School of Chemistry and Life Science, Anshan Normal University, Liaoning, Anshan, PR China.
Eur J Med Chem. 2019 Feb 15;164:678-688. doi: 10.1016/j.ejmech.2018.12.017. Epub 2018 Dec 9.
Bacterial infections are account for the majority of hospital-acquired and community-acquired infections. The emergency and widespread of drug-resistant pathogens has further worsened the situation. In recent years, various isatin derivatives have been screened for their anti-bacterial activities, and some of them demonstrated promising in vitro and in vivo potency. This review covers the recent advances of isatin derivatives including isatin-azole, isatin-quinoline/quinolone, isatin-furan/coumarin, isatin-hydrazone/(thio)semicarbazone, isatin dimers and isatin-indole hybrids as potential anti-bacterial agents. The enriched structure-activity relationship may pave the way for further rational development of isatin derivatives with broader spectrum, higher potency, lower toxicity and multiple mechanisms of action.
细菌感染是医院获得性和社区获得性感染的主要原因。耐药病原体的紧急和广泛出现使情况进一步恶化。近年来,各种靛红衍生物已被筛选出具有抗细菌活性,其中一些在体外和体内表现出有希望的活性。本综述涵盖了靛红衍生物的最新进展,包括靛红-唑、靛红-喹啉/喹诺酮、靛红-呋喃/香豆素、靛红-腙/(硫代)半卡巴腙、靛红二聚体和靛红-吲哚杂合作为潜在的抗菌剂。丰富的构效关系可能为进一步合理开发具有更广泛的谱、更高的效力、更低的毒性和多种作用机制的靛红衍生物铺平道路。