925924-95-4Relevant academic research and scientific papers
Synthesis and structure-activity relationships of 2-acylamino-4,6-diphenylpyridine derivatives as novel antagonists of GPR54
Kobayashi, Toshitake,Sasaki, Satoshi,Tomita, Naoki,Fukui, Seiji,Kuroda, Noritaka,Nakayama, Masaharu,Kiba, Atsushi,Takatsu, Yoshihiro,Ohtaki, Tetsuya,Itoh, Fumio,Baba, Atsuo
experimental part, p. 3841 - 3859 (2010/08/06)
GPR54 is a G protein-coupled receptor (GPCR) which was formerly an orphan receptor. Recent functional study of GPR54 revealed that the receptor has an essential role to modulate sex-hormones including GnRH. Though antagonists of GPR54 are expected to be novel drugs for sex-hormone dependent diseases such as prostate cancer or endometriosis, small molecule GPR54 antagonists have not been reported. We have synthesized a series of 2-acylamino-4,6-diphenylpyridines to identify potent GPR54 antagonists. Detailed structure-activity relationship studies led to compound 9l with an IC50 value of 3.7 nM in a GPR54 binding assay, and apparent antagonistic activity in a cellular functional assay.
