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.

引用

页码：223 / 236

页数：14