title: Identification of thieno[3,2-b]pyrroles as allosteric inhibitors of hepatitis C virus NS5B polymerase.
abstract: Thieno[3,2-b]pyrroles are a novel class of allosteric inhibitors of HCV NS5B RNA-dependent RNA polymerase which show potent affinity for the NS5B enzyme. Introduction of a polar substituent in the position N1 led to a compound that efficiently blocks subgenomic HCV RNA replication in HUH-7 cells with an EC50 of 2.9 microM.
authors.affiliation: Department of Medicinal Chemistry, IRBM-MRL Rome, Via Pontina, Km 30.600, 00040 Pomezia (Rome), Italy. jesus_ontoria@merck.com
authors.forename: Jesus M
authors.initials: JM
authors.lastname: Ontoria
authors.forename: Jose I
authors.initials: JI
authors.lastname: Martìn Hernando
authors.forename: Savina
authors.initials: S
authors.lastname: Malancona
authors.forename: Barbara
authors.initials: B
authors.lastname: Attenni
authors.forename: Ian
authors.initials: I
authors.lastname: Stansfield
authors.forename: Immacolata
authors.initials: I
authors.lastname: Conte
authors.forename: Caterina
authors.initials: C
authors.lastname: Ercolani
authors.forename: Jörg
authors.initials: J
authors.lastname: Habermann
authors.forename: Simona
authors.initials: S
authors.lastname: Ponzi
authors.forename: Marcello
authors.initials: M
authors.lastname: Di Filippo
authors.forename: Uwe
authors.initials: U
authors.lastname: Koch
authors.forename: Michael
authors.initials: M
authors.lastname: Rowley
authors.forename: Frank
authors.initials: F
authors.lastname: Narjes
mesh_terms: D000494:Allosteric Regulation; D011480:Protease Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D011758:Pyrroles / Q000737:chemistry* / Q000494:pharmacology; D017361:Viral Nonstructural Proteins / Q000037:antagonists & inhibitors*; D012324:RNA-Dependent RNA Polymerase
chemical_list: D011480:Protease Inhibitors; D011758:Pyrroles; D017361:Viral Nonstructural Proteins; C087036:NS-5 protein, hepatitis C virus; D012324:RNA-Dependent RNA Polymerase