Bioorganic & medicinal chemistry letters, 2011-01, Vol.21 (1), p.492-496
2011
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Details
- Autor(en) / Beteiligte
- Titel
- Discovery of isoindoline and tetrahydroisoquinoline derivatives as potent, selective PPARδ agonists
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2011-01, Vol.21 (1), p.492-496
- Ort / Verlag
- Amsterdam: Elsevier Ltd
- Erscheinungsjahr
- 2011
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- We describe the discovery of small molecule isoindoline and tetrahydroisoquinoline derivatives as agonists of human peroxisome proliferator-activated receptor δ (PPARδ that displayed excellent selectivity over the PPARα and PPARγ subtypes. Compound 18 demonstrated efficacy in upregulation of PDK4 in human primary myotubes, a biomarker for increased fatty acid oxidation. Small molecule isoindoline and tetrahydroisoquinoline derivatives have been identified as selective agonists of human peroxisome proliferator-activated receptor δ (PPARδ. Compound 18 demonstrated efficacy in a biomarker for increased fatty acid oxidation, with upregulation of pyruvate dehydrogenase kinase, isozyme 4 (PDK4) in human primary myotubes.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2010.10.117Titel-ID: cdi_proquest_miscellaneous_821198414
- Format
- –
- Schlagworte
- agonists, beta oxidation, Binding Sites, Biological and medical sciences, biomarkers, Catalytic Domain, Computer Simulation, General and cellular metabolism. Vitamins, Humans, Indoles - chemical synthesis, Indoles - chemistry, Indoles - pharmacology, Isoindolines, isozymes, Medical sciences, Pharmacology. Drug treatments, PPAR delta - agonists, PPAR delta - metabolism, PPARδ agonism, Protein-Serine-Threonine Kinases - genetics, Protein-Serine-Threonine Kinases - metabolism, pyruvate dehydrogenase (acetyl-transferring) kinase, Structure-Activity Relationship, Tetrahydroisoquinolines, Tetrahydroisoquinolines - chemical synthesis, Tetrahydroisoquinolines - chemistry, Tetrahydroisoquinolines - pharmacology