Abstract

SYNTHESIS OF PHARMACEUTICALLY IMPORTANT 1, 3, 4- THIADIAZOLE DERIVATIVES AS ANALGESIC AND ANTIPYRETIC AGENTS

Faruk Alam* and Biplab Kr. Dey

Abstract

Objective: Thiadiazole derivatives were reported to have wide range of biological activities. Hence present work was planned to synthesize thiadiazole derivatives and screen for their analgesic, antipyretic and anti-inflammatory. Methods: Thiosemicarbazide was made to react with aryl carboxylic acid in presence of concentrated sulphuric acid to form 5-(substituted phenyl)-2-amino -1, 3, 4-thiadiazole. To aromatic amines, chloroacetyl chloride was added drop wise in presence of glacial acetic acid and saturated solution of sodium acetate to form 2- chloro-N-substituted-phenyl-acetamide. This acetamide compound was reacted with 5-(substituted phenyl)-2-amino -1, 3, 4-thiadiazole in 1, 4- dioxane and triethylamine (TEA), refluxed for 3 hrs to form N- (substuted-phenyl)-2-[5-(3-substituted-phenyl)-1, 3, 4-thiadiazol-2-yl amino]-acetamide. Characterization of all the compounds was performed by IR, 1HNMR, Mass spectroscopic and elemental analysis. Results: The compounds IIIA10, VA17, 2b and 3b have showed significant analgesic, antipyretic and anti-inflammatory activity. Conclusion: The compounds bearing p-chlorophenyl and 2-nitrophenyl group at C5 position of the thiadiazole moiety have shown profound activity when compared to compounds which were lacking of these groups.

Keywords: Synthesis; characterization; 1, 3, 4-Thiadiazole; Analgesic activity; Antipyretic activity.