Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 48, Issue 19, Pages 5884-5887Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm0502236
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Structurally novel thrombin receptor (protease activated receptor 1, PAR-1) antagonists based on the natural product himbacine are described. The prototypical PAR-1 antagonist 55 showed a K-i of 2.7 nM in the binding assay, making it the most potent PAR-1 antagonist reported. 55 was highly active in several functional assays, showed excellent oral bioavailability in rat and monkey models, and showed complete inhibition of agonist-induced ex. vivo platelet aggregation in cynomolgus monkeys after oral administration.
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