Hepatitis C NS5B polymerase inhibitors: functional equivalents for the benzothiadiazine moiety

Douglas K Hutchinson; Charles A Flentge; Pamela L Donner; Rolf Wagner; Clarence J Maring; Warren M Kati; Yaya Liu; Sherie V Masse; Tim Middleton; Hongmei Mo; Debra Montgomery; Wen W Jiang; Gennadiy Koev; David W A Beno; Kent D Stewart; Vincent S Stoll; Akhteruzzaman Molla; Dale J Kempf

doi:10.1016/j.bmcl.2010.12.067

Hepatitis C NS5B polymerase inhibitors: functional equivalents for the benzothiadiazine moiety

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1876-9. doi: 10.1016/j.bmcl.2010.12.067. Epub 2011 Jan 13.

Authors

Douglas K Hutchinson¹, Charles A Flentge, Pamela L Donner, Rolf Wagner, Clarence J Maring, Warren M Kati, Yaya Liu, Sherie V Masse, Tim Middleton, Hongmei Mo, Debra Montgomery, Wen W Jiang, Gennadiy Koev, David W A Beno, Kent D Stewart, Vincent S Stoll, Akhteruzzaman Molla, Dale J Kempf

Affiliation

¹ Department of Antiviral Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA. hutsmi@sbcglobal.net

PMID: 21316235
DOI: 10.1016/j.bmcl.2010.12.067

Abstract

A series of quinoline derivatives was synthesized as potential bioisosteric replacements for the benzothiadiazine moiety of earlier Hepatitis C NS5B polymerase inhibitors. Several of these compounds exhibited potent activity in enzymatic and replicon assays.

MeSH terms

Benzothiadiazines / chemistry
Benzothiadiazines / pharmacology*
Hepacivirus / enzymology
Hepacivirus / physiology
Protease Inhibitors / chemistry
Protease Inhibitors / pharmacology*
Viral Nonstructural Proteins / antagonists & inhibitors*
Virus Replication

Substances

Benzothiadiazines
Protease Inhibitors
Viral Nonstructural Proteins
NS-5 protein, hepatitis C virus