title: HCV NS5B polymerase inhibitors 3: Synthesis and in vitro activity of 3-(1,1-dioxo-2H-[1,2,4]benzothiadiazin-3-yl)-4-hydroxy-2H-quinolizin-2-one derivatives.
abstract: 3-(1,1-Dioxo-2H-[1,2,4]benzothiadiazin-3-yl)-4-hydroxy-2H-quinolizin-2-one derivatives as potential anti-HCV drugs targeting NS5B polymerase have been investigated. Their synthesis, HCV NS5B polymerase inhibition, and replicon activity are discussed.
authors.affiliation: Discovery Research, InterMune, Inc., Brisbane, CA 94005, USA. gyiwang@yahoo.com
authors.forename: Guangyi
authors.initials: G
authors.lastname: Wang
authors.forename: Laiguo
authors.initials: L
authors.lastname: Zhang
authors.forename: Xiaomin
authors.initials: X
authors.lastname: Wu
authors.forename: Debasis
authors.initials: D
authors.lastname: Das
authors.forename: Donald
authors.initials: D
authors.lastname: Ruhrmund
authors.forename: Lisa
authors.initials: L
authors.lastname: Hooi
authors.forename: Shawn
authors.initials: S
authors.lastname: Misialek
authors.forename: P T
authors.initials: PT
authors.lastname: Ravi Rajagopalan
authors.forename: Brad O
authors.initials: BO
authors.lastname: Buckman
authors.forename: Karl
authors.initials: K
authors.lastname: Kossen
authors.forename: Scott D
authors.initials: SD
authors.lastname: Seiwert
authors.forename: Leonid
authors.initials: L
authors.lastname: Beigelman
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001581:Benzothiadiazines / Q000138:chemical synthesis* / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical / Q000379:methods; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D016174:Hepacivirus / Q000378:metabolism; D006526:Hepatitis C / Q000188:drug therapy*; D066298:In Vitro Techniques; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D008956:Models, Chemical; D015394:Molecular Structure; D011807:Quinolizines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D017361:Viral Nonstructural Proteins / Q000037:antagonists & inhibitors* / Q000737:chemistry; D012324:RNA-Dependent RNA Polymerase
chemical_list: D000998:Antiviral Agents; D001581:Benzothiadiazines; D004791:Enzyme Inhibitors; D011807:Quinolizines; D017361:Viral Nonstructural Proteins; C087036:NS-5 protein, hepatitis C virus; D012324:RNA-Dependent RNA Polymerase