Revisiting glitazars: thiophene substituted oxazole containing alpha-ethoxy phenylpropanoic acid derivatives as highly potent PPARalpha/gamma dual agonists devoid of adverse effects in rodents.

Article Details

Citation

Copy to clipboard

Raval P, Jain M, Goswami A, Basu S, Gite A, Godha A, Pingali H, Raval S, Giri S, Suthar D, Shah M, Patel P

Revisiting glitazars: thiophene substituted oxazole containing alpha-ethoxy phenylpropanoic acid derivatives as highly potent PPARalpha/gamma dual agonists devoid of adverse effects in rodents.

Bioorg Med Chem Lett. 2011 May 15;21(10):3103-9. doi: 10.1016/j.bmcl.2011.03.020. Epub 2011 Mar 28.

PubMed ID

21450468 [ View in PubMed

]

Abstract

In an effort to develop safe and efficacious compounds for the treatment of metabolic disorders, novel thiophene substituted oxazole containing alpha-alkoxy-phenylpropanoic acid derivatives are designed as highly potent PPARalpha/gamma dual agonists. These compounds were found to be efficacious at picomolar concentrations. Lead compound 18d has emerged as very potent PPARalpha/gamma dual agonist demonstrating potent antidiabetic and lipid lowering activity at a very low dose and did not exhibit any significant signs of toxicity in rodents.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Rosiglitazone	Peroxisome proliferator-activated receptor gamma	EC 50 (nM)	50	N/A	N/A	Details