Back to Search Start Over

Design of potent PPARalpha agonists

Authors :
Per, Sauerberg
John P, Mogensen
Lone, Jeppesen
Paul S, Bury
Jan, Fleckner
Grith S, Olsen
Claus B, Jeppesen
Erik M, Wulff
Pavel, Pihera
Miroslav, Havranek
Zdenek, Polivka
Ingrid, Pettersson
Source :
Bioorganicmedicinal chemistry letters. 17(11)
Publication Year :
2007

Abstract

Computational analysis of the ligand binding pocket of the three PPAR receptor subtypes was utilized in the design of potent PPARalpha agonists. Optimum PPARalpha potency and selectivity were obtained with substituents having van der Waals volume around 260. Compound 6 had a PPARalpha potency of 0.002 microM and a selectivity ratio to PPARgamma and PPARdelta of 410 and 2000, respectively.

Details

ISSN :
0960894X
Volume :
17
Issue :
11
Database :
OpenAIRE
Journal :
Bioorganicmedicinal chemistry letters
Accession number :
edsair.pmid..........23276e9575f5be16999ec507f7e7ebd6