Discovery of 2-(phenoxypyridine)-3-phenylureas as small molecule P2Y1 antagonists

H Chao, H Turdi, TF Herpin, JY Roberge…

文献索引：Chao, Hannguang; Turdi, Huji; Herpin, Timothy F.; Roberge, Jacques Y.; Liu, Yalei; Schnur, Dora M.; Poss, Michael A.; Rehfuss, Robert; Hua, Ji; Wu, Qimin; Price, Laura A.; Abell, Lynn M.; Schumacher, William A.; Bostwick, Jeffrey S.; Steinbacher, Thomas E.; Stewart, Anne B.; Ogletree, Martin L.; Huang, Christine S.; Chang, Ming; Cacace, Angela M.; Arcuri, Maredith J.; Celani, Deborah; Wexler, Ruth R.; Lawrence, R. Michael Journal of Medicinal Chemistry, 2013 , vol. 56, # 4 p. 1704 - 1714

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被引用次数: 21

摘要

Two distinct G protein-coupled purinergic receptors, P2Y1 and P2Y12, mediate ADP-driven platelet activation. The clinical effectiveness of P2Y12 blockade is well established. Recent preclinical data suggest that P2Y1 and P2Y12 inhibition provide equivalent antithrombotic efficacy, while targeting P2Y1 has the potential for reduced bleeding liability. In this account, the discovery of a 2-(phenoxypyridine)-3-phenylurea chemotype that inhibited ADP- ...