Peroxisome proliferator-activated receptors (PPAR), a type of nuclear receptor, act principally as lipid sensors and regulate whole body metabolism. There are three know isotypes: PPARg, PPARa, and PPARb/d. PPARg is commonly used as an agonist for the treatment of Type II diabetes. Looking beyond the metabolic interaction of PPARg, studies show that PPARg activation is also involved in other physiological events, including events known to play a role in neurological diseases, such as Alzheimer’s and Parkinson’s disease. Nevertheless, little is known about characterizing cofactor recruitment induced by PPAR ligands. The design and synthesis of novel ligands using medicinal chemistry techniques will provide resources to study the impact of receptor conformational changes on PPARg. The goal of this project was to synthesis compound 10221, Figure 1, as an inverse agonist to help study PPARg characterization, and its role in neurological diseases. 10221 is an eight-step synthesis, of the eight steps only two synthetic steps were completed.

Synthesis of compound 10221 for peroxisome proliferator-activated receptor interactions

255th National Meeting (2018)

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