210818-95-4Relevant academic research and scientific papers
Design and synthesis of a selective EP4-receptor agonist. Part 1: Discovery of 3,7-dithiaPGE1 derivatives and identification of their ω chains
Maruyama, Toru,Asada, Masaki,Shiraishi, Tai,Ishida, Akiharu,Yoshida, Hideyuki,Maruyama, Takayuki,Ohuchida, Shuichi,Nakai, Hisao,Kondo, Kigen,Toda, Masaaki
, p. 975 - 988 (2007/10/03)
Improvement of EP4-receptor selectivity and the agonist activity by introduction of heteroatoms into the α chain of PGE1 was investigated. Among the compounds tested, 3,7-dithiaPGE1 4a exhibited good EP4-receptor selectivity and agonist activity. Further modification of the ω chain of 3,7-dithiaPGE1 was performed to improve EP4-receptor selectivity and agonist activity. Of the compounds produced, 16-phenyl-ω-tetranor-3,7-dithiaPGE1 4p possessing moderate EP4-receptor selectivity and agonist activity, was identified as a new chemical lead for further optimization by modification of the aromatic moiety. Copyright
