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Volume 17
Main Index

Issue 1


Aromatic amino acid hydroxylase inhibitors. 3. In vitro inhibition by azadopamine analogs
L. E. Hare, M. C. Lu, C. B. Sullivan, P. T. Sullivan, R. E. Counsell, and P. A. Weinhold
pp 1 - 5; DOI:
10.1021/jm00247a001
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Enzyme inhibitors. 26. Bridging hydrophobic and hydrophilic regions on adenosine deaminase with some 9-(2-hydroxy-3-alkyl)adenines
Howard J. Schaeffer and Charles F. Schwender
pp 6 - 8; DOI:
10.1021/jm00247a002
PDF
Synthesis and enzymic evaluation of some N-alkyl branched chain piperidine salts and N-alkyl-3-(N,N-diethylcarbamoyl)piperidine salts as inhibitors of acetyl- and butyrylcholinesterase
James W. Stanley, Ian W. Mathison, and James G. Beasley
pp 8 - 12; DOI:
10.1021/jm00247a003
PDF
Synthesis and enzymic evaluation of pyridostigmine analogs used to probe the active sites of acetylcholinesterase and butyrylcholinesterase
O. Elmo Millner, James W. Stanley, and William P. Purcell
pp 13 - 18; DOI:
10.1021/jm00247a004
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Structure-activity relations in reactivators of organophosphorus-inhibited acetylcholinesterase. 7. 1-Aryl-2-hydroxyiminomethyl-3-methylimidazolium iodides
Palmarisa Franchetti, Mario Grifantini, Sante Martelli, and Maria L. Stein
pp 18 - 22; DOI:
10.1021/jm00247a005
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Sulfonamide structure-activity relations in a cell-free system. 2. Proof for the formation of a sulfonamide-containing folate analog
Lothar Bock, George H. Miller, Klaus J. Schaper, and Joachim K. Seydel
pp 23 - 28; DOI:
10.1021/jm00247a006
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Relation between .pi. and Rm values of sulfonamides
Gian L. Biagi, Anna M. Barbaro, Maria C. Guerra, Giorgio C. Forti, and Maria E. Fracasso
pp 28 - 33; DOI:
10.1021/jm00247a007
PDF
Semisynthetic cephalosporins. Synthesis and structure-activity relations of 7-mandelamido-3-cephem-4-carboxylic acids
J. R. E. Hoover, G. L. Dunn, D. R. Jakas, L. L. Lam, J. J. Taggart, J. R. Guarini, and L. Phillips
pp 34 - 41; DOI:
10.1021/jm00247a008
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Differential effects of benzodioxane, chroman, and dihydrobenzofuran analogs of clofibrate on various parameters of hepatic drug metabolism
Neil J. Lewis, Dennis R. Feller, Guiragos K. Poochikian, and Donald T. Witiak
pp 41 - 45; DOI:
10.1021/jm00247a009
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Disposition and metabolism of 4-methyl-2-(4-phenylbenzyl)-2-oxazoline-4-methanol in the rat and dog
Lennox B. Turnbull, Christopher P. Johnson, Ying Ho Chen, Lawrence F. Sancilio, and Robert B. Bruce
pp 45 - 48; DOI:
10.1021/jm00247a010
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Adrenergic agents. 1. Synthesis and potential .beta.-adrenergic agonist activity of some catechol amine analogs bearing a substituted amino functionality in the meta position
Carl Kaiser, Donald F. Colella, Mark S. Schwartz, Eleanor Garvey, and Joe R. Wardell
pp 49 - 57; DOI:
10.1021/jm00247a011
PDF
Analogs of phenothiazines. 5. Synthesis and neuropharmacological activity of some piperidylidene derivatives of thioxanthenes, xanthenes, dibenzoxepins, and acridans
Carl Kaiser, Philip J. Fowler, David H. Tedeschi, Bruce M. Lester, Eleanor Garvey, Charles L. Zirkle, Edward A. Nodiff, and Andrew J. Saggiomo
pp 57 - 62; DOI:
10.1021/jm00247a012
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Molecular structure and conformation of the nucleoside antibiotic derivative 2-methylformycin with a C-glycosidic bond
Jaime E. Abola, Michael J. Sims, Donald J. Abraham, Arthur F. Lewis, and Leroy B. Townsend
pp 62 - 65; DOI:
10.1021/jm00247a013
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Antidepressant agents. 1. Chemistry and pharmacology of amino-substituted spiro[5H-dibenzo[a,d]cycloheptene-5,1'-cycloalkanes]
B. Carnmalm, E. Jacupovic, L. Johansson, T. De Paulis, S. Ramsby, N. E. Stjernstrom, A. L. Renyi, S. B. Ross, and S. O. Ogren
pp 65 - 72; DOI:
10.1021/jm00247a014
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Aminoalkyldibenzo[a,e]cyclopropa[c]cycloheptene derivatives. Series of potent antidepressants
W. E. Coyne and J. W. Cusic
pp 72 - 75; DOI:
10.1021/jm00247a015
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Antimalarial drugs. 35. Synthesis and antimalarial effects of 1-(3,4-dichlorophenyl)-3-[4-[(1-ethyl-3-piperidyl)amino]-6-methyl-2-pyrimidinyl]guanidine and related substances
Edward F. Elslager, Leslie M. Werbel, Ann Curry, Nancy Headen, and Judith Johnson
pp 75 - 100; DOI:
10.1021/jm00247a016
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Synthesis of pivaloyloxymethyl 6-N'-cyanoamidinopenicillanates and the antibacterial activity of the corresponding acids
Hans Jorgen Petersen
pp 101 - 104; DOI:
10.1021/jm00247a017
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Antibacterial activity of 9(S)-erythromycylamine-aldehyde condensation products
E. H. Massey, B. S. Kitchell, L. D. Martin, and K. Gerzon
pp 105 - 107; DOI:
10.1021/jm00247a018
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Potential hypolipidemic agents. 7. Synthesis and lipid-lowering properties of 2-(dibenzofuranyloxy)-2-methylpropionates and related compounds
Goran Bondesson, Christina Hedbom, Thomas Hogberg, Olle Magnusson, Nils E. Stjernstrom, and Lars A. Carlson
pp 108 - 112; DOI:
10.1021/jm00247a019
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Synthesis of phosphoric acid isoesters of 2-phospho-, 3-phospho-, and 2,3-diphosphoglyceric acid
Francis R. Pfeiffer, Jeanette D. Mier, and Jerry A. Weisbach
pp 112 - 115; DOI:
10.1021/jm00247a020
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Monofluoromethanesulfonanilides. New series of bronchodilators
E. H. Banitt, W. E. Coyne, K. T. McGurran, and J. E. Robertson
pp 116 - 120; DOI:
10.1021/jm00247a021
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Synthesis of monoaryl- and diarylphosphorus analogs of methadone
William H. Shelver, Martin Schreibman, N. Stevan Tanner, and V. Subba Rao
pp 120 - 124; DOI:
10.1021/jm00247a022
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Stereochemical studies on medicinal agents. 16. Conformational studies of methadone and isomethadone utilizing circular dichroism and proton magnetic resonance
James G. Henkel, Kevin H. Bell, and Philip S. Portoghese
pp 124 - 129; DOI:
10.1021/jm00247a023
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Stereochemical studies on medicinal agents. 17. Synthesis, absolute configuration, and analgetic potency of enantiomeric diastereomers of 3-ethyl and 3-propyl derivatives of 1-methyl-4-phenyl-4-propionoxypiperidine
Kevin H. Bell and Philip S. Portoghese
pp 129 - 131; DOI:
10.1021/jm00247a024
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Analogs of phenothiazines. 6. Stereochemical assignment of isomeric aminoalkylidene derivatives of xanthenes and thioxanthenes with neuropharmacological activity
Carl Kaiser, Richard J. Warren, and Charles L. Zirkle
pp 131 - 133; DOI:
10.1021/jm00247a025
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Phenylmorphan agonists-antagonists
Helen H. Ong, Tokuro Ohishi, and Everette L. May
pp 133 - 134; DOI:
10.1021/jm00247a026
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Alkaloids in mammalian tissues. 4. Synthesis of (+)- and (-)-salsoline and isosalsoline
Sidney Teitel, Jay O'Brien, William Pool, and Arnold Brossi
pp 134 - 137; DOI:
10.1021/jm00247a027
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Synthesis and antibacterial activity of some substituted 4-quinolone-3-carboxylic acids
D. G. Markees, Linda S. Schwab, and A. Vegotsky
pp 137 - 139; DOI:
10.1021/jm00247a028
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Oral gold. Synthesis and antiarthritic properties of some large-ring gold chelates
Joseph Weinstock, Blaine M. Sutton, George Y. Kuo, Donald T. Walz, and Michael J. DiMartino
pp 139 - 140; DOI:
10.1021/jm00247a029
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Synthesis and biological properties of [2-L-.beta.-(pyrazolyl-3)alanine]-luteinizing hormone-releasing hormone
David H. Coy, Esther J. Coy, Yoshihiro Hirotsu, and Andrew V. Schally
pp 140 - 142; DOI:
10.1021/jm00247a030
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Potential antileprotic agents. 1. Inhibition of a model mycobacterial system by diaryl sulfones
W. T. Colwell, G. Chan, V. H. Brown, J. I. DeGraw, J. H. Peters, and N. E. Morrison
pp 142 - 144; DOI:
10.1021/jm00247a031
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Potential antileprotic agents. 2. Inhibition of mycobacterial dihydrofolic reductase
J. I. DeGraw, V. H. Brown, W. T. Colwell, and N. E. Morrison
pp 144 - 146; DOI:
10.1021/jm00247a032
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Estrogenic triarylcyclopropanes
G. R. Bedford, A. L. Walpole, and B. Wright
pp 147 - 149; DOI:
10.1021/jm00247a033
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Book Reviews

