Synthesis and evaluation of a series of benzopyran derivatives as PPAR alpha/gamma agonists.
A series of benzopyran derivatives were synthesized and evaluated for PPAR alpha/gamma agonist activities. Most of the compounds exhibit reasonable PPAR alpha and PPAR gamma agonist activities. In particular, compounds 7b, 8b, 8e and 8h with remarkable PPARg EC(50) values of 0.001microM are excellent full PPAR gamma 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 alpha/gamma agonists, and all of them gave comparable or stronger PPAR alpha/gamma agonist efficacy than that of the corresponding positive control.
Yu
Juanhong
J
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Graduate School of the Chinese Academy of Sciences, CAS, Shanghai 201203, China.
Tang
Lei
L
Yang
Yushe
Y
Ji
Ruyun
R
D001578:Benzopyrans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D006801:Humans; D015394:Molecular Structure; D047493:PPAR alpha / Q000819:agonists* / Q000378:metabolism; D047495:PPAR gamma / Q000819:agonists* / Q000378:metabolism; D013329:Structure-Activity Relationship
D001578:Benzopyrans; D047493:PPAR alpha; D047495:PPAR gamma