Structure–activity relationship studies on ortho-substituted cinnamic acids, a new class of selective EP 3 antagonists

…, N Lachance, M Labelle, LA Trimble, N Chauret…

文献索引：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; Carriere, Marie-Claude; Denis, Danielle; Greig, Gillian M.; Slipetz, Deborah; Metters, Kathleen M.; Gordon, Robert; Chan, Chi Chung; Zamboni, Robert J. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 3 p. 527 - 530

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被引用次数: 17

摘要

A series of novel ortho-substituted cinnamic acids have been synthesized, and their binding activity and selectivity on the four prostaglandin E2 receptors evaluated. Many of them are very potent and selective EP3 antagonists (Ki 3–10nM), while compound 9 is a very good and selective EP2 agonist (Ki 8nM). The biological profile of the EP2 agonist 9 in vivo and the metabolic profile of selected EP3 antagonists are also reported.