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. 2006 May 4;49(9):2750-7.
doi: 10.1021/jm060077j.

Discovery of SCH446211 (SCH6): a new ketoamide inhibitor of the HCV NS3 serine protease and HCV subgenomic RNA replication

Stéphane L Bogen  1 , Ashok Arasappan, Frank Bennett, Kevin Chen, Edwin Jao, Yi-Tsung Liu, Raymond G Lovey, Srikanth Venkatraman, Weidong Pan, Tajel Parekh, Russel E Pike, Sumei Ruan, Rong Liu, Bahige Baroudy, Sony Agrawal, Robert Chase, Paul Ingravallo, John Pichardo, Andrew Prongay, Jean-Marc Brisson, Tony Y Hsieh, Kuo-Chi Cheng, Scott J Kemp, Odile E Levy, Marguerita Lim-Wilby, Susan Y Tamura, Anil K Saksena, Viyyoor Girijavallabhan, F George Njoroge
Affiliations

Discovery of SCH446211 (SCH6): a new ketoamide inhibitor of the HCV NS3 serine protease and HCV subgenomic RNA replication

Stéphane L Bogen et al. J Med Chem. .

Abstract

Introduction of various modified prolines at P(2) and optimization of the P(1) side chain led to the discovery of SCH6 (24, Table 2), a potent ketoamide inhibitor of the HCV NS3 serine protease. In addition to excellent enzyme potency (K(i)*= 3.8 nM), 24 was also found to be a potent inhibitor of HCV subgenomic RNA replication with IC(50) and IC(90) of 40 and 100 nM, respectively. Recently, antiviral activity of 24 was demonstrated with inhibition of the full-length genotype 2a HCV genome. In addition, 24 was found to restore the responsiveness of the interferon regulatory factor 3 (IRF-3) in cells containing HCV RNA replicons.

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