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Lyubov Vinogradova¹, Alexey Lukin¹, Kristina Komarova¹

¹Lomonosov Institute of Fine Chemical Technologies, MIREA-Russian Technological University, 119454 Moscow, Russia.

Molecules (Basel, Switzerland)

|July 27, 2024

概括

合成了13种新型的5- ((5-nitro-2-furyl) -1,2,4-oxadiazoles,并对其抗菌活性进行了测试. 几种化合物对ESKAPE细菌和Mycobacterium结核病有强烈的活性,其中一些比现有的抗生素更强.

科学领域:

药用化学医学化学
有机合成有机合成
抗微生物药物发现发现

背景情况:

抗生素耐药细菌的增加,包括ESKAPE病原体,需要开发新的抗菌剂.
尼托福兰衍生物在历史上表现出作为抗菌化合物的前景.
1,2,4-oxadiazole支架为设计新型生物活性分子提供了一个多功能平台.

研究的目的:

为了合成和描述一系列新的3-替代的5-(5-酸-2-) -1,2,4-氧化醇.
评估这些化合物的体外抗菌活性,与一组临床相关的细菌进行对比,包括ESKAPE病原体.
研究结构-活性关系,并确定具有强效抗微生物特性的化合物.

主要方法:

从阿米诺尼特里尔中合成13种新的3-替代的5-(5-尼特罗-2-利) -1,2,4-氧沙醇.
使用磁盘扩散方法进行抗菌查,并确定最小抑制度 (MIC).
诱导适应对接 (IFD) 建模用于预测潜在的生物目标.

主要成果:

所有合成的化合物都对ESKAPE细菌表现出抗菌活性,对5种物种观察到显著的抑制.
化合物2h和2e表现出强烈的活性,其中2h显示出较低的MIC比对比剂对抗金黄色葡萄球菌.
化合物2e对阳性ESKAPE病原体和Mycobacterium结核病菌表现出活性,突出显示了其广泛的潜力.

结论:

新型3替代的5-(5-二-) -1,2,4-氧沙醇是抗菌剂的一个有前途的类别.
氧沙环上的结构变化会影响抗菌效能和选择性.
对这些化合物的进一步研究可能会导致对抗细菌感染的新治疗策略的开发.

关键词:

一个逃跑者.在M.结核病.它具有抗菌选择性的抗菌性.亚降解酶 (azoreductase) 是一种灵活的对接灵活的对接化酸的含量是多少亚降解酶的使用方法紧张的联结体蛋白相互作用

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