Design, Synthesis, and Activity Evaluation of GK/PPARγ Dual‐Target‐Directed Ligands as Hypoglycemic Agents

Apr 17, 2014ChemMedChem

Design and testing of compounds targeting GK and PPARγ to lower blood sugar

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Abstract

Three compounds demonstrated high potency toward glucokinase and moderate activity toward PPARγ.

  • A multi-target strategy was employed to develop agents for treating type 2 diabetes mellitus.
  • Dual-target molecules were created by integrating features from known glucokinase activators and PPARγ agonists.
  • The dual-target agents were assessed for their ability to activate transcription for both GK and PPARγ.
  • Preliminary analysis of structure-activity relationships was conducted for the synthesized compounds.
  • Molecular docking simulations were performed to explore the binding modes of one of the most effective compounds.

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