Discovery of novel S1P2 antagonists. Part 1: discovery of 1,3-bis(aryloxy)benzene derivatives.
作者信息
Kusumi Kensuke, Shinozaki Koji, Kanaji Toshiya, Kurata Haruto, Naganawa Atsushi, Otsuki Kazuhiro, Matsushita Takeshi, Sekiguchi Tetsuya, Kakuuchi Akito, Seko Takuya
机构信息
Minase Research Institute, Ono Pharmaceutical Co., Ltd, 3-1-1 Sakurai, Shimamoto, Mishima, Osaka 618-8585, Japan.
Ono Pharma UK Ltd, MidCity Place, 71 High Holborn, London WC1V 6EA, United Kingdom.
出版信息
Bioorg Med Chem Lett. 2015 Apr 1;25(7):1479-82. doi: 10.1016/j.bmcl.2015.02.029. Epub 2015 Feb 23.
The structure-activity relationships of a novel series of sphingosine-1-phosphate receptor antagonists have been examined in detail. The initial hit compound 1 was modified through synthesis to improve its S1P2 activity. The synthesis of a series of analogs revealed that 1,3-bis(aryloxy)benzene derivatives, as represented by 22, are potent and selective S1P2 antagonists.
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