AI Article Synopsis
- Researchers designed nitrogen heterocycles based on α-ethoxyphenylpropionic acid derivatives to target PPARα/γ receptors for treating type 2 diabetes (T2D).
- Among the compounds tested, 6-Benzoyl-benzothiazol-2-one demonstrated the best results after modifications, leading to a specific stereoisomer with an excellent in vitro pharmacological profile.
- This compound was identified as a potent full PPARγ agonist and a weak partial agonist for PPARα, showing effectiveness in reducing triglycerides, glucose, and insulin levels in ob/ob mice without causing significant weight gain, classifying it as a selective PPARγ modulator (SPPARγM).
Article Abstract
A series of nitrogen heterocycles containing α-ethoxyphenylpropionic acid derivatives were designed as dual PPARα/γ agonist ligands for the treatment of type 2 diabetes (T2D) and its complications. 6-Benzoyl-benzothiazol-2-one was the most tolerant of the tested heterocycles in which incorporation of O-methyl oxime ether and trifluoroethoxy group followed by enantiomeric resolution led to the ()-stereoisomer displaying the best in vitro pharmacological profile. Compound acted as a very potent full PPARγ agonist and a weak partial agonist on the PPARα receptor subtype. Compound showed high efficacy in an ob/ob mice model with significant decreases in serum triglyceride, glucose and insulin levels but mostly with limited body-weight gain and could be considered as a selective PPARγ modulator (SPPARγM).
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7006651 | PMC |
| http://dx.doi.org/10.1080/14756366.2020.1713771 | DOI Listing |
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