Design, synthesis, and structure-activity relationship of carbamate-tethered aryl propanoic acids as novel PPARalpha/gamma dual agonists.
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Kim NJ, Lee KO, Koo BW, Li F, Yoo JK, Park HJ, Min KH, Lim JI, Kim MK, Kim JK, Suh YG
Design, synthesis, and structure-activity relationship of carbamate-tethered aryl propanoic acids as novel PPARalpha/gamma dual agonists.
Bioorg Med Chem Lett. 2007 Jul 1;17(13):3595-8. Epub 2007 Apr 25.
- PubMed ID
- 17507225 [ View in PubMed]
- Abstract
We have developed a new class of PPARalpha/gamma dual agonists, which show excellent agonistic activity in PPARalpha/gamma transactivation assay. In particular, (R)-9d was identified as a potent PPARalpha/gamma dual agonist with EC(50)s of 0.377 microM in PPARalpha and 0.136 microM in PPARgamma, respectively. Interestingly, the structure-activity relationship revealed that the stereochemistry of the identified PPARalpha/gamma dual agonists significantly affects their agonistic activities in PPARalpha than in PPARgamma.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Gemfibrozil Peroxisome proliferator-activated receptor alpha EC 50 (nM) 193300 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor alpha EC 50 (nM) 3460 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor gamma EC 50 (nM) 30 N/A N/A Details