title: Discovery of 4H-pyrazolo[1,5-a]pyrimidin-7-ones as potent inhibitors of hepatitis C virus polymerase.
abstract: A series of 4H-pyrazolo[1,5-a]pyrimidin-7-one derivatives was synthesized and evaluated for inhibitory activity against HCV NS5B RNA-dependent RNA polymerase. A number of these compounds exhibited potent activity in enzymatic assay. The synthesis and structure-activity relationship are also described.
authors.affiliation: Schering-Plough Research Institute Cambridge, 320 Bent Street, Cambridge, MA 02141, United States. yongqi.deng@spcorp.com
authors.forename: Yongqi
authors.initials: Y
authors.lastname: Deng
authors.forename: Gerald W
authors.initials: GW
authors.lastname: Shipps
authors.forename: Tong
authors.initials: T
authors.lastname: Wang
authors.forename: Janeta
authors.initials: J
authors.lastname: Popovici-Muller
authors.forename: Kristin E
authors.initials: KE
authors.lastname: Rosner
authors.forename: M Arshad
authors.initials: MA
authors.lastname: Siddiqui
authors.forename: Jose
authors.initials: J
authors.lastname: Duca
authors.forename: Alan B
authors.initials: AB
authors.lastname: Cooper
authors.forename: Michael
authors.initials: M
authors.lastname: Cable
mesh_terms: D000998:Antiviral Agents / Q000737:chemistry / Q000494:pharmacology*; D016174:Hepacivirus / Q000201:enzymology*; D008958:Models, Molecular; D011485:Protein Binding; D011720:Pyrazoles / Q000737:chemistry / Q000494:pharmacology*; D011743:Pyrimidines / Q000737:chemistry / Q000494:pharmacology*; D012324:RNA-Dependent RNA Polymerase / Q000037:antagonists & inhibitors / Q000378:metabolism; D013329:Structure-Activity Relationship; D017361:Viral Nonstructural Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism*
chemical_list: D000998:Antiviral Agents; D011720:Pyrazoles; D011743:Pyrimidines; D017361:Viral Nonstructural Proteins; C087036:NS-5 protein, hepatitis C virus; D012324:RNA-Dependent RNA Polymerase