| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10593356 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
Abstract
A number of new amine scaffolds with good inhibitory activity in the ADP-induced platelet aggregation assay have been found to be potent antagonists of the P2Y1 receptor. SAR optimization led to the identification of isoindoline 3c and piperidine 4a which showed good in vitro binding and functional activities, as well as improved aqueous solubility. Among them, the piperidine 4a showed the best overall profile with favorable PK parameters.
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Authors
Réjean Ruel, Alexandre L'Heureux, Carl Thibeault, Philippe Lapointe, Alain Martel, Jennifer X. Qiao, Ji Hua, Laura A. Price, Qimin Wu, Ming Chang, Joanna Zheng, Christine S. Huang, Ruth R. Wexler, Robert Rehfuss, Patrick Y.S. Lam,