| Autor: |
Chackalamannil, S., Xia, Y., Greenlee, W. J., Clasby, M., Doller, D., Tsai, H., Asberom, T., Czarniecki, M., Ahn, H.-S., Boykow, G., Foster, C., Agans-Fantuzzi, J., Bryant, M., Lau, J., Chintala, M. |
| Zdroj: |
Journal of Medicinal Chemistry; September 2005, Vol. 48 Issue: 19 p5884-5887, 4p |
| Abstrakt: |
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 Ki 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. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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