pp 149 - 149; DOI:
10.1021/jm00247a600
PDF

Issue 2


Quantum statistical calculation for correlation of biological activity and chemical structure. 1. Drug-receptor interactions
Teng K. Lin
pp 151 - 154; DOI:
10.1021/jm00248a001
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Cycloalkanones. 3. Structure-activity relations of hypocholesterolemic cyclooctanone derivatives
G. L. Carlson, I. H. Hall, G. S. Abernethy, and C. Piantadosi
pp 154 - 157; DOI:
10.1021/jm00248a002
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Hansch analysis of the anabolic activities of some nandrolone esters
Mohammad A. Q. Chaudry and Kenneth C. James
pp 157 - 161; DOI:
10.1021/jm00248a003
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Potential psychotomimetics. 2. Rigid analogs of 2,5-dimethoxy-4-methylphenylisopropylamine (DOM, STP)
David E. Nichols, Charles F. Barfknecht, John P. Long, Robert T. Standridge, Henry G. Howell, Richard A. Partyka, and Donald C. Dyer
pp 161 - 166; DOI:
10.1021/jm00248a004
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Rigid analogs of indomethacin
Douglas R. Olson, William J. Wheeler, and Jack N. Wells
pp 167 - 171; DOI:
10.1021/jm00248a005
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.alpha.-(N)-Formylheteroaromatic thiosemicarbazones. Inhibition of tumor-derived ribonucleoside diphosphate reductase and correlation with in vivo antitumor activity
Frederic A. French, Erwin J. Blanz, Sue C. Shaddix, and R. Wallace Brockman
pp 172 - 181; DOI:
10.1021/jm00248a006
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Synthesis and biological activity of some 6,7-dihalo-.DELTA.5-pregnenes and some 6,6-dihalo-5,7-cyclo-5.beta.-pregnane derivatives
Perry Rosen, Alfred Boris, and Robert Karasiewicz
pp 182 - 184; DOI:
10.1021/jm00248a007
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Synthesis and biological activities of substituted glycyrrhetic acids
John S. Baran, Donna D. Langford, Chi D. Liang, and Barnett S. Pitzele
pp 184 - 191; DOI:
10.1021/jm00248a008
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Synthesis of 2-oxygenated glycyrrhetic acid derivatives
Barnett S. Pitzele
pp 191 - 194; DOI:
10.1021/jm00248a009
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Synthesis of tritium-labeled chlorambucil and aniline mustard of high specific activity
Michael Jarman, Leslie J. Griggs, and Michael J. Tisdale
pp 194 - 197; DOI:
10.1021/jm00248a010
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1,4-Benzodioxanes as reversible and irreversible antagonists at adrenergic receptors
B. P. Avner and D. J. Triggle
pp 197 - 200; DOI:
10.1021/jm00248a011
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1-Alkylamino-3-(2-thiazolyloxy)-2-propanols. Novel class of mixed myocardial .beta.-stimulants/.beta.-blockers
J. A. Edwards, B. Berkoz, G. S. Lewis, O. Halpern, J. H. Fried, A. M. Strosberg, L. M. Miller, S. Urich, F. Liu, and A. P. Roszkowski
pp 200 - 203; DOI:
10.1021/jm00248a012
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Furazanobenzofuroxan, furazanobenzothiadiazole, and their N-oxides. New class of vasodilator drugs
Peter B. Ghosh and Barry J. Everitt
pp 203 - 206; DOI:
10.1021/jm00248a013
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Antiparasitic 5-nitrothiazoles and 5-nitro-4-thiazolines. 4
Peter J. Islip, Michael D. Closier, and Martin C. Neville
pp 207 - 209; DOI:
10.1021/jm00248a014
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Optical isomers of aryl-2-piperidylmethanol antimalarial agents. Preparation, optical purity, and absolute stereochemistry
F. I. Carroll and J. T. Blackwell
pp 210 - 219; DOI:
10.1021/jm00248a015
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Folic acid analogs. Modifications in the benzene-ring region. 4. 3'-Ethyl- and 3'-isopropylfolic acids
Eugene C. Roberts and Y. Fulmer Shealy
pp 219 - 222; DOI:
10.1021/jm00248a016
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Synthesis and biological evaluation of isofolic acid
M. G. Nair and Charles M. Baugh
pp 223 - 226; DOI:
10.1021/jm00248a017
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Syntheses and biological activities of 7-ethyl-8-bromo-10-(1'-D-ribityl)isoalloxazine and 7-bromo-8-ethyl-10-(1'-D-ribityl)isoalloxazine, analogs riboflavine
John P. Lambooy
pp 227 - 230; DOI:
10.1021/jm00248a018
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Synthetic luteinizing hormone releasing factor. Short chain analogs
J. Rivier, M. Amoss, C. Rivier, and W. Vale
pp 230 - 233; DOI:
10.1021/jm00248a019
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Adrenocorticotropin. 45. Synthesis and steroidogenic activity of [1-alanine]-adrenocorticotropin-(1-20)-amide, [1-D-alanine]-adrenocorticotropin-(1-20)-amide, and [1-alanine-14C]-adrenocorticotropin-(1-20)-amide
James Blake and Choh Hao Li
pp 233 - 235; DOI:
10.1021/jm00248a020
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Hydrolysis of diacetylcycloserine. In vitro and in vivo studies
John Charles Howard, James C. McPherson, and Augustine H. L. Chuang
pp 236 - 238; DOI:
10.1021/jm00248a021
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Angiotensin-like and antagonistic activities of N-terminal modified [8-leucine]-angiotensin II peptides
Therezinha B. Paiva, Gilberto Goissis, Luiz Juliano, Maria E. Miyamoto, and Antonio C. M. Paiva
pp 238 - 241; DOI:
10.1021/jm00248a022
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Synthesis and anti-deoxyribonucleic acid virus activity of certain 9-.beta.-D-arabinofuranosyl-2-substituted adenine derivatives
Kenji Miyai, Lois B. Allen, John H. Huffman, Robert W. Sidwell, and Richard L. Tolman
pp 242 - 244; DOI:
10.1021/jm00248a023
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Synthesis and antifungal properties of 3-substituted as-triazino[5,6-c]quinolines
George C. Wright, Joseph E. Gray, and Chia-Nien Yu
pp 244 - 246; DOI:
10.1021/jm00248a024
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Radiopharmaceuticals. 12. New rapid synthesis of carbon-11-labeled norepinephrine hydrochloride
Joanna S. Fowler, Robert R. MacGregor, Azizullah N. Ansari, Harold L. Atkins, and Alfred P. Wolf
pp 246 - 248; DOI:
10.1021/jm00248a025
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Saligenin analogs of L-Dopa and DL-.alpha.-methyl-Dopa
Michael Atkinson, David Hartley, Lawrence H. C. Lunts, and Alexander C. Ritchie
pp 248 - 249; DOI:
10.1021/jm00248a026
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5-Hydroxy-5-phenyllevulinic acid. Novel microbial metabolite with analgesic activity
E. R. Wetzel, A. C. Osterberg, and D. B. Borders
pp 249 - 250; DOI:
10.1021/jm00248a027
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[1-.beta.-Mercapto-.beta.,.beta.-diethylpropionic acid]-8-lysine-vasopressin, a potent inhibitor of 8-lysine-vasopressin and of oxytocin
Douglas F. Dyckes, John J. Nestor, Martha F. Ferger, and Vincent Du Vigneaud
pp 250 - 252; DOI:
10.1021/jm00248a028
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Synthesis and some pharmacological properties of 8-.epsilon.-hydroxynorleucine-vasopressin
Patricia Dreyfuss
pp 252 - 255; DOI:
10.1021/jm00248a029
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4(1H)-Quinolones. 2. Antimalarial effect of some 2-methyl-3-(1-alkenyl- or -3-alkyl-4(1H)-quinolones
Adria C. Casey
pp 255 - 256; DOI:
10.1021/jm00248a030
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Book Reviews

pp 257 - 258; DOI:
10.1021/jm00248a600
PDF

Issue 3


Synthesis and biological activity of 9-.beta.-D-arabinofuranosyladenine cyclic 3',5'-phosphate and 9-.beta.-D-arabinofuranosylguanine cyclic 3',5'-phosphate
A. Mohsin Mian, Richard Harris, Robert W. Sidwell, Roland K. Robins, and Tasneem A. Khwaja
pp 259 - 263; DOI:
10.1021/jm00249a001
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Synthesis and antitumor activity of .alpha.- and .beta.-2'-deoxy-6-selenoguanosine and certain related derivatives
George H. Milne and Leroy B. Townsend
pp 263 - 268; DOI:
10.1021/jm00249a002
PDF
5-Alkylpyrimidine nucleosides. Preparation and properties of 5-ethyl-2'-deoxycytidine and related nucleosides
T. Kulikowski and D. Shugar
pp 269 - 273; DOI:
10.1021/jm00249a003
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6-Phenyl-4,5-dihydro-3(2H)-pyridazinones. Series of hypotensive agents
William V. Curran and Adma Ross
pp 273 - 281; DOI:
10.1021/jm00249a004
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6-(Substituted phenyl)-5-substituted-4,5-dihydro-3(2H)-pyridazinones. Antihypertensive agents
Francis J. McEvoy and George R. Allen
pp 281 - 286; DOI:
10.1021/jm00249a005
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Benzoxocin and benzoxonin derivatives. Novel groups of terpenophenols with central nervous system activity
Shlomo Houry, Raphael Mechoulam, Philip J. Fowler, Edward Macko, and Bernard Loev
pp 287 - 293; DOI:
10.1021/jm00249a006
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Benzodiazepines. 4. 2-Oxyamino-5-phenyl-3-H-1,4-benzodiazepines
Jackson Hester and Allan D. Rudzik
pp 293 - 295; DOI:
10.1021/jm00249a007
PDF
Alkaloid studies. 9. Preparation of 18-acylyohimban-17-ones and their conversion to new heterocyclic yohimbans
J. Donald Albright and Leon Goldman
pp 296 - 300; DOI:
10.1021/jm00249a008
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Ergot alkaloids. Ergolines and related compounds as inhibitors of prolactin release
John M. Cassady, George S. Li, Ernest B. Spitzner, Heinz G. Floss, and James A. Clemens
pp 300 - 307; DOI:
10.1021/jm00249a009
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Inhibition of prolactin by ergoline congeners
Charles F. Barfknecht, David B. Rusterholz, and Jonathan A. Parsons
pp 308 - 312; DOI:
10.1021/jm00249a010
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Descarboxylysergic acid (9,10-didehydro-6-methylergoline)
Nicholas J. Bach, David A. Hall, and Edmund C. Kornfeld
pp 312 - 314; DOI:
10.1021/jm00249a011
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Synthesis and biological activity of some analogs of the gonadotropin releasing hormone
W. Arnold, G. Flouret, R. Morgan, R. Rippel, and W. White
pp 314 - 319; DOI:
10.1021/jm00249a012
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Antigenic determinants of the polypeptide, poly(L-tyrosyl-L-glutamyl-L-alanylglycyl)glycine-1-14C ethyl ester
Brian J. Johnson and Charles Cheng
pp 320 - 322; DOI:
10.1021/jm00249a013
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Angiotensin II analogs. 11. Des-aspartyl-angiotensin II
Eugene C. Jorgensen, Ilona C. Kiraly-Olah, Thomas C. Lee, and Graham C. Windridge
pp 323 - 326; DOI:
10.1021/jm00249a014
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Folic acid antagonists. Methotrexate analogs containing spurious amino acids. Dichlorohomofolic acid
William W. Lee, Abelardo P. Martinez, and Leon Goodman
pp 326 - 330; DOI:
10.1021/jm00249a015
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Structure activity relations. 7. Structure-activity relations of fenamic acids
Hiroshi Terada, Saburo Muraoka, and Toshio Fujita
pp 330 - 334; DOI:
10.1021/jm00249a016
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Synthesis and biological evaluation of some 14-O-acyl derivatives of adriamycin
Federico Arcamone, Giovanni Franceschi, Anacleto Minghetti, Sergio Penco, Silvio Redaelli, Aurelio DiMarco, Anna M. Casazza, Teresa Dasdia, and Giovianna DiFronzo
pp 335 - 337; DOI:
10.1021/jm00249a017
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Steroidal imidazole-1-carboxylic acid esters
Kenneth E. Fahrenholtz, Alfred Boris, Thomas W. Kennedy, and R. W. Kierstead
pp 337 - 342; DOI:
10.1021/jm00249a018
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CNDO [complete neglect of differential overlap]/2 study of the antibacterial activity of penicillins and cephalosporins
W. C. Topp and B. G. Christensen
pp 342 - 347; DOI:
10.1021/jm00249a019
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Experimental antileukemic agents. Coralyne, analogs, and related compounds
Kwang-Yuen Zee-Cheng, Kenneth D. Paull, and C. C. Cheng
pp 347 - 351; DOI:
10.1021/jm00249a020
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9,11-Seco steroids. Attempt to separate biological activities via ring cleavage
Leland J. Chinn, John H. Dygos, Stanley E. Mares, Richard L. Aspinall, and Robert E. Ranney
pp 351 - 354; DOI:
10.1021/jm00249a021
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1,6-Diammonium-2,4-hexadiyne analogs of hexamethonium
Joseph G. Cannon, Lester E. Johnson, John Paul Long, and Sharon Heintz
pp 355 - 358; DOI:
10.1021/jm00249a022
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Use of sodium cyanoborohydride in the preparation of biologically active nitroxides
Gerald M. Rosen
pp 358 - 360; DOI:
10.1021/jm00249a023
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2'-0-Methyl ether of 1-.beta.-D-arabinofuranosylcytosine
John A. Montgomery and Anne G. Laseter
pp 360 - 361; DOI:
10.1021/jm00249a024
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Antiviral agents. 1-Aralkyloxyadenosines
W. M. Shannon, A. Shortnacy, G. Arnett, and J. A. Montgomery
pp 361 - 363; DOI:
10.1021/jm00249a025
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Isosteres of natural phosphates. 2. Synthesis of the monosodium salt of 4-hydroxy-3-oxobutyl-l-phosphonic acid an isostere of dihydroxyacetone phosphate
Stephen L. Goldstein, Diza Braksmayer, Burton E. Tropp, and Robert Engel
pp 363 - 364; DOI:
10.1021/jm00249a026
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Cyclization of lactamimide ketones to imidazo[1,2-.alpha.]azacycloalkanes with hypoglycemic activity
George P. Claxton, J. Martin Grisar, and Norbert L. Wiech
pp 364 - 367; DOI:
10.1021/jm00249a027
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Aryl 5-nitro-2-furyl ketone antifungal agents
S. S. Pelosi and J. E. Gray
pp 367 - 369; DOI:
10.1021/jm00249a028
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Synthesis of 7H-pyrimido [4,5-b] [1,4] thiazines related to 7,8-dihydropteridines of biological importance
Young Ho Kim and Henry G. Mautner
pp 369 - 371; DOI:
10.1021/jm00249a029
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Total synthesis and resolution of terreic acid
John C. Sheehan and Young S. Lo
pp 371 - 372; DOI:
10.1021/jm00249a030
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Synthesis of 2,4-diamino-5-[4-arylthiophenyl]-and 5-[4-arylsulfonylphenyl]pyrimidines as antimalarials
Bijan P. Das and David W. Boykin
pp 372 - 374; DOI:
10.1021/jm00249a031
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Quinazolines and 1,4-benzodiazepines. 64. Comparison of the stereochemistry of diazepam with that of close analogs with marginal biological activity
Leo H. Sternbach, Fred D. Sancilio, and John F. Blount
pp 374 - 377; DOI:
10.1021/jm00249a032
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Determination of the absolute configuration of (+)-2-(6-methoxy-2-naphthyl)propionic acid
J. Riegl, M. L. Maddox, and I. T. Harrison
pp 377 - 378; DOI:
10.1021/jm00249a033
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Anticonvulsant activity of substituted Indolealkylamines
V. K. Agarwal, A. K. Chaturvedi, T. K. Gupta, Surendra S. Parmar, and Benjamin De Boer
pp 378 - 380; DOI:
10.1021/jm00249a034
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Identification of two metabolites of hydralazine from human urine
Sylvai B. Zak, Thomas G. Gilleran, Jerrold Karliner, and George Lukas
pp 381 - 382; DOI:
10.1021/jm00249a035
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Book Reviews

