HCV NS5B polymerase inhibitors 1: Synthesis and in vitro activity of 2-(1,1-dioxo-2H-[1,2,4]benzothiadiazin-3-yl)-1-hydroxynaphthalene derivatives.
2-(1,1-Dioxo-2H-[1,2,4]benzothiadiazin-3-yl)-1-hydroxynaphthalene derivatives as potential anti-HCV drugs targeting NS5B polymerase have been investigated. Their synthesis, HCV NS5B polymerase inhibition and replicon activity are discussed.
Wang
Guangyi
G
Discovery Research, InterMune, Inc., Brisbane, CA 94005, USA. gyiwang@yahoo.com
He
Yanzhen
Y
Sun
Jun
J
Das
Debasis
D
Hu
Mougang
M
Huang
Jianhua
J
Ruhrmund
Donald
D
Hooi
Lisa
L
Misialek
Shawn
S
Ravi Rajagopalan
P T
PT
Stoycheva
Antitsa
A
Buckman
Brad O
BO
Kossen
Karl
K
Seiwert
Scott D
SD
Beigelman
Leonid
L
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*; D006801:Humans; D066298:In Vitro Techniques; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D008956:Models, Chemical; D015394:Molecular Structure; D009281:Naphthalenes / Q000037:antagonists & inhibitors* / Q000737:chemistry; D009284:Naphthols / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D017361:Viral Nonstructural Proteins / Q000037:antagonists & inhibitors*; D012324:RNA-Dependent RNA Polymerase
D000998:Antiviral Agents; D001581:Benzothiadiazines; D004791:Enzyme Inhibitors; D009281:Naphthalenes; D009284:Naphthols; D017361:Viral Nonstructural Proteins; C031721:naphthalene; C087036:NS-5 protein, hepatitis C virus; D012324:RNA-Dependent RNA Polymerase