Bell Roel P L, Verdijk Dennis, Relou Mike, Smith Dennis, Regeling Henk, Ebbers Eelco J, Leemhuis Frank M C, Oniciu Daniela C, Cramer Clay T, Goetz Brian, Pape Michael E, Krause Brian R, Bisgaier Charles L, Dasseux Jean-Louis
MercaChem BV, Toernooiveld 100, 6525 EC Nijmegen, The Netherlands.
Bioorg Med Chem. 2005 Jan 3;13(1):223-36. doi: 10.1016/j.bmc.2004.09.046.
A series of cycloalkyl-substituted oxo-alkanedicarboxylic acids have been prepared by the TosMIC methodology departing from haloalkyl-substituted cycloalkylcarboxylic esters. cyclopropyl derivatives showed IC(50) activity in the 0.3-1.0 microM range on the de novo incorporation of radiolabeled acetate into lipids in primary cultures of rat hepatocytes, and they showed lipid-regulating properties when tested in vivo in female obese Zucker fatty rats.
通过TosMIC方法，以卤代烷基取代的环烷基羧酸酯为原料，制备了一系列环烷基取代的氧代链烷二羧酸。环丙基衍生物在大鼠原代肝细胞中将放射性标记的乙酸盐从头掺入脂质的过程中，表现出0.3 - 1.0微摩尔范围内的IC(50)活性，并且在雌性肥胖Zucker脂肪大鼠体内进行测试时，它们表现出脂质调节特性。
