Discovery of heteroaryl sulfonamides as new EP1 receptor selective antagonists

…, T Maruyama, S Ohuchida, H Nakai, K Kondo…

文献索引：Naganawa, Atsushi; Matsui, Toshiaki; Saito, Tetsuji; Ima, Masaki; Tatsumi, Tadashi; Yamamoto, Shingo; Murota, Masayuki; Yamamoto, Hiroshi; Maruyama, Takayuki; Ohuchida, Shuichi; Nakai, Hisao; Kondo, Kigen; Toda, Masaaki Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 19 p. 6628 - 6639

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被引用次数: 9

摘要

4-({2-[Isobutyl (phenylsulfonyl) amino]-5-(trifluoromethyl) phenoxy} methyl) benzoic acid (1) is a functional PGE2 antagonist selective for EP1 receptor subtype. Analogs of 1, in which the phenyl-sulfonyl moiety has been replaced with more hydrophilic heteroarylsulfonyl moieties, exhibited more optimized antagonist activity, while some of them showed in vivo antagonist activity. Structure–activity relationship (SAR) studies are also presented.