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Fusaric acid and derivatives as novel antimicrobial agents
Medicinal Chemistry Research ( IF 2.6 ) Pub Date : 2020-07-05 , DOI: 10.1007/s00044-020-02596-3
Tung Truong Thanh , Thang Nguyen Quoc , Huy Luong Xuan

The synthesis and screening of several fusaric acid (FA) and analogues against five common clinical pathogens (gram-positive and gram-negative) and in vitro hemolytic activity assay in human red blood cells, for the first time, were reported. The biological results reveal that FA and its analogues exhibited moderate antimicrobial activities. Compounds 25 and 7 showed growth inhibitory activity in gram-positive bacteria. Compounds 6 and 9 showed growth inhibitory activity in both gram-positive and gram-negative bacteria. None of the compounds induce hemolysis, which is potent for future drug development on this template. In addition, the structure–activity relationship and docking studies are discussed.

中文翻译:

富马酸及其衍生物作为新型抗菌剂

首次报道了针对五种常见临床病原体(革兰氏阳性和革兰氏阴性)的几种富斯酸(FA)及其类似物的合成和筛选,以及人类红细胞中的体外溶血活性测定。生物学结果表明,FA及其类似物表现出中等的抗菌活性。化合物257在革兰氏阳性细菌中显示出生长抑制活性。化合物69在革兰氏阳性和革兰氏阴性细菌中均显示出生长抑制活性。这些化合物均不诱导溶血,这对于此模板上的未来药物开发很有效。此外,还讨论了结构-活性关系和对接研究。
更新日期:2020-07-05
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