pp 382 - 382; DOI:
10.1021/jm00249a600
PDF

Issue 4


Diarylcyclobutane analogs of diethylstilbestrol
John E. Lawson, Ronnie D. Dennis, Robert F. Majewski, and Duane G. Gallo
pp 383 - 386; DOI:
10.1021/jm00250a001
PDF
Synthesis, estrogenic activity, and electrophilic reactivity of an N-acetoxy-N-acetamido analog of diethylstilbestrol
Helmut Bartsch, Mark Dworkin, James A. Miller, and Elizabeth C. Miller
pp 386 - 389; DOI:
10.1021/jm00250a002
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Total synthesis of bisnorpenicillin V
Jos Hoogmartens, Paul J. Claes, and Hubert Vanderhaeghe
pp 389 - 392; DOI:
10.1021/jm00250a003
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New streptozotocin analogs with improved antileukemic activity
Allan N. Fujiwara, Edward M. Acton, and David W. Henry
pp 392 - 396; DOI:
10.1021/jm00250a004
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Oximes of 3-formylrifamycin SV. Synthesis, antibacterial activity, and other biological properties
Renato Cricchio, Giancarlo Lancini, Giovanni Tamborini, and Piero Sensi
pp 396 - 403; DOI:
10.1021/jm00250a005
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Synthesis, chemistry, and biological activity of 5-thiocyanatopyrimidine nucleosides as potential masked thiols
Tomoako Nagamachi, Jean L. Fourrey, Paul F. Torrence, James A. Waters, and Bernhard Witkop
pp 403 - 406; DOI:
10.1021/jm00250a006
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Synthesis and biological activity of some 8-substituted seleno cyclic nucleotides and related compounds
Shih-Hsi Chu, Chyng-Yann Shiue, and Ming-Yu Chu
pp 406 - 409; DOI:
10.1021/jm00250a007
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Discriminant analysis of the relation between physical properties and the inhibition of monoamine oxidase by aminotetralins and aminoindans
Yvonne C. Martin, James B. Holland, Charles H. Jarboe, and Nicholas Plotnikoff
pp 409 - 413; DOI:
10.1021/jm00250a008
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Mouse liver glyoxalase I inhibition by S-substituted glutathiones
Marian V. Kester, Jon A. Reese, and Scotty J. Norton
pp 413 - 416; DOI:
10.1021/jm00250a009
PDF
Optically active amines. XV. Action of (S)- and (R)-para-substituted amphetamine hydrochlorides and (.alpha.S)- and (.alpha.R)-p-chloronorephedrine and (.alpha.S)- and (.alpha.R)-p-chloronorpseudoephedrine hydrochlorides on the level of 5-hydroxytryptamine and the activity of tryptophan hydroxylase in rat brain
Howard E. Smith, Elizabeth P. Burrows, Jeffrey D. Miano, Charles D. Mount, Elaine Sanders-Bush, and Fridolin Sulser
pp 416 - 421; DOI:
10.1021/jm00250a010
PDF
Synthesis and antireserpine activity of peptides of L-dopa
Arthur M. Felix, Donald P. Winter, Su-Sun Wang, Irina D. Kulesha, William R. Pool, Dorothy L. Hane, and Herbert Sheppard
pp 422 - 426; DOI:
10.1021/jm00250a011
PDF
.alpha.-Methyldopamine derivatives. Synthesis and pharmacology
Robert J. Borgman, Michael R. Baylor, Joseph J. McPhillips, and Robert E. Stitzel
pp 427 - 430; DOI:
10.1021/jm00250a012
PDF
Synthesis of analogs of [8-isoleucine]angiotensin II with variations in position 1
Mahesh C. Khosla, Madeline M. Hall, Robert R. Smeby, and F. Merlin Bumpus
pp 431 - 433; DOI:
10.1021/jm00250a013
PDF
Thyroxine analogs. 22. Thyromimetic activity of halogen-free derivatives of 3,5-dimethyl-L-thyronine
Eugene C. Jorgensen, Wallace J. Murray, and Paul Block
pp 434 - 439; DOI:
10.1021/jm00250a014
PDF
Molecular orbital studies on the conformation of hallucinogenic indolealkylamines and related compounds. Isolated molecules and the solvent effect
B. Pullman, Ph. Courriere, and H. Berthod
pp 439 - 447; DOI:
10.1021/jm00250a015
PDF
Inhibitors of polyamine biosynthesis. 1. .alpha.-Methyl-(+-)-ornithine, an inhibitor of ornithine decarboxylase
Mahmoud M. Abdel-Monem, Nancy E. Newton, and Charles E. Weeks
pp 447 - 451; DOI:
10.1021/jm00250a016
PDF
Nitrofurfuryl heterocycles. 12. 4-Amino-6-(5-nitro-2-furyl)isoxazolo[5,4-d]pyrimidines and 4-amino-2-(5-nitro-2-furyl)pyrimido[4,5-d]pyrimidines
Homer A. Burch, Louis E. Benjamin, H. Eric Russell, and Raymond Freedman
pp 451 - 453; DOI:
10.1021/jm00250a017
PDF
Structure-activity studies on narcotic antagonists. 1. N-Substituted ethyl 3-phenylpyrrolidine-3-carboxylates and ethyl 3-phenylnipecotates
Ronald L. Jacoby, Karl A. Nieforth, and Robert E. Willette
pp 453 - 455; DOI:
10.1021/jm00250a018
PDF
Cyclopentane analog of muscarone
Fulvio Gualtieri, Mario Giannella, Carlo Melchiorre, and Maria Pigini
pp 455 - 457; DOI:
10.1021/jm00250a019
PDF
Carbocyclic analogs of muscarine. Oxidation of desethermuscarine to desethermuscarone
Richard S. Givens and Donald R. Rademacher
pp 457 - 459; DOI:
10.1021/jm00250a020
PDF
Synthesis and central nervous system activity of 1,2,3,4-tetrahydro-1-amino-4-phenylnaphthalenes
Lewis A. Walter, Wei K. Chang, Joanne Kenney, and Irina D. Kulecha
pp 459 - 463; DOI:
10.1021/jm00250a021
PDF
Synthesis and pharmacological properties of 5a,6,7,8,9,10,10a,11-octahydrobenzo[b]cyclohepta[e][1,4]thiazine derivatives
Franco M. Moracci, Felice Liberatore, Paolo Marchini, Gaetano Liso, and Mario Cardellini
pp 463 - 465; DOI:
10.1021/jm00250a022
PDF
Procedure for preparing tritium-labeled tertiary amines. Synthesis of endo-etheno-6,7,8,14-tetrahydrooripavine-6,14-3H derivatives
John W. Lewis, Michael J. Rance, and G. Raymond Young
pp 465 - 466; DOI:
10.1021/jm00250a023
PDF
Synthesis and biological activity of 2'-amino-2'-deoxy-5-fluorouridine
R. A. Sharma, M. Bobek, and A. Bloch
pp 466 - 468; DOI:
10.1021/jm00250a024
PDF
Antimalarials. 2. .alpha.-Di-n-butylaminomethyl-2-(p-chlorophenyl)-5-quinazolinemethanol
Philip A. Cruickshank and William E. Hymans
pp 468 - 469; DOI:
10.1021/jm00250a025
PDF
Antimicrobial activity of 8-deazafolic acid
Joseph I. DeGraw, Roy L. Kisliuk, Yvette Gaumont, and Charles M. Baugh
pp 470 - 471; DOI:
10.1021/jm00250a026
PDF
Histamine N-methyltransferase. Inhibition and potentiation by trans- and cis-1,5-diphenyl-3-dimethylaminopyrrolidine
Patrick E. Hanna and Ronald T. Borchardt
pp 471 - 473; DOI:
10.1021/jm00250a027
PDF
Synthesis of some trinucleoside monophosphates of biological interest
Eric J. Norman and Joseph Nagyvary
pp 473 - 475; DOI:
10.1021/jm00250a028
PDF
9-Nor-.DELTA.8-tetrahydrocannabinol, a cannabinoid of metabolic interest
Raymond S. Wilson and Everette L. May
pp 475 - 476; DOI:
10.1021/jm00250a029
PDF
Book Reviews

