Development of a highly selective EP2-receptor agonist. Part 1: identification of 16-hydroxy-17, 17-trimethylene PGE 2 derivatives

…, H Harada, M Ogawa, T Maruyama, S Ohuchida…

文献索引：Tani, Kousuke; Naganawa, Atsushi; Ishida, Akiharu; Sagawa, Kenji; Harada, Hiroyuki; Ogawa, Mikio; Maruyama, Takayuki; Ohuchida, Shuichi; Nakai, Hisao; Kondo, Kigen; Toda, Masaaki Bioorganic and Medicinal Chemistry, 2002 , vol. 10, # 4 p. 1093 - 1106

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被引用次数: 14

摘要

Design and synthesis of an EP2-receptor selective agonist began with the chemical modification of α-and ω-chains of butaprost 1a, which exhibits an affinity for the IP-receptor. Two series of prostaglandin (PG) analogues with a 16-hydroxy-17, 17-trimethylene moiety as an ω-chain were identified. Among those tested, 4a, b, e, f, h and 6a, b, e, f, h were found to be highly selective EP2-receptor agonists. Structure–activity relationships are ...