新型选择性EP(3)拮抗剂——邻位取代肉桂酸的构效关系研究
Structure-activity relationship studies on ortho-substituted cinnamic acids, a new class of selective EP(3) antagonists.
作者信息
Belley Michel, Gallant Michel, Roy Bruno, Houde Karine, Lachance Nicolas, Labelle Marc, Trimble Laird A, Chauret Nathalie, Li Chun, Sawyer Nicole, Tremblay Nathalie, Lamontagne Sonia, Carrière Marie-Claude, Denis Danielle, Greig Gillian M, Slipetz Deborah, Metters Kathleen M, Gordon Robert, Chan Chi Chung, Zamboni Robert J
机构信息
Merck Frosst Centre for Therapeutic Research, PO Box 1005, Pointe Claire-Dorval, Québec, Canada H9R 4P8.
出版信息
Bioorg Med Chem Lett. 2005 Feb 1;15(3):527-30. doi: 10.1016/j.bmcl.2004.11.051.
A series of novel ortho-substituted cinnamic acids have been synthesized, and their binding activity and selectivity on the four prostaglandin E(2) receptors evaluated. Many of them are very potent and selective EP(3) antagonists (K(i) 3-10 nM), while compound 9 is a very good and selective EP(2) agonist (K(i) 8 nM). The biological profile of the EP(2) agonist 9 in vivo and the metabolic profile of selected EP(3) antagonists are also reported.
已经合成了一系列新型邻位取代肉桂酸，并评估了它们对四种前列腺素E(2)受体的结合活性和选择性。其中许多是非常有效的选择性EP(3)拮抗剂（K(i)为3 - 10 nM），而化合物9是一种非常好的选择性EP(2)激动剂（K(i)为8 nM）。还报道了EP(2)激动剂9的体内生物学特性以及所选EP(3)拮抗剂的代谢特性。
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