| Literature DB >> 19285390 |
Salvatore Avolio1, Keith Robertson, Josè Ignacio Martin Hernando, Jillian DiMuzio, Vincenzo Summa.
Abstract
A novel series of hepatitis C virus (HCV) NS3/4A protease inhibitors bearing a P2-P4 macrocycle and a P1-P1' alpha-ketoamide serine trap is reported. The NS3 protease, which is essential for viral replication, is considered one of the most attractive targets for developing novel anti-HCV therapies. The optimization of both the macrocycle and the warhead portions led to the discovery of compounds 8b and 8 g with a good activity both in the enzyme as well as in the cell based (replicon) assays with favorable PK profile in a preclinical species.Entities:
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Year: 2009 PMID： 19285390 DOI： 10.1016/j.bmcl.2009.02.079
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823