Design, Synthesis and Pharmacological Evaluation of Pyrazoline Substituted Benzimidazole Derivatives as Antibacterial and Antifungal Agents

Abstract

Background: Benzimidazoles are important heterocyclic compounds possessing a variety of biological activities such as anticancer, antioxidant, antiinflammatory, analgesic, anti-viral, anti-bacterial, anti-fungal and hypoglycemic activities. Pyrazolines are used as antitumor, immunosuppressive, antibacterial and anti tubercular agents. Aim : The present research focused on incorporating pyrazoline nucleus into benzimidazole nucleus to form a potent antibacterial and antifungal agent. Method: The in silico design of novel pyrazoline substituted benzimidazole derivatives was done using PASS software and the compounds found to be active in in silico studies are synthesized and in vitro screening of the compounds are done for antibacterial and antifungal activities. Results: In vitro screening of the selected derivatives for antibacterial activity showed very good results. Analogue BZ-6 was found to inhibit the growth of gram negative organism and analogue BZ-3 was found to inhibit the growth of gram positive organism with respect to the standard drug Gentamicin. Antifungal screening of the compounds were done in Candida albicans using cotrimazole as standard. Analogue BZ-4 was found to inhibit the proliferation of the organism. Conclusion: Pyrazoline substituted Benzimidazole molecules are potent antibacterial agents but none of them are potent antifungal agents. Further modification of the molecule is needed to improve its antifungal activity.

Keywords: Antibacterial, Antifungal, Benzimidazole, Pyrazoline.

Cite this Article

Remya R.S. Design, Synthesis and Pharmacological Evaluation of Pyrazoline Substituted Benzimidazole Derivatives as Antibacterial and Antifungal Agents. Research & Reviews: A Journal Pharmaceutical Science. 2020; 11(3):
29–41p.