Synthesis and Evaluation of Antifungal Activity of Benzotriazole Derivatives

Abstract

The present research work is related to synthesis of different derivatives of benzotriazole at the laboratory scale. By reacting substituted orthochloronitrobenzene with hydrazine hydrate in the presence of sodium carbonate gives substituted 1-hydroxy benzotriazole. Further First series of 1- (benzoyloxy) benzotriazole have been synthesized by esterification reaction of 1-hydroxy-bezotriazole with substituted benzoic acid by using dicyclohexylcarbdiimide (DCC) as a catalyst, second series of 1-(benzoyloxy)- 6-chloro benzotriazole have been synthesized by esterification reaction of 1- hydroxy-6-chloro benzotriazole with substituted benzoic acid by using dicyclohexylcarbdiimide (DCC) as a catalyst, and third series of 1- (benzoyloxy)-6-nitro benzotriazole have been synthesized by esterification reaction of 1-hydroxy-6-nitro benzotriazole with substituted benzoic acid by using dicyclohexylcarbdiimide (DCC) as a catalyst All the compounds have been evaluated for in-vitro antifungal activity (MIC) against Trichophyton rubrum, Epidermophyton floccosum and Malassazia furfur by using tube dilution method & activity was compared with Ketoconazole. In the primary screening some of the compounds exhibited appreciable activity. The purity of synthesized compounds was checked by using TLC & structure of the synthesized compounds is confirmed on the basis of spectral data.