Synthesis and evaluation of a series of benzopyran derivatives as PPAR alpha/gamma agonists.

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Yu J, Tang L, Yang Y, Ji R

Synthesis and evaluation of a series of benzopyran derivatives as PPAR alpha/gamma agonists.

Eur J Med Chem. 2008 Nov;43(11):2428-35. doi: 10.1016/j.ejmech.2008.01.029. Epub 2008 Feb 2.

PubMed ID

18329751 [ View in PubMed

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Abstract

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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Rosiglitazone	Peroxisome proliferator-activated receptor gamma	EC 50 (nM)	20	N/A	N/A	Details