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Discovery of functionalized bisimidazoles bearing cyclic aliphatic-phenyl motifs as HCV NS5A inhibitors.

Abstract：

:This Letter describes the discovery of a number of functionalized bisimidazoles bearing a cyclohexylphenyl, piperidylphenyl, or bicyclo[2,2,2]octylphenyl motif as HCV NS5A inhibitors. Compounds 2c, 4b and 6 have demonstrated low single-digit nM potency in gt-1a replicon and double-digit pM potency in gt-1b replicon, respectively. Moreover, both 4b and 6 have, respectively, exhibited good oral bioavailability in rats with a favorable liver/plasma ratio of the drug concentration.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Zhong M,Peng E,Huang N,Huang Q,Huq A,Lau M,Colonno R,Li L

doi

10.1016/j.bmcl.2014.10.057

subject

Has Abstract

pub_date

2014-12-15 00:00:00

pages

5731-5737

issue

24

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(14)01117-2

journal_volume

24

pub_type

杂志文章

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