Tetrahydrobenzothiophene inhibitors of hepatitis C virus NS5B polymerase

M G Laporte; T A Lessen; L Leister; D Cebzanov; E Amparo; C Faust; D Ortlip; T R Bailey; T J Nitz; S K Chunduru; D C Young; C J Burns

doi:10.1016/j.bmcl.2005.09.047

Tetrahydrobenzothiophene inhibitors of hepatitis C virus NS5B polymerase

Bioorg Med Chem Lett. 2006 Jan 1;16(1):100-3. doi: 10.1016/j.bmcl.2005.09.047. Epub 2005 Nov 2.

Authors

M G Laporte¹, T A Lessen, L Leister, D Cebzanov, E Amparo, C Faust, D Ortlip, T R Bailey, T J Nitz, S K Chunduru, D C Young, C J Burns

Affiliation

¹ ViroPharma Incorporated, 397 Eagleview Boulevard, Exton, PA 19341, USA. mlaporte@gentara.net

PMID: 16260131
DOI: 10.1016/j.bmcl.2005.09.047

Abstract

A novel series of selective HCV NS5B RNA dependent RNA polymerase inhibitors has been disclosed. These compounds contain an appropriately substituted tetrahydrobenzothiophene scaffold. This communication will detail the SAR and activities of this series.

MeSH terms

Caco-2 Cells
Chemistry, Pharmaceutical / methods*
Drug Design
Drug Evaluation, Preclinical
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
Hepacivirus / enzymology*
Humans
Models, Chemical
Protein Structure, Tertiary
RNA-Dependent RNA Polymerase / antagonists & inhibitors
Structure-Activity Relationship
Sulfonamides / chemistry
Thiophenes / chemistry*
Thiophenes / pharmacology*
Viral Nonstructural Proteins / antagonists & inhibitors*

Substances

Enzyme Inhibitors
Sulfonamides
Thiophenes
Viral Nonstructural Proteins
NS-5 protein, hepatitis C virus
RNA-Dependent RNA Polymerase