Synthesis and evaluation of a series of benzopyran derivatives as PPAR α/γ agonists

A series of benzopyran derivatives were synthesized and evaluated for PPAR α/γ agonist activities. Most of the compounds exhibit reasonable PPAR α and PPAR γ agonist activities. In particular, compounds 7b, 8b, 8e and 8h with remarkable PPARg EC50 values of 0.001 μM are excellent full PPAR γ agonists with the functional potency about 130, 20 times stronger than that of leading compound 5 and rosiglitazone, respectively. Compounds 7a, 7c, 7d and 8a are dual PPAR α/γ agonists, and all of them gave comparable or stronger PPAR α/γ agonist efficacy than that of the corresponding positive control.

Graphical abstractA new series of benzopyran derivatives were synthesized as continuing work of compound 5. Their PPAR agonist activities were evaluated and most of the compounds exhibit reasonable PPAR α and PPAR γ agonist activities. In particular, compounds 7b, 8b, 8e and 8h with remarkable PPAR γ EC50 values of 0.001 μM are excellent full PPAR γ agonists. Figure optionsDownload full-size imageDownload as PowerPoint slide