Thiazolidinediones as antidiabetic agents: A critical review

Thiazolidinediones (TZDs) are an important class of insulin sensitizers used in the treatment of Type 2 diabetes mellitus (T2DM).

• TZDs were initially recognized for their effects on lowering blood sugar and lipid levels.
• These drugs primarily activate Peroxisome Proliferators Activated Receptors (PPARs), specifically PPAR-γ, to exert their antidiabetic effects.
• Previous TZDs were full agonists of PPAR-γ but associated with serious side effects, leading to their withdrawal or modification.
• Recent research has focused on developing dual agonists and selective modulators of PPARs to enhance safety and efficacy.
• Alternative approaches that do not involve PPAR activation, such as targeting various receptors and enzymes, are being explored to overcome TZD-related issues.
• This report reviews the evolution of TZDs, including their chemistry, mechanisms, and recent advancements in the field.

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