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

Toshitake Kobayashi, Satoshi Sasaki, Naoki Tomita, Seiji Fukui, Noritaka Kuroda, Masaharu Nakayama, Atsushi Kiba, Yoshihiro Takatsu, Tetsuya Ohtaki, Fumio Itoh, Atsuo Baba
Bioorganic & medicinal chemistry · 2010 · doi:10.1016/j.bmc.2010.04.036 · PMID:20457527
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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 series of 2-acylamino-4,6-diphenylpyridines to identify potent GPR54 antagonists. Detailed structure-activity relationship studies led to compound 9l with an IC(50) value of 3.7nM in a GPR54 binding assay, and apparent antagonistic activity in a cellular functional assay.

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Condition tags

endometriosis

MeSH descriptors

Pyridines Pyridines Receptors, G-Protein-Coupled Animals CHO Cells Cricetinae Cricetulus Humans Inhibitory Concentration 50 Pyridines Pyridines Receptors, G-Protein-Coupled Receptors, G-Protein-Coupled Receptors, Kisspeptin-1 Structure-Activity Relationship

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europepmc
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pubmed
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