Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of unsymmetrical 1-hydroxy-4,4-dialkyl-3-oxo-3,4-dihydronaphthalene benzothiadiazine derivatives.
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.
Krueger
A Chris
AC
Infectious Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA. a.chris.krueger@abbott.com
Madigan
Darold L
DL
Green
Brian E
BE
Hutchinson
Douglas K
DK
Jiang
Wen W
WW
Kati
Warren M
WM
Liu
Yaya
Y
Maring
Clarence J
CJ
Masse
Sherie V
SV
McDaniel
Keith F
KF
Middleton
Tim R
TR
Mo
Hongmei
H
Molla
Akhteruzzaman
A
Montgomery
Debra A
DA
Ng
Teresa I
TI
Kempf
Dale J
DJ
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
D000473:Alkanes; D000998:Antiviral Agents; D001581:Benzothiadiazines; D017361:Viral Nonstructural Proteins; C087036:NS-5 protein, hepatitis C virus; D012324:RNA-Dependent RNA Polymerase