Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 47, Issue 7, Pages 1605-1608Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm0342414
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From the discovery of competitive hexapeptide inhibitors, potent and selective HCV NS3 protease macrocyclic inhibitors have been identified. Structure-activity relationship studies were per-formed focusing on optimizing the N-terminal carbamate and the aromatic substituent on the (4R)-hydroxyproline moiety. Inhibitors meeting the potency criteria in the cell-based assay and with improved oral bioavailability in rats were identified. BILN 2061 was selected as the best compound, the first NS3 protease inhibitor reported with antiviral activity in man.
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