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Design, synthesis, and biological evaluation of novel thiazolidinediones as PPARγ/FFAR1 dual agonists
Creation and testing of new thiazolidinedione compounds that activate both PPARγ and FFAR1 receptors
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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.
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