Chemistry

   

Evaluation of in Vitro Anthelmintic Activities of Novel 1,2,3 e Benzotriazole Derivatives Synthesized in Ultrasonic and Solvent Free Conditions

Authors: M.S. Sudhir, R. Venkata Nadh

Objectives: To determine anthelmintic activity of the synthesized novel 1,2,3 e benzotriazole derivatives under ultrasonication in solvent free conditions. Methods: Newer “1e(1Hebenzo[d][1,2,3]triazole-1-carbonyl) derivatives” (5Ae5P) were synthesizedby using“1Hebenzo[d][1,2,3]triazole” (1)as the startingmaterialunder ultrasonicated and solvent-free conditions. The resulting products were isolated and characterized by melting points and spectral studies. All the products were assayed for anthelmintic activity against Pheretima posthuma using albendazole and mebendazole as reference compounds. Results: All the newer 1,2,3 e benzotriazole derivatives synthesized by ultrasound activation in solventefree condition were obtained in moderate to good yields in the range of 71e82%. The data interpretation of the spectral values with reference to standard values confirmed the structures of the synthesized compounds. Out of the sixteen synthesized derivatives, four compounds (5B, 5F, 5J and 5N) showed anthelmintic activity in dose-dependent manner giving shortest time of paralysis and death with different concentrations of the derivatives. Among these four derivatives, 5J showed superior activity. Conclusion: Out of the sixteen synthesized derivatives, four compounds (5B, 5F, 5J and 5N) containing p-nitrophenyl substituent attached to azo group of benzotriazole moieties exhibited equal or comparable anthelmintic activity with reference to albendazole. The superior activity of compound 5J might be due to attachment of additional p-nitrophenyl substituent to the cyano group.

Comments: 6 Pages. OK

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[v1] 2019-05-19 05:48:13

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