pp 476 - 476; DOI:
10.1021/jm00250a600
PDF

Issue 5


Quantitative structure-activity relations in anticancer agents. Activity of selected nitrosoureas against a solid tumor, the Lewis lung carcinoma
John A. Montgomery, Joseph G. Mayo, and Corwin Hansch
pp 477 - 480; DOI:
10.1021/jm00251a001
PDF
Antifilarial agents. Diazabicyclooctanes and diazabicycloheptanes as bridged analogs of diethylcarbamazine
Priscilla A. Sturm, David W. Henry, P. E. Thompson, J. B. Zeigler, and J. W. McCall
pp 481 - 487; DOI:
10.1021/jm00251a002
PDF
2,4,5-Trimethylpyrrole-3-carboxylic acid esters of various alkaloids
James A. Waters, Cyrus R. Creveling, and Bernhard Witkop
pp 488 - 491; DOI:
10.1021/jm00251a003
PDF
New nonsteroidal antiinflammatory agent. 3. Analogs of 2-substituted 5-benzothiazoleacetic acids and their derivatives
Hiroki Miyamatsu, Shinji Ueno, Mitsuhiro Shimizu, Jinichi Hosono, Masazumi Tomari, Keiichi Seida, Tadayuki Suzuki, and Jin Wada
pp 491 - 496; DOI:
10.1021/jm00251a004
PDF
Quinuclidine chemistry. 2. Synthesis and antiinflammatory properties of 2-substituted benzhydryl-3-quinuclidinols
E. J. Warawa, N. J. Mueller, and R. Jules
pp 497 - 501; DOI:
10.1021/jm00251a005
PDF
Molecular orbital studies on the mechanism of drug-receptor interaction. 1. Adrenergic drugs. Conformation and reactivity of isoproterenol and 1-(p-nitrophenyl)-2-isopropylaminoethanol
Carlo Petrongolo, Jacopo Tomasi, Bruno Macchia, and Franco Macchia
pp 501 - 507; DOI:
10.1021/jm00251a006
PDF
.beta.-Adrenoceptor studies. 1. In vitro .beta.-adrenergic blocking, antiarrhythmic, and local anesthetic activities of a new series of aromatic bis(2-hydroxy-3-isopropylaminopropyl) ethers
J. Zaagsma and W. Th. Nauta
pp 507 - 513; DOI:
10.1021/jm00251a007
PDF
Bronchodilators giving reduced cardiovascular effects. Relative biological activities of the four isomers of 1-(3,4-dihydroxyphenyl)-2-isopropylaminobutanol
Michael J. Mardle, Harry Smith, Barbara A. Spicer, and Robert H. Poyser
pp 513 - 516; DOI:
10.1021/jm00251a008
PDF
Naphthothiophenes. 4. Preparation of multisubstituted 4-naphtho[2,1-b]thiophenemethanols and the effect of side chain modification on antimalarial activity of 8-trifluoromethyl-4-naphtho[2,1-b] thiophenemethanols
Bijan P. Das, Merrill E. Nuss, and David W. Boykin
pp 516 - 519; DOI:
10.1021/jm00251a009
PDF
Antimalarials. 6. Synthesis, antimalarial activity, and configurations of racemic .alpha.-(2-piperidyl)-4-pyridinemethanols
M. P. LaMontagne, A. Markovac, and P. Blumbergs
pp 519 - 523; DOI:
10.1021/jm00251a010
PDF
Substituent effects upon the base hydrolysis of penicillins and cephalosporins. Competitive intramolecular nucleophilic amino attack in cephalosporins
Joseph M. Indelicato, Theresa T. Norvilas, Ralph R. Pfeiffer, William J. Wheeler, and William L. Wilham
pp 523 - 527; DOI:
10.1021/jm00251a011
PDF
Effect of 6-.alpha. substitution in penicillins and 7-.alpha. substitution in cephalosporins upon .beta.-lactam reactivity
Joseph M. Indelicato and William L. Wilham
pp 528 - 529; DOI:
10.1021/jm00251a012
PDF
Derivatives of 3,4-dihydrocarbostyril as .beta.-adrenergic blocking agents
Kazuyuki Nakagawa, Nanami Murakami, Shiro Yoshizaki, Michiaki Tominaga, Hideo Mori, Youichi Yabuuchi, and Shigeyuki Shintani
pp 529 - 533; DOI:
10.1021/jm00251a013
PDF
Substructural analysis. Novel approach to the problem of drug design
Richard D. Cramer, George Redl, and Charles E. Berkoff
pp 533 - 535; DOI:
10.1021/jm00251a014
PDF
Preparation and antitumor activity of 4'-thio analogs of 2,2'-anhydro-1-.beta.-D-arabinofuranosylcytosine
N. Ototani and Roy L. Whistler
pp 535 - 537; DOI:
10.1021/jm00251a015
PDF
Hydroxyproline analogs of bradykinin
John Morrow Stewart, James W. Ryan, and A. H. Brady
pp 537 - 539; DOI:
10.1021/jm00251a016
PDF
Analogs of the abortifacient aminoglutethimide
Rolf Paul, Richard P. Williams, and Elliott Cohen
pp 539 - 541; DOI:
10.1021/jm00251a017
PDF
.beta.-Lactams. 35. Antibacterial activity of monocyclic .beta.-lactams
Ajay K. Bose, M. S. Manhas, J. C. Kapur, S. D. Sharma, and S. G. Amin
pp 541 - 544; DOI:
10.1021/jm00251a018
PDF
Synthesis and antiinflammatory activity of a series of 2-aroyl-1,1a,2,6b-tetrahydrocycloprop[b]indole-1-carboxylic acids
William J. Welstead, Harold F. Stauffer, and Lawrence F. Sancilio
pp 544 - 547; DOI:
10.1021/jm00251a019
PDF
Efficient and selective method for the synthesis of 2-(4-fluorophenyl)-1-(2-hydroxyethyl)-5-nitroimidazole (flunidazole)
Edward J. J. Grabowski, Thomas M. H. Liu, Ludwig Salce, and Erwin F. Schoenewaldt
pp 547 - 549; DOI:
10.1021/jm00251a020
PDF
Synthesis and biological properties of 5-aryl-4H-1,2,4-thiadiazine 1,1-dioxides
W. L. Matier, W. T. Comer, and A. W. Gomoll
pp 549 - 552; DOI:
10.1021/jm00251a021
PDF
Synthesis and antifolate activity of 10-deazaminopterin
Joseph I. DeGraw, Roy L. Kisliuk, Yvette Gaumont, Charles M. Baugh, and M. G. Nair
pp 552 - 553; DOI:
10.1021/jm00251a022
PDF
Synthesis of 1-deaza-N10-methylfolic acid and related compounds
Robert D. Elliott, Carroll Temple, and John A. Montgomery
pp 553 - 555; DOI:
10.1021/jm00251a023
PDF
Ethambutol. Synthesis of an unsaturated analog
Luigi Bernardi, Maurizio Foglio, and Aldemio Temperilli
pp 555 - 556; DOI:
10.1021/jm00251a024
PDF
Synthesis of pure p-chlorophenyl-L-alanine form L-phenylalanine
Richard A. Houghten and Henry Rapoport
pp 556 - 558; DOI:
10.1021/jm00251a025
PDF
Potential bioreductive alkylating agents. 3. Synthesis and antineoplastic activity of acetoxymethyl and corresponding ethyl carbamate derivatives of benzoquinones
Ai Jeng Lin, Charles W. Shansky, and Alan C. Sartorelli
pp 558 - 561; DOI:
10.1021/jm00251a026
PDF
Heterocyclic steroids. 5. Sulfur, selenium, and tellurium 5.alpha.-androstane derivatives and their 7.alpha.-methylated congeners
Galal Zanati, Gunhild Gaare, and Manfred E. Wolff
pp 561 - 563; DOI:
10.1021/jm00251a027
PDF
Synthesis and antimalarial activity of anthracene amino alcohols
Eugene L. Stogryn
pp 563 - 565; DOI:
10.1021/jm00251a028
PDF
Rigid amino acids related to .alpha.-methyldopa
Joseph G. Cannon, John P. O'Donnell, John P. Rosazza, and Charles R. Hoppin
pp 565 - 568; DOI:
10.1021/jm00251a029
PDF
Book Reviews

pp 568 - 568; DOI:
10.1021/jm00251a600
PDF

Issue 6


Hypothalamic hormones. 55. Analogs of the luteinizing hormone-releasing hormone to study conformational aspects of the aromatic amino acid moieties and inhibition
John Humphries, George Fisher, Yieh-Ping Wan, Karl Folkers, and Cyril Y. Bowers
pp 569 - 571; DOI:
10.1021/jm00252a001
PDF
Aminobenzoic acid diuretics. 6. 4-Substituted 3-alkylthio-5-sulfamoylbenzoic and 5-sulfamoylthiosalicylic acids
Peter W. Feit, Ole B. Tvaermose Nielsen, and Herta Bruun
pp 572 - 578; DOI:
10.1021/jm00252a002
PDF
Puromycin analogs. Ribosomal binding with diastereomeric carbocyclic puromycin analogs
Robert Vince and Susan Daluge
pp 578 - 583; DOI:
10.1021/jm00252a003
PDF
Ab initio calculations on large molecules using molecular fragments. Lincomycin model studies
Lester L. Shipman, Ralph E. Christoffersen, and B. Vernon Cheney
pp 583 - 590; DOI:
10.1021/jm00252a004
PDF
Ab initio calculations on large molecules using molecular fragments. Structural correlations between natural substrate moieties and some antibiotic inhibitors of peptidyl transferase
B. Vernon Cheney
pp 590 - 599; DOI:
10.1021/jm00252a005
PDF
Microbial transformations of antitumor compounds. 1. Conversion of acronycine to 9-hydroxyacronycine by Cunninghamella echinulata
Ronald E. Betts, David E. Walters, and John P. Rosazza
pp 599 - 602; DOI:
10.1021/jm00252a006
PDF
Chemistry of adamantane. VII. Adamantanealkanamines as potential antidepressant and anti-Parkinson agents
Jiban K. Chakrabarti, Michael J. Foulis, Terrence M. Hotten, Stephen S. Szinai, and Alec Todd
pp 602 - 609; DOI:
10.1021/jm00252a007
PDF
Synthesis and structure-activity relations of a series of antibacterially active 5-(5-nitro-2-furfurylidene)thiazolones, 5-(5-nitro-2-furylpropenylidene)thiazolones, and 6-(5-nitro-2-furyl)-4H-1,3-thiazinones
Eva B. Akerblom
pp 609 - 615; DOI:
10.1021/jm00252a008
PDF
Synthesis of potential antimalarial agents. Preparation of some 6-amino-5,8-dimethoxyquinolines and the corresponding 6-amino-5,8-quinolinediones
Carroll Temple, Jerry D. Rose, and John A. Montgomery
pp 615 - 619; DOI:
10.1021/jm00252a009
PDF
8-(.omega.-Aminoalkylamino)quinolines as potential prophylactic antimalarials
William P. Wetter and C. DeWitt Blanton
pp 620 - 624; DOI:
10.1021/jm00252a010
PDF
Synthesis and pharmacological evaluation of 2,3-dihydro-1H-thieno[2,3-e][1,4]diazepines
Francis J. Tinney, Joseph P. Sanchez, and Joan A. Nogas
pp 624 - 630; DOI:
10.1021/jm00252a011
PDF
Potential antitumor agents. 9. 2-Formyl(m-amino)phenylpyridine thiosemicarbazones
Krishna C. Agrawal, Ai Jeng Lin, Barbara A. Booth, J. Randall Wheaton, and Alan C. Sartorelli
pp 631 - 635; DOI:
10.1021/jm00252a012
PDF
Synthesis and antiinflammatory activity of some 1-alkyl-4-phenylpyrido[2,3-d]pyrimidin-2(1H)-ones
G. E. Hardtmann, B. Huegi, G. Koletar, S. Kroin, H. Ott, J. W. Perrine, and E. I. Takesue
pp 636 - 639; DOI:
10.1021/jm00252a013
PDF
Substituted azopurines. 1. Synthesis of 8,8'-dioxo-6,6'-azopurine
Joseph R. Davis, Arun L. Jadhav, and Jawed Fareed
pp 639 - 642; DOI:
10.1021/jm00252a014
PDF
Synthesis and enzymic activity of 1,2,4-triazole-3-carboxamide 6'-deoxyhomoribonucleoside-6'-phosphonic acid and related compounds
Mercedes Fuertes, Joseph T. Witkowski, David G. Streeter, and Roland K. Robins
pp 642 - 645; DOI:
10.1021/jm00252a015
PDF
3-Substituted 5,7-dimethylpyrazolo[1,5-a]pyrimidines, 3',5'-cyclic AMP phosphodiesterase inhibitors
Thomas Novinson, Ruth Hanson, M. K. Dimmitt, Lionel N. Simon, Roland K. Robins, and Darrell E. O'Brien
pp 645 - 648; DOI:
10.1021/jm00252a016
PDF
Fibrin-stabilizing factor inhibitors. 11. Monodansylated weak aliphatic diamines
Christine Ljunggren, Kurt J. Hoffmann, Pal Stenberg, Uno Svensson, J. Lars. G. Nilsson, Ann Hartkoorn, and Ragnar Lunden
pp 649 - 651; DOI:
10.1021/jm00252a017
PDF
10-Alkyl- and 10-aminoalkyl-2,2'-bis(trifluoromethyl)-3,10'-biphenothiazines
Kuppuswamy Nagarajan, Joy David, and Agasaladinni N. Goud
pp 652 - 653; DOI:
10.1021/jm00252a018
PDF
Microbial hydroxylation of acronycine
D. R. Brannon, D. R. Horton, and Gordon H. Svoboda
pp 653 - 654; DOI:
10.1021/jm00252a019
PDF
4-(and 5-)(2-Thienyl)-1-naphthaleneacetic acids as antiinflammatory agents
James S. Kaltenbronn and Tae O. Rhee
pp 654 - 657; DOI:
10.1021/jm00252a020
PDF
6-Phenyl-6-propionoxyperhydrobenzo[c]quinolizines as potential analgetics
M. E. Rogers and J. Sam
pp 657 - 659; DOI:
10.1021/jm00252a021
PDF
Total synthesis of the antitumor antibiotic daunorubicin. Coupling of the sugar and aglycone
Edward M. Acton, Allan N. Fujiwara, and David W. Henry
pp 659 - 660; DOI:
10.1021/jm00252a022
PDF
Book Reviews

