1130322-33-6Relevant articles and documents
II. Novel HCV NS5B polymerase inhibitors: Discovery of indole C2 acyl sulfonamides
Anilkumar, Gopinadhan N.,Selyutin, Oleg,Rosenblum, Stuart B.,Zeng, Qingbei,Jiang, Yueheng,Chan, Tin-Yau,Pu, Haiyan,Wang, Li,Bennett, Frank,Chen, Kevin X.,Lesburg, Charles A.,Duca, Jose,Gavalas, Stephen,Huang, Yuhua,Pinto, Patrick,Sannigrahi, Mousumi,Velazquez, Francisco,Venkatraman, Srikanth,Vibulbhan, Bancha,Agrawal, Sony,Ferrari, Eric,Jiang, Chuan-Kui,Huang,Shih, Neng-Yang,George Njoroge,Kozlowski, Joseph A.
scheme or table, p. 713 - 717 (2012/02/04)
Development of SAR at the C2 position of indole lead 1, a palm site inhibitor of HCV NS5B polymerase (NS5B IC50 = 0.053 μM, replicon EC50 = 4.8 μM), is described. Initial screening identified an acyl sulfonamide moiety as an isostere for the C2 carboxylic acid group. Further SAR investigation resulted in identification of acyl sufonamide analog 7q (NS5B IC50 = 0.039 μM, replicon EC50 = 0.011 μM) with >100-fold improved replicon activity.