Further SAR studies on novel small molecule inhibitors of the hepatitis C (HCV) NS5B polymerase.
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.
Reddy
T Jagadeeswar
TJ
Shire BioChem Inc., 275 Armand-Frappier, Laval, Quebec, Canada H7V 4A7. treddy@ca.shire.com
Chan
Laval
L
Turcotte
Nathalie
N
Proulx
Melanie
M
Pereira
Oswy Z
OZ
Das
Sanjoy K
SK
Siddiqui
Arshad
A
Wang
Wuyi
W
Poisson
Carl
C
Yannopoulos
Constantin G
CG
Bilimoria
Darius
D
L'Heureux
Lucille
L
Alaoui
Hicham M A
HM
Nguyen-Ba
Nghe
N
D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D016174:Hepacivirus / Q000187:drug effects / Q000201:enzymology*; D006801:Humans; D012324:RNA-Dependent RNA Polymerase / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D017361:Viral Nonstructural Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism
D004791:Enzyme Inhibitors; D017361:Viral Nonstructural Proteins; C087036:NS-5 protein, hepatitis C virus; D012324:RNA-Dependent RNA Polymerase