✦ LIBER ✦

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

✍ Scribed by Sanjay Dashrath Vaidya; Bobba Venkata Siva Kumar; Ramanatham Vinod Kumar; Umesh Nanasaheb Bhise; Uday Chandrakant Mashelkar

Publisher: Journal of Heterocyclic Chemistry
Year: 2007
Tongue: English
Weight: 445 KB
Volume: 44
Category: Article
ISSN: 0022-152X
DOI: 10.1002/jhet.5570440327

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✦ Synopsis

Abstract

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Synthesis of a series of novel class of N‐substituted‐2‐(benzo[d]isoxazol‐3‐ylmethyl)‐1__H__‐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.

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