| Literature DB >> 22784640 |
Gopi Kumar Mittapalli1, Fang Zhao, Andrew Jackson, Hongfeng Gao, Haekyung Lee, Stephine Chow, Maninder Pal Kaur, Natalie Nguyen, Robert Zamboni, Jeffrey McKelvy, Flossie Wong-Staal, James E Macdonald.
Abstract
The manuscript reports an identification of a highly potent, orally bioavailable hepatitis C virus entry inhibitor through optimization of a previously reported class of molecules (1) that were not stable in the rat plasma. Compound 39 (ITX 4520) exhibited an excellent PK profile in both rats and dogs with good oral exposure, half-life and oral bioavailability. The compound is also well-tolerated in the preliminary in vivo toxicity studies and has been selected as a pre-clinical candidate for our HCV clinical pipeline.Entities:
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Year: 2012 PMID： 22784640 DOI： 10.1016/j.bmcl.2012.06.038
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823