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

被引：5
作者：
Bell, RPL
Verdijk, D
Relou, M
Smith, D
Regeling, H
Ebbers, EJ
Leemhuis, FMC
Oniciu, DC
Cramer, CT
Goetz, B
Pape, ME
Krause, BR
Dasseux, JL
机构：
[1] Pfizer Global Res & Dev, Esper Therapeut Div, Ann Arbor, MI 48108 USA
[2] MercaChem BV, NL-6525 EC Nijmegen, Netherlands
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2005年 / 13卷 / 01期
关键词：
dyslipidemia; HDL-cholesterol; TosMic; cycloalkyl;
D O I：
10.1016/j.bmc.2004.09.046
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
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 muM 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. (C) 2004 Elsevier Ltd. All rights reserved.
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收藏
页码：223 / 236
页数：14
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