Pradhan Tathagata, Gupta Ojasvi, Kumar Vivek, Chawla Gita
Department of Pharmaceutical Chemistry, School of Pharmaceutical Education and Research, Jamia Hamdard University, New Delhi, India.
Arch Pharm (Weinheim). 2023 Feb;356(2):e2200452. doi: 10.1002/ardp.202200452. Epub 2022 Nov 15.
The thiazolidine-4-one scaffold has recently emerged as a potential pharmacophore having clinical significance for medicinal chemists. This heterocyclic ring has been reported to possess a plethora of biological activities, including antidiabetic activity that has inspired researchers to integrate this core with different pharmacophoric fragments to design novel and effective antidiabetic leads. The antidiabetic activity has been observed due to the ability of the thiazolidine-4-one nucleus to interact with different biological targets, including peroxisome proliferator-activated receptor γ, protein tyrosine phosphatase 1B, aldose reductase, α-glucosidase, and α-amylase. The present review discusses the mode of action of thiazolidine-4-ones through these antidiabetic drug targets. This review attempts to summarize and analyze the recent developments with regard to the antidiabetic potential of thiazolidine-4-ones covering different synthetic strategies, structure-activity relationships, and docking studies reported in the literature. The significance of various structural modifications at C-2, N-3, and C-5 of the thiazolidine-4-one ring has also been discussed in this manuscript. This comprehensive compilation will provide an inevitable scope for the design and development of potential antidiabetic drug candidates having a thiazolidine-4-one core.
噻唑烷-4-酮骨架最近已成为一种对药物化学家具有临床意义的潜在药效基团。据报道，这个杂环具有大量生物活性，包括抗糖尿病活性，这激发了研究人员将这个核心与不同的药效基团片段整合，以设计新型有效的抗糖尿病先导化合物。由于噻唑烷-4-酮核能够与不同的生物靶点相互作用，包括过氧化物酶体增殖物激活受体γ、蛋白酪氨酸磷酸酶1B、醛糖还原酶、α-葡萄糖苷酶和α-淀粉酶，因此观察到了抗糖尿病活性。本综述讨论了噻唑烷-4-酮通过这些抗糖尿病药物靶点的作用模式。这篇综述试图总结和分析关于噻唑烷-4-酮抗糖尿病潜力的最新进展，涵盖文献中报道的不同合成策略、构效关系和对接研究。本文还讨论了噻唑烷-4-酮环在C-2、N-3和C-5处各种结构修饰的意义。这种全面的汇编将为设计和开发具有噻唑烷-4-酮核心的潜在抗糖尿病候选药物提供必然的空间。
