期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 2, 期 3, 页码 207-212出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml1002426
关键词
Hepatitis C; NS3/4A; HCV; macrocycle; ring-closing metathesis
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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