Biological evaluation of novel benzisoxazole derivatives as PPARδ agonists

Bioorg Med Chem. 2011 May 15;19(10):3255-64. doi: 10.1016/j.bmc.2011.03.053. Epub 2011 Mar 31.

Abstract

We discovered novel peroxisome proliferator-activated receptor δ agonists with a characteristic benzisoxazole ring. Compound 5 exhibited potent human PPARδ transactivation activity. Furthermore, it stimulated the differentiation of oligodendrocyte precursor cells in vitro. This indicates that this potential drug may be effective for the treatment of demyelinating disorders such as multiple sclerosis.

MeSH terms

  • Animals
  • Cell Differentiation / drug effects
  • Cell Line
  • Cells, Cultured
  • Cerebral Cortex / cytology
  • Humans
  • Isoxazoles / chemistry*
  • Isoxazoles / pharmacology*
  • Oligodendroglia / cytology
  • Oligodendroglia / drug effects
  • PPAR delta / agonists*
  • PPAR delta / metabolism*
  • Rats
  • Rats, Wistar

Substances

  • 1,2-benzisoxazole
  • Isoxazoles
  • PPAR delta