4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part I: synthesis and pharmacological evaluation.
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Parmenon C, Guillard J, Caignard DH, Hennuyer N, Staels B, Audinot-Bouchez V, Boutin JA, Dacquet C, Ktorza A, Viaud-Massuard MC
4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part I: synthesis and pharmacological evaluation.
Bioorg Med Chem Lett. 2008 Mar 1;18(5):1617-22. doi: 10.1016/j.bmcl.2008.01.067. Epub 2008 Jan 19.
- PubMed ID
- 18255290 [ View in PubMed]
- Abstract
Type-2 diabetes (T2D) is a complex metabolic disease characterized by insulin resistance in the liver and peripheral tissues accompanied by a defect in pancreatic beta-cell. Since their discovery three subtypes of Peroxisomes Proliferators Activated Receptors were identified namely PPARalpha, PPARgamma and PPARbeta/(delta). We were interested in designing novel PPARgamma selective agonists and/or dual PPARalpha/gamma agonists. Based on the typical topology of synthetic PPAR agonists, we focused our design approach on 4,4-dimethyl-1,2,3,4-tetrahydroquinoline as novel cyclic tail.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Rosiglitazone Peroxisome proliferator-activated receptor alpha EC 50 (nM) 10000 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor alpha EC 50 (nM) 4 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor gamma Ki (nM) 8 N/A N/A Details Tesaglitazar Peroxisome proliferator-activated receptor alpha EC 50 (nM) 414 N/A N/A Details Tesaglitazar Peroxisome proliferator-activated receptor alpha EC 50 (nM) 37 N/A N/A Details Tesaglitazar Peroxisome proliferator-activated receptor gamma Ki (nM) 18 N/A N/A Details