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Discovery of Novel Seven-Membered Prostacyclin Analogues as Potent and Selective Prostaglandin FP and EP3 Dual Agonists. | LitMetric

Discovery of Novel Seven-Membered Prostacyclin Analogues as Potent and Selective Prostaglandin FP and EP3 Dual Agonists.

ACS Med Chem Lett

Medicinal Chemistry Research Laboratories, Department of Biology & Pharmacology, and Discovery Research Alliance, Ono Pharmaceutical Co., Ltd. , 3-1-1 Sakurai, Shimamoto-cho, Mishima-gun, Osaka 618-8585, Japan.

Published: January 2017

AI Article Synopsis

Article 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 , a nonselective agonist for prostaglandin receptors, replacement of the core structure with an octahydro-2-cyclopenta[]oxepine scaffold led to the discovery of the potent and selective FP and EP3 dual agonist as a lead compound for the development of an antiglaucoma agent.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5238478PMC
http://dx.doi.org/10.1021/acsmedchemlett.6b00415DOI Listing

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