| Autor: |
Chelliah MV; Central Nervous System and Cardiovascular Chemical Research, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, USA. mariappan.chelliah@spcorp.com, Chackalamannil S, Xia Y, Eagen K, Clasby MC, Gao X, Greenlee W, Ahn HS, Agans-Fantuzzi J, Boykow G, Hsieh Y, Bryant M, Palamanda J, Chan TM, Hesk D, Chintala M |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 2007 Oct 18; Vol. 50 (21), pp. 5147-60. Date of Electronic Publication: 2007 Sep 14. |
| DOI: |
10.1021/jm070704k |
| Abstrakt: |
Pursuing our earlier efforts in the himbacine-based thrombin receptor antagonist area, we have synthesized a series of compounds that incorporate heteroatoms in the C-ring of the tricyclic motif. This effort has resulted in the identification of several potent heterocyclic analogs with excellent affinity for the thrombin receptor. Several of these compounds demonstrated robust inhibition of platelet aggregation in an ex vivo model in cynomolgus monkeys following oral administration. A detailed profile of 28b, a benchmark compound in this series, with a Ki of 4.3 nM, is presented. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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