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., ...Daha Fazla

ARCHIV DER PHARMAZIE, cilt.348, sa.1, ss.10-22, 2015 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Cilt numarası: 348 Konu: 1
  • Basım Tarihi: 2015
  • Doi Numarası: 10.1002/ardp.201400247
  • Dergi Adı: ARCHIV DER PHARMAZIE
  • Sayfa Sayıları: ss.10-22

Özet

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.