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Synthesis and SAR of sulfoxide substituted carboxyquinolines as NK3 receptor antagonists |
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| Authors: | Xiong Hui Kang James Woods James M McCauley John P Koether Gerard M Albert Jeffrey S Hinkley Lindsay Li Yan Gadient Reto A Simpson Thomas R |
| Affiliation: | CNS Discovery, AstraZeneca Pharmaceuticals, 1800 Concord Pike, Wilmington, DE, USA |
| Abstract: | 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. |
| Keywords: | Neurokinins NK3 receptor antagonists Carboxyquinolines Sulfoxides |
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