Structure-activity relationship (SAR) optimization of 6-(Indol-2-yl) pyridine-3-sulfonamides: Identification of potent, selective, and orally bioavailable small molecules targeting hepatitis C (HCV) NS4B
A novel, potent, and orally bioavailable inhibitor of hepatitis C RNA replication targeting NS4B, compound 4t (PTC725), has been identified through chemical optimization of the 6-(indol-2-yl)pyridine-3-sulfonamide 2 to improve DMPK and safety properties.
Zhang, Nanjing,Zhang, Xiaoyan,Zhu, Jin,Turpoff, Anthony,Chen, Guangming,Morrill, Christie,Huang, Song,Lennox, William,Kakarla, Ramesh,Liu, Ronggang,Li, Chunshi,Ren, Hongyu,Almstead, Neil,Venkatraman, Srikanth,Njoroge, F. George,Gu, Zhengxian,Clausen, Valerie,Graci, Jason,Jung, Stephen P.,Zheng, Yingcong,Colacino, Joseph M.,Lahser, Fred,Sheedy, Josephine,Mollin, Anna,Weetall, Marla,Nomeir, Amin,Karp, Gary M.
p. 2121 - 2135
(2014/04/03)
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