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作为潜在的抗菌剂的皮拉和异醇衍生物的探索小说:设计,合成,结构活动关系研究和抗生物膜活动与分子对接模拟

Khadija E Saadon¹, Ahmed Ragab^2,3, Nadia M H Taha¹

¹Department of Chemistry, Faculty of Science (Girls), Al-Azhar University, Nasr City, Cairo, Egypt.

Drug development research

|November 17, 2025

概括

合成了新的pyrazole和isoxazole衍生物,并对细菌和真菌进行了测试. 几种化合物显示出显著的抗微生物活性,其中一些抑制生物膜形成,并显示出新抗生素开发的有前途性质.

科学领域:

药用化学医学化学
有机合成有机合成
微生物学微生物学

背景情况:

抗微生物药物耐药性是一个日益增长的全球健康威胁.
迫切需要新的抗微生物药物来对抗耐药性微生物感染.

研究的目的:

合成和表征新型皮拉和异醇衍生物.
评估这些衍生品的抗微生物和抗菌膜活性.
探索它们作为新型抗生素的潜在潜力.

主要方法:

皮拉和异醇衍生物的多组分反应合成.
使用FT-IR,NMR,质谱和元素分析进行表征.
针对细菌和真菌菌株的抗微生物敏感性测试 (MIC,MBC,MFC).
生物膜抑制测定.生物膜抑制测定.
分子对接模拟和in-silico药理动力学/毒性预测.

主要成果:

成功合成了一系列新的pyrazole和isoxazole衍生物.
显示出针对格拉姆阳性和格拉姆阴性细菌以及Candida albicans的显著抗菌活性.
14,17,20和24的化合物表现出强烈的活性,MIC值较低.
衍生品14显示出优异的生物膜抑制活性 (96.17%).
接研究表明与LasR的潜在相互作用,而in-silico分析表明了有利的药理动力学和安全性.

结论:

合成的pyrazole和isoxazole衍生物具有显著的抗微生物和抗菌膜特性.
衍生物14是作为新型抗生素进一步开发的有希望的候选者.
这些化合物代表了发现新抗菌剂的宝贵支架.

关键词:

抗微生物活性的抗微生物活性.细菌生物膜的活动.乙基瓦尼林是什么?乙基瓦尼林是什么?在中进行的ADMET研究.皮拉和伊索克萨的使用情况

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