pp 660 - 660; DOI:
10.1021/jm00252a600
PDF

Issue 7


Quantitative structure-activity relation of reversible dihydrofolate reductase inhibitors. Diaminotriazines
Corwin Hansch and Carlo Silipo
pp 661 - 667; DOI:
10.1021/jm00253a001
PDF
Potential bioreductive alkylating agents. 4. Inhibition of coenzyme Q enzyme systems by lipoidal benzoquinone and naphthoquinone derivatives
Ai Jen Lin, Ronald S. Pardini, Brian J. Lillis, and Alan C. Sartorelli
pp 668 - 672; DOI:
10.1021/jm00253a002
PDF
Cysteine scavengers. 2. Synthetic .alpha.-methylenebutyrolactones as potential tumor inhibitors
Andre Rosowsky, Nickolas Papathanasopoulos, Herbert Lazarus, George E. Foley, and Edward J. Modest
pp 672 - 676; DOI:
10.1021/jm00253a003
PDF
Potential antimalarials. 8. 10-Substituted 9-phenanthrenemethanols
Lee C. Washburn and D. E. Pearson
pp 676 - 682; DOI:
10.1021/jm00253a004
PDF
Synthesis of analogs of 6-arylthio-, 6-arylsulfinyl-, and 6-arylsulfonyl-2,4-diaminoquinazolines as potential antimalarial agents
John B. Hynes, Wallace T. Ashton, Hugh G. Merriman, and Flornoy C. Walker
pp 682 - 684; DOI:
10.1021/jm00253a005
PDF
Quinoline derivatives as antiallergy agents
Charles M. Hall, Herbert G. Johnson, and John B. Wright
pp 685 - 690; DOI:
10.1021/jm00253a006
PDF
D-(R)- and L-(S)-3-Alkylaminopyrrolidino-substituted dihydrodibenzo[b,f]- and -[b,e]thiepins, xanthenes, and diphenylmethanes
Donald T. Witiak, Song Y. Hsu, James E. Ollmann, Robert K. Griffith, Shiv K. Seth, and Michael C. Gerald
pp 690 - 696; DOI:
10.1021/jm00253a007
PDF
Synthesis of L-1-deoxyfluoroglycerol and its 3-phosphate ester. Effects of the L and D enantiomers in BDF1 mice
Thomas P. Fondy, Richard W. Pero, Katherine L. Karker, Gurdev S. Ghangas, and Frederick H. Batzold
pp 697 - 702; DOI:
10.1021/jm00253a008
PDF
Amine functions of reduced basicity. Hypoglycemic and natriuretic .alpha.-alkoxybenzylamidoximes, amidines, and cycloamidines
Denis M. Bailey, C. George DeGrazia, David Wood, James Siggins, Homer R. Harding, Gordon O. Potts, and Thomas W. Skulan
pp 702 - 708; DOI:
10.1021/jm00253a009
PDF
Blood glucose lowering sulfonamides with asymmetric carbon atoms. 1
C. Rufer, H. Biere, H. Ahrens, O. Loge, and E. Schroeder
pp 708 - 715; DOI:
10.1021/jm00253a010
PDF
Blood glucose lowering sulfonamides with asymmetric carbon atoms. 2
H. Biere, C. Rufer, H. Ahrens, O. Loge, and E. Schroeder
pp 716 - 721; DOI:
10.1021/jm00253a011
PDF
Hypolipidemic substituted 1,3-benzodioxole-2-carboxylates
J. Martin Grisar, George P. Claxton, Roger A. Parker, Frank P. Palopoli, and Takashi Kariya
pp 721 - 725; DOI:
10.1021/jm00253a012
PDF
3-Aryl-3-hydroxyquinolizidines with potential hypotensive, antidepressant, and analgetic activity
M. E. Rogers, Joseph Sam, and N. P. Plotnikoff
pp 726 - 729; DOI:
10.1021/jm00253a013
PDF
Structure-activity relations of the mitomycins and certain synthetic analogs
William A. Remers and Cynthia S. Schepman
pp 729 - 732; DOI:
10.1021/jm00253a014
PDF
Analgesics. 1. Selected 5-substituted 5-propionoxybarbituric acids
Julius A. Vida, Carlos M. Samour, Mary H. O'Dea, Theodore S. T. Wang, William R. Wilber, and John F. Reinhard
pp 732 - 736; DOI:
10.1021/jm00253a015
PDF
Benzamidopiperidines. 2. Heterocyclic compounds related to indoramin
John L. Archibald and Gerald A. Benke
pp 736 - 739; DOI:
10.1021/jm00253a016
PDF
Benzamidopiperidines. 3. Carbocyclic derivatives related to indoramin
John L. Archibald, Paula Fairbrother, and John L. Jackson
pp 739 - 744; DOI:
10.1021/jm00253a017
PDF
1,4-Bis(2-indol-3-ylethyl)piperazines
John L. Archibald and Meier E. Freed
pp 745 - 747; DOI:
10.1021/jm00253a018
PDF
Chemical conversion of the psychotomimetic amine 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane to 5-hydroxy-2,6-dimethylindole
Jonathan S. Zweig and Neal Castagnoli
pp 747 - 749; DOI:
10.1021/jm00253a019
PDF
Quantum statistical calculation for the correlation of biological activity and chemical structure. 2. Drug-membrane penetrations
Teng K. Lin
pp 749 - 751; DOI:
10.1021/jm00253a020
PDF
Quantum statistical calculation for the correlation of biological activity and chemical structure. 3. Disopyramide phosphate and related compounds as antiarrhythmic agents
Teng K. Lin, Y. W. Chien, R. R. Dean, J. E. Dutt, H. W. Sause, C. H. Yen, and P. K. Yonan
pp 751 - 753; DOI:
10.1021/jm00253a021
PDF
Quantitative structure-activity analysis in a series of antimycotically active N-hydroxypyridones
Walter Dittmar, Eike Druckrey, and Hansjoerg Urbach
pp 753 - 756; DOI:
10.1021/jm00253a022
PDF
Nitrofurans with high renal excretion
Eva B. Akerblom
pp 756 - 758; DOI:
10.1021/jm00253a023
PDF
Potential anticancer agents. 10. Synthesis of N-[4-[[(2,4-diamino-7-pteridyl)methyl]-N10-methylamino]benzoyl)glutamic acid
Dan C. Suster, Liviu V. Feyns, Gheorghe Ciustea, Georgeta Botez, Vasile Dobre, Ralph Bick, and Ion Niculescu-Duvaz
pp 758 - 760; DOI:
10.1021/jm00253a024
PDF
In vitro and in vivo activity of certain thiosemicarbazones against Trypanosoma cruzi
H. Robert Wilson, Ganapathi R. Revankar, and Richard L. Tolman
pp 760 - 761; DOI:
10.1021/jm00253a025
PDF
Potential antileprotic agents. 3. Inhibition of mycobacterial dihydrofolic reductase by 2,4-diamino-5-methyl-6-alkylquinazolines
J. I. DeGraw, V. H. Brown, W. T. Colwell, and N. E. Morrison
pp 762 - 764; DOI:
10.1021/jm00253a026
PDF
Thymidine 5' variants as inhibitors of thymidylate kinase
J. J. Baker, P. Mellish, C. Riddle, A. R. Somerville, and J. R. Tittensor
pp 764 - 766; DOI:
10.1021/jm00253a027
PDF
3-Onium derivatives of 1,4-benzodiazepin-2-ones with tertiary organic bases
T. Kovac, F. Kajfez, V. Sunjic, and M. Oklobdzija
pp 766 - 769; DOI:
10.1021/jm00253a028
PDF
Formation of germine 3,15-diacetate via the isomerization of germine 3,16-diacetate
Edward M. Cohen, Rezso Aczel, Mary L. Torchiana, Roger Tull, and Edward J. J. Grabowski
pp 769 - 770; DOI:
10.1021/jm00253a029
PDF
Polymeric salicylate derivatives
Abraham Havron, Ben-Z. Weiner, and Albert Zilkha
pp 770 - 772; DOI:
10.1021/jm00253a030
PDF
Immunosuppressive and antiinflammatory activities of cinanserin and its analogs
Robert C. Millonig, Blanche J. Amrein, Joel Kirschbaum, and Sidney M. Hess
pp 772 - 775; DOI:
10.1021/jm00253a031
PDF
Antiparasitic thiocyanatobenzothiazoles
Robert J. Alaimo, Stanford S. Pelosi, Christopher J. Hatton, and Joseph E. Gray
pp 775 - 776; DOI:
10.1021/jm00253a032
PDF
Optimization of alkyl modifications by Fibonacci search
Thomas M. Bustard
pp 777 - 778; DOI:
10.1021/jm00253a033
PDF
Preparation of morphine-6-3H and its isotopic stability in man and in rat
Jack Fishman, Baiba Norton, Mary L. Cotter, and Elliot F. Hahn
pp 778 - 781; DOI:
10.1021/jm00253a034
PDF
Synthesis and some pharmacological properties of 8-L-homoarginine-vasopressin and of 1-deamino-8-L-homoarginine-vasopressin
Gunnar Lindeberg, Miklos Bodanszky, Margot Acosta, and Wilbur H. Sawyer
pp 781 - 783; DOI:
10.1021/jm00253a035
PDF
Book Reviews

