abstract：:2,9beta-Dimethyl-2'-hydroxy-6,7-benzomorphan (18) has been synthesized from m-methoxyphenylacetone (6a) or m-methoxyphenylacetonitrile (1) via bromo-alpha-tetralone (10). Isomeric bromo-alpha-tetralone 9, instead of undergoing cyclization to a 6,7-benzomorphan, gave aromatization product 12. The structures and stereoc...

journal_title：Journal of medicinal chemistry

authors： Inoue H,O-ishi T,May EL

更新日期：1975-08-01 00:00:00

abstract：:Several 1,3-disubstituted and 1-substituted derivatives of 5-propionoxy-5-(1-phenylethyl)barbituric acid were synthesized and evaluated for analgesic activity. Three of these compounds, 1,3-bis(methoxymethyl)-5-propionoxy-5-(1-phenylethyl)barbituric acid (2), 1,3-dimethyl-5-propionoxy-5-(1-phenylethyl)barbituric acid...

journal_title：Journal of medicinal chemistry

authors： Vida JA,Samour CM,O'Dea MH,Reinhard JF

更新日期：1975-07-01 00:00:00

abstract：:9,11-Secoestradiol (9) and 11-hydroxy-9,11-secoestradiol (12) have been synthesized starting from 17-acetoxyestradiol 3-methyl ether (1) and found to possess significant antifertility activity in rats. 3-Methoxy-9,11-seco-9-oxo-17beta-acetoxyestra-1,3,5(10)-trien-11-oic acid (2), prepared by CrO3 oxidation of 1, on h...

journal_title：Journal of medicinal chemistry

authors： Kole P,Ray S,Kamboj VP,Anand N

更新日期：1975-07-01 00:00:00

abstract：:Some 2-aryloxymethyl-2,3,5,6-tetrahydro-1,4-oxazines have been shown to possess marked antidepressant activity. The 1,4-oxazines were synthesized by lithium aluminum hydride reduction of the readily available 6-aryloxymethyl-2,3,5,6-tetrahydro-1,4-oxazin-3-ones. High antidepressant activity was associated with ortho s...

journal_title：Journal of medicinal chemistry

authors： Greenwood DT,Mallion KB,Todd AH,Turner RW

更新日期：1975-06-01 00:00:00

abstract：:4-Amino-5-arylpyrimidines were synthesized by a variety of methods and have demonstrated antiinflammatory activity in the carrageenan-induced edema in the rat but displayed little activity against adjuvant-induced arthritis in rats or against uv-induced erythema in guinea pigs. ...

journal_title：Journal of medicinal chemistry

authors： Lang SA Jr,Cohen E

更新日期：1975-06-01 00:00:00

abstract：:Syntheses of the decapeptide luteinizing hormone-releasing hormone, less thanGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2 are described. The basic properties of arginine can provide a simple repetitive isolation procedure for arginine-containing peptides. The biological activities of the decapeptide, of a range of frag...

journal_title：Journal of medicinal chemistry

authors： Schafer DJ,Black AD,Bower JD

更新日期：1975-06-01 00:00:00

abstract：:Several compounds having portions of the camptothecin ring system were prepared. These compounds were screened against L1210 lymphoid leukemia with negative results. Two of the analogs which contained the pyridine and hydroxylactone D and E rings were also screened for inhibition of DNA and RNA syntheses in HeLa cells...

journal_title：Journal of medicinal chemistry

authors： Horwitz SB,Bristol JA,Comins DL,Davenport RW,Kane MJ,Lyle RE,Maloney JR,Portlock DE

更新日期：1975-05-01 00:00:00

abstract：:A number of 3-bromo-, 3-nitro-, and 3-ethoxycarbonyl-5,7-dialkylpyrazolo[1,5-a]pyrimidines were synthesized and screened as in vitro cAMP phosphodiesterase inhibitors. The condensation of 3-aminopyrazole with symmetrical beta-diketones (acetylacetone, heptane-3,5-dione, etc.) afforded symmetrical dialkylpyrazolo[1,5-a...

journal_title：Journal of medicinal chemistry

authors： Novinson T,Miller JP,Scholten M,Robins RK,Simon LN,O'Brien DE,Meyer RB Jr

更新日期：1975-05-01 00:00:00

abstract：:The natural abundance 13C magnetic resonance spectra of a series of sulfonamide drugs(sulfanilamide, sulfaguanidine,sulfathiazole, sulfasuxidine, sulfadiazine, sulfamerazine, sulfamethiazine, and sulfapyridine) have been determined at 25.15 MHz employing the pulse Fourier transform technique. The chemical shefts have ...

journal_title：Journal of medicinal chemistry

authors： Chang C,Floss HG,Peck GE

更新日期：1975-05-01 00:00:00

abstract：:The Free-Wilson equations are derived for the case of symmetrical substitution and are applied, in four modifications, to in vitro inhibitory activity of 77 organic disulfides against Histoplasma capsulatum. Substituent constants are listed to aid in the design of new inhibitory agents against this human pathogen (and...

