Synthesis of new 4,5-dihydrofuranoindoles and their evaluation as HCV NS5B polymerase inhibitors.
The synthesis of substituted 3,4-dihydrofuranoindoles is reported. These new indole compounds were used to synthesize potent HCV NS5B inhibitors. The binding mode of the dihydrofuranoindole-derived inhibitors was established via X-ray crystallographic studies.
Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033-1300, USA. francisco.velazquez@merck.com
Francisco
F
Velázquez
Srikanth
S
Venkatraman
Charles A
CA
Lesburg
José
J
Duca
Stuart B
SB
Rosenblum
Joseph A
JA
Kozlowski
F George
FG
Njoroge
D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D016174:Hepacivirus / Q000187:drug effects* / Q000201:enzymology; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D008958:Models, Molecular; D054730:Protein Interaction Domains and Motifs; D012324:RNA-Dependent RNA Polymerase / Q000037:antagonists & inhibitors*; D017361:Viral Nonstructural Proteins / Q000037:antagonists & inhibitors*
D004791:Enzyme Inhibitors; D007211:Indoles; D017361:Viral Nonstructural Proteins; C087036:NS-5 protein, hepatitis C virus; D012324:RNA-Dependent RNA Polymerase