Synthesis and structure-activity relationships of a new class of selective EP3 receptor agonist, 13,14-didehydro-16-phenoxy analogues of prostaglandin E1.

Y Shimazaki,K Kameo,T Tanami, H Tanaka,N Ono,Y Kiuchi,S Okamoto, F Sato,A Ichikawa

BIOORGANIC & MEDICINAL CHEMISTRY（2000）

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摘要

A series of 13,14-didehydro-16-phenoxy analogues of prostaglandin E-1 was synthesized and their agonistic activity on EP receptor subtypes was evaluated. 13,14-Didehydro-16-phenoxy-1-decarboxy analogues, 7e and 7f, display highly selective activity on the EP3 receptor subtype, thus, their utility as a selective anti-ulcer agent can be expected. (C) 2000 Elsevier Science Ltd. All rights reserved.

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prostaglandins,agonists,receptors,substituent effects

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