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Coumarin hybrid derivatives as promising leads to treat tuberculosis: Recent developments and critical aspects of structural design to exhibit anti-tubercular activity
Tuberculosis ( IF 2.8 ) Pub Date : 2021-01-06 , DOI: 10.1016/j.tube.2020.102050
Dinesh S Reddy 1 , Manasa Kongot 1 , Amit Kumar 1
Affiliation  

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.



中文翻译:

香豆素杂化衍生物有望治疗肺结核:结构设计的最新发展和关键方面表现出抗肺结核活性

结核病 (TB) 是一种高度传染性的空气传播疾病,世界上近 25% 的人口感染了它。多重耐药结核病 (MDR-TB)、广泛耐药结核病 (XDR-TB) 和极少数情况下的完全耐药结核病 (TDR-TB) 等挑战强调了开发新型结核病药物的迫切需求。此外,由于结核病患者的高毒性和易感性,长期和多药物治疗方案遭受主要缺点。这需要加大研究力度,以确定可以以最小的副作用解决这些问题的新型分子支架。在这一追求中,研究人员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希望的候选者。香豆素是天然存在的化合物,以其低毒性和多样的生物活性而闻名。香豆素的生物谱引起了医学研究人员对香豆素支架作为抗结核药物的相关性的研究。在这篇综述中,我们关注香豆素的最新发展及其表现出抗结核 (anti-TB) 活性所需的结构设计的关键方面。所提供的信息将帮助药物化学家设计和鉴定用于结核病治疗的更新分子类似物,并拓宽探索下一代有效但更安全的基于香豆素的抗结核病药物的范围。在这篇综述中,我们关注香豆素的最新发展及其表现出抗结核 (anti-TB) 活性所需的结构设计的关键方面。所提供的信息将帮助药物化学家设计和鉴定用于结核病治疗的更新分子类似物,并拓宽探索下一代有效但更安全的基于香豆素的抗结核病药物的范围。在这篇综述中,我们关注香豆素的最新发展及其表现出抗结核 (anti-TB) 活性所需的结构设计的关键方面。所提供的信息将帮助药物化学家设计和鉴定用于结核病治疗的更新分子类似物,并拓宽探索下一代有效但更安全的基于香豆素的抗结核病药物的范围。

更新日期:2021-02-02
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