title: Hepatitis C NS5B polymerase inhibitors: 4,4-Dialkyl-1-hydroxy-3-oxo-3,4-dihydronaphthalene-3-yl benzothiadiazine derivatives.
abstract: 4,4-Dialkyl-1-hydroxy-3-oxo-3.4-dihydronaphthalene-3-yl benzothiadiazine derivatives were synthesized and evaluated as inhibitors of genotypes 1a and 1b HCV NS5B polymerase. A number of these compounds exhibited potent activity against genotypes 1a and 1b HCV polymerase in both enzymatic and cell culture activities. A representative compound also showed favorable pharmacokinetics in the rat.
authors.affiliation: Department of Antiviral Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA. douglas.hutchinson@abbott.com
authors.forename: Douglas K
authors.initials: DK
authors.lastname: Hutchinson
authors.forename: Teresa
authors.initials: T
authors.lastname: Rosenberg
authors.forename: Larry L
authors.initials: LL
authors.lastname: Klein
authors.forename: Todd D
authors.initials: TD
authors.lastname: Bosse
authors.forename: Daniel P
authors.initials: DP
authors.lastname: Larson
authors.forename: Wenping
authors.initials: W
authors.lastname: He
authors.forename: Wen W
authors.initials: WW
authors.lastname: Jiang
authors.forename: Warren M
authors.initials: WM
authors.lastname: Kati
authors.forename: William E
authors.initials: WE
authors.lastname: Kohlbrenner
authors.forename: Yaya
authors.initials: Y
authors.lastname: Liu
authors.forename: Sherie V
authors.initials: SV
authors.lastname: Masse
authors.forename: Tim
authors.initials: T
authors.lastname: Middleton
authors.forename: Akhteruzzaman
authors.initials: A
authors.lastname: Molla
authors.forename: Debra A
authors.initials: DA
authors.lastname: Montgomery
authors.forename: David W A
authors.initials: DW
authors.lastname: Beno
authors.forename: Kent D
authors.initials: KD
authors.lastname: Stewart
authors.forename: Vincent S
authors.initials: VS
authors.lastname: Stoll
authors.forename: Dale J
authors.initials: DJ
authors.lastname: Kempf
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D019540:Area Under Curve; D002626:Chemistry, Pharmaceutical / Q000379:methods; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D005838:Genotype; D007262:Infusions, Intravenous; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D051381:Rats; D017361:Viral Nonstructural Proteins / Q000037:antagonists & inhibitors* / Q000235:genetics; D012324:RNA-Dependent RNA Polymerase
chemical_list: D000998:Antiviral Agents; D004791:Enzyme Inhibitors; D017361:Viral Nonstructural Proteins; C087036:NS-5 protein, hepatitis C virus; D012324:RNA-Dependent RNA Polymerase