Discovery of new chemical leads for selective EP1 receptor antagonists

…, M Iwahashi, T Kambe, M Koketsu, H Yamamoto…

Index: 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 Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 16 p. 5562 - 5577

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Citation Number: 10

Abstract

A series of 4-({2-[alkyl (phenylsulfonyl) amino] phenoxy} methyl) benzoic acids were identified as functional PGE2 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.