 2,2-disubstituted vinyl)aryloxy]acetic acids
Otto W. Woltersdorf, Charles M. Robb, John B. Bicking, L. Sherman Watson, and Edward J. Cragoe
pp 972 - 975; DOI:
10.1021/jm00229a024
PDF
Synthesis and antimineralocorticoid activities of some 7.alpha.-cyano and 7.alpha.-alkoxycarbonylamino steroidal spirolactones
Richard M. Weier and Lorenz M. Hofmann
pp 975 - 977; DOI:
10.1021/jm00229a025
PDF
On the use of Fibonacci searches in structure-activity studies
Stanley N. Deming
pp 977 - 978; DOI:
10.1021/jm00229a026
PDF
Antimalarials. 9. Methylthio- and methylsulfonyl-substituted 9-phenanthrenemethanols
A. Markovac and M. P. LaMontagne
pp 978 - 982; DOI:
10.1021/jm00229a027
PDF
A new class of diuretics with the 1,4-dioxino[2,3-g]quinolone structure
J. Van Dijk, J. Hartog, and T. A. C. Boschman
pp 982 - 983; DOI:
10.1021/jm00229a028
PDF
Book Reviews

pp 984 - 986; DOI:
10.1021/jm00229a600
PDF

Issue 8


Centrally acting emetics. 10. Rigid dopamine congeners derived from octahydrobenzo[f]quinoline
Joseph G. Cannon, Gerard J. Hatheway, John Paul Long, and Fouad M. Sharabi
pp 987 - 993; DOI:
10.1021/jm00230a001
PDF
Synthesis and biological properties of some spin-labeled 9-aminoacridines
Birandra K. Sinha, Richard L. Cysyk, David B. Millar, and Colin F. Chignell
pp 994 - 998; DOI:
10.1021/jm00230a002
PDF
Synthesis and biological properties of 4-amino- and 4-bromo-4-norpyridoxol. New approaches for the modification of the 4 position of vitamin B6
W. Korytnyk, A. C. Ghosh, P. G. G. Potti, and S. C. Srivastava
pp 999 - 1002; DOI:
10.1021/jm00230a003
PDF
Cysteine derivatives with reactive groups as potential antitumor agents
B. Paul and W. Korytnyk
pp 1002 - 1007; DOI:
10.1021/jm00230a004
PDF
Synthesis and biological evaluation of .omega.-homologues of prostaglandin E1
Esam Z. Dajani, Leonard F. Rozek, John H. Sanner, and Masateru Miyano
pp 1007 - 1010; DOI:
10.1021/jm00230a005
PDF
Tyrosylated analogues of somatostatin
Jean E. Rivier, Marvin R. Brown, and Wylie W. Vale
pp 1010 - 1013; DOI:
10.1021/jm00230a006
PDF
Nucleic acids. 16. Orally active derivatives of ara-cytidine
W. J. Wechter, D. T. Gish, M. E. Greig, G. D. Gray, T. E. Moxley, S. L. Kuentzel, L. G. Gray, A. J. Gibbons, R. L. Griffin, and G. L. Neil
pp 1013 - 1017; DOI:
10.1021/jm00230a007
PDF
Synthesis of tetrazole ribonucleosides and their evaluation as antiviral agents. 2. 5-Amino-1-(.beta.-D-ribofuranosyl)-1H-tetrazole and 5-amino-2-(.beta.-D-ribofuranosyl)-2H-tetrazole
Mohindar S. Poonian, Eugene F. Nowoswiat, John F. Blount, and Michael J. Kramer
pp 1017 - 1020; DOI:
10.1021/jm00230a008
PDF
Synthesis and antiviral and antimicrobial activity of certain 1-.beta.-D-ribofuranosyl-4,5-disubstituted imidazoles
Prem C. Srivastava, David G. Streeter, Thomas R. Matthews, Lois B. Allen, Robert W. Sidwell, and Roland K. Robins
pp 1020 - 1026; DOI:
10.1021/jm00230a009
PDF
Synthesis and anti-DNA virus activity of the 5'-monophosphate and the cyclic 3',5'-monophosphate of 9-(.beta.-D-xylofuranosyl)guanine
Ganapathi R. Revankar, John H. Huffman, Robert W. Sidwell, Richard L. Tolman, Roland K. Robins, and Lois B. Allen
pp 1026 - 1028; DOI:
10.1021/jm00230a010
