873945-07-4Relevant academic research and scientific papers
Synthesis and evaluation of a series of benzopyran derivatives as PPAR α/γ agonists
Yu, Juanhong,Tang, Lei,Yang, Yushe,Ji, Ruyun
, p. 2428 - 2435 (2008/12/23)
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.
