Novel thiazolones as HCV NS5B polymerase allosteric inhibitors: Further designs, SAR, and X-ray complex structure

Structure–activity relationships (SAR) of 1 against HCV NS5B polymerase were described. SAR explorations and further structure-based design led to the identifications of 2 and 3 as novel HCV NS5B inhibitors. X-ray structure of 3 in complex with NS5B polymerase was obtained at a resolution of 2.2 Å, and confirmed the design.

Graphical abstractThe follow-up designs and more detailed SAR of thiazolone derivatives as novel inhibitors of HCV NS5B polymerase were described. The X-ray complex structure for the new inhibitor was obtained at a resolution of 2.2 Å, and confirmed the design.Figure optionsDownload full-size imageDownload as PowerPoint slide