pp 783 - 784; DOI:
10.1021/jm00253a600
PDF

Issue 8


Boron hydride derivatives for neutron capture therapy. Antibody approach
Hou S. Wong, Eugene I. Tolpin, and William N. Lipscomb
pp 785 - 791; DOI:
10.1021/jm00254a001
PDF
Binding studies of boron hydride derivatives to proteins for neutron capture therapy
Eugene I. Tolpin, Hou S. Wong, and William N. Lipscomb
pp 792 - 796; DOI:
10.1021/jm00254a002
PDF
Protein-binding polyhedral boranes. 1
R. L. Sneath, A. H. Soloway, and A. S. Dey
pp 796 - 799; DOI:
10.1021/jm00254a003
PDF
Application of the sequential simplex method in designing drug analogs
Ferenc Darvas
pp 799 - 804; DOI:
10.1021/jm00254a004
PDF
Conformational analysis of acridan derivatives by nuclear magnetic resonance spectroscopy. Relation between conformation and pharmacological activity
Manvendra B. Shambhu, R. Rao Koganty, and George A. Digenis
pp 805 - 809; DOI:
10.1021/jm00254a005
PDF
Hydrogen bond breaking potency of fluorocarbon anesthetics
Therese Di Paolo and C. Sandorfy
pp 809 - 814; DOI:
10.1021/jm00254a006
PDF
Theoretical approach to structure-activity relations of chloramphenicol and congeners
Hans D. Hoeltje and Lemont B. Kier
pp 814 - 819; DOI:
10.1021/jm00254a007
PDF
.beta.-Amino ketones. Synthesis and some biological activities in mice of 3,3-dialkyl-1,2,3,4-tetrahydro-4-quinolinones and related Mannich bases
Aspi B. Daruwala, James E. Gearien, William J. Dunn, Phillipe S. Benoit, and Ludwig Bauer
pp 819 - 824; DOI:
10.1021/jm00254a008
PDF
Antifungal activity of bischelates of 5-, 7-, and 5,7-halogenated 8-quinolinols with copper(II). Determination of approximate dimensions of the long and short axes of the pores in the fungal spore wall
Herman Gershon
pp 824 - 827; DOI:
10.1021/jm00254a009
PDF
Antiviral agents. Chemical modifications of a disulfide antibiotic, acetylaranotin
K. C. Murdock
pp 827 - 835; DOI:
10.1021/jm00254a010
PDF
Structure and antischistosomal activity in the nitrofurylvinyl and the niridazole series. Noninterchangeability of the nitroheterocyclic rings
Youlin Lin, Peter B. Hulbert, Ernest Bueding, and Cecil H. Robinson
pp 835 - 840; DOI:
10.1021/jm00254a011
PDF
Synthesis of alkyl-substituted .alpha.,.beta.-unsaturated .gamma.-lactones as potential antitumor agents
Gary A. Howie, Peter E. Manni, and John M. Cassady
pp 840 - 843; DOI:
10.1021/jm00254a012
PDF
Hypothalamic hormones. 54. Synthesis and some biological activities of substance P
George H. Fisher, John Humphries, Karl Folkers, Bengt Pernow, and Cyril Y. Bowers
pp 843 - 846; DOI:
10.1021/jm00254a013
PDF
Synthesis and hypocholesterolemic activities of eritadenine derivatives
Kentaro Okumura, Kazuo Matsumoto, Masaharu Fukamizu, Harunori Yasuo, Yoshihiko Taguchi, Yukio Sugihara, Ichizo Inoue, Masahiko Seto, Yasuhiko Sato, and et al.
pp 846 - 855; DOI:
10.1021/jm00254a014
PDF
Binding to deoxyribonucleic acid and inhibition of ribonucleic acid polymerase by analogs of chloroquine
Victor E. Marquez, Joseph W. Cranston, Raymond W. Ruddon, and Joseph H. Burckhalter
pp 856 - 862; DOI:
10.1021/jm00254a015
PDF
Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 1. Modification of the amino acid portion of S-adenosylhomocysteine
Ronald T. Borchardt and Yih Shiong Wu
pp 862 - 868; DOI:
10.1021/jm00254a016
PDF
Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 2. Modification of the base portion of S-adenosylhomocysteine
Ronald T. Borchardt, Joan A. Huber, and Yih Shiong Wu
pp 868 - 873; DOI:
10.1021/jm00254a017
PDF
Four cyclic disulfide pentapeptides possessing the ring of isotocin and glumitocin
Clark W. Smith, Victor J. Hruby, and Martha F. Ferger
pp 873 - 876; DOI:
10.1021/jm00254a018
PDF
Stereochemical aspects and metabolite formation in the in vivo metabolism of the psychotomimetic amine, 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane
S. B. Matin, P. S. Callery, J. S. Zweig, A. O'Brien, R. Rapoport, and N. Castagnoli
pp 877 - 882; DOI:
10.1021/jm00254a019
PDF
Bis basic-substituted polycyclic aromatic compounds. New class of antiviral agents. 2. Tilorone and related bis-basic ethers of fluorenone, fluorenol, and fluorene
Edwin R. Andrews, Robert W. Fleming, J. Martin Grisar, James C. Kihm, David L. Wenstrup, and Gerald D. Mayer
pp 882 - 886; DOI:
10.1021/jm00254a020
PDF
Bis basic-substituted polycyclic aromatic compounds. New class of antiviral agents. 3. 2,7-Bis(aminoacyl)fluorenes and -fluorenones
William L. Albrecht, Robert W. Fleming, Stephen W. Horgan, James C. Kihm, and Gerald D. Mayer
pp 886 - 889; DOI:
10.1021/jm00254a021
PDF
Bis basic-substituted polycyclic aromatic compounds. New class of antiviral agents. 4. Bis basic sulfonamides of anthraquinone
J. Martin Grisar, Kenneth R. Hickey, Robert W. Fleming, and Gerald D. Mayer
pp 890 - 893; DOI:
10.1021/jm00254a022
PDF
Coenzyme Q. 167. Antimetabolites of coenzyme Q. 19. Synthesis and bioassays of new dimethoxyalkylmercapto-1,4-benzoquinones
Ronald J. Wikholm, Yoshifumi Iwamoto, Conny B. Bogentoft, Thomas H. Porter, and Karl Folkers
pp 893 - 896; DOI:
10.1021/jm00254a023
PDF
Antineoplastic agents. 36. Acetylenic carrier groups
George R. Pettit and Edris I. Saldana
pp 896 - 898; DOI:
10.1021/jm00254a024
PDF
Quantitative reexamination of structure-activity relations in the .DELTA.6-6-substituted progesterone series
Manfred E. Wolff and Corwin Hansch
pp 898 - 900; DOI:
10.1021/jm00254a025
PDF
Radioprotective activity of p-aminopropiophenone. Structure-activity investigation
Thomas J. Fitzgerald, John Doull, and Frederick G. DeFeo
pp 900 - 902; DOI:
10.1021/jm00254a026
PDF
Synthesis of seleno-toluidine blue
John T. Groves, S. Martin Lindenauer, B. J. Haywood, J. A. Knol, and Jerome S. Schultz
pp 902 - 904; DOI:
10.1021/jm00254a027
PDF
Centrally acting muscle relaxants. Isomeric 9,10-dihydroxy-1,2,3,4,4a,9,10,10a(trans-4a,10a)-octahydrophenanthrenes and their carbamate esters
Wendel L. Nelson and Bob E. Sherwood
pp 904 - 907; DOI:
10.1021/jm00254a028
PDF
Importance of the nitrogen lone electron pair orientation in stereospecific opiates
B. Belleau, T. Conway, F. R. Ahmed, and A. D. Hardy
pp 907 - 908; DOI:
10.1021/jm00254a029
PDF
Clastic binding on the opiate receptor
B. Belleau and P. Morgan
pp 908 - 909; DOI:
10.1021/jm00254a030
PDF
Book Reviews

pp 910 - 910; DOI:
10.1021/jm00254a600
PDF

Issue 9


Prostaglandin nomenclature
Norman A. Nelson
pp 911 - 918; DOI:
10.1021/jm00255a001
PDF
Chemoimmunotherapy of cancer. 1
A. H. Soloway, I. Agranat, A. R. Chase, R. E. Hernandez, E. S. Kimball, T. Cascieri, and C. H. Cox
pp 918 - 922; DOI:
10.1021/jm00255a002
PDF
Potential antitumor agents. 14. Acridylmethanesulfonanilides
Bruce F. Cain, Ralph N. Seelye, and Graham J. Atwell
pp 922 - 930; DOI:
10.1021/jm00255a003
PDF
Potential antitumor agents. 15. Bisquaternary salts
Graham J. Atwell and Bruce F. Cain
pp 930 - 934; DOI:
10.1021/jm00255a004
PDF
Potential antitumor agents. 11. Inhibitors of alkaline phosphatase, an enzyme involved in the resistance of neoplastic cells to 6-thiopurines
Krishna C. Agrawal, Men H. Lee, Barbara A. Booth, E. Colleen Moore, and Alan C. Sartorelli
pp 934 - 938; DOI:
10.1021/jm00255a005
PDF
Conformational requirements of substrate and inhibitor on acetylcholinesterase
George H. Cocolas, J. Gregory Cranford, and Hye Sook Choi
pp 938 - 943; DOI:
10.1021/jm00255a006
PDF
Inhibition of mammalian dihydrofolate reductase by selected 2,4-diaminoquinazolines and related compounds
W. E. Richter and J. J. McCormack
pp 943 - 947; DOI:
10.1021/jm00255a007
PDF
Rifamycin derivatives as inhibitors of a ribonucleic acid instructed deoxyribonucleic acid polymerase function. Effect of lipophilicity
Allan N. Tischler, Frances M. Thompson, Louis J. Libertini, and Melvin Calvin
pp 948 - 952; DOI:
10.1021/jm00255a008
PDF
Glycoside cleavage reactions on erythromycin A. Preparation of erythronolide A
Ronald A. LeMahieu, Mathew Carson, Richard W. Kierstead, Lucy M. Fern, and E. Grunberg
pp 953 - 956; DOI:
10.1021/jm00255a009
PDF
Hantzsch-type dihydropyridine hypotensive agents
Bernard Loev, Marjorie M. Goodman, Kenneth M. Snader, Ralph Tedeschi, and Edward Macko
pp 956 - 965; DOI:
10.1021/jm00255a010
PDF
Bis-basic-substituted polycyclic aromatic compounds. New class of antiviral agents. 5. Bis-basic ethers of anthraquinone and bisalkamine esters of anthraquinonedicarboxylic acids
Arthur D. Sill, Edwin R. Andrews, F. William Sweet, Jake W. Hoffman, Paul L. Tiernan, J. Martin Grisar, Robert W. Fleming, and Gerald D. Mayer
pp 965 - 968; DOI:
10.1021/jm00255a011
PDF
[1-.beta.-Mercapto-.beta.,.beta.-diethylpropionic acid, 4-leucine]-8-lysine-vasopressin and [1-.beta.-mercapto-.beta.,.beta.-diethylpropionic acid, 4-leucine]oxytocin, compounds possessing antihormonal properties
Douglas F. Dyckes, John J. Nestor, Martha F. Ferger, Vincent Du Vigneaud, and W. Y. Chan
pp 969 - 972; DOI:
10.1021/jm00255a012
PDF
Amodiaquine analogs. Synthesis of 6-(N,N-diethylamino)methyl-4-hydroxy]anilino]-5,8-dimethoxy-2,4-dimethylquinoline and related compounds
Carroll Temple, Jerry D. Rose, and John A. Montgomery
pp 972 - 977; DOI:
10.1021/jm00255a013
PDF
Synthesis and antimicrobial activity of aliphatic nitro compounds
Nigel G. Clark, Betty Croshaw, Brian E. Leggetter, and David F. Spooner
pp 977 - 981; DOI:
10.1021/jm00255a014
PDF
Reinvestigation of a nonadditive quantitative structure-activity relation
Arthur Cammarata and Thomas M. Bustard
pp 981 - 985; DOI:
10.1021/jm00255a015
PDF
Carbon-13 magnetic resonance study. Structure of the metabolites of orally administered quinidine in humans
F. I. Carroll, Doris Smith, Monroe E. Wall, and Charles G. Moreland
pp 985 - 987; DOI:
10.1021/jm00255a016
PDF
Stereochemistry and absolute configuration of the analgesic agonist-antagonist (-)-5-m-hydroxyphenyl-2-methylmorphan
Todd G. Cochran
pp 987 - 989; DOI:
10.1021/jm00255a017
PDF
Stereochemical studies on medicinal agents. 18. Absolute configuration and analgetic potency of trimeperidine enantiomers
David Fries and Philip S. Portoghese
pp 990 - 993; DOI:
10.1021/jm00255a018
PDF
Structural modification study of the antimalarial 2-(p-chlorophenyl)-2-(4-piperidyl)tetrahydrofuran
Daniel J. McCaustland, Ping-Lu Chien, William H. Burton, and C. C. Cheng
pp 993 - 1000; DOI:
10.1021/jm00255a019
PDF
Synthesis of some N-carboxylic acid derivatives of 3-phenoxypyrrolidines, 4-phenoxypiperidines, and 3-phenoxynortropanes with muscle relaxant and anticonvulsant activities
Robert F. Boswell, Grover C. Helsley, Robert L. Duncan, William H. Funderburk, and David N. Johnson
pp 1000 - 1008; DOI:
10.1021/jm00255a020
PDF
Antihypertensive activity of 1-dimethylphosphinylmethyl-4-arylpiperazines
Edward J. Glamkowski, Joseph Strupczewski, Erhard Wolf, and David L. Woodward
pp 1008 - 1009; DOI:
10.1021/jm00255a021
PDF
Antimalarials. 3. Fluorenemethanols
Edward R. Atkinson and Felix E. Granchelli
pp 1009 - 1012; DOI:
10.1021/jm00255a022
PDF
Antimalarials. 4. Tetrahydroquinolinemethanols
Edward R. Atkinson
pp 1012 - 1013; DOI:
10.1021/jm00255a023
PDF
Antineoplastic agents. 34. Helenium autumnale
George R. Pettit, John C. Budzinski, Gordon M. Cragg, Peter Brown, and LaRea D. Johnston
pp 1013 - 1016; DOI:
10.1021/jm00255a024
PDF
Synthesis and biological activities of analogs of the luteinizing hormone-releasing hormone (LH-RH) modified in position 2
Richard W. A. Rees, Theodore J. Foell, Sie-Yearl Chai, and Norman Grant
pp 1016 - 1019; DOI:
10.1021/jm00255a025
PDF
Synthesis and antiprotozoal activity of 1-(3-chloro-2-hydroxypropyl)-substituted nitroimidazoles
Max Hoffer and Emanuel Grunberg
pp 1019 - 1020; DOI:
10.1021/jm00255a026
PDF
Conformationally restricted analogs of histamine H1 receptor antagonists. 2-Phenyl- and 2-benzyl-1,2,3,4-tetrahydro-4-dimethylaminoisoquinoline
Patrick E. Hanna, Vernon R. Grund, and M. W. Anders
pp 1020 - 1023; DOI:
10.1021/jm00255a027
PDF
Quinazolines as inhibitors of dihydrofolate reductase. 2
John B. Hynes, Wallace T. Ashton, Dale Bryansmith, and James H. Freisheim
pp 1023 - 1025; DOI:
10.1021/jm00255a028
PDF
Mesoionic purinone analogs. 7. In vitro antibacterial activity of mesoionic 1,3,4-thiadiazolo[3,2,-a]pyrimidine-5,7-diones
Robert A. Coburn, Richard A. Glennon, and Zdzislaw F. Chmielewicz
pp 1025 - 1027; DOI:
10.1021/jm00255a029
PDF
Synthesis of the .alpha. and .beta. anomers of 1-(2-deoxy-D-ribofuranosyl)-4-pyridone
Warren J. Woodford, Barbara A. Swartz, Conrad J. Pillar, Arieh Kampf, and Mathias P. Mertes
pp 1027 - 1029; DOI:
10.1021/jm00255a030
PDF
Single-step phosphorylation of 5-fluoro-2'-deoxyuridine to 5-fluoro-2'-deoxyuridine 5'-phosphate
Tony M. K. Chiu and R. Bruce Dunlap
pp 1029 - 1030; DOI:
10.1021/jm00255a031
PDF
Synthesis and biological properties of 6'-amino-6'-deoxygentamicin A
Tattanahalli L. Nagabhushan and Peter J. L. Daniels
pp 1030 - 1031; DOI:
10.1021/jm00255a032
PDF
3-Hydroxy-1-nitrophenyl-1H-pyrazolo[3,4-b]pyridines as selective inhibitors of rat liver xanthine oxidase
Surendra S. Parmar, B. R. Pandey, C. Dwivedi, and Basheer Ali
pp 1031 - 1033; DOI:
10.1021/jm00255a033
PDF
Cycloserine carbamates
Jimmie D. Weaver, Neal F. Busch, and Charles H. Stammer
pp 1033 - 1035; DOI:
10.1021/jm00255a034
PDF
Book Reviews

