Hepatitis C virus NS3-4A serine protease inhibitors: SAR of P2′ moiety with improved potency

We have discovered that introduction of appropriate amino acid derivatives at P2′ position improved the binding potency of P3-capped α-ketoamide inhibitors of HCV NS3 serine protease. X-ray crystal structure of one of the inhibitors (43) bound to the protease revealed the importance of the P2′ moiety.

Graphical abstractIntroduction of appropriate amino acid derivatives at P′2 position improved the binding potency of P3-capped α-ketoamide inhibitors of HCV NS3 serine protease. X-ray crystal structure of one of the inhibitors (43) bound to the protease revealed the importance of the P′2 moiety.Figure optionsDownload full-size imageDownload as PowerPoint slide