1292822-05-9Relevant academic research and scientific papers
Synthesis and SAR of sulfoxide substituted carboxyquinolines as NK3 receptor antagonists
Xiong, Hui,Kang, James,Woods, James M.,McCauley Jr., John P.,Koether, Gerard M.,Albert, Jeffrey S.,Hinkley, Lindsay,Li, Yan,Gadient, Reto A.,Simpson, Thomas R.
, p. 1896 - 1899 (2011/05/05)
The neurokinin-3 (NK3) receptor is regarded as a potential novel target for treating patients with schizophrenia. Herein we report the synthesis and SAR of a series of C3-alkylsulfoxide substituted quinolines as potent NK3 receptor antagonists. These compounds have excellent NK3 functional activity, good selectivity and drug-like properties. Several key compounds have good in vitro/in vivo DMPK characteristics, and are active in a gerbil locomotor activity model.
