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香豆素杂合衍生物作为有前途的抗结核治疗先导物:为展现抗结核活性进行结构设计的最新进展和关键方面。

Coumarin hybrid derivatives as promising leads to treat tuberculosis: Recent developments and critical aspects of structural design to exhibit anti-tubercular activity.

机构信息

Centre for Nano and Material Sciences, Jain University, Jain Global Campus, Jakkasandra Post, Bangalore, 562112, India.

Centre for Nano and Material Sciences, Jain University, Jain Global Campus, Jakkasandra Post, Bangalore, 562112, India.

出版信息

Tuberculosis (Edinb). 2021 Mar;127:102050. doi: 10.1016/j.tube.2020.102050. Epub 2021 Jan 6.

DOI:10.1016/j.tube.2020.102050
PMID:33540334
Abstract

Tuberculosis (TB) is a highly contagious airborne disease with nearly 25% of the world's population infected with it. Challenges such as multi drug resistant TB (MDR-TB), extensive drug resistant TB (XDR-TB) and in rare cases totally drug resistant TB (TDR-TB) emphasizes the critical and urgent need in developing novel TB drugs. Moreover, the prolonged and multi drug treatment regime suffers a major drawback due to high toxicity and vulnerability in TB patients. This calls for intensified research efforts in identifying novel molecular scaffolds which can combat these issues with minimal side effects. In this pursuit, researchers have screened many bio-active molecules among which coumarin have been identified as promising candidates for TB drug discovery and development. Coumarins are naturally occurring compounds known for their low toxicity and varied biological activity. The biological spectrum of coumarin has intrigued medicinal researchers to investigate coumarin scaffolds for their relevance as anti-TB drugs. In this review we focus on the recent developments of coumarin and its critical aspects of structural design required to exhibit anti-tubercular (anti-TB) activity. The information provided will help medicinal chemists to design and identify newer molecular analogs for TB treatment and also broadens the scope of exploring future generation potent yet safer coumarin based anti-TB agents.

摘要

结核病(TB)是一种高度传染性的空气传播疾病,全球近 25%的人口感染了这种疾病。耐多药结核病(MDR-TB)、广泛耐药结核病(XDR-TB)和在极少数情况下完全耐药结核病(TDR-TB)等挑战强调了开发新型结核病药物的关键和紧迫需求。此外,由于结核病患者的毒性和脆弱性较高,延长和多药物治疗方案存在主要缺点。这需要加强研究工作,以确定新型分子支架,这些支架可以在最小的副作用下对抗这些问题。在这方面的追求中,研究人员已经筛选了许多生物活性分子,其中香豆素已被确定为结核病药物发现和开发的有前途的候选药物。香豆素是天然存在的化合物,以低毒性和多种生物活性而闻名。香豆素的生物学范围引起了药用研究人员的兴趣,他们研究了香豆素支架作为抗结核病药物的相关性。在这篇综述中,我们重点介绍了香豆素的最新发展,以及为了表现出抗结核(抗 TB)活性而需要的结构设计的关键方面。提供的信息将有助于药物化学家设计和识别治疗结核病的新型分子类似物,并拓宽了探索下一代更有效但更安全的基于香豆素的抗结核病药物的范围。

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