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Eur J Med Chem. 2015 Jan 7;89:172-8. doi: 10.1016/j.ejmech.2014.10.042. Epub 2014 Oct 16.

Thiazolidone derivatives as inhibitors of chikungunya virus.

Author information

1
Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Mesra, Ranchi 835215, Jharkhand, India.
2
Institute of Biochemistry, Center for Structural and Cell Biology in Medicine, University of Lübeck, 23538 Lübeck, Germany; German Center for Infection Research (DZIF), Lübeck, Germany.
3
UMR_D 190 "Emergence des Pathologies Virales", Aix-Marseille University, IRD French Institute of Research for Development, EHESP French School of Public Health, Marseille, France.
4
UMR_D 190 "Emergence des Pathologies Virales", Aix-Marseille University, IRD French Institute of Research for Development, EHESP French School of Public Health, Marseille, France. Electronic address: Xavier.De-Lamballerie@medecine.univ-mrs.fr.
5
Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Mesra, Ranchi 835215, Jharkhand, India. Electronic address: drvenkatesanj@gmail.com.

Abstract

A series of arylalkylidene derivatives of 1,3-thiazolidin-4-one (1-20) were synthesized and tested for their antiviral activity against chikungunya virus (LR2006_OPY1) in Vero cell culture by CPE reduction assay. Five compounds (7-9, 16 and 19) were identified to have anti-ChikV activity at lower micro molar concentration. The compounds 7, 8, 9, 16 and 19 inhibited the virus at 0.42, 4.2, 3.6, 40.1 and 6.8 μM concentrations respectively. Molecular docking simulation has been carried out using the available X-ray crystal structure of the ChikV nsp2 protease, in order to elucidate the possible mechanism of action. Interaction of ligands with ChikV nsp2 protease (PDB Code: 3TRK) suggested the possible mechanism of protease inhibition to act as potent anti-ChikV agents.

KEYWORDS:

Antiviral; Chikungunya virus; Molecular docking; Thiazolidinone; nsp2 protease

PMID:
25462237
DOI:
10.1016/j.ejmech.2014.10.042
[Indexed for MEDLINE]

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