PDF
Design of substrate-site-directed irreversible inhibitors of adenosine 5'-phosphate aminohydrolase. Effect of substrate substituents on affinity for the substrate site
Alexander Hampton, Takuma Sasaki, Florian Perini, Lewis A. Slotin, and Francis Kappler
pp 1029 - 1033; DOI:
10.1021/jm00230a011
PDF
Theoretical model-based equations for the linear free energy relations of the biological activity of ionizable substances. 1. Equilibrium-controlled potency
Yvonne C. Martin and James J. Hackbarth
pp 1033 - 1039; DOI:
10.1021/jm00230a012
PDF
Quantitative structure-activity relationships. 3. A comparison of different Free-Wilson models
Hugo Kubinyi and Ott H. Kehrhahn
pp 1040 - 1049; DOI:
10.1021/jm00230a013
PDF
Clonidine and related analogues. Quantitative correlations
Bruno Rouot, Gerard Leclerc, Camille G. Wermuth, Francois Miesch, and Jean Schwartz
pp 1049 - 1054; DOI:
10.1021/jm00230a014
PDF
(-)-3-Isothujone, a small nonnitrogenous molecule with antinociceptive activity in mice
Kenner C. Rice and Raymond S. Wilson
pp 1054 - 1057; DOI:
10.1021/jm00230a015
PDF
Synthesis and pharmacology of novel anxiolytic agents derived from 2-[(dialkylamino)methyl-4H-triazol-4-yl]benzophenones and related heterocyclic benzophenones
Martin Gall, J. B. Hester, A. D. Rudzik, and Robert A. Lahti
pp 1057 - 1064; DOI:
10.1021/jm00230a016
PDF
Conversion of N-alkylaminobenzophenones to benzodiazepines in vivo
Robert A. Lahti and Martin Gall
pp 1064 - 1067; DOI:
10.1021/jm00230a017
PDF
Synthesis of 3-iodo-L-thyronine and its iodinated derivatives
Paul Block
pp 1067 - 1069; DOI:
10.1021/jm00230a018
PDF
Antifungal activity of 4-substituted crotonic acid esters
Herman Gershon, Larry Shanks, and Daniel E. Gawiak
pp 1069 - 1072; DOI:
10.1021/jm00230a019
PDF
Synthesis and antimicrobial evaluation of substituted 5,6-dihydro-5-nitrouracils
Robert A. Long, Thomas R. Matthews, and Roland K. Robins
pp 1072 - 1074; DOI:
10.1021/jm00230a020
PDF
Optical isomers of 2-(2-ethoxyphenoxymethyl)tetrahydro-1,4-oxazine (viloxazine) and related compounds
Ralph Howe, Thomas Leigh, Balbir S. Rao, and Alexander H. Todd
pp 1074 - 1076; DOI:
10.1021/jm00230a021
PDF
Book Reviews

pp 1077 - 1078; DOI:
10.1021/jm00230a600
PDF

Issue 9


Irreversible enzyme inhibitors. Inhibitors of guinea pig complement derived by quaternization of substituted pyridines with benzyl halides
Michael H. Doll and B. R. Baker
pp 1079 - 1088; DOI:
10.1021/jm00231a001
PDF
Structure-activity relationships in immunochemistry. 4. Inhibition of complement by benzylpyridinium ions. On the predictive value of correlation equations
Corwin Hansch, Masafumi Yoshimoto, and Michael H. Doll
pp 1089 - 1093; DOI:
10.1021/jm00231a002
PDF
Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 4. Further modifications of the amino acid and base portions of S-adenosyl-L-homocysteine
R. T. Borchardt, J. A. Huber, and Yih Shiong Wu
pp 1094 - 1099; DOI:
10.1021/jm00231a003
PDF
Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 5. Role of the asymmetric sulfonium pole in the enzymic binding of S-adenosyl-L-methionine
R. T. Borchardt and Yih Shiong Wu
pp 1099 - 1103; DOI:
10.1021/jm00231a004
