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Xanthone: A Promising Antimycobacterial Scaffold
Medicinal Chemistry ( IF 2.3 ) Pub Date : 2021-05-01 , DOI: 10.2174/1573406416666200619114124
Tilal Elsaman 1 , Malik Suliman Mohamed 2 , Eyman Mohamed Eltayib 2 , Abualgasim Elgaili Abdalla 3 , Magdi Awadalla Mohamed 1
Affiliation  

Background: Tuberculosis (TB) is one of the infectious diseases associated with high rate of morbidity and mortality and still remains one of the top-ten leading causes of human death in the world. The development of new anti-TB drugs is mandatory due to the existence of latent infection as well as the expansion of the resistant Mycobacterium tuberculosis (MBT) strains. Xanthones encompass a wide range of structurally diverse bioactive compounds, obtained either naturally or through chemical synthesis. There is a growing body of literature that recognizes the antitubercular activity of xanthone derivatives.

Objective: The objective of this review is to highlight the main natural sources along with the critical design elements, structure-activity relationships (SARs), modes of action and pharmacokinetic profiles of xanthone-based anti-TB compounds.

Methods: In the present review, the anti-TB activity of xanthones reported in the literature from 1972 to date is presented and discussed.

Results: Exploration of xanthone scaffold led to the identification of several members of this class having superior activity against both sensitive and resistant MBT strains with distinctive mycobacterial membrane disrupting properties. However, studies regarding their modes of action, pharmacokinetic properties and safety are limited.

Conclusion: Comprehendible data and information are afforded by this review and it would certainly provide scientists with new thoughts and means which will be conducive to design and develop new drugs with excellent anti-TB activity through exploration of xanthone scaffold.



中文翻译:

黄嘌呤:有希望的抗分枝杆菌支架

背景:结核病(TB)是与高发病率和高死亡率相关的传染病之一,并且仍然是世界上导致人类死亡的十大主要原因之一。由于存在潜在感染以及耐药结核分枝杆菌(MBT)菌株的扩大,必须开发新的抗结核药物。Xanthones涵盖了多种结构多样的生物活性化合物,可以通过自然或化学合成获得。越来越多的文献认识到x吨酮衍生物的抗结核活性。

目的:本综述的目的是强调主要的天然来源以及基于黄酮的抗结核化合物的关键设计要素,结构-活性关系(SAR),作用方式和药代动力学特征。

方法:在本综述中,介绍并讨论了1972年至今文献中报道的氧杂蒽酮的抗TB活性。

结果:x吨酮支架的探索导致鉴定出具有抗分枝杆菌膜破坏特性的敏感和耐药MBT菌株均具有优异活性的几类成员。然而,关于它们的作用方式,药代动力学性质和安全性的研究是有限的。

结论:本综述提供了全面的数据和信息,必将为科学家提供新的思想和手段,这将有助于通过探索黄酮骨架来设计和开发具有优异抗结核活性的新药物。

更新日期:2021-04-13
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