title: Discovery of thiophene-2-carboxylic acids as potent inhibitors of HCV NS5B polymerase and HCV subgenomic RNA replication. Part 1: Sulfonamides.
abstract: The discovery of a novel class of HCV NS5B polymerase inhibitors, 3-arylsulfonylamino-5-phenyl-thiophene-2-carboxylic acids is described. SAR studies have yielded several potent inhibitors of HCV polymerase as well as of HCV subgenomic RNA replication in Huh-7 cells.
authors.affiliation: Shire BioChem Inc., 275 Armand-Frappier, Laval, Quebec, Canada H7V 4A7. lchan@ca.shire.com
authors.forename: Laval
authors.initials: L
authors.lastname: Chan
authors.forename: Sanjoy K
authors.initials: SK
authors.lastname: Das
authors.forename: T Jagadeeswar
authors.initials: TJ
authors.lastname: Reddy
authors.forename: Carl
authors.initials: C
authors.lastname: Poisson
authors.forename: Mélanie
authors.initials: M
authors.lastname: Proulx
authors.forename: Oswy
authors.initials: O
authors.lastname: Pereira
authors.forename: Marc
authors.initials: M
authors.lastname: Courchesne
authors.forename: Caroline
authors.initials: C
authors.lastname: Roy
authors.forename: Wuyi
authors.initials: W
authors.lastname: Wang
authors.forename: Arshad
authors.initials: A
authors.lastname: Siddiqui
authors.forename: Constantin G
authors.initials: CG
authors.lastname: Yannopoulos
authors.forename: Nghe
authors.initials: N
authors.lastname: Nguyen-Ba
authors.forename: Denis
authors.initials: D
authors.lastname: Labrecque
authors.forename: Richard
authors.initials: R
authors.lastname: Bethell
authors.forename: Martine
authors.initials: M
authors.lastname: Hamel
authors.forename: Philippe
authors.initials: P
authors.lastname: Courtemanche-Asselin
authors.forename: Lucille
authors.initials: L
authors.lastname: L'Heureux
authors.forename: Maud
authors.initials: M
authors.lastname: David
authors.forename: Olivier
authors.initials: O
authors.lastname: Nicolas
authors.forename: Stéphanie
authors.initials: S
authors.lastname: Brunette
authors.forename: Darius
authors.initials: D
authors.lastname: Bilimoria
authors.forename: Jean
authors.initials: J
authors.lastname: Bédard
mesh_terms: D002264:Carboxylic Acids; D006528:Carcinoma, Hepatocellular / Q000737:chemistry / Q000201:enzymology / Q000821:virology; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D016679:Genome, Viral; D016174:Hepacivirus / Q000201:enzymology*; D006801:Humans; D008113:Liver Neoplasms / Q000737:chemistry / Q000201:enzymology / Q000821:virology; D012367:RNA, Viral / Q000378:metabolism*; D012324:RNA-Dependent RNA Polymerase / Q000037:antagonists & inhibitors; D012093:Replicon / Q000187:drug effects; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology*; D013876:Thiophenes / Q000737:chemistry / Q000494:pharmacology*; D017361:Viral Nonstructural Proteins / Q000037:antagonists & inhibitors*; D014779:Virus Replication / Q000187:drug effects
chemical_list: D002264:Carboxylic Acids; D004791:Enzyme Inhibitors; D012367:RNA, Viral; D013449:Sulfonamides; D013876:Thiophenes; D017361:Viral Nonstructural Proteins; C550746:2-thiophene carboxylic acid; C087036:NS-5 protein, hepatitis C virus; D012324:RNA-Dependent RNA Polymerase