PDF
Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 6. Structural modifications of S-adenosylmethionine
R. T. Borchardt, Yih Shiong Wu, J. A. Huber, and A. F. Wycpalek
pp 1104 - 1110; DOI:
10.1021/jm00231a005
PDF
Reduced 8-aminoquinoline analogues as potential antimalarial agents
F. I. Carroll, J. T. Blackwell, Abraham Philip, and Charles E. Twine
pp 1111 - 1119; DOI:
10.1021/jm00231a006
PDF
.beta.-Adrenergic blocking agents. 13. (3-Amino-2-hydroxypropoxy)benzamides
L. H. Smith
pp 1119 - 1123; DOI:
10.1021/jm00231a007
PDF
Potential antitumor agents. 19. Multiply substituted 4'-(9-acridinylamino)methanesulfonanilides
Bruce F. Cain and Graham J. Atwell
pp 1124 - 1129; DOI:
10.1021/jm00231a008
PDF
Structural requirements for biological activity among antileukemic glaucarubolone ester quassinoids
S. Morris Kupchan, John A. Lacadie, Gary A. Howie, and Barry R. Sickles
pp 1130 - 1133; DOI:
10.1021/jm00231a009
PDF
Phosphorus-nitrogen compounds. 20. Thiophosphorus hydrazones
L. A. Cates, Y. M. Cho, L. K. Smith, L. Williams, and T. L. Lemke
pp 1133 - 1137; DOI:
10.1021/jm00231a010
PDF
Sympathomimetic amines having a carbostyril nucleus
Shiro Yoshizaki, Kaoru Tanimura, Shigeharu Tamada, Youichi Yabuuchi, and Kazuyuki Nakagawa
pp 1138 - 1142; DOI:
10.1021/jm00231a011
PDF
Bis-basic-substituted polycyclic aromatic compounds. A new class of antiviral agents. 7. Bisalkamine esters of 9-oxoxanthene-2,7-dicarboxylic acid, 3,6-bis-basic ethers of xanthen-9-one, and 2,7-bis(aminoacyl)xanthen-9-ones, -xanthenes, and -thioxanthenes
Albert A. Carr, Joyce F. Grunwell, Arthur D. Sill, Donald R. Meyer, F. William Sweet, B. Joseph Scheve, J. Martin Grisar, Robert W. Fleming, and Gerald D. Mayer
pp 1142 - 1148; DOI:
10.1021/jm00231a012
PDF
Synthesis and antimycotic properties of 1-(2-alkyl-2-phenylethyl)-1H-imidazoles
J. Heeres, L. J. J. Backx, and J. M. Van Cutsem
pp 1148 - 1155; DOI:
10.1021/jm00231a013
PDF
Stereochemical studies on medicinal agents. 20. Absolute configuration and analgetic potency of .alpha.-promedol enantiomers. The role of the C-4 chiral center in conferring stereoselectivity in axial- and equatorial-phenylprodine congeners
David S. Fries and Philip S. Portoghese
pp 1155 - 1158; DOI:
10.1021/jm00231a014
PDF
Benzo[g]quinolines. 3. Influence of carbon-5 substituents on narcotic antagonist and antiwrithing activities of derivatives of cis-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]quinolin-7-ol
William F. Michne
pp 1159 - 1161; DOI:
10.1021/jm00231a015
PDF
Synthesis and anticonvulsant properties of 1-(10-cyano- and -10-bromo-5H-dibenzo[a,d]cyclohepten-5-yl)-4-[(arylmethylene)amino]piperazines
Charles R. Ellefson and John W. Cusic
pp 1161 - 1164; DOI:
10.1021/jm00231a016
PDF
9-Nor-9-hydroxyhexahydrocannabinols. Synthesis, some behavioral and analgesic properties, and comparison with the tetrahydrocannabinols
Raymond S. Wilson, Everette L. May, Billy R. Martin, and William L. Dewey
pp 1165 - 1167; DOI:
10.1021/jm00231a017
PDF
Metabolic N-demethylation of nicotine. Trapping of a reactive iminium species with cyanide ion
Nguyen Trong Lang, Larry D. Gruenke, and Neal Castagnoli Jr.
