4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part I: synthesis and pharmacological evaluation

Bioorg Med Chem Lett. 2008 Mar 1;18(5):1617-22. doi: 10.1016/j.bmcl.2008.01.067. Epub 2008 Jan 19.


Type-2 diabetes (T2D) is a complex metabolic disease characterized by insulin resistance in the liver and peripheral tissues accompanied by a defect in pancreatic beta-cell. Since their discovery three subtypes of Peroxisomes Proliferators Activated Receptors were identified namely PPARalpha, PPARgamma and PPARbeta/(delta). We were interested in designing novel PPARgamma selective agonists and/or dual PPARalpha/gamma agonists. Based on the typical topology of synthetic PPAR agonists, we focused our design approach on 4,4-dimethyl-1,2,3,4-tetrahydroquinoline as novel cyclic tail.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Hypoglycemic Agents / chemistry*
  • Hypoglycemic Agents / pharmacology*
  • Molecular Structure
  • PPAR alpha / agonists*
  • PPAR gamma / agonists*
  • Quinolines / chemistry*
  • Quinolines / pharmacology*
  • Structure-Activity Relationship


  • 4,4-dimethyl-1,2,3,4-tetrahydroquinoline
  • Hypoglycemic Agents
  • PPAR alpha
  • PPAR gamma
  • Quinolines