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Synthesis,anti‐bacterial,anti‐asthmatic and anti‐diabetic activities of novel N‐substituted‐2‐(benzo[d]isoxazol‐3‐ylmethyl)‐1H‐benzimidazoles
Authors:Sanjay Dashrath Vaidya  Bobba Venkata Siva Kumar  Ramanatham Vinod Kumar  Umesh Nanasaheb Bhise  Uday Chandrakant Mashelkar
Institution:1. Glenmark Research Center, Plot No. A‐607, T.T.C.Industrial Area, M.I.D.C. Mahape Navi Mumbai‐400 709, India;2. Oraganic Research Laboratory, Patkar College, S. V. Road, Goregaon(West), Mumbai‐400 062, India
Abstract: chemical structure image Synthesis of a series of novel class of N‐substituted‐2‐(benzod]isoxazol‐3‐ylmethyl)‐1H‐benzimidazoles ( 4 ) by the condensation of o‐phenylenediamine ( 1 ) with benzod]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.
Keywords:
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