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Discovery of SCH446211 (SCH6): a new ketoamide inhibitor of the HCV NS3 serine protease and HCV subgenomic RNA replication. 2006
Stéphane L Bogen, and
Ashok Arasappan, and
Frank Bennett, and
Kevin Chen, and
Edwin Jao, and
Yi-Tsung Liu, and
Raymond G Lovey, and
Srikanth Venkatraman, and
Weidong Pan, and
Tajel Parekh, and
Russel E Pike, and
Sumei Ruan, and
Rong Liu, and
Bahige Baroudy, and
Sony Agrawal, and
Robert Chase, and
Paul Ingravallo, and
John Pichardo, and
Andrew Prongay, and
Jean-Marc Brisson, and
Tony Y Hsieh, and
Kuo-Chi Cheng, and
Scott J Kemp, and
Odile E Levy, and
Marguerita Lim-Wilby, and
Susan Y Tamura, and
Anil K Saksena, and
Viyyoor Girijavallabhan, and
F George Njoroge
Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, USA. Stephane.Bogen@spcorp.com
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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