Author/Authors :
Atsushi Naganawa، نويسنده , , Tetsuji Saito، نويسنده , , Yuuki Nagao، نويسنده , , Hiromu Egashira، نويسنده , , Maki Iwahashi، نويسنده , , Tohru Kambe، نويسنده , , Masatoshi Koketsu، نويسنده , , Hiroshi Yamamoto، نويسنده , , Michiyoshi Kobayashi، نويسنده , , Takayuki Maruyama، نويسنده , , Shuichi Ohuchida، نويسنده , , Hisao Nakai، نويسنده , , Kigen Kondo، نويسنده , , Masaaki Toda، نويسنده ,
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.
Keywords :
Prostaglandin , EP1 receptor , Antagonist , Sulfonamide