-92 % )Synthesis 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.
Synthesis of a series of novel substituted benzimidazole derivatives by the condensation of ophenylenediamine (OPDA, 1) with 4-bromobenzoic acid (2) and subsequent reactions of the benzimidazole with different electrophilic reagents is reported. The latter compounds were reacted with styrene and tert-butyl acrylate following Heck Coupling. All the compounds synthesized were screened for their potential anti-bacterial, anti-asthmatic and anti-diabetic properties, which exibibited some promising results towards testing organism in vivo.
Studies. -Most of the products (VI) (12 examples) are moderately active against different strains of bacteria such as E. coli, S. aureus, and P. aeruginosa. Derivatives (VIb) and (VIc) are found to have a higher biological activity against E. coli and S. aureus. -(MASHELKAR*, U. C.; RANE, D. M.; Indian J. Chem., Sect. B: Org.
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