Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 2, Issue 3, Pages 207-212Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml1002426
Keywords
Hepatitis C; NS3/4A; HCV; macrocycle; ring-closing metathesis
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The discovery of MK-1220 is reported along with the development of a series of HCV NS3/4A protease inhibitors containing a P2 to P4 macrocyclic constraint with improved preclinical pharmacokinetics. Optimization of the P2 heterocycle substitution pattern as well as the P3 amino acid led to compounds with greatly improved plasma exposure following oral dosing in both rats and dogs while maintaining excellent enzyme potency and cellular activity. These studies led to the identification of MK-1220.
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