Synthesis and antimicrobial evaluation of 5-aryl-1,3,4-thiadiazole-2-ylamine derivatives

Abstract

Thiadiazoles occur in nature in four isomeric forms and it contain five membered ring system with two nitrogen and one sulphur atom. In this paper we have synthesized thiadiazole derivatives and confirmed their antimicrobial potential. In literature thiadiazole & their derivatives have been reported as antimicrobial, antiinflammatory, anti-tubercular, antidiabetic, diuretics, antidepressant, and anticonvulsant, anti-HIV & anticancer. Thiadiazoles are prepared with the help of benzoyl chloride and hydrazine and evaluated for antimicrobial activity against gram positive species Bacillus subtilis, S.pyogenes and gram negative species Pseudomonas aeruginosa, Escherichia coli and for antifungal Candida albicans, Aspergillus niger species were used. In synthesized derivatives having substitution with strong electron withdrawing groups has highest activity than electron donating substituted compounds. Trimethoxy and dimethoxy thiadiazole parts have lowest activity than monomethoxy substituted compounds. It may be due to hindrance problem at the binding site. In all cases unsubstituted derivatives have moderate activity due to weak binding with the target site