Asada Masaki, Obitsu Tetsuo, Kinoshita Atsushi, Nakai Yoshihiko, Nagase Toshihiko, Sugimoto Isamu, Tanaka Motoyuki, Takizawa Hiroya, Yoshikawa Ken, Sato Kazutoyo, Narita Masami, Ohuchida Shuichi, Nakai Hisao, Toda Masaaki
Minase Research Institute, Ono Pharmaceutical Co., Ltd, Shimamoto, Mishima, Osaka 618-8585, Japan.
Bioorg Med Chem Lett. 2010 Apr 15;20(8):2639-43. doi: 10.1016/j.bmcl.2010.02.034. Epub 2010 Feb 13.
A series of novel N-acylsulfonamide analogs were synthesized and evaluated for their binding affinity and antagonist activity for the EP3 receptor subtype. Representative compounds were also evaluated for their inhibitory effect on PGE(2)-induced uterine contraction in pregnant rats. Among those tested, a series of N-acylbenzenesulfonamide analogs were found to be more potent than the corresponding carboxylic acid analogs in both the in vitro and in vivo evaluations. The structure activity relationships (SAR) are also discussed.
合成了一系列新型N-酰基磺酰胺类似物，并对其与EP3受体亚型的结合亲和力和拮抗剂活性进行了评估。还评估了代表性化合物对孕鼠中前列腺素E2（PGE(2)）诱导的子宫收缩的抑制作用。在测试的化合物中，一系列N-酰基苯磺酰胺类似物在体外和体内评估中均比相应的羧酸类似物更有效。还讨论了构效关系（SAR）。
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