Related Experiment Video
Updated: Jan 17, 2026

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
Thiazolidine-2,4-Dione: Bridging the Gap Between Synthesis, SAR, and Biological Activities, and Computational
Nirmala V Shinde1, Vrushali P Patole1, Siddhi M Chandak1
1Department of Pharmaceutical Chemistry, SMBT college of Pharmacy, Dhamangaon, Nashik, Maharashtra-422403 India.
Introduction:
Thiazolidinedione is one of the most important classes in medicinal chemistry. Thiazolidine-2,4-dione (TZD) is a versatile scaffold, best known for its use in the development of anti-diabetic drugs such as pioglitazone and rosiglitazone. Beyond their well-established antidiabetic properties, TZDs exhibit a wide range of biological activities including anticancer, anti-inflammatory, antibacterial, and neuroprotective effects, making them potential candidates for various therapeutic applications.
Methodology:
This review focuses on the complete journey of TZD derivatives-from their synthetic design to their inclusion in commercialized pharmaceutical products. Structure-activity relationship (SAR) studies were analyzed to understand how modifications in the TZD core affect binding affinity, selectivity, and therapeutic efficacy. In addition, the review consolidates findings from biological evaluations and computational studies that provide deeper insights into the mechanism of action and pharmacological potential of TZD derivatives.
Conclusion:
This review highlights the significance of the TZD scaffold as a multifunctional pharmacophore in drug discovery. By integrating synthetic strategies, SAR analysis, and advanced computational tools, TZD derivatives continue to show great potential for the development of new therapeutic agents for various diseases. The combined understanding of chemistry and biological activities of TZDs paves the way for innovative research and future drug design.
More Related Videos
Related Concept Videos
Structure-Activity Relationships and Drug Design
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence...
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
The direct-acting...
Adrenergic Agonists: Chemistry and Structure-Activity Relationship
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of...
Cholinergic Antagonists: Chemistry and Structure-Activity Relationship
Aryldiazonium Salts to Azo Dyes: Diazo Coupling

