2-Aminoquinoline melanin-concentrating hormone (MCH) 1R antagonists

J Jiang, M Hoang, JR Young, D Chaung, R Eid…

Index: 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. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 20 p. 5270 - 5274

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Citation Number: 24

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.