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Inhibitors of hepatitis C virus NS3/4A: alpha-ketoamide based macrocyclic inhibitors.

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Avolio S,Robertson K,Hernando JI,DiMuzio J,Summa V

doi

10.1016/j.bmcl.2009.02.079

subject

Has Abstract

pub_date

2009-04-15 00:00:00

pages

2295-8

issue

8

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(09)00233-9

journal_volume

19

pub_type

杂志文章

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