title: Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of unsymmetrical 1-hydroxy-4,4-dialkyl-3-oxo-3,4-dihydronaphthalene benzothiadiazine derivatives.
abstract: Substituted 1-hydroxy-4,4-dialkyl-3-oxo-3,4-dihydronaphthalene benzothiadiazine derivatives were investigated as inhibitors of genotype 1 HCV polymerase. Structure-activity relationship patterns for this class of compounds are discussed. It was found that the saturated alkane dialkyl units provided the most active analogs.
authors.affiliation: Infectious Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA. a.chris.krueger@abbott.com
authors.forename: A Chris
authors.initials: AC
authors.lastname: Krueger
authors.forename: Darold L
authors.initials: DL
authors.lastname: Madigan
authors.forename: Brian E
authors.initials: BE
authors.lastname: Green
authors.forename: Douglas K
authors.initials: DK
authors.lastname: Hutchinson
authors.forename: Wen W
authors.initials: WW
authors.lastname: Jiang
authors.forename: Warren M
authors.initials: WM
authors.lastname: Kati
authors.forename: Yaya
authors.initials: Y
authors.lastname: Liu
authors.forename: Clarence J
authors.initials: CJ
authors.lastname: Maring
authors.forename: Sherie V
authors.initials: SV
authors.lastname: Masse
authors.forename: Keith F
authors.initials: KF
authors.lastname: McDaniel
authors.forename: Tim R
authors.initials: TR
authors.lastname: Middleton
authors.forename: Hongmei
authors.initials: H
authors.lastname: Mo
authors.forename: Akhteruzzaman
authors.initials: A
authors.lastname: Molla
authors.forename: Debra A
authors.initials: DA
authors.lastname: Montgomery
authors.forename: Teresa I
authors.initials: TI
authors.lastname: Ng
authors.forename: Dale J
authors.initials: DJ
authors.lastname: Kempf
mesh_terms: D000473:Alkanes; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001581:Benzothiadiazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D016174:Hepacivirus / Q000187:drug effects* / Q000201:enzymology; D020128:Inhibitory Concentration 50; D012093:Replicon / Q000187:drug effects; D013329:Structure-Activity Relationship; D017361:Viral Nonstructural Proteins / Q000037:antagonists & inhibitors*; D012324:RNA-Dependent RNA Polymerase
chemical_list: D000473:Alkanes; D000998:Antiviral Agents; D001581:Benzothiadiazines; D017361:Viral Nonstructural Proteins; C087036:NS-5 protein, hepatitis C virus; D012324:RNA-Dependent RNA Polymerase