Synthesis and structure–activity relationships of 2-acylamino-4, 6-diphenylpyridine derivatives as novel antagonists of GPR54

T Kobayashi, S Sasaki, N Tomita, S Fukui…

Index: Kobayashi, Toshitake; Sasaki, Satoshi; Tomita, Naoki; Fukui, Seiji; Kuroda, Noritaka; Nakayama, Masaharu; Kiba, Atsushi; Takatsu, Yoshihiro; Ohtaki, Tetsuya; Itoh, Fumio; Baba, Atsuo Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 11 p. 3841 - 3859

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Citation Number: 20

Abstract

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 ...