Design and Synthesis of Novel Substituted (R) 4-[2-Pyridylmethoxy] Phenyl Methyl Sulphinyl Substituted Benzimidazoles and Evaluation of their Biological Activity

R Rajesh, N Nagaraju and C Ram

Abstract

A series of substituted (R)-4-[2-pyridylmethoxy] phenyl methyl sulphinyl substituted benzimidazole derivatives 10a to 10l were synthesized by asymmetric oxidation of 4-[2-pyridylmethoxy] phenyl methyl thio substituted benzimidazoles (7a to 7l). All the targeted compounds were characterized by IR, 1H NMR and Mass spectral studies. The anti-microbial activity of synthesized compounds were screened against different strains of bacteria (S.Aureus, E. Fecalis, S. Mutans, Klebsiella) with reference to the standard ciprofloxacin and fungi (A.Niger, A.Flavus) was evaluated with reference to the standard Fluconazole. The results showed that some of the synthesized (10a-10l) compounds exhibited moderate anti-bacterial and anti-fungal activities, among which compounds 10g, 10h and 10i exhibited about 36% zone of inhibition activities against E. Fecalis, Klebsiella and A.Niger. Further these compounds were screened for anti-inflammatory activities, these synthesized title compounds exhibited as potent against MMP-2 and MMP-9.

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