新型选择性EP1受体拮抗剂化学先导物的发现
Discovery of new chemical leads for selective EP1 receptor antagonists.
作者信息
Naganawa Atsushi, Saito Tetsuji, Nagao Yuuki, Egashira Hiromu, Iwahashi Maki, Kambe Tohru, Koketsu Masatoshi, Yamamoto Hiroshi, Kobayashi Michiyoshi, Maruyama Takayuki, Ohuchida Shuichi, Nakai Hisao, Kondo Kigen, Toda Masaaki
机构信息
Minase Research Institute, Ono Pharmaceutical Co., Ltd, Shimamoto, Mishima, Osaka, Japan.
出版信息
Bioorg Med Chem. 2006 Aug 15;14(16):5562-77. doi: 10.1016/j.bmc.2006.04.038. Epub 2006 May 12.
A series of 4-([2-[alkyl(phenylsulfonyl)amino]phenoxy]methyl)benzoic acids were identified as functional PGE(2) antagonists with selectivity for the EP1 receptor subtype starting from a chemical lead 1, which was found while screening our in-house compound library. Discovery of the optimized analogs 21-23 is presented here and structure-activity relationships (SAR) are also discussed.
从化学先导物1开始，一系列4-([2-[烷基(苯基磺酰基)氨基]苯氧基]甲基)苯甲酸被鉴定为对EP1受体亚型具有选择性的功能性前列腺素E2（PGE(2)）拮抗剂，该先导物是在筛选我们的内部化合物库时发现的。本文介绍了优化类似物21-23的发现，并讨论了构效关系（SAR）。
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