Concise perspectives on some synthetic thiazolidine-2,4-dione derivatives and their specific pharmacodynamic aspects

Life Sci. 2021 Apr 15:271:119182. doi: 10.1016/j.lfs.2021.119182. Epub 2021 Feb 9.

Abstract

Glitazones are synthetic derivatives of thiazolidinedione, and are designated as oral anti-diabetic agents, primarily acting on peroxisome proliferator-activated receptor-gamma (PPAR-γ) receptors and driving some crucial metabolic pathways linked to glucose and lipid metabolism at transcriptional level. Despite presenting adverse effects, including weight gain, fluid retention, prostate hyperplasia, hyperinsulinemia, and myocardial infarction, they are still preferred in clinical settings due to their utmost efficacy and selectivity. However, these complications kept glitazones restrained for long-term usage. The present review briefly highlights some important synthetic derivatives of thiazolidine2,4-dione and emphasizes the influence of various structural manipulations on their bio-efficacy.

Keywords: Anti-diabetic; Insulin resistance; PPAR-γ; Side effects; Thiazolidinedione.

Publication types

  • Review

MeSH terms

  • Animals
  • Diabetes Mellitus, Type 2 / drug therapy
  • Diabetes Mellitus, Type 2 / metabolism
  • Glucose / antagonists & inhibitors
  • Glucose / metabolism
  • Humans
  • Hypoglycemic Agents / chemistry*
  • Hypoglycemic Agents / metabolism*
  • Hypoglycemic Agents / therapeutic use
  • Insulin Resistance / physiology
  • PPAR gamma / metabolism
  • Protein Structure, Secondary
  • Protein Structure, Tertiary
  • Thiazolidinediones / chemistry*
  • Thiazolidinediones / metabolism*
  • Thiazolidinediones / therapeutic use

Substances

  • Hypoglycemic Agents
  • PPAR gamma
  • Thiazolidinediones
  • thiazolidine-2,4-dione
  • Glucose