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

Jun 17, 2022Archiv der Pharmazie

Medicinal uses of 2,4-thiazolidinedione compounds as infection fighters, cancer treatments, and diabetes drugs: A review

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Abstract

2,4-Thiazolidinedione (2,4-TZD) offers a diverse range of biological activities and opportunities for structural modification.

2,4-TZD is associated with various pharmacological activities, including antimicrobial, anticancer, and antidiabetic effects.
Common modifications are made at the N-3 position and the active methylene at C-5 of the 2,4-TZD structure.
The review discusses both market-available and clinically developed drugs based on 2,4-TZD derivatives.
Different synthetic methods for creating the 2,4-TZD core are outlined.
The study highlights the importance of substitutions at N-3 and C-5 for enhancing drug efficacy.

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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.

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

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