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ID: ALA3352512

Journal: Eur J Med Chem

Title: Thiazolidone derivatives as inhibitors of chikungunya virus.

Authors: Jadav SS, Sinha BN, Hilgenfeld R, Pastorino B, de Lamballerie X, Jayaprakash V.

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.

CiteXplore: 25462237

DOI: 10.1016/j.ejmech.2014.10.042