DESIGN, SYNTHESIS AND EVALUATION OF PYRAZOLE SUBSTITUTED BENZIMIDAZOLE AS AN ANTI-TUBERCULAR, ANTI-FUNGAL AND ANTI-MICROBIAL AGENT

Authors

  • VIJAY BABU A. Department of Pharmaceutical Chemistry, SRM College of Pharmacy, SRM Institute of Science and Technology, Kattankulathur, Chengalpattu-603203, Tamil Nadu, India
  • PRIYA D. Dr. APJ Abdul Kalam Research Lab, SRM College of Pharmacy, SRM Institute of Science and Technology, Kattankulathur, Chengalpattu-603203, Tamil Nadu, India

Keywords:

Pyrazole, Docking, ADMET, Anti-tubercular, Anti-Fungal, Anti- microbial

Abstract

Background:

A series of pyrazole substituted benzimidazole derivatives were subjected to in silico studies to identify a new lead for anti-tubercular, antimicrobial and antifungal activity.

Methodology:

Docking studies was carried out against Mycobacterium tuberculosis InhA bound with ETH-NAD adduct - PDB ID: 2H9I and Crystal structure of S. aureus TyrRS in complex with SB-239629 -PDB ID: 1JIJ.

Results:

Based on the binding interactions, binding energies, and ADMET predictions, the most active compounds were produced, consisting of a para-halo phenyl substitution at the pyrazole nucleus that was connected to benzimidazole. The synthesized compounds were evaluated for tuberculostatic activity using microplate Almar blue assay method, and anti-microbial and anti-fungal activity by disc diffusion method.

Conclusion:

Compound 5c with chloro substituted phenyl ring on the pyrazole showed moderate anti-tubercular, mild antifungal and anti-microbial activity. This compound may thus represent a novel, multi target molecule having a selective class of anti-tubercular, anti-fungal and anti-microbial activity.

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Published

21-06-2022

How to Cite

A., V. B., & D., P. (2022). DESIGN, SYNTHESIS AND EVALUATION OF PYRAZOLE SUBSTITUTED BENZIMIDAZOLE AS AN ANTI-TUBERCULAR, ANTI-FUNGAL AND ANTI-MICROBIAL AGENT. International Journal of Applied Pharmaceutics, 14. Retrieved from https://innovareacademics.in/journals/index.php/ijap/article/view/45559

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