5-aryl thiazolidine-2,4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents.
Article Details
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Desai RC, Han W, Metzger EJ, Bergman JP, Gratale DF, MacNaul KL, Berger JP, Doebber TW, Leung K, Moller DE, Heck JV, Sahoo SP
5-aryl thiazolidine-2,4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents.
Bioorg Med Chem Lett. 2003 Aug 18;13(16):2795-8.
- PubMed ID
- 12873517 [ View in PubMed]
- Abstract
A novel series of 5-aryl thiazolidine-2,4-diones based dual PPARalpha/gamma agonists was identified. A number of highly potent and orally bioavailable analogues were synthesized. Efficacy study results of some of these analogues in the db/db mice model of type 2 diabetes showed them superior to rosiglitazone in correcting hyperglycemia and hypertriglyceridemia.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Rosiglitazone Peroxisome proliferator-activated receptor alpha IC 50 (nM) >50000 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor alpha EC 50 (nM) >3000 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor delta IC 50 (nM) >50000 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor delta EC 50 (nM) >3000 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor gamma EC 50 (nM) 20 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor gamma IC 50 (nM) 250 N/A N/A Details