Structure-activity relationship studies on ortho-substituted cinnamic acids, a new class of selective EP3 antagonists
Structure-activity relationship studies on ortho-substituted cinnamic acids, a new class of selective EP3 antagonists
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DOI：
10.1016/j.bmcl.2004.11.051
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发表时间：
2005-02-01
影响因子：
2.7
通讯作者：
Zamboni, RJ
中科院分区：
文献类型：
--
作者：
Belley, M;Gallant, M;Zamboni, RJ
合成了一系列新的邻位取代的肉桂酸，并评价了它们对四种前列腺素E1受体的结合活性和选择性。它们中的许多是非常有效的和选择性的EP 3拮抗剂（Ki 3-10 nM），而化合物9是非常好的和选择性的EP 2激动剂（Ki 8 nM）。还报道了EP 2激动剂9在体内的生物学特征和所选EP 3拮抗剂的代谢特征。(C)2004爱思唯尔有限公司保留所有权利。
A series of novel ortho-substituted cinnamic acids have been synthesized, and their binding activity and selectivity on the four prostaglandin E, receptors evaluated. Many of them are very potent and selective EP3 antagonists (K-i 3-10 nM), while compound 9 is a very good and selective EP2 agonist (K-i 8 nM). The biological profile of the EP2 agonist 9 in vivo and the metabolic profile of selected EP3 antagonists are also reported. (C) 2004 Elsevier Ltd. All rights reserved.