pp 1168 - 1169; DOI:
10.1021/jm00231a018
PDF
Book Reviews

pp 1169 - 1170; DOI:
10.1021/jm00231a600
PDF

Issue 10


A practical synthesis of codeine from dihydrothebainone
Dwight D. Weller and Henry Rapoport
pp 1171 - 1175; DOI:
10.1021/jm00232a001
PDF
Conversion of thebaine to codeine
Randy B. Barber and Henry Rapoport
pp 1175 - 1180; DOI:
10.1021/jm00232a002
PDF
Modification of the 5' position of purine nucleosides. 1. Synthesis and biological properties of alkyl adenosine-5'-carboxylates
Raj N. Prasad, Anthony Fung, Karin Tietje, Herman Stein, and Harold D. Brondyk
pp 1180 - 1186; DOI:
10.1021/jm00232a003
PDF
Analogs of 8-azaguanosine
Robert D. Elliott and John A. Montgomery
pp 1186 - 1191; DOI:
10.1021/jm00232a004
PDF
Inhibitors of tRNA methyltransferases. S-Adenosylsulfonium salts
Margaret E. Gnegy and Frederick J. Lotspeich
pp 1191 - 1195; DOI:
10.1021/jm00232a005
PDF
(2-Piperidine)- and (2-pyrrolidine)ethanones and -ethanols as inhibitors of blood platelets aggregation
J. Martin Grisar, George P. Claxton, Kenneth T. Stewart, Robert D. MacKenzie, and Takashi Kariya
pp 1195 - 1201; DOI:
10.1021/jm00232a006
PDF
Catechol O-methyltransferase. 9. Mechanism of inactivation by 6-hydroxydopamine
R. T. Borchardt, J. R. Reid, D. R. Thakker, Y. O. Liang, R. W. Wightman, and R. N. Adams
pp 1201 - 1209; DOI:
10.1021/jm00232a007
PDF
Potential antitumor agents. 14. 4-Substituted 2-formylpyridine thiosemicarbazones
Krishna C. Agrawal, Barbara A. Booth, Suzanne M. DeNuzzo, and Alan C. Sartorelli
pp 1209 - 1214; DOI:
10.1021/jm00232a008
PDF
Synthesis and antilipidemic properties of cis-7-chloro-3a,8b-dihydro-3a-methylfuro[3,4-b]benzofuran-3(1H)-one, a tricyclic clofibrate related lactone having a structural resemblance to mevalonolactone
Donald T. Witiak, Eiichi Kuwano, Dennis R. Feller, John R. Baldwin, Howard A. I. Newman, and Shankar K. Sankarappa
pp 1214 - 1220; DOI:
10.1021/jm00232a009
PDF
3,3-Diphenyl-3-(2-alkyl-1,3,4-oxadiazol-5-yl)propylcycloalkylamines, a novel series of antidiarrheal agents
Gilbert W. Adelstein, Chung H. Yen, Esam Z. Dajani, and Robert G. Bianchi
pp 1221 - 1225; DOI:
10.1021/jm00232a010
PDF
Cinnoline-3-propionic acids, a new series of orally active antiallergic substances
David Holland, Geraint Jones, Paul W. Marshall, and Gwenda D. Tringham
pp 1225 - 1228; DOI:
10.1021/jm00232a011
PDF
Structure of the peptide antibiotic polypeptin
John A. Sogn
pp 1228 - 1231; DOI:
10.1021/jm00232a012
PDF
Investigation of the effect of the solvent medium on the conformational behavior of phenylethylamines by empirical method
Mahadevappa Kumbar
pp 1232 - 1238; DOI:
10.1021/jm00232a013
PDF
Physicochemical-activity relationships in asymmetrical analogues of methoxychlor
Peter J. Goodford, Alan T. Hudson, G. Clive Sheppey, Raymond Wootton, Malcolm H. Black, Graeme J. Sutherland, and John C. Wickham
pp 1239 - 1247; DOI:
10.1021/jm00232a014
PDF
Correlation of opiate receptor affinity with analgetic effects of meperidine homologs
Candace B. Pert, Solomon H. Snyder, and Philip S. Portoghese
pp 1248 - 1250; DOI:
10.1021/jm00232a015
PDF
Charge distribution of histamine monocation in its "essential" conformation
W. G. Richards and Jenifer Wallis
pp 1250 - 1252; DOI:
10.1021/jm00232a016
PDF
Adrenocorticotropin. 49. Synthesis and biological activity of [2-.delta.-aminovaleric acid,5-arginine]adrenocorticotropin-(2-19)
