alpha-Cycloalkyl-substituted omega-keto-dicarboxylic acids as lipid regulating agents.
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.
Bell
Roel P L
RP
MercaChem BV, Toernooiveld 100, 6525 EC Nijmegen, The Netherlands.
Verdijk
Dennis
D
Relou
Mike
M
Smith
Dennis
D
Regeling
Henk
H
Ebbers
Eelco J
EJ
Leemhuis
Frank M C
FM
Oniciu
Daniela C
DC
Cramer
Clay T
CT
Goetz
Brian
B
Pape
Michael E
ME
Krause
Brian R
BR
Bisgaier
Charles L
CL
Dasseux
Jean-Louis
JL
D000818:Animals; D002478:Cells, Cultured; D003998:Dicarboxylic Acids / Q000737:chemistry / Q000494:pharmacology*; D022781:Hepatocytes / Q000187:drug effects / Q000378:metabolism; D008055:Lipids / Q000097:blood*; D008074:Lipoproteins / Q000097:blood*; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D013058:Mass Spectrometry; D051381:Rats; D017207:Rats, Sprague-Dawley
D003998:Dicarboxylic Acids; D008055:Lipids; D008074:Lipoproteins