The synthesis of three isotopomers of 2-methyl-2-(4-[3-[1-(4-methylbenzyl)-5-oxo-4,5-dihydro-1H-[1,2,4]triazol-3-yl]propyl]phenoxy)propionic acid, a potent and selective peroxisome proliferator-activated receptor alpha agonist

被引：2

作者：

Kuo, Fengjiun ^{[1
]}

Clodfelter, Dean K. ^{[1
]}

Farid, Nagy A. ^{[1
]}

Wheeler, William J. ^{[1
]}

McKendry, Lennon H. ^{[1
]}

机构：

[1] Eli Lilly & Co, Lilly Corp Ctr, Lilly Res Labs, Indianapolis, IN 46285 USA

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2007年 / 50卷 / 7-8期

关键词：

PPAR alpha; C-14; tritium; SLIS; dyslipidemia;

D O I：

10.1002/jlcr.1395

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Although fenofibrate (1a) is commercially available and clinically effective in lowering serum triglycerides, its activity and sub-type selectivity at the PPAR alpha receptors are only moderate; therefore, there exists a need for more potent and sub-type selective PPAR alpha agonists. To that end, discovery efforts have identified 2-methyl-2-(4-[3-[1-(4methylbenzyl)-5-oxo-4,5-dihydro-1H-[1,2,4]tiiazol-3-yl]propyl]phenoxy)propionic acid (2), a potent and selective human PPAR alpha receptor agonist. In support of pre-clinical ADME studies and bioanalysis, three isotopomers of 2 have been synthesized. The results of these efforts are described below. Copyright (c) 2007 John Wiley & Sons, Ltd.

引用

页码：693 / 701

页数：9

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