Phenylpropanoic acid derivatives bearing a benzothiazole ring as PPARdelta-selective agonists

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4351-7. doi: 10.1016/j.bmcl.2007.05.017. Epub 2007 May 13.

Abstract

To find novel PPARdelta-selective agonists, we designed and synthesized phenylpropanoic acid derivatives bearing 6-substituted benzothiazoles. Optimization of this series led to the identification of a potent and selective PPARdelta agonist 17. Molecular modeling suggested that compound 17 occupies the Y-shaped pocket of PPARdelta appropriately.

MeSH terms

  • Benzothiazoles / chemistry*
  • Humans
  • Models, Molecular
  • PPAR delta / agonists*
  • Phenylpropionates / pharmacology*
  • Pyrimidines / pharmacology

Substances

  • Benzothiazoles
  • PPAR delta
  • Phenylpropionates
  • Pyrimidines
  • pirinixic acid