Synthesis and structure-activity relationships of a new class of selective EP3 receptor agonist, 13,14-didehydro-16-phenoxy analogues of prostaglandin E1.
A series of 13,14-didehydro-16-phenoxy analogues of prostaglandin E1 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.
Shimazaki
Y
Y
Medicinal Research Center, Taisho Pharmaceutical Co., Ltd., Ohmiya, Saitama, Japan. s14801@ccm.taisho.co.jp
Kameo
K
K
Tanami
T
T
Tanaka
H
H
Ono
N
N
Kiuchi
Y
Y
Okamoto
S
S
Sato
F
F
Ichikawa
A
A
D000527:Alprostadil / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D015394:Molecular Structure; D018078:Receptors, Prostaglandin E / Q000819:agonists*; D058308:Receptors, Prostaglandin E, EP3 Subtype; D013057:Spectrum Analysis; D013329:Structure-Activity Relationship
D018078:Receptors, Prostaglandin E; D058308:Receptors, Prostaglandin E, EP3 Subtype; D000527:Alprostadil