James Blake and Choh Hao Li
pp 1252 - 1254; DOI:
10.1021/jm00232a017
PDF
Pharmacological activity of nitroxide analogs of dichloroisoproterenol and propranolol
Elmer J. Rauckman, Gerald M. Rosen, and Robert J. Lefkowitz
pp 1254 - 1256; DOI:
10.1021/jm00232a018
PDF
Cycloalkanones. 9. Comparison of analogs which inhibit cholesterol and fatty acid synthesis
Iris H. Hall and Gerald L. Carlson
pp 1257 - 1261; DOI:
10.1021/jm00232a019
PDF
Coralyne. Intercalation with DNA as a possible mechanism of antileukemic action
W. David Wilson, Alice N. Gough, James J. Doyle, and Michael W. Davidson
pp 1261 - 1263; DOI:
10.1021/jm00232a020
PDF
Book Reviews

pp 1263 - 1264; DOI:
10.1021/jm00232a600
PDF

Issue 11


Nucleosides. 1. 9-(3'-Alkyl-3'-deoxy-.beta.-D-ribofuranosyl)adenines as lipophilic analogs of cordycepin. Synthesis and preliminary biological studies
Andre Rosowsky, Herbert Lazarus, and Ayako Yamashita
pp 1265 - 1270; DOI:
10.1021/jm00233a001
PDF
Phenylalanyl transfer ribonucleic acid synthetase from Escherichia coli B. Potent inhibition by analogs of N-benzyl-2-phenylethylamine
Robert T. Anderson and Daniel V. Santi
pp 1270 - 1275; DOI:
10.1021/jm00233a002
PDF
Phenylalanyl transfer ribonucleic acid synthetase from rat liver. Analysis of phenylalanine and adenosine 5'-triphosphate binding sites and comparison to the enzyme from Escherichia coli
Daniel V. Santi and Robert W. Webster
pp 1276 - 1279; DOI:
10.1021/jm00233a003
PDF
Evidence for species-specific substrate-site-directed inactivation of rabbit adenylate kinase by N6-(6-iodoacetamido-n-hexyl)adenosine 5'-triphosphate
Alexander Hampton, Lewis A. Slotin, and Ram R. Chawla
pp 1279 - 1283; DOI:
10.1021/jm00233a004
PDF
Active-site-directed alkylation of chymotrypsin by reagents utilizing various departing groups
David Larsen and Elliott Shaw
pp 1284 - 1286; DOI:
10.1021/jm00233a005
PDF
Synthesis of biologically active retroenantiomers of angiotensin peptides
Gilberto Goissis, Viviane L. A. Nouailhetas, and Antonio C. M. Paiva
pp 1287 - 1290; DOI:
10.1021/jm00233a006
PDF
Protein-binding polyhedral boranes. 3
R. L. Jr. Sneath, J. E. Wright, A. H. Soloway, S. M. O'Keefe, A. S. Dey, and W. D. Smolnycki
pp 1290 - 1294; DOI:
10.1021/jm00233a007
PDF
Polyglutamyl and polylysyl derivatives of the lysine analogs of folic acid and homofolic acid
Laurence T. Plante, Elizabeth J. Crawford, and Morris Friedkin
pp 1295 - 1299; DOI:
10.1021/jm00233a008
PDF
Use of cluster analysis in the development of structure-activity relations for antitumor triazenes
W. J. Dunn, M. J. Greenberg, and Soledad S. Callejas
pp 1299 - 1301; DOI:
10.1021/jm00233a009
PDF
Potential central nervous system antitumor agents. Aziridinylbenzoquinones. 2
Feng-Te Chou, A. Hameed Khan, and John S. Driscoll
pp 1302 - 1308; DOI:
10.1021/jm00233a010
PDF
Stereochemical studies on medicinal agents. 21. Investigation of the role of conformational factors in the action of diphenylpropylamines. Synthesis and analgetic potency of 5-methylmethadone diastereomers
James G. Henkel, Eric P. Berg, and Philip S. Portoghese
pp 1308 - 1314; DOI:
10.1021/jm00233a011
PDF
Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines] as potential central nervous system agents. 1
Victor J. Bauer, Brian J. Duffy, David Hoffman, Solomon S. Klioze, Raymond W. Kosley, Arthur R. McFadden, Lawrence L. Martin, Helen H. Ong, and Harry M. Geyer
