%0 Journal Article
%9 ACL : Articles dans des revues avec comité de lecture répertoriées par l'AERES
%A Jadav, S. S.
%A Sinha, B. N.
%A Hilgenfeld, R.
%A Pastorino, B.
%A de Lamballerie, Xavier
%A Jayaprakash, V.
%T Thiazolidone derivatives as inhibitors of chikungunya virus
%D 2015
%L PAR00012711
%G ENG
%J European Journal of Medicinal Chemistry
%@ 0223-5234
%K Thiazolidinone ; Antiviral ; Chikungunya virus ; nsp2 protease ; Molecular ; docking
%M ISI:000348003500018
%P 172-178
%R 10.1016/j.ejmech.2014.10.042
%U https://www.documentation.ird.fr/hor/PAR00012711
%V 89
%W Horizon (IRD)
%X 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.
%$ 052