A one pot synthesis of novel bioactive tri-substitute-condensed-imidazopyridines that targets snake venom phospholipase a(2)

Anilkumar, N. C. and Sundaram, M. S. and Mohan, C. D. and Rangappa, S. and Bulusu, K. C. and Fuchs, J. E. and Girish, K. S. and Bender, A. and Basappa and Rangappa, K. S. (2015) A one pot synthesis of novel bioactive tri-substitute-condensed-imidazopyridines that targets snake venom phospholipase a(2). PLOS ONE, 10 (7). ISSN 1932-6203

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Abstract

Drugs such as necopidem, saripidem, alpidem, zolpidem, and olprinone contain nitrogen-containing bicyclic, condensed-imidazo1,2-alpha]pyridines as bioactive scaffolds. In this work, we report a high-yield one pot synthesis of 1-(2-methyl-8-aryl-substitued-imidazo1,2-alpha]pyridin-3-yl)ethan-1-o nefor the first-time. Subsequently, we performed in silico mode-of-action analysis and predicted that the synthesized imidazopyridines targets Phospholipase A(2) (PLA(2)). In vitro analysis confirmed the predicted target PLA(2) for the novel imidazopyridine derivative1-(2-Methyl-8-naphthalen-1-yl-imidazo1,2-alpha]pyridine-3-y l)-ethanone (compound 3f) showing significant inhibitory activity towards snake venom PLA(2) with an IC50 value of 14.3 mu M. Evidently, the molecular docking analysis suggested that imidazopyridine compound was able to bind to the active site of the PLA(2) with strong affinity, whose affinity values are comparable to nimesulide. Furthermore, we estimated the potential for oral bio-availability by Lipinski's Rule of Five. Hence, it is concluded that the compound 3f could be a lead molecule against snake venom PLA(2).

Item Type:	Article
Subjects:	C Chemical Science > Biochemistry C Chemical Science > Chemistry
Divisions:	Department of > Biochemistry Department of > Chemistry
Depositing User:	Users 19 not found.
Date Deposited:	03 Jun 2019 05:55
Last Modified:	03 Jun 2019 05:55
URI:	http://eprints.uni-mysore.ac.in/id/eprint/2082

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