Jadav S. S., Sinha B. N., Hilgenfeld R., Pastorino B., de Lamballerie Xavier, Jayaprakash V. (2015). Thiazolidone derivatives as inhibitors of chikungunya virus. European Journal of Medicinal Chemistry, 89, p. 172-178. ISSN 0223-5234.
Titre du document
Thiazolidone derivatives as inhibitors of chikungunya virus
Jadav S. S., Sinha B. N., Hilgenfeld R., Pastorino B., de Lamballerie Xavier, Jayaprakash V.
Source
European Journal of Medicinal Chemistry, 2015,
89, p. 172-178 ISSN 0223-5234
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 mu M 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.