Abstract
A series of nineteen 2-aryl-4H-chromen-4-one derivatives 2a-2s were synthesized and evaluated for their antiviral activity against Chikungunya virus (LR2006_OPY1) in Vero cell culture by CPE reduction assay. Three compounds 2a, 2b and 2g, were found to be active at concentration of (IC50) 0.44 M, 0.45 M and 2.02 M, respectively. Compounds having heterocyclic ring 2a and 2b at the 2nd position of the chromenone were found to be potent inhibitor of ChikV. Cytotoxicity studies were performed using Vero cell culture, compounds 2a and 2b exhibited SI of >100. Molecular docking simulation has been carried out to understand the possible mechanism of action.
Keywords: 2-aryl-4H-chromen-4-one derivatives against chikungunya virus (ChikV). CPE reduction assay, Cell viability assays, molecular docking studies.
Letters in Drug Design & Discovery
Title:Synthesis and Antiviral Activity of 2-aryl-4H-chromen-4-one Derivatives Against Chikungunya Virus
Volume: 13 Issue: 10
Author(s): Vishnu N. Badavath, Surender S. Jadav, Boris Pastorino, Xavier de Lamballerie, Barij N. Sinha and Venkatesan Jayaprakash
Affiliation:
Keywords: 2-aryl-4H-chromen-4-one derivatives against chikungunya virus (ChikV). CPE reduction assay, Cell viability assays, molecular docking studies.
Abstract: A series of nineteen 2-aryl-4H-chromen-4-one derivatives 2a-2s were synthesized and evaluated for their antiviral activity against Chikungunya virus (LR2006_OPY1) in Vero cell culture by CPE reduction assay. Three compounds 2a, 2b and 2g, were found to be active at concentration of (IC50) 0.44 M, 0.45 M and 2.02 M, respectively. Compounds having heterocyclic ring 2a and 2b at the 2nd position of the chromenone were found to be potent inhibitor of ChikV. Cytotoxicity studies were performed using Vero cell culture, compounds 2a and 2b exhibited SI of >100. Molecular docking simulation has been carried out to understand the possible mechanism of action.
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Badavath N. Vishnu, Jadav S. Surender, Pastorino Boris, Lamballerie de Xavier, Sinha N. Barij and Jayaprakash Venkatesan, Synthesis and Antiviral Activity of 2-aryl-4H-chromen-4-one Derivatives Against Chikungunya Virus, Letters in Drug Design & Discovery 2016; 13 (10) . https://dx.doi.org/10.2174/1570180813666160711163349
DOI https://dx.doi.org/10.2174/1570180813666160711163349 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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