Research and Development, Bristol-Myers Squibb Company, Pennington, NJ 08534, USA.
Bioorg Med Chem Lett. 2013 Dec 15;23(24):6825-8. doi: 10.1016/j.bmcl.2013.10.009. Epub 2013 Oct 11.
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.
已经发现了一些具有良好抑制活性的新型胺骨架，它们在 ADP 诱导的血小板聚集试验中是 P2Y1 受体的有效拮抗剂。SAR 优化导致鉴定出异吲哚啉 3c 和哌啶 4a，它们表现出良好的体外结合和功能活性，以及提高的水溶解度。其中，哌啶 4a 具有最理想的整体特征，具有有利的 PK 参数。
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