Antidiabetic Potential of Thiazolidinedione Derivatives with Efficient Design, Molecular Docking, Structural Activity Relationship, and Biological Activity: an Update Review (2021-2023)

Overview

Journal Mol Divers

Date 2024 Jan 22

PMID 38253844

Authors

Anchal Sharma

Nitish Kumar

Harmandeep Kaur Gulati

Rupali Rana

Jyoti

Aanchal Khanna

Muskan

Jatinder Vir Singh

Preet Mohinder Singh Bedi

Affiliations

Soon will be listed here.

Abstract

Thiazolidinedione has been used successfully by medicinal chemists all over the world in the development of potent antidiabetic derivatives. The few compounds with excellent antidiabetic potency that we have identified in this review could be used as a lead for further research into additional antidiabetic mechanisms. The information provided in this review regarding the design, biological activity, structure-activity relationships, and docking studies may be useful for scientists who wish to further explore this scaffold in order to fully utilize its biological potential and develop antidiabetic agents that would overcome the limitations of currently available medications for the treatment of diabetes. This review outlines the antidiabetic potential of Thiazolidinedione-based derivatives that have been published in the year 2021- till date.

Citing Articles

CADD based designing and biological evaluation of novel triazole based thiazolidinedione coumarin hybrids as antidiabetic agent.

Sharma A, Narang A, Kumar N, Rana R, Megha , Pooja Sci Rep. 2025; 15(1):4302.

PMID: 39905269 PMC: 11794853. DOI: 10.1038/s41598-025-88944-y.

References

Hegazi R, El-Gamal M, Abdel-Hady N, Hamdy O . Epidemiology of and Risk Factors for Type 2 Diabetes in Egypt. Ann Glob Health. 2016; 81(6):814-20. DOI: 10.1016/j.aogh.2015.12.011. View

Hajji S, Aljenaee K, Garrahy A, Byrne M . Successful transition from insulin to sulfonylurea, on second attempt, in a 24-year-old female with neonatal diabetes secondary to KCNJ11 gene mutation. BMJ Case Rep. 2021; 14(4). PMC: 8043004. DOI: 10.1136/bcr-2020-239973. View

Mifsud S, Schembri E, Fava S . A case of severe relapsing sulphonylurea-induced hypoglycaemia. BMJ Case Rep. 2019; 12(12). PMC: 7001685. DOI: 10.1136/bcr-2019-231368. View

Sartore G, Ragazzi E, Caprino R, Lapolla A . Long-term HbA1c variability and macro-/micro-vascular complications in type 2 diabetes mellitus: a meta-analysis update. Acta Diabetol. 2023; 60(6):721-738. PMC: 10148792. DOI: 10.1007/s00592-023-02037-8. View

Doyle-Delgado K, Chamberlain J, Shubrook J, Skolnik N, Trujillo J . Pharmacologic Approaches to Glycemic Treatment of Type 2 Diabetes: Synopsis of the 2020 American Diabetes Association's Standards of Medical Care in Diabetes Clinical Guideline. Ann Intern Med. 2020; 173(10):813-821. DOI: 10.7326/M20-2470. View

Lebovitz H . Thiazolidinediones: the Forgotten Diabetes Medications. Curr Diab Rep. 2019; 19(12):151. PMC: 6881429. DOI: 10.1007/s11892-019-1270-y. View

Ahn S, Lee M, An S, Hyun S, Hwang J, Lee J . 2-Formyl-komarovicine promotes adiponectin production in human mesenchymal stem cells through PPARγ partial agonism. Bioorg Med Chem. 2018; 26(5):1069-1075. DOI: 10.1016/j.bmc.2018.01.019. View

Lehmann J, Moore L, Wilkison W, Willson T, Kliewer S . An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma). J Biol Chem. 1995; 270(22):12953-6. DOI: 10.1074/jbc.270.22.12953. View

Dirven H, Vist G, Bandhakavi S, Mehta J, Fitch S, Pound P . Performance of preclinical models in predicting drug-induced liver injury in humans: a systematic review. Sci Rep. 2021; 11(1):6403. PMC: 7973584. DOI: 10.1038/s41598-021-85708-2. View

10.

Babai S, Auclert L, Le-Louet H . Safety data and withdrawal of hepatotoxic drugs. Therapie. 2018; 76(6):715-723. DOI: 10.1016/j.therap.2018.02.004. View

11.

Mannucci E, Dicembrini I . Drugs for type 2 diabetes: role in the regulation of bone metabolism. Clin Cases Miner Bone Metab. 2015; 12(2):130-4. PMC: 4625768. DOI: 10.11138/ccmbm/2015.12.2.130. View

12.

Good A, Liu J, Hirth B, Asmussen G, Xiang Y, Biemann H . Implications of promiscuous Pim-1 kinase fragment inhibitor hydrophobic interactions for fragment-based drug design. J Med Chem. 2012; 55(6):2641-8. DOI: 10.1021/jm2014698. View

13.

Mueller A . A Note about Crosslinking Density in Imprinting Polymerization. Molecules. 2021; 26(17). PMC: 8434133. DOI: 10.3390/molecules26175139. View

14.

Shang J, Brust R, Griffin P, Kamenecka T, Kojetin D . Quantitative structural assessment of graded receptor agonism. Proc Natl Acad Sci U S A. 2019; 116(44):22179-22188. PMC: 6825269. DOI: 10.1073/pnas.1909016116. View

15.

Chrysanthopoulos P, Mujumdar P, Woods L, Dolezal O, Ren B, Peat T . Identification of a New Zinc Binding Chemotype by Fragment Screening. J Med Chem. 2017; 60(17):7333-7349. DOI: 10.1021/acs.jmedchem.7b00606. View

16.

Kumar H, Aggarwal N, Marwaha M, Deep A, Chopra H, Matin M . Thiazolidin-2,4-Dione Scaffold: An Insight into Recent Advances as Antimicrobial, Antioxidant, and Hypoglycemic Agents. Molecules. 2022; 27(19). PMC: 9572748. DOI: 10.3390/molecules27196763. View

17.

Dreyer C, Krey G, Keller H, Givel F, Helftenbein G, Wahli W . Control of the peroxisomal beta-oxidation pathway by a novel family of nuclear hormone receptors. Cell. 1992; 68(5):879-87. DOI: 10.1016/0092-8674(92)90031-7. View

18.

Meirhaeghe A, Amouyel P . Impact of genetic variation of PPARgamma in humans. Mol Genet Metab. 2004; 83(1-2):93-102. DOI: 10.1016/j.ymgme.2004.08.014. View

19.

Chittiboyina A, Venkatraman M, Mizuno C, Desai P, Patny A, Benson S . Design and synthesis of the first generation of dithiolane thiazolidinedione- and phenylacetic acid-based PPARgamma agonists. J Med Chem. 2006; 49(14):4072-84. DOI: 10.1021/jm0510880. View

20.

Madhavan G, Chakrabarti R, Vikramadithyan R, Mamidi R, Balraju V, Rajesh B . Synthesis and biological activity of novel pyrimidinone containing thiazolidinedione derivatives. Bioorg Med Chem. 2002; 10(8):2671-80. DOI: 10.1016/s0968-0896(02)00107-4. View