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Design and biological evaluation of novel, balanced dual PPARalpha/gamma agonists.
- Source :
-
ChemMedChem [ChemMedChem] 2009 Jun; Vol. 4 (6), pp. 951-6. - Publication Year :
- 2009
-
Abstract
- An X-ray-guided design approach led to the identification of a novel, balanced class of alpha-ethoxy-phenylpropionic acid-derived dual PPARalpha/gamma agonists. The series shows a wide range of PPARalpha/gamma ratios within a rather narrow structural space. Advanced compounds possess favorable physicochemical and pharmacokinetic profiles and show a high efficacy in T2D and dyslipidemia animal models.
- Subjects :
- Animals
Computer Simulation
Crystallography, X-Ray
Diabetes Mellitus, Type 2 drug therapy
Drug Design
Humans
Hypolipidemic Agents chemical synthesis
Hypolipidemic Agents pharmacokinetics
Mice
PPAR alpha metabolism
PPAR gamma metabolism
Phenylpropionates chemical synthesis
Phenylpropionates pharmacokinetics
Rats
Stereoisomerism
Structure-Activity Relationship
Hypolipidemic Agents chemistry
PPAR alpha agonists
PPAR gamma agonists
Phenylpropionates chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1860-7187
- Volume :
- 4
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- ChemMedChem
- Publication Type :
- Academic Journal
- Accession number :
- 19326383
- Full Text :
- https://doi.org/10.1002/cmdc.200800425