Abstract

RECENT ADVANCES IN BIOLOGICAL ACTIVITIES, SYNTHETIC STRATERGIES AND STRUCTURE ACTIVITY RELATIONSHIP OF THIAZOLIDINEDIONE DERIVATIVES: A REVIEW

*Elizabeth George P., *Sunitha Sukumaran, Anitta Antony and Sandra Wilson

ABSTRACT

Thiazolidinediones (TZDs), also known as glitazones, are a versatile class of compounds originally introduced for the treatment of type 2 diabetes mellitus due to their antihyperglycemic properties. These compounds are peroxisome proliferator-activated receptor gamma (PPAR-γ) agonists, playing a critical role in improving insulin sensitivity and regulating glucose and lipid metabolism. In addition to their antidiabetic effects, TZDs exhibit a broad spectrum of biological activities, including antihyperlipidemic, anti-inflammatory, antioxidant, anticancer, antimicrobial, and antiviral properties. Structurally, TZDs are derivatives of the thiazolidine ring, and their pharmacological potential is largely influenced by substitutions at specific positions on the ring. Extensive research has explored the synthesis of novel TZD derivatives, optimizing their activity profiles and reducing adverse effects such as hepatotoxicity. Emerging studies highlight their role in dual PPARα/γ activation, aldose reductase inhibition, and α-glucosidase inhibition, broadening their therapeutic applications. Furthermore, TZDs show promise as anticancer agents, targeting key signaling pathways, and as antimicrobial agents capable of addressing drug-resistant pathogens. This review encapsulates the structural diversity, mechanisms of action, and therapeutic potential of TZDs, emphasizing their contribution to modern medicinal chemistry and their prospects as multifunctional pharmacological agents.

Keywords: Thiazolidinediones, peroxisome proliferator-activated receptors (PPARs), aldose reductase inhibition, ?-glucosidase inhibition.