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Discovery of heteroaryl sulfonamides as new EP1 receptor selective antagonists |
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| Authors: | 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 |
| Affiliation: | Minase Research Institute, Ono Pharmaceutical Co., Ltd, Shimamoto, Mishima, Osaka 618-8585, Japan. naganawa@ono.co.jp |
| Abstract: | 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. |
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