Title of article
Discovery of heteroaryl sulfonamides as new EP1 receptor selective antagonists Original Research Article
Author/Authors
Atsushi Naganawa، نويسنده , , Toshiaki Matsui، نويسنده , , Tetsuji Saito، نويسنده , , Masaki Ima، نويسنده , , Tadashi Tatsumi، نويسنده , , Shingo Yamamoto، نويسنده , , Masayuki Murota، نويسنده , , Hiroshi Yamamoto، نويسنده , , Takayuki Maruyama، نويسنده , , Shuichi Ohuchida، نويسنده , , Hisao Nakai، نويسنده , , Kigen Kondo، نويسنده , , Masaaki Toda، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
12
From page
6628
To page
6639
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.
Keywords
Prostaglandin , EP1 receptor , Antagonist , Sulfonamide
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2006
Journal title
Bioorganic and Medicinal Chemistry
Record number
1305136
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