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2,4-噻唑烷二酮衍生物的药用视角:近期进展洞察

Medicinal Perspective of 2,4-Thiazolidinediones Derivatives: An Insight into Recent Advancements.

机构信息

School of Pharmaceutical Sciences, Lovely Professional University, Jalandhar-Delhi G.T. Road, Phagwara, Punjab, 144411, India.

School of bioengineering and biosciences, Lovely Professional University, Jalandhar-Delhi G.T. Road, Phagwara, Punjab, 144411, India.

出版信息

ChemistryOpen. 2024 Nov;13(11):e202400147. doi: 10.1002/open.202400147. Epub 2024 Sep 9.

Abstract

2,4-Thiazolidinedione derivatives represent nitrogen-containing heterocyclic compounds utilized in type 2 diabetes mellitus management. Recent advances in medicinal chemistry have unveiled diverse therapeutic potentials and structural modifications of these derivatives. This review delves into novel TZD derivatives, encompassing their synthesis, structure-activity relationships, and pharmacokinetic profiles. Various therapeutic potentials of TZDs are explored, including anticancer, antimicrobial, anti-inflammatory, antioxidant, anticonvulsant, antihyperlipidemic, anticorrosive, and antitubercular activities. Additionally, it addresses mitigating side effects associated with marketed TZD derivatives such as weight gain, oedema, fractures, and congestive heart failure in type 2 diabetes mellitus management. The review elaborates on in vivo, in vitro, and ex vivo studies supporting different biological activities, alongside predicting ADME and drug-likeness properties of TZDs. Computational studies are also integrated to elucidate binding modes and affinities of novel TZD derivatives. Furthermore, a plethora of novel TZD derivatives with varied and enhanced therapeutic potentials are presented, warranting further evaluation of their biological activities.

摘要

2,4-噻唑烷二酮衍生物是一类含氮杂环化合物,在 2 型糖尿病的治疗中得到了广泛应用。近年来,医学化学领域的研究进展揭示了这些衍生物在治疗多种疾病方面的巨大潜力和结构修饰的多样性。本综述深入探讨了新型 TZD 衍生物的研究进展,包括它们的合成、构效关系以及药代动力学特征。此外,还探讨了 TZDs 在抗癌、抗菌、抗炎、抗氧化、抗惊厥、降血脂、抗腐蚀和抗结核等方面的治疗潜力。同时,还讨论了如何减轻 TZD 衍生物在 2 型糖尿病治疗中引发的体重增加、水肿、骨折和充血性心力衰竭等副作用。本文详细阐述了支持不同生物活性的体内、体外和离体研究,并对 TZDs 的 ADME 和类药性进行了预测。还整合了计算研究以阐明新型 TZD 衍生物的结合模式和亲和力。最后,提出了大量具有不同和增强的治疗潜力的新型 TZD 衍生物,值得进一步评估它们的生物活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05ec/11564877/2551b00c1878/OPEN-13-e202400147-g012.jpg

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