噻唑烷二酮作为 PPAR-γ 激动剂的吉祥支架:对抗胰岛素抵抗性糖尿病的可能机制

Sourav Basak , Anjali Murmu , Balaji Wamanrao Matore , Partha Pratim Roy , Jagadish Singh
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引用次数: 0

摘要

噻唑烷二酮(TZD)在激活 PPAR-γ 受体方面起着至关重要的作用,PPAR-γ 受体通过与 DNA 结合,与视黄醇受体形成复合物,有助于抑制胰岛素抵抗性糖尿病。TZD 衍生物是含硫和氮的杂环化合物,因其具有大量药理活性而在合成化学领域产生了巨大影响。TZD 有助于改善 II 型糖尿病患者的胰岛素抵抗,并通过氧化碳水化合物降低血糖水平。TZD 支架是一种五环含硫化合物,带有两个羰基和一个α-氢,为这种生物活性分子的结构改造提供了巨大的可能性,其中 N-3 & C-5 位置是 TZD 核结构改造的最多用途位置。在这篇综述中,我们重点简要介绍了 TZD 的抗糖尿病活性、作用机理、结构活性关系以及主要药源 TZD 的各种合成方法,希望这将有助于为未来的研究人员提供有关该分子的知识。
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Thiazolidinedione an auspicious scaffold as PPAR-γ agonist: its possible mechanism to Manoeuvre against insulin resistant diabetes mellitus

Thiazolidinedione (TZD) plays a crucial role in activating PPAR-γ receptor, which helps to inhibit insulin-resistant diabetes mellitus through binding with DNA by forming a complex with retinoid receptors. TZD derivatives are the sulphur and nitrogen containing heterocyclic compounds that have a massive impact in synthetic chemistry for their plethora of pharmacological activities. TZD helps to improve insulin resistance and lowering the blood glucose level through oxidation of carbohydrate in case of type II diabetes mellitus. TZD scaffold is a pentacyclic sulphur-containing compound with two carbonyl groups and an alpha hydrogen offering a huge possibility in structural modification of this biologically active molecule, here N-3 & C-5 positions are the most versatile site for structural modification in TZD nucleus. In this review, we focus on a brief description of its antidiabetic activity with its mechanism of action, structure activity relationship and various synthetic approach of the main pharmacophore TZD and hope it will help to develop idea about this moiety for future researchers.

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