Synthesis, characterisation and antimicrobial screening of some 1- substituted benzimidazole derivatives


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2

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1

Abstract :

The 1-substituted benzimidazoles (7a-j) were prepared by mannich reaction with benzimidazole derivatives (5), formaldehyde and different aromatic amines (6a-j). The pthalic anhydride (1) condensation with glycine (2) gives acetyl isoindoline derivatives (3), it cyclized with ortho phenylene diamine (4) gives benzimidazole derivatives (5). The yield of the synthesized benzimidazoles ranged from 52-76%. The structures of the synthesized compounds were characterized and confirmed by IR spectroscopy and physical analysis. All the compounds were screened for their in vitro antimicrobial activity against standard pathological bacterial and fungal strains shows moderate to good effective zone of inhibitions. All the compounds, exhibited a MIC values ranging between 12.8 to 102.4 μg for bacterial species. For fungal species, MIC values ranging between 12.8 to 25.6μg against Aspergillus strain. The results obtained suggest marked antibacterial and antifungal activity of the benzimidazoles at the MIC levels examined. The compounds 7d and 7i had better activity against the tested bacterial and fungal strains. The compound was showed comparatively strong activity against fungal strain than the tested bacterial species.
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