233750-49-7Relevant academic research and scientific papers
Discovery of a novel EP2/EP4 dual agonist with high subtype-selectivity
Kambe, Tohru,Maruyama, Toru,Nakano, Masayuki,Nakai, Yoshihiko,Yoshida, Tadahiro,Matsunaga, Naoki,Oida, Hiroji,Konaka, Akira,Maruyama, Takayuki,Nakai, Hisao,Toda, Masaaki
, p. 396 - 401 (2012)
A series of γ-lactam prostaglandin E1 analogs bearing a 16-phenyl moiety in the ω-chain and aryl moiety in the α-chain were synthesized and biologically evaluated. Among the tested compounds, γ-lactam PGE analog 3 designed as a structural hybrid of 1 and 2 was discovered as the most optimized EP2/EP4 dual agonist with excellent subtype-selectivity (Ki values: mEP2 = 9.3 nM, mEP4 = 0.41 nM). A structure-activity relationship study is presented.
Discovery of novel prostaglandin analogs as potent and selective EP2/EP4 dual agonists
Kambe, Tohru,Maruyama, Toru,Nakai, Yoshihiko,Yoshida, Hideyuki,Oida, Hiroji,Maruyama, Takayuki,Abe, Nobutaka,Nishiura, Akio,Nakai, Hisao,Toda, Masaaki
, p. 2235 - 2251 (2012/05/20)
To identify potent EP2/EP4 dual agonists with excellent subtype selectivity, a series of γ-lactam prostaglandin E analogs bearing a 16-phenyl ω-chain were synthesized and evaluated. Structural hybridization of 1 and 2, followed by more detailed chemical m
