Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10595588 | Bioorganic & Medicinal Chemistry Letters | 2013 | 5 Pages |
Abstract
A series of novel 2-phenylindole analogs were synthesized and evaluated for activity in subgenomic HCV replicon inhibition assays. Several compounds containing small alkyl sulfonamides on the phenyl ring exhibiting submicromolar EC50 values against the genotype 1b replicon were identified. Among these, compound 25d potently inhibited the 1b replicon (EC50 = 0.17 μM) with 147-fold selectivity with respect to cytotoxicity. Compound 25d was stable in the presence of human liver microsomes and had a good pharmacokinetic profile in rats with an IV half-life of 4.3 h and oral bioavailability (F) of 58%.
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Guangming Chen, Hongyu Ren, Anthony Turpoff, Alexander Arefolov, Richard Wilde, James Takasugi, Atiyya Khan, Neil Almstead, Zhengxian Gu, Takashi Komatsu, Connie Freund, Jamie Breslin, Joseph Colacino, Jean Hedrick, Marla Weetall, Gary M. Karp,