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2-Aminoquinoline melanin-concentrating hormone (MCH)1R antagonists |
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| Authors: | Jiang Jinlong Hoang Myle Young Jonathan R Chaung Danny Eid Ronsar Turner Cherilyn Lin Peter Tong Xinchun Wang Junying Tan Carina Feighner Scott Palyha Oksana Hreniuk Donna L Pan Jie Sailer Andreas W MacNeil Douglas J Howard Andrew Shearman Lauren Stribling Sloan Camacho Ramon Strack Alison Van der Ploeg Lex H T Goulet Mark T DeVita Robert J |
| Institution: | Department of Medicinal Chemistry, PO Box 2000, Rahway, NJ 07065-0900, USA. |
| Abstract: | A series of 2-aminoquinoline compounds was prepared and evaluated in MCH1R binding and functional antagonist assays. Small dialkyl, methylalkyl, methylcycloalkyl, and cyclic amines were tolerated at the quinoline 2-position. The in vivo efficacy of compound 12 was explored and compared to that of a related inactive analog to determine their effects on food intake and body weight in rodents. |
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