|
|||||
|
|
Discovery of a novel series of melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity |
|
| Authors: | Mihalic Jeffrey T Chen Xiaoqi Fan Pingchen Chen Xi Fu Ying Liang Lingming Reed Michael Tang Liang Chen Jin-Long Jaen Juan Li Leping Dai Kang |
| Affiliation: | Department of Medicinal Chemistry, Amgen, South San Francisco, CA 94080, USA. jmihalic@amgen.com |
| Abstract: | A new class of MCHR1 antagonists was discovered via a high-throughput screen. Optimization of the lead structure resulted in the identification of indole 10e. This compound possesses good pharmacokinetic properties across preclinical species and is efficacious in reducing food consumption in an MCH cannulated rat model and a cynomolgus monkey food consumption model. |
| Keywords: | MCHR1 Melanin concentrating hormone |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |