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噻唑烷二酮-2,4-二酮的医学前景综述:治疗2型糖尿病的卓越骨架

An overview on medicinal perspective of thiazolidine-2,4-dione: A remarkable scaffold in the treatment of type 2 diabetes.

作者信息

Bansal Garima, Thanikachalam Punniyakoti Veeraveedu, Maurya Rahul K, Chawla Pooja, Ramamurthy Srinivasan

机构信息

Department of Pharmaceutical Chemistry, ISF College of Pharmacy, Ghal Kalan, Moga, Punjab 142001, India.

GRT Institute of Pharmaceutical Education and Research, GRT Mahalakshmi Nagar, Tiruttani, India.

出版信息

J Adv Res. 2020 Jan 22;23:163-205. doi: 10.1016/j.jare.2020.01.008. eCollection 2020 May.

Abstract

Diabetes or diabetes mellitus is a complex or polygenic disorder, which is characterized by increased levels of glucose (hyperglycemia) and deficiency in insulin secretion or resistance to insulin over an elongated period in the liver and peripheral tissues. Thiazolidine-2,4-dione (TZD) is a privileged scaffold and an outstanding heterocyclic moiety in the field of drug discovery, which provides various opportunities in exploring this moiety as an antidiabetic agent. In the past few years, various novel synthetic approaches had been undertaken to synthesize different derivatives to explore them as more potent antidiabetic agents with devoid of side effects (i.e., edema, weight gain, and bladder cancer) of clinically used TZD (pioglitazone and rosiglitazone). In this review, an effort has been made to summarize the up to date research work of various synthetic strategies for TZD derivatives as well as their biological significance and clinical studies of TZDs in combination with other category as antidiabetic agents. This review also highlights the structure-activity relationships and the molecular docking studies to convey the interaction of various synthesized novel derivatives with its receptor site.

摘要

糖尿病或糖尿病 mellitus 是一种复杂的或多基因疾病,其特征是葡萄糖水平升高(高血糖症),且在较长时间内肝脏和外周组织中胰岛素分泌不足或对胰岛素产生抵抗。噻唑烷 -2,4- 二酮(TZD)是药物发现领域中一种具有优势的骨架和出色的杂环部分,这为将该部分开发为抗糖尿病药物提供了各种机会。在过去几年中,人们采用了各种新颖的合成方法来合成不同的衍生物,以探索它们作为更有效的抗糖尿病药物,同时避免临床使用的 TZD(吡格列酮和罗格列酮)的副作用(即水肿、体重增加和膀胱癌)。在本综述中,我们努力总结了 TZD 衍生物各种合成策略的最新研究工作,以及它们作为抗糖尿病药物与其他类别联合使用时的生物学意义和临床研究。本综述还强调了构效关系和分子对接研究,以阐述各种合成的新型衍生物与其受体位点的相互作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/071b/7052407/dbc0af6864c8/ga1.jpg

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