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含4-哌啶酮化合物作为姜黄素模拟物的合成及生物性质

Synthesis and bio-properties of 4-piperidone containing compounds as curcumin mimics.

作者信息

Girgis Adel S, D'Arcy Padraig, Aboshouk Dalia R, Bekheit Mohamed S

机构信息

Department of Pesticide Chemistry, National Research Centre Dokki Giza 12622 Egypt

Department of Biomedical and Clinical Sciences, Linköping University SE-581 83 Linköping Sweden.

出版信息

RSC Adv. 2022 Oct 31;12(48):31102-31123. doi: 10.1039/d2ra05518j. eCollection 2022 Oct 27.

Abstract

The broad spectrum of curcumin's beneficial properties has encouraged medicinal researchers to investigate its therapeutic efficacy against diverse diseases. The clinical potential of curcumin is, however limited due to its poor pharmacodynamic/pharmacokinetic properties (such as low solubility, pH instability, poor absorption in circulation, rapid elimination from the body and photochemical degradation). 3,5-Bis(ylidene)-4-piperidone scaffolds are considered a curcumin mimic that exhibit diverse bio-properties. The current review provides a brief overview of these mimics and highlights biological activities relevant to drug development.

摘要

姜黄素广泛的有益特性促使医学研究人员研究其对多种疾病的治疗效果。然而,由于姜黄素较差的药效学/药代动力学特性(如低溶解度、pH值不稳定性、循环中吸收不良、体内快速消除和光化学降解),其临床应用潜力有限。3,5-双(亚甲基)-4-哌啶酮支架被认为是一种具有多种生物特性的姜黄素类似物。本综述简要概述了这些类似物,并强调了与药物开发相关的生物活性。

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