pp 1315 - 1324; DOI:
10.1021/jm00233a012
PDF
Lipid solubility and affinity for N-demethylation of dansylamides in isolated rat hepatocytes
J. Scott Hayes and Klaus Brendel
pp 1324 - 1328; DOI:
10.1021/jm00233a013
PDF
Hashish. 16. Unsaturated side-chain analogs of .DELTA.8-tetrahydrocannabinol with potent biological activity
Raj K. Razdan, Haldean C. Dalzell, Patricia Herlihy, and John F. Howes
pp 1328 - 1330; DOI:
10.1021/jm00233a014
PDF
Cardenolide analogs. 1. A 17.beta.-unsaturated aldehyde
Dwight S. Fullerton, Marvin C. Pankaskie, Khalil Ahmed, and Arthur H. L. From
pp 1330 - 1333; DOI:
10.1021/jm00233a015
PDF
Some novel potential alkylating agents derived from diethylstilbestrol
I. M. Roushdi, A. Mohsen, M. E. Omar, M. S. Ragab, and M. Awad
pp 1333 - 1336; DOI:
10.1021/jm00233a016
PDF
Potential bioreductive alkylating agents. 7. Antitumor effects of phenyl-substituted 2-chloromethyl-3-phenyl-1,4-naphthoquinones
Ai Jeng Lin and Alan C. Sartorelli
pp 1336 - 1338; DOI:
10.1021/jm00233a017
PDF
Preparation and antitumor activities of some derivatives of 5-methoxysterigmatocystin
John M. Essery, Frances A. O'Herron, Donald N. McGregor, and William T. Bradner
pp 1339 - 1342; DOI:
10.1021/jm00233a018
PDF
Synthesis and biological activity of 3,5-dinitro-4- and -2-(1H-purin-6-ylthio)benzoates, prodrugs of 6-mercaptopurine
Robert Drawbaugh, Charlene Bouffard, and Michael Strauss
pp 1342 - 1345; DOI:
10.1021/jm00233a019
PDF
Some 10-substituted 5-ethyl-10-dialkylaminoalkyl-10,11-dihydro-5H-dibenz[b,f]azepines as potential antiarrhythmic agents
Charles R. Ellefson and John W. Cusic
pp 1345 - 1349; DOI:
10.1021/jm00233a020
PDF
Iodo-bis(quaternary ammonium) salts. Potential cartilage-selective x-ray contrast agents
Steven P. Van Ootegham, Ronald G. Smith, G. Doyle Daves, Edwin M. Chang, Aziza El-Mazati, George D. Olsen, and William K. Riker
pp 1349 - 1352; DOI:
10.1021/jm00233a021
PDF
Synthesis and antihypertensive activity of some imidazoindole derivatives
P. K. Adhikary, S. K. Das, and B. A. Hess
pp 1352 - 1354; DOI:
10.1021/jm00233a022
PDF
A circular dichroism study of the interaction of sodium and potassium ions with methionine enkephalin
Jacques H. Poupaert, Philip S. Portoghese, and Victor Garsky
pp 1354 - 1356; DOI:
10.1021/jm00233a023
PDF
Book Reviews

pp 1357 - 1358; DOI:
10.1021/jm00233a600
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Issue 12


Studies in the design of x-ray contrast agents. Synthesis, hydrophobicity, and solubility of some iodoresorcyl bis(.beta.-glucosides)
Frederick L. Weitl, Milos Sovak, Terry M. Williams, and Joseph H. Lang
pp 1359 - 1362; DOI:
10.1021/jm00234a001
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Iodine-containing organic carbonates as investigative radiopaque compounds
B. N. Newton
pp 1362 - 1366; DOI:
10.1021/jm00234a002
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Pyridoxal phosphate. 5. 2-Formylethynylphosphonic acid and 2-formylethylphosphonic acid, potent inhibitors of pyridoxal phosphate binding and probes of enzyme topography
A. J. Rudinskas and T. L. Hullar
pp 1367 - 1371; DOI:
10.1021/jm00234a003
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Design of substrate-site-directed inhibitors of adenylate kinase and hexokinase. Effect of substrate substituents on affinity for the adenine nucleotide sites
