Further SAR studies on novel small molecule inhibitors of the hepatitis C (HCV) NS5B polymerase

T Jagadeeswar Reddy; Laval Chan; Nathalie Turcotte; Melanie Proulx; Oswy Z Pereira; Sanjoy K Das; Arshad Siddiqui; Wuyi Wang; Carl Poisson; Constantin G Yannopoulos; Darius Bilimoria; Lucille L'Heureux; Hicham M A Alaoui; Nghe Nguyen-Ba

doi:10.1016/s0960-894x(03)00670-x

Further SAR studies on novel small molecule inhibitors of the hepatitis C (HCV) NS5B polymerase

Bioorg Med Chem Lett. 2003 Oct 6;13(19):3341-4. doi: 10.1016/s0960-894x(03)00670-x.

Authors

T Jagadeeswar Reddy¹, Laval Chan, Nathalie Turcotte, Melanie Proulx, Oswy Z Pereira, Sanjoy K Das, Arshad Siddiqui, Wuyi Wang, Carl Poisson, Constantin G Yannopoulos, Darius Bilimoria, Lucille L'Heureux, Hicham M A Alaoui, Nghe Nguyen-Ba

Affiliation

¹ Shire BioChem Inc., 275 Armand-Frappier, Laval, Quebec, Canada H7V 4A7. treddy@ca.shire.com

PMID: 12951122
DOI: 10.1016/s0960-894x(03)00670-x

Abstract

Herein, we describe the structure-activity relationship (SAR) of N,N-disubstituted phenylalanine series of NS5B polymerase inhibitors of hepatitis C. The NS5B polymerase inhibitory activity of the most active compound exhibited an IC(50) of 2.7 microM.

MeSH terms

Enzyme Inhibitors / chemistry*
Enzyme Inhibitors / pharmacology
Hepacivirus / drug effects
Hepacivirus / enzymology*
Humans
RNA-Dependent RNA Polymerase / antagonists & inhibitors*
Structure-Activity Relationship
Viral Nonstructural Proteins / antagonists & inhibitors*
Viral Nonstructural Proteins / metabolism

Substances

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