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Hydroxamic acids block replication of hepatitis C virus.

Abstract：

:Intrigued by the role of protein acetylation in hepatitis C virus (HCV) replication, we tested known histone deacetylase (HDAC) inhibitors and a focused library of structurally simple hydroxamic acids for inhibition of a HCV subgenomic replicon. While known HDAC inhibitors with varied inhibitory profiles proved to be either relatively toxic or ineffective, structure-activity relationship (SAR) studies on cinnamic hydroxamic acid and benzo[b]thiophen-2-hydroxamic acid gave rise to compounds 22 and 53, which showed potent and selective anti-HCV activity and therefore are promising starting points for further structural optimization and mechanistic studies.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Ai T,Xu Y,Qiu L,Geraghty RJ,Chen L

doi

10.1021/jm501330g

subject

Has Abstract

pub_date

2015-01-22 00:00:00

pages

785-800

issue

2

eissn

0022-2623

issn

1520-4804

journal_volume

58

pub_type

杂志文章

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