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Design of potent PPARalpha agonists
- 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.
- Subjects :
- Crystallography
Phenylpropionates
Computers
Drug Design
Animals
PPAR alpha
Ligands
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 17
- Issue :
- 11
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.pmid..........23276e9575f5be16999ec507f7e7ebd6