Synthesis, anti‐bacterial, anti‐asthmatic and anti‐diabetic activities of novel N‐substituted‐2‐(benzo[d]isoxazol‐3‐ylmethyl)‐1H‐benzimidazoles

Abstract

Abstractmagnified imageSynthesis of a series of novel class of N‐substituted‐2‐(benzo[d]isoxazol‐3‐ylmethyl)‐1H‐benzimidazoles (4) by the condensation of o‐phenylenediamine (1) with benzo[d]isoxazol‐3‐yl‐acetic acid (2) and subsequent reactions with different types of electrophiles have been reported. Some compounds exhibited promising anti‐bacterial activity against Salmonella typhimurium, however poor activity against Staphylococcus aureus. The compound 4t was found to have high activity even at 1 μg/ml compared to Cephalexin against S. aureus. The biological activity against PDE‐IV for potential anti‐asthmatic effect and against DP‐IV and PTP‐1B for potential anti‐diabetic effects was disappointing.