Design, synthesis, and biological evaluation of novel thiazolidinediones as PPARγ/FFAR1 dual agonists

Jan 18, 2016European journal of medicinal chemistry

Creation and testing of new thiazolidinedione compounds that activate both PPARγ and FFAR1 receptors

AI simplified

Abstract

Nine newly designed compounds showed promising dual activity as insulin sensitizers and secretagogues.

  • The study identified nineteen compounds designed for agonistic activity on PPARγ and FFAR1.
  • Two compounds, 11a and 5b, exhibited affinities in the low micromolar range on both receptors.
  • Activation of FFAR1 has been associated with enhanced insulin secretion in diabetic patients.
  • Some thiazolidinediones (TZDs) are known to activate FFAR1 with micromolar potency.
  • PPARγ regulates processes related to fat cell formation and glucose metabolism.

AI simplified

Full Text

Full text is available at the source.

what lands in your inbox each week:

  • 📚7 fresh studies
  • 📝plain-language summaries
  • direct links to original studies
  • 🏅top journal indicators
  • 📅weekly delivery
  • 🧘‍♂️always free