Discovery of Novel Seven-Membered Prostacyclin Analogues as Potent and Selective Prostaglandin FP and EP3 Dual Agonists.
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ABSTRACT:
SUBMITTER: Sugimoto I
PROVIDER: S-EPMC5238478 | biostudies-literature | 2017 Jan
REPOSITORIES: biostudies-literature
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Discovery of Novel Seven-Membered Prostacyclin Analogues as Potent and Selective Prostaglandin FP and EP3 Dual Agonists.
Sugimoto Isamu I Kambe Tohru T Okino Tomotaka T Obitsu Tetsuo T Ohta Nobukazu N Nishiyama Taihei T Kinoshita Akihiro A Fujimoto Taku T Egashira Hiromu H Yamane Shinsaku S Shuto Satoshi S Tani Kousuke K Maruyama Toru T
ACS medicinal chemistry letters 20161213 1
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 <b>5b</b>, a nonselective agonist for prostaglandin receptors, replacement of the core structure with an octahydro-2<i>H</i>-cyclopenta[<i>b</i>]oxepine scaffold led to the discovery of the potent and selective FP a ...[more]
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