The medicinal perspective of 2,4‐thiazolidinediones based ligands as antimicrobial, antitumor and antidiabetic agents: A review

Abstract

2,4-Thiazolidinedione (2,4-TZD), commonly known as glitazone, is a ubiquitous heterocyclic pharmacophore possessing a plethora of pharmacological activities and offering a vast opportunity for structural modification. The diverse range of biological activities endowed with a novel mode of action, low cost, and easy synthesis has attracted the attention of medicinal chemists. Several researchers have integrated the TZD core with different structural fragments to develop a wide range of lead molecules against various clinical disorders. The most common sites for structural modifications at the 2,4-TZD nucleus are the N-3 and the active methylene at C-5. The review covers the recent development of TZD derivatives such as antimicrobial, anticancer, and antidiabetic agents. Various 2,4-TZD based agents or drugs, which are either under clinical development or in the market, are discussed in the study. Different synthetic methodologies for synthesizing the 2,4-TZD core are also included in the manuscript.The importance of various substitutions at N-3 and C-5 and the mechanisms of action and structure-activity relationships are also discussed. We hope this study will serve as a valuable tool for the scientific community engaged in the structural exploitation of the 2,4-TZD core for developing novel drug m\olecules for life-threatening ailments.

Updated Organic Composition and Potential Therapeutic Properties of Different Varieties of Olive Leaves from Olea europaea

“…Since GLP-1 has poor stability, GLP-1 agonists with longer half-lives and dipeptidyl peptide-4 (DPP-4) inhibitors are used in combination to treat T2DM. Thiazolidinediones (TZDs) enhance insulin sensitivity in skeletal muscle, liver, and adipose tissue and promote fat redistribution from liver and skeletal muscle to adipocytes [ 58 , 59 , 60 ]. Metformin, the most commonly prescribed drug for diabetes, may also increase insulin sensitivity in peripheral tissues during fasting [ 61 , 62 , 63 , 64 , 65 , 66 ].…”

Molecular Docking, Synthesis, and Characterization of Furanyl‐Pyrazolyl Acetamide and 2,4‐Thiazolidinyl‐Furan‐3‐Carboxamide Derivatives as Neuroinflammatory Protective Agents

“…(Figure 1). [32][33][34][35][36] Among them, succinimide-thiazolidinedione [37] and thiazolidinedione-1,3,4-oxadiazole showed anti-diabetic effects, [38] thiazolidinedione-oxoindoline [39] and thiazolidinedione-indole hybrids [40] showed anticancer and 1,3,4-thiadiazole-thiazolidinedione hybrids [41] demonstrated significant anti-inflammatory activity.…”

PPARG stimulation restored lung mRNA expression of core clock, inflammation‐ and metabolism‐related genes disrupted by reversed feeding in male mice

“…Activation of PPARG is a possible tool for the realization of pleiotropic effects. Such influence might be maintained by 2,4‐thiazolidinediones (glitazone) and its derivate with a plethora of pharmacological activities (Kajal et al, 2022 ).…”