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.

A 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 as PowerPoint slide