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Synthesis and pharmacological evaluation of some 3-substituted octahydropyrido(2,1-c)(1,4)oxazines.
J. Med. Chem. 19(2) , 334-6, (1976) 1976-02-01 3-Phenyloctahydropyrido[2,1-c][1,4]oxazine hydrochloride and the 10R and 10S diastereomers have been synthesized from (+/-)-, (+)-, and (-)-2-piperidinemethanol. Treatment of 2-piperidinemethanol with alpha-bromoacetophenone gave 3-hydroxy-3-phenyloctahydropy... |
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Synthesis of N-hydroxythiourea.
J. Med. Chem. 19(2) , 336-7, (1976) 1976-02-01 The synthesis of the title compound (1) was accomplished by the conversion of 2,4-dimethoxybenzylamine (2) into an isothiocyanate (3) using thiocarbonyl diimidazole. Treatment of 3 with hydroxylamine and removal of the DMB group with trifluoroacetic acid gave... |
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Cycloalkanones. 8. Hypocholesterolemic activity of long-chain ketones related to pentadecanone.
J. Med. Chem. 19(2) , 219-22, (1976) 1976-02-01 Aliphatic analogs of 2,8-dibenzylcyclooctanone which includes C15-C18 ketones have been investigated for hypocholesterolemic activity in rats. The position of the carbonyl group in the chain for maximum activity appears to be the 2 position. 2-Hexadecanone re... |
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S-Aristeromycinyl-L-homocysteine, a potent inhibitor of S-adenosylmethionine-dependent transmethylations.
J. Med. Chem. 19 , 197-198, (1976) 1976-01-01
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Antimalarials. Synthesis and antimalarial activity of 1-(4-methoxycinnamoyl)-4-(5-phenyl-4-oxo-2-oxazolin-2-yl)piperazine and derivatives.
J. Med. Chem. 18(12) , 1216-23, (1975) 1975-12-01 The preparation and activity against Plasmodium berghei of derivatives of 1-(4-methoxycinnamoyl)-4-(5-phenyl-4-oxo-2-oxazolin-2-yl)piperazine are described. Replacement of the cinnamoyl group was accomplished by acylation or alkylation of 1-(5-phenyl-4-oxo-2-... |
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Synthesis and antiinflammatory activity of some 2-heteroaryl-alpha-methyl-5-benzoxazoleacetic acids.
J. Med. Chem. 18(11) , 1158-9, (1975) 1975-11-01 The syntheses of eight of the title compounds are described. The compounds possessed activity comparable with that of the previously tested 2-substituted phenyl analogs in the carrageenan-induced rat paw edema test. |
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A lapachol derivative active against mouse lymphocytic leukemia P-388.
J. Med. Chem. 18(11) , 1159-61, (1975) 1975-11-01 Lapachol [2-hydroxy-3-(3-methyl-2-butenyl)-1,4-naphthoquinone] and its analogs [2-(3,7-dimethyl-2,6-octadienyl)-3-hydroxy-1,4-naphthoquinone and 2-(3,3-dibromo-2-propenyl)-3-hydroxy-1,4-naphthoquinone] have been described, among almost a hundred synthesized a... |
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Inhibitors of nucleoside transport. A structure-activity study using human erythrocytes.
J. Med. Chem. 18 , 968, (1975) 1975-10-01 The passage of nucleosides across the plasma membrane of erythrocytes is a membrane-mediated process which is strongly inhibited by derivatives of 9-beta-D-ribofuranosylpurine (1) with S, O, or N atoms at the purine 6 position bearing variously substituted ar... |
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Preparation and properties of 5-phenylphenoxymethylpenicillin.
J. Med. Chem. 18(5) , 486-90, (1975) 1975-05-01 Cycloaddition of azidoacetyl chloride to benzyl D-5,5-dimethyl-5-phenyl-2-thiazoline-4-carboxylate (1a) gave 5-phenyl-6alpha-azidopenicillanate (2a). By catalytic reduction of 2a and reaction with phenoxyacetyl chloride, 5-phenyl-6-epiphenoxymethylpenicillin ... |
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Adenosine cyclic 3',5',-monophosphate phosphodiesterasr inhibitors. 2.3-Substituted 5,7-dialkylpyrazolo [1,5-a]pyrimidines.
J. Med. Chem. 18(5) , 460-4, (1975) 1975-05-01 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... |