Discovery of highly potent small molecule Hepatitis C Virus entry inhibitors

Gopi Kumar Mittapalli; Andrew Jackson; Fang Zhao; Haekyung Lee; Stephine Chow; Jeffrey McKelvy; Flossie Wong-Staal; James E Macdonald

doi:10.1016/j.bmcl.2011.09.019

Discovery of highly potent small molecule Hepatitis C Virus entry inhibitors

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6852-5. doi: 10.1016/j.bmcl.2011.09.019. Epub 2011 Sep 16.

Authors

Gopi Kumar Mittapalli¹, Andrew Jackson, Fang Zhao, Haekyung Lee, Stephine Chow, Jeffrey McKelvy, Flossie Wong-Staal, James E Macdonald

Affiliation

¹ iTherX Pharmaceuticals, Inc., PO Box 910530, San Diego, CA 92191-0530, USA.

PMID: 21978675
DOI: 10.1016/j.bmcl.2011.09.019

Abstract

Novel, highly potent small molecule HCV entry inhibitors are reported. The SAR exploration of a hit molecule identified from screening of a compound library led to the identification of highly potent compounds with IC(50) values of <5 nM in the tissue culture HCV infectious assay.

MeSH terms

Animals
Antiviral Agents / chemistry*
Antiviral Agents / pharmacokinetics
Antiviral Agents / pharmacology*
Drug Discovery
Hepacivirus / drug effects*
Hepacivirus / physiology
Hepatitis C / drug therapy*
Humans
Inhibitory Concentration 50
Rats
Small Molecule Libraries / chemistry*
Small Molecule Libraries / pharmacokinetics
Small Molecule Libraries / pharmacology*
Structure-Activity Relationship
Virus Internalization / drug effects*

Substances

Antiviral Agents
Small Molecule Libraries