Coumarin-containing hybrids and their antibacterial activities,Archiv der Pharmazie

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Coumarin-containing hybrids and their antibacterial activities
Archiv der Pharmazie ( IF 4.3 ) Pub Date : 2020-04-06 , DOI: 10.1002/ardp.201900380
Dongxu Feng ₁ , Aihua Zhang ₂ , Yuan Yang _{2,

3} , Peng Yang ₃

Affiliation

Infections caused by Gram‐positive and ‐negative bacteria are one of the foremost causes of morbidity and mortality globally. Antibiotics are the mainstay of therapy for bacterial infections, but the emergence and wide spread of drug‐resistant pathogens have already become a huge issue for public healthcare systems. The coumarin moiety, which is ubiquitous in nature, could bind to the B subunit of DNA gyrase in bacteria and inhibit DNA supercoiling by blocking the ATPase activity; hence, coumarin derivatives possess potential antibacterial activity. Several coumarin‐containing hybrids such as coumermycin A1, clorobiocin, and novobiocin have already been used in clinical practice for the treatment of various bacterial infections; thus, it is conceivable that hybridization of the coumarin moiety with other antibacterial pharmacophores may provide opportunities for the development of novel antibiotics. This review outlines the advances in coumarin‐containing hybrids with antibacterial potential in the recent 5 years and the structure–activity relationships are also discussed.

中文翻译：

含香豆素的杂化物及其抗菌活性

由革兰氏阳性和阴性细菌引起的感染是全球发病率和死亡率的首要原因之一。抗生素是治疗细菌感染的中流砥柱，但耐药病原体的出现和广泛传播已经成为公共医疗系统面临的一个巨大问题。自然界中普遍存在的香豆素部分可以与细菌中DNA促旋酶的B亚基结合，通过阻断ATP酶活性来抑制DNA超螺旋；因此，香豆素衍生物具有潜在的抗菌活性。几种含有香豆素的混合物，如香豆霉素 A1、氯霉素和新生霉素，已经在临床实践中用于治疗各种细菌感染；因此，可以想象，香豆素部分与其他抗菌药效团的杂交可能为开发新型抗生素提供机会。本综述概述了近 5 年来具有抗菌潜力的含香豆素杂化物的进展，并讨论了构效关系。

更新日期：2020-04-06

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