Journal of medicinal chemistry

Synthesis and structure-activity relationships of uracil nucleotide derivatives and analogues as agonists at human P2Y2, P2Y4, and P2Y6 receptors

A El-Tayeb, A Qi, CE Müller

文献索引：El-Tayeb, Ali; Qi, Aidong; Mueller, Christa E. Journal of Medicinal Chemistry, 2006 , vol. 49, # 24 p. 7076 - 7087

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被引用次数: 85

摘要

A series of UTP, UDP, and UMP derivatives and analogues were synthesized and evaluated at the human pyrimidinergic P2Y receptor subtypes P2Y2, P2Y4, and P2Y6 stably expressed in 1321N1 astrocytoma cells. Substituents at N3 of UTP were poorly tolerated by P2Y2 and P2Y4 receptors. In contrast, a large phenacyl substituent at N3 of UDP was well tolerated by the P2Y6 receptor, yielding a potent and selective P2Y6 receptor agonist (3- ...