2-Acylamino-4,6-diphenylpyridine derivatives as novel GPR54 antagonists with good brain exposure and in vivo efficacy for plasma LH level in male rats

A series of 2-acylamino-4,6-diphenylpyridine derivatives as small molecule GPR54 antagonists were synthesized, and led to compound 15a with potent antagonistic activity, good brain exposure, and in vivo efficacy.