Synthesis and Biological Evaluation of Imidazole derivatives against the Metallo-Β-Lactamase IMP-1

Bharat Kumar Tyagi; Chandra Kishore Tyagi

doi:10.5958/2231-5691.2020.00026.X

Asian Journal of Pharmaceutical Research

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2231-5691 (Online)
2231-5683 (Print)

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Synthesis and Biological Evaluation of Imidazole derivatives against the Metallo-Β-Lactamase IMP-1

Author(s): Bharat Kumar Tyagi, Chandra Kishore Tyagi

Email(s): kishore198012@gmail.com

DOI: 10.5958/2231-5691.2020.00026.X

Address: Bharat Kumar Tyagi, Chandra Kishore Tyagi
Sri Satya Sai University of Technology and Medical Sciences, Village Pachama, Sehore-466001, Madhya Pradesh.
*Corresponding Author

Published In: Volume - 10, Issue - 3, Year - 2020

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ABSTRACT:
Mutations in bacteria can result in antibiotic resistance due to the overuse or abuse of ß-lactam antibiotics. One strategy which bacteria can become resistance toward antibiotics is secreting of metallo-ß-lactamase enzymes that can open the lactam ring of the ß-lactam antibiotic and inactivate them. This issue is a threat for human health and one strategy to overcome this situation is co-administration of ß-lactam antibiotics with an inhibitor. So far, no clinically available inhibitors of metallo ß-lactamases (MBLs) reported and the clinically inhibitors of serine ß-lactamase are useless for MBLs. Accordingly, finding a potent inhibitor of the MBLs being very important. In this study, imidazole derivatives primarily were synthesized and their inhibitory activity was measured. Later in silico binding model was used to predict the configuration and conformation of the ligands into the active site of enzyme. Two molecules demonstrated with IC50 of 39 µM and 46 µM against MBL (IMP-1).

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Cite this article:
Bharat Kumar Tyagi, Chandra Kishore Tyagi. Synthesis and Biological Evaluation of Imidazole derivatives against the Metallo-Β-Lactamase IMP-1. Asian J. Pharm. Res. 2020; 10(3):140-148. doi: 10.5958/2231-5691.2020.00026.X

Cite(Electronic):
Bharat Kumar Tyagi, Chandra Kishore Tyagi. Synthesis and Biological Evaluation of Imidazole derivatives against the Metallo-Β-Lactamase IMP-1. Asian J. Pharm. Res. 2020; 10(3):140-148. doi: 10.5958/2231-5691.2020.00026.X Available on: https://asianjpr.com/AbstractView.aspx?PID=2020-10-3-2

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DOI: 10.5958/2231–5691