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Bioorg Med Chem Lett. 2013 Dec 15;23(24):6825-8. doi: 10.1016/j.bmcl.2013.10.009. Epub 2013 Oct 11.

Potent P2Y1 urea antagonists bearing various cyclic amine scaffolds.

Author information

  • 1Research and Development, Bristol-Myers Squibb Company, Pennington, NJ 08534, USA. Electronic address: rejean.ruel@umontreal.ca.

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.

Copyright © 2013 Elsevier Ltd. All rights reserved.

KEYWORDS:

Isoindolines; P2Y(1) antagonists; Piperidines; Purinergic receptors; Tetrahydroisoquinolines

PMID:
24269480
[PubMed - indexed for MEDLINE]
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