Alexander Hampton, Lewis A. Slotin, Francis Kappler, Takuma Sasaki, and Florian Perini
pp 1371 - 1377; DOI:
10.1021/jm00234a004
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Quinazolines and 1,4-benzodiazepines. 75. 7-Hydroxyaminobenzodiazepines and derivatives
Armin Walser, Gladys Zenchoff, and R. Ian Fryer
pp 1378 - 1381; DOI:
10.1021/jm00234a005
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Stereochemical studies of adrenergic drugs. Optically active derivatives of imidazolines
Duane D. Miller, Fu-Lian Hsu, Robert R. Ruffolo, and Popat N. Patil
pp 1382 - 1384; DOI:
10.1021/jm00234a006
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Preparation, hydrolysis, and oral absorption of lactonyl esters of penicillins
J. Peter Clayton, Martin Cole, Stephen W. Elson, Harry Ferres, John C. Hanson, Linda W. Mizen, and Robert Sutherland
pp 1385 - 1391; DOI:
10.1021/jm00234a007
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Trichothecene analogs. 1. 1,5-Dioxaspiro[2.5]octanes
Dwight S. Fullerton, Chi-Ming Chen, and Iris H. Hall
pp 1391 - 1395; DOI:
10.1021/jm00234a008
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Steroidal 3,5-dienes
Philip M. Weintraub, Paul L. Tiernan, Harvey D. Benson, Joyce F. Grunwell, J. O'Neal Johnston, and V. Petrow
pp 1395 - 1399; DOI:
10.1021/jm00234a009
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Phenylalkylamines with potential psychotherapeutic utility. 1. 2-Amino-1-(2,5-dimethoxy-4-methylphenyl)butane
Robert T. Standridge, Henry G. Howell, Jonas A. Gylys, Richard A. Partyka, and Alexander T. Shulgin
pp 1400 - 1404; DOI:
10.1021/jm00234a010
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Aryl-s-tetrazines with antiinflammatory activity
S. A. Lang, B. D. Johnson, E. Cohen, A. E. Sloboda, and E. Greenblatt
pp 1404 - 1409; DOI:
10.1021/jm00234a011
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Potential antitumor agents. 20. Structure-activity-site relations for the 4'-(9-acridinylamino)alkanesulfonanilides
Bruce F. Cain and Graham J. Atwell
pp 1409 - 1416; DOI:
10.1021/jm00234a012
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Potential antitumor agents. 18. Bisquaternary ammonium heterocycles
Bruce F. Cain and Graham J. Atwell
pp 1417 - 1419; DOI:
10.1021/jm00234a013
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para-Substituted N-acetyl-L(S)- and -D(R)-.alpha.-amino-N-phenylglutarimides. A structure-activity study of substituent effects on stereoselective anticonvulsant activity
Donald T. Witiak, Wayne L. Cook, Tribhuwan K. Gupta, and Michael C. Gerald
pp 1419 - 1422; DOI:
10.1021/jm00234a014
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Carcinogenicity of derivatives of polynuclear compounds
Richard M. Peck, Tie Keng Tan, and Evelyn B. Peck
pp 1422 - 1423; DOI:
10.1021/jm00234a015
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Synthesis and antitumor activity of 4'-deoxydaunorubicin and 4'-deoxyadriamycin
Federico Arcamone, Sergio Penco, Silvio Redaelli, and Stephen Hanessian
pp 1424 - 1425; DOI:
10.1021/jm00234a016
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Additions and Corrections - Synthesis of Substituted 4-Dimethylaminoazobenzenes and a Study of Their Effect on Lactobacillus casei and Escherichia coli.
