Discovery of Novel Seven-Membered Prostacyclin Analogues as Potent and Selective Prostaglandin FP and EP3 Dual Agonists.
Basic Information
ID: ALA3870361
Journal: ACS Med Chem Lett
Title: Discovery of Novel Seven-Membered Prostacyclin Analogues as Potent and Selective Prostaglandin FP and EP3 Dual Agonists.
Authors: Sugimoto I, Kambe T, Okino T, Obitsu T, Ohta N, Nishiyama T, Kinoshita A, Fujimoto T, Egashira H, Yamane S, Shuto S, Tani K, Maruyama T.
Abstract: A novel series of prostaglandin analogues with a seven-membered ring scaffold was designed, synthesized, and evaluated for the functional activation of prostaglandin receptors to identify potent and subtype-selective FP and EP3 dual agonists. Starting from the prostacyclin derivative 5b, a nonselective agonist for prostaglandin receptors, replacement of the core structure with an octahydro-2H-cyclopenta[b]oxepine scaffold led to the discovery of the potent and selective FP and EP3 dual agonist 11b as a lead compound for the development of an antiglaucoma agent.
CiteXplore: 28105284
DOI: 10.1021/acsmedchemlett.6b00415
Patent ID: ┄