Authors
Ashok Arasappan, Frank Bennett, Stephane L Bogen, Srikanth Venkatraman, Melissa Blackman, Kevin X Chen, Siska Hendrata, Yuhua Huang, Regina M Huelgas, Latha Nair, Angela I Padilla, Weidong Pan, Russell Pike, Patrick Pinto, Sumei Ruan, Mousumi Sannigrahi, Francisco Velazquez, Bancha Vibulbhan, Wanli Wu, Weiying Yang, Anil K Saksena, Viyyoor Girijavallabhan, Neng-Yang Shih, Jianshe Kong, Tao Meng, Yan Jin, Jesse Wong, Paul McNamara, Andrew Prongay, Vincent Madison, John J Piwinski, Kuo-Chi Cheng, Richard Morrison, Bruce Malcolm, Xiao Tong, Robert Ralston, F George Njoroge
Publication date
2010/5/13
Journal
ACS medicinal chemistry letters
Volume
1
Issue
2
Pages
64-69
Publisher
American Chemical Society
Description
Boceprevir (SCH 503034), 1, a novel HCV NS3 serine protease inhibitor discovered in our laboratories, is currently undergoing phase III clinical trials. Detailed investigations toward a second generation protease inhibitor culminated in the discovery of narlaprevir (SCH 900518), 37, with improved potency (∼10-fold over 1), pharmacokinetic profile and physicochemical characteristics, currently in phase II human trials. Exploration of synthetic sequence for preparation of 37 resulted in a route that required no silica gel purification for the entire synthesis.
Total citations
Scholar articles
Discovery of narlaprevir (SCH 900518): a potent, second generation HCV NS3 serine protease inhibitor
A Arasappan, F Bennett, SL Bogen, S Venkatraman… - ACS medicinal chemistry letters, 2010