Design and synthesis of a selective EP4-receptor agonist. Part 1: discovery of 3,7-dithiaPGE1 derivatives and identification of their omega chains |
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Authors: | Maruyama Toru Asada Masaki Shiraishi Tai Egashira Hiromu Yoshida Hideyuki Maruyama Takayuki Ohuchida Shuichi Nakai Hisao Kondo Kigen Toda Masaaki |
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Affiliation: | Minase Research Institute, Ono Pharmaceutical Co., Ltd., Shimamoto, Mishima, 618-8585, Osaka, Japan. to.maruyama@ono.co.jp |
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Abstract: | Improvement of EP4-receptor selectivity and the agonist activity by introduction of heteroatoms into the alpha 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 omega chain of 3,7-dithiaPGE1 was performed to improve EP4-receptor selectivity and agonist activity. Of the compounds produced, 16-phenyl-omega-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. |
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