Some thiazolo[4,5-d]pyrimidine-7(6H)-one derivatives were evaluated in vivo for their analgesic and anti-inflammatory activities. The results were compared with that of acetyl salicylic acid and phenylbutazone. Compounds 3b and 3h were the most active in the anti-inflammatory paw edema inhibition test. In terms of the analgesic activity (acetic acid writhing test), the most active compound was 2a followed by 31. The most active members of the series were investigated for their ED50 values and ulcerogenic potential.
In this study, by starting from ethyl 4-amino-2,3-dihydro-3-methyl-2-thioxothiazole-5-carboxylate (1), the compounds having 2,3-dihydro-3-methyl-5-mercapto-6-methyl/ethyl-2- thioxothiazolo[4,5-d]pyrimidin-7(6H)-one (2a, 2b) structure and their 5-(4'-nonsubstituted/-substituted benzoylmethyl)thio derivatives (3a-h) were synthesized. The chemical structures of the compounds were proved by IR, 1H-NMR and elemental analysis data. In vitro antimicrobial activities of the synthesized compounds were investigated against some bacteria and yeasts using the microdilution method. In view of the antimicrobial activity results, a significant inhibitory effect was observed only for compound 2a against Gram-positive bacteria and yeasts, whereas the other compounds had no remarkable activity against the tested microorganisms.
In this study, by starting from ethyl 4-amino-2,3-dihydro-3-phenyl-2-thioxothiazole-5-carboxylate (1), three compounds having 2,3-dihydro-3-phenyl-5-mercapto-6-alkyl/phenyl-2-thioxothiazolo[4,5- d]pyrimidin-7(6H)-one (2a-c) structure and their 5-(4'-nonsubstituted/-substituted benzoylmethyl)thio derivatives (3a-l) were synthesized. The antimicrobial activities of the synthesized compounds were investigated against some bacteria and fungi using the microdilution method. 2,3-Dihydro-3,6-diphenyl-5-(4'-bromobenzoylmethyl)thio-2-thioxothiazolo [4,5-d]pyrimidin-7(6H) one (3k) possessing remarkable activity against Gram-positive bacteria and yeast like fungi was found to be the most active compound in this series.
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