journal_title：Journal of medicinal chemistry

authors： Schaad LJ,Werner RH,Dillon L,Field L,Tate CE

更新日期：1975-04-01 00:00:00

abstract：:The N-demethylation of 1-(N-methyl-N-trideuteriomethylamino)-3-phenylpropane (1) by rodent liver homogenates was studied. The ratio of 1-trideuteriomethylamino-3-phenylpropane (2)/1-methylamino-3-phenylpropane (3) was determined by gc-ms. The ratio of 2/3 in the product of N-demethylation of 1 by liver homogenate from...

journal_title：Journal of medicinal chemistry

authors： Abdel-Monem MM

更新日期：1975-04-01 00:00:00

abstract：:Several derivatives of erythro-beta-hydroxy-DL-aspartic acid (1) were prepared as a potential inhibitors of L-asparagine synthetase (ASase) from rat Novikoff hepatoma. Benzylation of 1 gave the dibenzyl ester 2 which upon coupling with carbobenzoxyglycine afforded the blocked dipeptide 3. Deblocking of 3 gave glycl-er...

journal_title：Journal of medicinal chemistry

authors： Mokotoff M,Bagaglio JF,Parikh BS

更新日期：1975-04-01 00:00:00

abstract：:Quantitative structure-activity relationship studies have been performed on two types of sulfonamides with hypoglycemic activity. In the case of the 2-benzenesulfonamidopyrimidines, substituted in the 5 position of the pyrimidine ring a correlation between hydrophobic forces, expressed as Rm values, and the binding to...

journal_title：Journal of medicinal chemistry

authors： Seydel JK,Ahrens H,Losert W

更新日期：1975-03-01 00:00:00

abstract：:A series of amino acids, amidino acids, and amidino esters was synthesized and the compounds were evaluated for their inhibitory activity against bovine trypsin, bovine thrombin, and porcine pancreatic kallikrein and as anticoagulants. Among these compounds, ethyl 4-amidino-2-iodophenoxyacetate was found to be the mos...

journal_title：Journal of medicinal chemistry

authors： Geratz JD,Mar EC,Loeffler LJ,Fox LB

更新日期：1975-03-01 00:00:00

abstract：:The synthesis of a series of 2-, 3-, and 4-substituted benzylamine derivatives is described. These compounds were studied for their effect on experimental cardiac arrhythmias. Many of the derivatives, but in particular 2-(p-methoxyphenylethynyl)benzylamine (3d), alpha,alpha-dimethyl-4y(phenylethynyl)benzylamine (7a), ...

journal_title：Journal of medicinal chemistry

authors： Remy DC,Van Saun WA Jr,Engelhardt EL

更新日期：1975-02-01 00:00:00

abstract：:In an attempt to relate the hallucinogenic potencies in man of some biologically important amphetamines and phenethylamines, the 1-octanol-water partition coefficients for 11 amphetamines were determined. Using these values and published Hansch pi constants, the log P for 17 additional amines was estimated. It was fou...

journal_title：Journal of medicinal chemistry

authors： Barfknecht CF,Nichols DE

更新日期：1975-02-01 00:00:00

abstract：:Major urinary metabolites of carbidopa have been identified. Estimates were made based on the recovery or radio activity or by glc analysis of pooled urine of the amounts of the urinary metabolites II (2-methyl-3'-methoxy-4'-hydroxyphenylpropionic acid), III (2-methyl-3,4-dihydroxyphenylpropionic acid), IV (3,4-dihydr...

journal_title：Journal of medicinal chemistry

authors： Vickers S,Stuart EK,Hucker HB

更新日期：1975-02-01 00:00:00

abstract：:The effect of incorporation of an eleostearoyl group into molecules of aralkylhydrazines on their monoamine oxidase inhibitory potency was investigated in vitro and in vivo. The results showed that on a molar basis the hydrazides possessed an in vitro potency lower than and an in vivo potency and acute toxicity compar...

journal_title：Journal of medicinal chemistry

authors： Hsu SY,Huang CL,Waters IW

更新日期：1975-01-01 00:00:00

abstract：:Certain structural similarities between prostaglandins with close-packed side chains and the perhydrocyclopentanophenanthrene nucleus of steroids prompted the synthesis and biological evaluation of 6beta, 17 beta-dihydroxy-5alpha-androstane-2alpha-carboxylic acid (30), its 6-deoxy derivative 28, and the corresponding ...

journal_title：Journal of medicinal chemistry

authors： Venton DL,Counsell RE,Sanner JH,Sierra K

更新日期：1975-01-01 00:00:00

abstract：:Synthesis and biological activity of 17-esters of 6-dehydro-16-methylene-17 alpha-hydroxyprogesterone are presented. A systematic study of the influence of the alteration of halogen at 6 and the acyl group at 17 on the progestational and antiandrogenic activities of the resulting structures is described. A convenien...

journal_title：Journal of medicinal chemistry

authors： Shapiro EL,Weber L,Harris H,Miskowicz C,Neri R,Herzog HL

更新日期：1972-07-01 00:00:00