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

magnified image 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...

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Bibliographic Details
Published in:Journal of heterocyclic chemistry 2007-05, Vol.44 (3), p.685-691
Main Authors: Vaidya, Sanjay Dashrath, Kumar, Bobba Venkata Siva, Kumar, Ramanatham Vinod, Bhise, Umesh Nanasaheb, Mashelkar, Uday Chandrakant
Format: Article
Language:English
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Summary:magnified image 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.
ISSN:0022-152X
1943-5193
DOI:10.1002/jhet.5570440327