2-Aminothiazole based P2Y1 antagonists as novel antiplatelet agents

2-Aminothiazole based P2Y1 antagonists as novel antiplatelet agents

ADP receptors, P2Y1 and P2Y12 have been recognized as potential targets for antithrombotic drugs. A series of P2Y1 antagonists that contain 2-aminothiazoles as urea surrogates were discovered. Extensive SAR of the thiazole ring is described. The most potent compound 7j showed good P2Y1 binding (Ki=1...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2013-07, Vol.23 (14), p.4206-4209
Hauptverfasser: Pi, Zulan, Sutton, James, Lloyd, John, Hua, Ji, Price, Laura, Wu, Qimin, Chang, Ming, Zheng, Joanna, Rehfuss, Robert, Huang, Christine S., Wexler, Ruth R., Lam, Patrick Y.S.
Format: Artikel
Sprache:eng
Schlagworte:
adenosine diphosphate
Aminothiazole as urea surrogates
Antagonism
antagonists
Antithrombotic
chemistry
drugs
P2Y1 antagonists
Platelet aggregation
rats
receptors
urea
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Beschreibung
Zusammenfassung:ADP receptors, P2Y1 and P2Y12 have been recognized as potential targets for antithrombotic drugs. A series of P2Y1 antagonists that contain 2-aminothiazoles as urea surrogates were discovered. Extensive SAR of the thiazole ring is described. The most potent compound 7j showed good P2Y1 binding (Ki=12nM), moderate antagonism of platelet aggregation (PA IC50=5.2μM) and acceptable PK in rats.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2013.05.025