α-cycloalkyl-substituted ω-keto-dicarboxylic acids as lipid regulating agents

Autor: Roel P L, Bell, Dennis, Verdijk, Mike, Relou, Dennis, Smith, Henk, Regeling, Eelco J, Ebbers, Frank M C, Leemhuis, Daniela C, Oniciu, Clay T, Cramer, Brian, Goetz, Michael E, Pape, Brian R, Krause, Charles L, Bisgaier, Jean-Louis, Dasseux
Rok vydání: 2005
Předmět:
Zdroj: Bioorganic & Medicinal Chemistry. 13:223-236
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2004.09.046
Popis: A series of cycloalkyl-substituted oxo-alkanedicarboxylic acids have been prepared by the TosMIC methodology departing from haloalkyl-substituted cycloalkylcarboxylic esters. cyclopropyl derivatives showed IC50 activity in the 0.3–1.0 μM 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.
Databáze: OpenAIRE