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
Department of Medicinal Chemistry, PO Box 2000, Rahway, NJ 07065-0900, USA.
Bioorg Med Chem Lett. 2006 Oct 15;16(20):5270-4. doi: 10.1016/j.bmcl.2006.08.006. Epub 2006 Aug 17.
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.
制备了一系列2-氨基喹啉化合物，并在MCH1R结合和功能拮抗剂试验中进行了评估。喹啉2位可耐受小的二烷基、甲基烷基、甲基环烷基和环胺。研究了化合物12的体内疗效，并与相关的无活性类似物进行比较，以确定它们对啮齿动物食物摄入量和体重的影响。
