Synthesis of thiazolone-based sulfonamides as inhibitors of HCV NS5B polymerase

Yili Ding; Kenneth L Smith; Chamakura V N S Varaprasad; Eugene Chang; John Alexander; Nanhua Yao

doi:10.1016/j.bmcl.2006.08.104

Synthesis of thiazolone-based sulfonamides as inhibitors of HCV NS5B polymerase

Bioorg Med Chem Lett. 2007 Feb 1;17(3):841-5. doi: 10.1016/j.bmcl.2006.08.104. Epub 2006 Sep 20.

Authors

Yili Ding¹, Kenneth L Smith, Chamakura V N S Varaprasad, Eugene Chang, John Alexander, Nanhua Yao

Affiliation

¹ Drug Discovery, Valeant Pharmaceuticals Research & Development, 3300 Hyland Avenue Costa Mesa, CA 92626, USA. [email protected]

PMID: 16990004
DOI: 10.1016/j.bmcl.2006.08.104

Abstract

Several thiazolone-based sulfonamides were prepared, utilizing various hetero-aryl sulfonyl chlorides and different aldehydes, as inhibitors of NS5B polymerase, to target HCV. The best compound showed 0.6 microM [corrected] of IC50 inhibitory activity.

MeSH terms

Antiviral Agents / chemical synthesis*
Antiviral Agents / pharmacology*
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / pharmacology*
Indicators and Reagents
Structure-Activity Relationship
Sulfonamides / chemical synthesis*
Sulfonamides / pharmacology*
Thiazoles / chemical synthesis*
Thiazoles / pharmacology*
Viral Nonstructural Proteins / antagonists & inhibitors*

Substances

Antiviral Agents
Enzyme Inhibitors
Indicators and Reagents
Sulfonamides
Thiazoles
Viral Nonstructural Proteins
NS-5 protein, hepatitis C virus