pp 1036 - 1036; DOI:
10.1021/jm00255a600
PDF

Issue 10


Crystal structures of analgesics. Hydrochlorides of (-)-isomethadone, .alpha.-methadol, and .alpha.-methadyl acetate
Eli Shefter
pp 1037 - 1040; DOI:
10.1021/jm00256a001
PDF
In pursuit of analgetic agents. Hydro-1,3-ethanoindeno[2,1-c]pyridines and homologs
Robert L. Clarke, Anthony J. Gambino, and Sol J. Daum
pp 1040 - 1046; DOI:
10.1021/jm00256a002
PDF
Synthetic analgesics. Synthesis and pharmacology of the diastereoisomers of N-[3-methyl-1-(2-phenylethyl)-4-piperidyl]-N-phenylpropanamide and N-[3-methyl-1-(1-methyl-2-phenylethyl)-4-piperidyl]-N-phenylpropanamide
Willem F. M. Van Bever, Carlos J. E. Niemegeers, and Paul A. J. Janssen
pp 1047 - 1051; DOI:
10.1021/jm00256a003
PDF
Potential nonequilibrium analgetic receptor inactivators. Further pharmacologic studies of N-acylanileridines
A. E. Takemori, Allen Ward, P. S. Portoghese, and V. G. Telang
pp 1051 - 1054; DOI:
10.1021/jm00256a004
PDF
Chemistry and pharmacology of apoise. 7. Susceptibility of some branched-chain sugar nucleosides to enzymic deamination
Jean M. J. Tronchet, Jeannine Tronchet, and Rene Graf
pp 1055 - 1056; DOI:
10.1021/jm00256a005
PDF
Stereoisomeric lactoyl-.beta.-methylcholine iodides. Interaction with cholinesterase and acetylcholinesterase
M. M.-L. Chan and J. B. Robinson
pp 1057 - 1060; DOI:
10.1021/jm00256a006
PDF
Luteinizing hormone-releasing hormone and analogs. Synthesis and biological activity
Hans Immer, Vern R. Nelson, Clara Revesz, Kazimir Sestanj, and Manfred Goetz
pp 1060 - 1065; DOI:
10.1021/jm00256a007
PDF
Mercaptopyridinecarboxylic acids. Synthesis and hypoglycemic activity
Benjamin Blank, Nicholas W. DiTullio, Clara K. Miao, Franklin F. Owings, John G. Gleason, Stephen T. Ross, Charles E. Berkoff, Harry L. Saunders, J. Delarge, and C. L. Lapiere
pp 1065 - 1071; DOI:
10.1021/jm00256a008
PDF
Adrenergic agents. 2. Synthesis and potential .beta.-adrenergic agonist activity of some ring-chlorinated relatives of isoproterenol
Carl Kaiser, Donald F. Colella, Alex M. Pavloff, and Joe R. Wardell
pp 1071 - 1075; DOI:
10.1021/jm00256a009
PDF
Pyrimidine nucleosides. 6. Synthesis and anticancer activities of N4-substituted 2,2'-anhydronucleosides
Tadashi Kanai, Motonobu Ichino, Akio Hoshi, Fumihiko Kanzawa, and Kazuo Kuretani
pp 1076 - 1078; DOI:
10.1021/jm00256a010
PDF
Synthesis, in vivo effects, metabolism, and excretion of 5-(p-hydroxyanilino)-1,2,3,4-thiatriazole in the beagle dog
George J. Ikeda, Charles B. Estep, Leo H. Wiemeler, and Arthur Alter
pp 1079 - 1082; DOI:
10.1021/jm00256a011
PDF
Anticoccidial agents. 1. Synthesis and anticoccidial activity of 4-deoxypyridoxol and its esters
Yasuhiro Morisawa, Mitsuru Kataoka, Taiichiro Watanabe, Noritoshi Kitano, and Toshiaki Matsuzawa
pp 1083 - 1086; DOI:
10.1021/jm00256a012
PDF
Synthesis and biological activity of some aporphine derivatives related to apomorphine
Walfred S. Saari, Stella W. King, Victor J. Lotti, and Alexander Scriabine
pp 1086 - 1090; DOI:
10.1021/jm00256a013
PDF
Aporphines. 11. Synthesis and dopaminergic activity of monohydroxyaporphines. Total synthesis of (+-)-11-hydroxyaporphine, (+-)-11-hydroxynoraporphine, and (+-)-11-hydroxy-N-propylnoraporphine
John L. Neumeyer, Felix E. Granchelli, K. Fuxe, U. Ungerstedt, and H. Corrodi
pp 1090 - 1095; DOI:
10.1021/jm00256a014
PDF
Synthesis and antimalarial evaluation of 9,10-dihydrophenanthrene amino alcohols
Adrienne S. Dey and John L. Neumeyer
pp 1095 - 1100; DOI:
10.1021/jm00256a015
PDF
Structure-activity relations in psychotomimetic phenylalkylamines
F. A. B. Aldous, B. C. Barrass, K. Brewster, D. A. Buxton, D. M. Green, R. M. Pinder, P. Rich, M. Skeels, and K. J. Tutt
pp 1100 - 1111; DOI:
10.1021/jm00256a016
PDF
3-[.alpha.-(tert-Butylamino)methyl]-5-hydroxy-m-xylene-.alpha.,.alpha.'-diol, a selective bronchodilator
Charles F. Schwender, Brooks R. Sunday, John Shavel, and Ralph E. Giles
pp 1112 - 1115; DOI:
10.1021/jm00256a017
PDF
Isosteres of natural phosphates. 3. Synthesis of the dilithium salt of 4,4-diethoxy-3-hydroxybutyl-1-phosphonic acid, an isostere of glyceraldehyde 3-phosphate
Stephen L. Goldstein, Maria Pulcrano, Burton E. Tropp, and Robert Engel
pp 1115 - 1117; DOI:
10.1021/jm00256a018
PDF
14-Hydroxycodeinone. Improved synthesis
Frank M. Hauser, Tek-Kuei Chen, and Frank I. Carroll
pp 1117 - 1117; DOI:
10.1021/jm00256a019
PDF
2-Aryl-3-dimethylphosphinylpropionic acids as potential nonsteroidal antiinflammatory agents
V. Brian Anderson, Richard C. Allen, Jeffrey C. Wilker, and William J. Novick
pp 1117 - 1118; DOI:
10.1021/jm00256a020
PDF
N.omega.-(2-Mercaptoethyl) derivatives of ornithine and lysine as antiradiation agents
James R. Piper, Lucy M. Rose, Anne G. Laseter, Thomas P. Johnston, and Marie M. Grenan
pp 1119 - 1120; DOI:
10.1021/jm00256a021
PDF
Synthesis of dl-3-(hydroxymethyl)tyrosine
Theodore S. T. Wang and Julius A. Vida
pp 1120 - 1122; DOI:
10.1021/jm00256a022
PDF
Amino-imino tautomerism in the antibiotic formycin A as studied by CNDO/2 molecular orbital theory
Gerald P. Ceasar and James J. Greene
pp 1122 - 1124; DOI:
10.1021/jm00256a023
PDF
Application of regular solution theory to biomembranes
Lorna J. Bennett and Keith W. Miller
pp 1124 - 1125; DOI:
10.1021/jm00256a024
PDF
Annelated thyroxine analogs
Michael T. Cox, W. Gary Bowness, and Jim J. Holohan
pp 1125 - 1127; DOI:
10.1021/jm00256a025
PDF
Potential antifertility agents. 5. 2,3-Diphenyl-1-(N-methyl-N-propargyl)aminoindenes
R. R. Crenshaw, Thomas A. Jenks, and Gabriel Bialy
pp 1127 - 1128; DOI:
10.1021/jm00256a026
PDF
Book Reviews

