Synthesis and evaluation of azaindole-alpha-alkyloxyphenylpropionic acid analogues as PPARalpha/gamma agonists

Zhefeng Cai; Jun Feng; Yanshen Guo; Pingping Li; Zhufang Shen; Fengming Chu; Zongru Guo

doi:10.1016/j.bmc.2005.09.040

Synthesis and evaluation of azaindole-alpha-alkyloxyphenylpropionic acid analogues as PPARalpha/gamma agonists

Bioorg Med Chem. 2006 Feb 1;14(3):866-74. doi: 10.1016/j.bmc.2005.09.040. Epub 2005 Oct 24.

Authors

Zhefeng Cai¹, Jun Feng, Yanshen Guo, Pingping Li, Zhufang Shen, Fengming Chu, Zongru Guo

Affiliation

¹ Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China.

PMID: 16249089
DOI: 10.1016/j.bmc.2005.09.040

Abstract

A series of azaindole-alpha-alkyloxyphenylpropionic acid analogues was synthesized and evaluated for PPAR agonist activities. Structure-activity relationship was developed for PPARalpha/gamma dual agonism. One of the synthesized compound 7a was identified as a potent, selective PPARalpha/gamma dual agonist.

MeSH terms

Animals
Cell Line
Drug Design
Humans
In Vitro Techniques
Mice
PPAR alpha / agonists*
PPAR gamma / agonists*
Phenylpropionates / chemical synthesis*
Phenylpropionates / chemistry
Phenylpropionates / pharmacology*
Recombinant Fusion Proteins / agonists
Structure-Activity Relationship

Substances

PPAR alpha
PPAR gamma
Phenylpropionates
Recombinant Fusion Proteins