Evaluation of in vitro anthelmintic activities of novel 1,2,3 – benzotriazole derivatives synthesized in ultrasonic and solvent free conditions

Objectives To determine anthelmintic activity of the synthesized novel 1,2,3 – benzotriazole derivatives under ultrasonication in solvent free conditions. Methods Newer “1–(1H–benzo[d][1,2,3]triazole-1-carbonyl) derivatives” (5A–5P) were synthesized by using “1H–benzo[d][1,2,3]triazole” (1) as the starting material under 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 – benzotriazole derivatives synthesized by ultrasound activation in solvent–free condition were obtained in moderate to good yields in the range of 71–82%. 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.