- Development of a highly selective EP2-receptor agonist. Part 1: Identification of 16-hydroxy-17,17-trimethylene PGE2 derivatives
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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 discussed. Copyright
- Tani, Kousuke,Naganawa, Atsushi,Ishida, Akiharu,Sagawa, Kenji,Harada, Hiroyuki,Ogawa, Mikio,Maruyama, Takayuki,Ohuchida, Shuichi,Nakai, Hisao,Kondo, Kigen,Toda, Masaaki
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p. 1093 - 1106
(2007/10/03)
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- Cycloalkyl-prostaglandin E2 derivatives
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A omega -cycloalkyl-prostaglandin E2 derivatives of the formula (I) wherein R is carboxy or hydroxymethyl; R1 is oxo, methylene or halogen atom; R2 is H, OH or C1-4 alkoxy; R3 is H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C1-8 alkyl, C2-8 alkenyl or C2-8 alkynyl substituted by 1-3 of substituent selected from halogen atom, C1-4 alkoxy, C3-7 cycloalkyl, phenyl, or phenyl substituted by 1-3 of substituent selected from halogen atom, C1-4 alkyl, C1-4 alkoxy, nitro, trifluoromethyl; n is 0-4; and non-toxic salt thereof, prodrug thereof and cyclodextrin clathrate thereof can strongly bind on EP2 subtype receptor. Therefore, they are useful for prevention and/or treatment of immune disease (autoimmune disease, organ transplantation, etc.), asthma, abnormal bone formation, neuron cell death, liver damage, abortion, premature birth or retina neuropathy of glaucoma etc.
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