2. Academic Validation
  3. Thiazolidone derivatives as inhibitors of chikungunya virus

Thiazolidone derivatives as inhibitors of chikungunya virus

  • Eur J Med Chem. 2015 Jan 7;89:172-8. doi: 10.1016/j.ejmech.2014.10.042.
Surender Singh Jadav 1,  Barij Nayan Sinha 1,  Rolf Hilgenfeld 2,  Boris Pastorino 3,  Xavier de Lamballerie 4,  Venkatesan Jayaprakash 5
Affiliations

Affiliations

  • 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: [email protected].
  • 5 Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Mesra, Ranchi 835215, Jharkhand, India. Electronic address: [email protected].
PMID: 25462237 DOI: 10.1016/j.ejmech.2014.10.042
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.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-117289
    99.37%, Arylalkylidene Derivative