Inhibitors of HCV NS5B polymerase. Part 2: Evaluation of the northern region of (2Z)-2-benzoylamino-3-(4-phenoxy-phenyl)-acrylic acid.
A novel series of non-nucleoside HCV NS5B polymerase inhibitors was prepared from a (2Z)-2-benzoylamino-3-(4-phenoxy-phenyl)-acrylic acid template. Solution and solid phase analog synthesis focused on the northern region of the template combined with structure based design led to the discovery of several potent and orally bioavailable lead compounds.
Pfefferkorn
Jeffrey A
JA
Pfizer Global Research & Development, Michigan Laboratories, Ann Arbor, 48105, USA. jeffrey.a.pfefferkorn@pfizer.com
Nugent
Richard
R
Gross
Rebecca J
RJ
Greene
Meredith
M
Mitchell
Mark A
MA
Reding
Matthew T
MT
Funk
Lee A
LA
Anderson
Rebecca
R
Wells
Peter A
PA
Shelly
John A
JA
Anstadt
Robert
R
Finzel
Barry C
BC
Harris
Melissa S
MS
Kilkuskie
Robert E
RE
Kopta
Laurice A
LA
Schwende
Francis J
FJ
D000179:Acrylates / Q000737:chemistry* / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D012324:RNA-Dependent RNA Polymerase / Q000037:antagonists & inhibitors*; D017361:Viral Nonstructural Proteins / Q000037:antagonists & inhibitors*
C504932:(2Z)-2-benzoylamino-3-(4-phenoxy-phenyl)-acrylic acid; D000179:Acrylates; D004791:Enzyme Inhibitors; D017361:Viral Nonstructural Proteins; C087036:NS-5 protein, hepatitis C virus; D012324:RNA-Dependent RNA Polymerase