Hydroxamic acids block replication of hepatitis C virus

J Med Chem. 2015 Jan 22;58(2):785-800. doi: 10.1021/jm501330g.

Teng Ai ¹, Yanli Xu, Li Qiu, Robert J Geraghty, Liqiang Chen

Affiliations

Affiliation

1 Center for Drug Design, Academic Health Center, University of Minnesota , 516 Delaware Street S.E., Minneapolis, Minnesota 55455, United States.

PMID: 25490700 DOI: 10.1021/jm501330g

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.

Name
Email *

	Sorry, but the email address you supplied was invalid.