Novel 4-Thiazolidinones as Non-Nucleoside Inhibitors of Hepatitis C Virus NS5B RNA-Dependent RNA Polymerase


Cakir G., KÜÇÜKGÜZEL İ. , Guhamazumder R., TATAR E. , Manvar D., Basu A., ...More

ARCHIV DER PHARMAZIE, vol.348, no.1, pp.10-22, 2015 (Journal Indexed in SCI) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 348 Issue: 1
  • Publication Date: 2015
  • Doi Number: 10.1002/ardp.201400247
  • Title of Journal : ARCHIV DER PHARMAZIE
  • Page Numbers: pp.10-22

Abstract

In continuation of our efforts to develop new derivatives as hepatitis C virus (HCV) NS5B inhibitors, we synthesized novel 5-arylidene-4-thiazolidinones. The novel compounds 29-42, together with their synthetic precursors 22-28, were tested for HCV NS5B inhibitory activity; 12 of these compounds displayed IC50 values between 25.3 and 54.1 mu M. Compound 33, an arylidene derivative, was found to be the most active compound in this series with an IC50 value of 25.3 mu M. Molecular docking studies were performed on the thumb pocket-II of NS5B to postulate the binding mode for these compounds.