Abstract
We describe the structure-activity relationship of the C7-position of pyrano[3,4-b]indole-based inhibitors of HCV NS5B polymerase. Further exploration of the allosteric binding site led to the discovery of the significantly more potent compounds 13 and 14.
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
-
Allosteric Site
-
Crystallography, X-Ray
-
Drug Discovery*
-
Enzyme Inhibitors* / chemical synthesis
-
Enzyme Inhibitors* / chemistry
-
Enzyme Inhibitors* / pharmacology
-
Hepacivirus / drug effects*
-
Hepacivirus / enzymology*
-
Indoles* / chemical synthesis
-
Indoles* / chemistry
-
Indoles* / pharmacology
-
Inhibitory Concentration 50
-
Models, Molecular
-
Molecular Structure
-
Pyrans* / chemical synthesis
-
Pyrans* / chemistry
-
Pyrans* / pharmacology
-
Structure-Activity Relationship
-
Viral Nonstructural Proteins / antagonists & inhibitors*
Substances
-
Enzyme Inhibitors
-
Indoles
-
Pyrans
-
Viral Nonstructural Proteins
-
NS-5 protein, hepatitis C virus