Girgis M. Bebawi, and L. P. Lambooy
pp 1425 - 1425; DOI:
10.1021/jm00234a600
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Additions and Corrections - ara-Cytidine Acylates. Use of Drug Design Predictors in Structure-Activity Relationship Correlation.
W. J. Wechter, M. A. Johnson, C. M. Hall, D. T .Warner, A. E. Berger, A. H. Wenzel, D. T .Gish, and G. L. Neil
pp 1425 - 1425; DOI:
10.1021/jm00234a601
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Additions and Corrections - Non-Computer Approach to Structure-Activity Study. An Expanded Fibronacci Search Applied to Structurally Diverse Types of Compounds.
Norman J. Santora, and King Auyang
pp 1425 - 1425; DOI:
10.1021/jm00234a602
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Additions and Corrections - Synthesis and Antibacterial Evaluatoin of 1,2,3,4-Tetrahydro-4-oxo-1,8-naphthyridine-3-carboxylic Acid Esters, Carbonitriles, and Carboxamides.
Arthur A. Santilli, Anthony C. Scotese, and John A. Yurchenco
pp 1425 - 1425; DOI:
10.1021/jm00234a603
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Additions and Corrections - Quantum Chemical Studies of Merperidine and Prodine.
Gilda H. Loew, and J. Randal Jester
pp 1425 - 1426; DOI:
10.1021/jm00234a604
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Additions and Corrections - Difference in Antimalarial Activity between Certain Amino Alcohol Diastereomers.
Ping-Lu Chien, and C. C. Cheng
pp 1426 - 1426; DOI:
10.1021/jm00234a605
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Additions and Corrections - Cycloalkanones. 8. Hypocholesterolemic Activity of Long-Chain Ketones Related to Pentadecanone.
Steven D. Wyrick, Iris H. Hall, C. Piantadosi, and Charles R. Fenske
pp 1426 - 1426; DOI:
10.1021/jm00234a606
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Additions and Corrections - Novel Pyrazolo, Isoxazolo, and Thiazolo Steroidal Systems and Model Analogs Containing Dimethoxylaryl (or Dihydroxylaryl) Groups and Derivatives. Synthesis, Spectral Properties, and Biological Activity.
M. M .Hashem, K. D. Berlin, R. W. Chesnut, and N. N .Durham
pp 1426 - 1426; DOI:
10.1021/jm00234a607
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Additions and Corrections - Synthesis and Structure-Activity Relationships of Heterocyclic Compounds Containing a Trimethoxyarene Function.
E. A. Mawdsley, K. D. Berlin, R. W. Chesnut, and N. N. Durham
pp 1426 - 1426; DOI:
10.1021/jm00234a608
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Additions and Corrections - Cysteine Derivatives with Reactive Groups as Potential Antitumor Agents.
B. Paul, and W. Korytnyk
pp 1426 - 1426; DOI:
10.1021/jm00234a609
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