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Benzimidazoles and its derivatives are most prominent biological active compounds in nature. Mannich reaction is one of the versatile reaction used in synthetic tools, Substituted Benzimidazole prepared from condensation between various acids and ortho phenylene diamine followed by reacting with secondary amine. The synthesized molecules were in substantial yield and characterized by physiochemically, IR, 1H-NMR spectral data and in silico prediction. All the values of the synthesized benzimidazole derivatives were found to be in compliance with standard values stated according to the Lipinski’s rule of five. The synthesized compounds were screened with antibacterial activity by standard tetracycline and antifungal activity was determined using standard fluconazole. The results shown significant inhibitory activity against the microbes with the 200 mcg/ml which produce 100% inhibition. Over the series 5D (a) and (b) shown good antibacterial and antifungal effect.
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