Hydroxamic acids block replication of hepatitis c virus

Teng Ai, Yanli Xu, Li Qiu, Robert J. Geraghty, Liqiang Chen

Research output: Contribution to journalArticlepeer-review

30 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)785-800
Number of pages16
JournalJournal of medicinal chemistry
Volume58
Issue number2
DOIs
StatePublished - Jan 22 2015

Bibliographical note

Publisher Copyright:
© 2014 American Chemical Society.

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