title: Further SAR studies on novel small molecule inhibitors of the hepatitis C (HCV) NS5B polymerase.
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.
authors.affiliation: Shire BioChem Inc., 275 Armand-Frappier, Laval, Quebec, Canada H7V 4A7. treddy@ca.shire.com
authors.forename: T Jagadeeswar
authors.initials: TJ
authors.lastname: Reddy
authors.forename: Laval
authors.initials: L
authors.lastname: Chan
authors.forename: Nathalie
authors.initials: N
authors.lastname: Turcotte
authors.forename: Melanie
authors.initials: M
authors.lastname: Proulx
authors.forename: Oswy Z
authors.initials: OZ
authors.lastname: Pereira
authors.forename: Sanjoy K
authors.initials: SK
authors.lastname: Das
authors.forename: Arshad
authors.initials: A
authors.lastname: Siddiqui
authors.forename: Wuyi
authors.initials: W
authors.lastname: Wang
authors.forename: Carl
authors.initials: C
authors.lastname: Poisson
authors.forename: Constantin G
authors.initials: CG
authors.lastname: Yannopoulos
authors.forename: Darius
authors.initials: D
authors.lastname: Bilimoria
authors.forename: Lucille
authors.initials: L
authors.lastname: L'Heureux
authors.forename: Hicham M A
authors.initials: HM
authors.lastname: Alaoui
authors.forename: Nghe
authors.initials: N
authors.lastname: Nguyen-Ba
mesh_terms: 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
chemical_list: D004791:Enzyme Inhibitors; D017361:Viral Nonstructural Proteins; C087036:NS-5 protein, hepatitis C virus; D012324:RNA-Dependent RNA Polymerase