pp 1129 - 1130; DOI:
10.1021/jm00256a600
PDF

Issue 11


Compounds related to 4-diisopropylamino-2-phenyl-2-(2-pyridyl)butyramide. Synthesis and antiarrhythmic activity
Chung H. Yen, Harman S. Lowrie, and Richard R. Dean
pp 1131 - 1135; DOI:
10.1021/jm00257a001
PDF
Synthesis, stereochemistry, and antiarrhythmic activity of some 8-substituted decahydroisoquinolines
Ian W. Mathison and Phillip H. Morgan
pp 1136 - 1139; DOI:
10.1021/jm00257a002
PDF
Pyrrolo[4,3,2-de]isoquinolines with central nervous system and antihypertensive activities
Christopher A. Demerson, Adolph H. Philipp, Leslie G. Humber, Michael J. Kraml, Marie P. Charest, Helen Tom, and Ivan Vavra
pp 1140 - 1145; DOI:
10.1021/jm00257a003
PDF
Potential antitumor agents. 10. Synthesis and biochemical properties of 5-N-alkylamino-, N,N-dialkylamino-, and N-alkylacetamido-1-formylisoquinoline thiosemicarbazones
Paul D. Mooney, Barbara A. Booth, E. Colleen Moore, Krishna C. Agrawal, and Alan C. Sartorelli
pp 1145 - 1150; DOI:
10.1021/jm00257a004
PDF
Bis-basic-substituted polycyclic aromatic compounds. New class of antiviral agents. 6. Bis-basic-substituted fluoranthenes
William L. Albrecht, Robert W. Fleming, Stephen W. Horgan, Barbara A. Deck, Jake W. Hoffmann, and Gerald D. Mayer
pp 1150 - 1156; DOI:
10.1021/jm00257a005
PDF
Agonist and antagonist relations in 1- and 8-substituted analogs of angiotensin II
Mahesh C. Khosla, Madeline M. Hall, Robert R. Smeby, and F. Merlin Bumpus
pp 1156 - 1160; DOI:
10.1021/jm00257a006
PDF
Structure-activity relations in immunochemistry. 2. Inhibition of complement by benzamidines
Corwin Hansch and Masafumi Yoshimoto
pp 1160 - 1167; DOI:
10.1021/jm00257a007
PDF
Imidazole derivatives as inhibitors of cyclic nucleotide phosphodiesterases
Russell Buchman, Peter F. Heinstein, and Jack N. Wells
pp 1168 - 1173; DOI:
10.1021/jm00257a008
PDF
Inhibition of tyrosinase-catalyzed melanin formation by catechol phenyl sulfones
Jerome F. Siuda and Ayman Habal
pp 1173 - 1177; DOI:
10.1021/jm00257a009
PDF
Nonsteroidal antiinflammatory agents. 1. 2,4-Diphenylthiazole-5-acetic acid and related compounds
Kevan Brown, David P. Cater, John F. Cavalla, David Green, Robert A. Newberry, and Alan B. Wilson
pp 1177 - 1181; DOI:
10.1021/jm00257a010
PDF
Preparation and antiinflammatory activity of some nonacidic trisubstituted imidazoles
Joseph G. Lombardino and Edward H. Wiseman
pp 1182 - 1188; DOI:
10.1021/jm00257a011
PDF
1-(3,4-Dichlorobenzamidomethyl)cyclohexyldimethylamine and related compounds as potential analgesics
N. J. Harper, G. B. A. Veitch, and D. G. Wibberley
pp 1188 - 1193; DOI:
10.1021/jm00257a012
PDF
Analgesics. 2. Selected 5-substituted 5-(1-phenylethyl)barbituric acids
Julius A. Vida, Carlos M. Samour, Mary H. O'Dea, Theodore S. T. Wang, and John F. Reinhard
pp 1194 - 1197; DOI:
10.1021/jm00257a013
PDF
Analogs of 5'-deoxy-5'-(methylthio)adenosine
John A. Montgomery, Anita T. Shortnacy, and H. Jeanette Thomas
pp 1197 - 1207; DOI:
10.1021/jm00257a014
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Methotrexate analogs. 3. Synthesis and biological properties of some side-chain altered analogs
Michael Chaykovsky, Andre Rosowsky, Nickolas Papathanasopoulos, Katherine K. N. Chen, Edward J. Modest, Roy L. Kisliuk, and Yvette Gaumont
pp 1212 - 1216; DOI:
10.1021/jm00257a015
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Quinazolines. 12. 1,3-Diaminobenzo[f]quinazolines containing long-chain alkyl or chloro substituents on the central ring. Synthesis and biological evaluation as candidate antifolate and antimalarial agents
Andre Rosowsky, Ping C. Huang, Nickolas Papathanasopoulos, and Edward J. Modest
pp 1217 - 1222; DOI:
10.1021/jm00257a016
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Synthesis and biological activity of DL-3-(5-benzimidazolyl)-2-methylalanine
Nicolas Zenker, Victor H. Morgenroth, and Jeremy Wright
pp 1223 - 1225; DOI:
10.1021/jm00257a017
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Synthesis of .alpha.-heterosubstituted nitrosamines. Novel test substances for cancer and mutagenesis research
Dieter Seebach and Dieter Enders
pp 1225 - 1227; DOI:
10.1021/jm00257a018
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Synthesis and pharmacology of homoarginine bradykinin analogs
Max E. Safdy and Phyllis A. Lyons
pp 1227 - 1228; DOI:
10.1021/jm00257a019
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Quinazolines and 1,4-benzodiazepines. 69. 1-Vinyl-1,4-benzodiazepin-2-ones and 1-vinylquinazolin-2(1H)-ones
A. Walser and R. I. Fryer
pp 1228 - 1230; DOI:
10.1021/jm00257a020
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.alpha.-(Ureidomethylene)lactones and derived 5-(hyroxyalkyl)uracils
George H. Denny and Malcolm A. Ryder
pp 1230 - 1231; DOI:
10.1021/jm00257a021
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Antihypertensives. 1. Syntheses of thiazino-, thiazepino-, and thiazoninoethylguanidines
Lawrence D. Wise, Glenn C. Morrison, Katherine Egan, Michael A. Commarato, Gregory Kopia, and Edmund C. Lattime
pp 1232 - 1234; DOI:
10.1021/jm00257a022
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Anticoccidial agents. 2. Synthesis and anticoccidial activity of pyridoxol analogs
Yasuhiro Morisawa, Mitsuru Kataoka, Taiichiro Watanabe, Noritoshi Kitano, and Toshiaki Metsuzawa
pp 1235 - 1237; DOI:
10.1021/jm00257a023
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Synthesis and metabolic behavior of the suggested active species of isophosphamide having cytostatic activity
Akira Takamizawa, Saichi Matsumoto, Tsuyoshi Iwata, Yoshihiro Tochino, Ken Katagiri, Kenji Yamaguchi, and Osamu Shiratori
pp 1237 - 1239; DOI:
10.1021/jm00257a024
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Nucleoside Peptides. 6. Synthesis of Certain N-[5-Amino-1-(β-D-ribofuranosyl)imidazole-4-carbonyl]amino Acids Related to Naturally Occurring Intermediates in the Purine Biosynthetic Pathway
Prem C. Srivastava, Robert W. Mancuso, Robert J. Rousseau, and Roland K. Robins
pp 1207 - 1211; DOI:
10.1021/jm00257a600
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Book Reviews

pp 1239 - 1240; DOI:
10.1021/jm00257a601
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Issue 12


Synthetic fibrinolytic agents. 1. N-Monoacyl, N-monoalkyl, and related bis(tetrahydroisoquinolines)
Ronald L. Buchanan, Vilmars Sprancmanis, Thomas A. Jenks, R. R. Crenshaw, George M. Luke, Henry M. Holava, and Richard A. Partyka
pp 1241 - 1248; DOI:
10.1021/jm00258a002
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Synthetic fibrinolytic agents. 2. Selected N-monosubstituted bis(tetrahydroisoquinolines) designed to possess enhanced bioavailability
Ronald L. Buchanan, Vilmars Sprancmanis, Thomas A. Jenks, R. R. Crenshaw, and George M. Luke
pp 1248 - 1253; DOI:
10.1021/jm00258a003
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Cycloalkanones. 4. Antifertility activity
Iris H. Hall, Gerald L. Carlson, G. Shuford Abernethy, and Claude Piantadosi
pp 1253 - 1257; DOI:
10.1021/jm00258a004
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Potential antifertility agents. 6. Synthesis and biological activities of optical isomers of 4.beta.-(p-methoxyphenyl)-2.beta.-methylcyclohexane-.alpha.-carboxylic acid and related compounds
R. R. Crenshaw, Thomas A. Jenks, George M. Luke, and Gabriel Bialy
pp 1258 - 1261; DOI:
10.1021/jm00258a005
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Potential antifertility agents. 7. Synthesis and biological activities of 2-, 3-, and 6-alkyl-substituted 4-aryl-2-methylcyclohexanecarboxylic acids
R. R. Crenshaw, George M. Luke, Thomas A. Jenks, and Gabriel Bialy
pp 1262 - 1268; DOI:
10.1021/jm00258a006
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Synthesis and antifolate activity of isoaminopterin
M. G. Nair, L. P. Mercer, and Charles M. Baugh
pp 1268 - 1272; DOI:
10.1021/jm00258a007
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Pyrimido[4,5-c]isoquinolines. 2. Synthesis and biological evaluation of some 6-alkyl-, 6-aralkyl-, and 6-aryl-1,3-diamino-7,8,9,10-tetrahydropyrimido[4,5-c]isoquinolines as potential folate antagonists
Andre Rosowsky and Nickolas Papathanasopoulos
pp 1272 - 1276; DOI:
10.1021/jm00258a008
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Synthesis of 6-(phenylhydrazino)uracils and their inhibition of a replication-specific deoxyribonucleic acid polymerase
George E. Wright and Neal C. Brown
pp 1277 - 1282; DOI:
10.1021/jm00258a009
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Synthesis and biological activity of selected 2-substituted 6-(.beta.-D-ribofuranosyl)oxazolo[5,4-d]pyrimidin-7-ones
Vemanna D. Patil, Dean S. Wise, Leroy B. Townsend, and Alexander Bloch
pp 1282 - 1285; DOI:
10.1021/jm00258a010
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Analogs of S-adenosylhomocysteine as potential inhibitors of biological transmethylation. Inhibition of several methylases by S-tubercidinylhomocysteine
James K. Coward, Donald L. Bussolotti, and Chi-Deu Chang
pp 1286 - 1289; DOI:
10.1021/jm00258a011
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Enzyme inhibitors. Inhibition of brain choline acetyltransferase by derivatives of 4-styrylpyrimidine
Raymond E. Gibson and B. R. Baker
pp 1290 - 1293; DOI:
10.1021/jm00258a012
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Study of pituitary hormone analogs for their inhibitory properties and resistance to carboxamidopeptidases. [9-L-Proline]oxytocin, [9-L-glutamic acid]oxytocin, and [8-L-lysine,9-glycine methylamide]oxytocin
Z. Grzonka, J. D. Glass, I. L. Schwartz, and Roderich Walter
pp 1294 - 1298; DOI:
10.1021/jm00258a013
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Effect of lipophilic substituents on some biological properties of indoles
Calvert W. Whitehead and Celia A. Whitesitt
pp 1298 - 1304; DOI:
10.1021/jm00258a014
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Selective binding of metal ions to macromolecules using bifunctional analogs of EDTA
Michael W. Sundberg, Claude F. Meares, David A. Goodwin, and Carol I. Diamanti
pp 1304 - 1307; DOI:
10.1021/jm00258a015
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Methotrexate analogs. 4. 7-Methyl derivatives of methotrexate and dichloromethotrexate. New synthesis and some biological studies
Andre Rosowsky and Katherine K. N. Chen
pp 1308 - 1311; DOI:
10.1021/jm00258a016
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Semisynthetic .beta.-lactam antibiotics. 6. Sulfocephalosporins and their antipseudomonal activities
Hiroaki Nomura, Takeshi Fugono, Takenori Hitaka, Isao Minami, Toshiyuki Azuma, Shiro Morimoto, and Toru Masuda
pp 1312 - 1315; DOI:
10.1021/jm00258a017
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Novel tricyclic systems. Oxazole, thiazole, and imidazole analogs of the amitriptyline type
Eugene E. Galantay, Ronald Simpson, George Corriveau, Max Denzer, Douglas C. Knorr, Robert J. Strohschein, Nicholas A. Paolella, Yasuyuki Uike, John H. Gogerty, and et al.
pp 1316 - 1327; DOI:
10.1021/jm00258a018
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Improved synthesis and additional pharmacology of the potent analgetic (-)-5-m-hydroxyphenyl-2-methylmorphan
Michael E. Rogers and Everette L. May
pp 1328 - 1330; DOI:
10.1021/jm00258a019
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Deuterium isotope effects in the in vivo metabolism of cotinine
Ermias Dagne, Larry Gruenke, and Neal Castagnoli
pp 1330 - 1333; DOI:
10.1021/jm00258a020
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Triarylhaloethylenes as gonadotropin inhibitors
Frank P. Palopoli, Vernon J. Feil, Dorsey E. Holtkamp, and Alfred Richardson
pp 1333 - 1335; DOI:
10.1021/jm00258a021
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Polymeric anions and biological activities. Effects on intramuscular and intraperitoneal Walker carcinosarcoma 256 of the rat
Ernest M. Hodnett and Joseph T. H. Tai
pp 1335 - 1337; DOI:
10.1021/jm00258a022
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Antiinflammatory sydnones. 1
H. Wagner and John B. Hill
pp 1337 - 1338; DOI:
10.1021/jm00258a023
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Additions and Corrections - Thia Steroids. III Derivatives of 2-Thia-A-nor-5α-androstan-17β-ol as Probes of Steroid-Receptor Interactions.
Manfred E. Wolff, Galal Zanati, G. Shanmugasundarum, Sharad Gupte, and Gunhild Aadahl
pp 1339 - 1339; DOI:
10.1021/jm00258a600
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Additions and Corrections - Diamidino-α,ω-diphenoxyalkanes. Structure-Activity Relationships for the Inhibition of Thrombin, Pancreatic Kallikrein, and Trypsin.
J. D. Geratz, Alan C. Whitmore, Michael C.-F. Cheng, and Claude Piantadosi
pp 1339 - 1339; DOI:
10.1021/jm00258a601
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Additions and Corrections - "Aromatic" Substituent Constants for Structure-Activity Correlations.
Corwin Hansch, Albert Leo, Stefan H. Unger, Ki Hwan Kim, Donald Nikaitani, and Eric J. Lien
pp 1339 - 1339; DOI:
10.1021/jm00258a602
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Additions and Corrections - Strategy in Drug Design. Cluster Analysis as an Aid in the Selection of Substituents.
Corwin Hansch, Stefan H. Unger, and Alan B. Forsythe
pp 1339 - 1339; DOI:
10.1021/jm00258a603
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Additions and Corrections - Synthesis and Biological Activity of Some Analogs of the Gonadotropin Releasing Hormone.
W. Arnold, G. Flouret, R. Morgan, R. Rippel, and W. White
pp 1339 - 1339; DOI:
10.1021/jm00258a604
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Book Reviews

pp 1339 - 1342; DOI:
10.1021/jm00258a605
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