Novel P4 truncated tripeptidyl alpha-ketoamides as HCV protease inhibitors.
We describe herein the synthesis and evaluation of two series of P-4 truncated tripeptidyl alpha-ketoamides as HCV serine protease inhibitors. The most promising compound disclosed in this communication 7b demonstrated enzyme binding affinity (K(i)) at 0.27 uM.
Lamar
Jason
J
Lilly Research Laboratory, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
Victor
Frantz
F
Snyder
Nancy
N
Johnson
Robert B
RB
Wang
Q May
QM
Glass
John I
JI
Chen
Shu-Hui
SH
D000577:Amides / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D016174:Hepacivirus / Q000187:drug effects* / Q000201:enzymology; D006801:Humans; D009842:Oligopeptides / Q000737:chemistry* / Q000494:pharmacology; D012093:Replicon / Q000187:drug effects; D012697:Serine Endopeptidases / Q000378:metabolism*; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology
D000577:Amides; D009842:Oligopeptides; D015842:Serine Proteinase Inhibitors; D012697:Serine Endopeptidases