Shandong Key Laboratory of Biophysics, Institute of Biophysics, Dezhou University, Dezhou, Shandong, China.
School of Life Sciences, Dezhou University, Dezhou, Shandong, China.
Arch Pharm (Weinheim). 2020 Oct;353(10):e2000143. doi: 10.1002/ardp.202000143. Epub 2020 Jul 15.
The emergence and worldwide spread of drug-resistant bacteria have already posed a serious threat to human life, creating the urgent need to develop potent and novel antibacterial drug candidates with high efficacy. Indole and isatin (indole-2,3-dione) present a wide structural and mechanistic diversity, so their derivatives possess various pharmacological properties and occupy a salient place in the development of new drugs. Indole/isatin-containing hybrids, which demonstrate a promising activity against a panel of clinically important Gram-positive and Gram-negative bacteria, are privileged scaffolds for the discovery of novel antibacterial candidates. This review, covering articles published between January 2015 and May 2020, focuses on the development and structure-activity relationship (SAR) of indole/isatin-containing hybrids with potential application for fighting bacterial infections, to facilitate further rational design of novel drug candidates.
耐药菌的出现和全球传播已经对人类生命构成了严重威胁,因此迫切需要开发高效、新型的抗菌药物候选物。吲哚和色酮(吲哚-2,3-二酮)具有广泛的结构和机制多样性,因此它们的衍生物具有多种药理学特性,在新药开发中占有重要地位。含有吲哚/色酮的杂合体对一组临床重要的革兰氏阳性和革兰氏阴性菌表现出有希望的活性,是发现新型抗菌候选物的优势骨架。本文综述了 2015 年 1 月至 2020 年 5 月期间发表的文章,重点介绍了具有潜在应用价值的含吲哚/色酮杂合体的开发和构效关系(SAR),以促进新型候选药物的合理设计。
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