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氨基甘油酸的结合物与 Stapled 作为一种向抗生素耐药细菌的方法

Julia Macyszyn¹, Michał Burmistrz¹, Adam Mieczkowski²

¹Centre of New Technologies, University of Warsaw, Banacha 2c, 02-097 Warsaw, Poland.

|June 5, 2023

概括

结合氨基糖化物 (AMG) 和的新混合抗微生物药物显示出对抗多药耐药细菌的增强活性. 这些新型结合物提供了一种有前途的策略来对抗耐药细菌菌株,具有低毒性.

科学领域:

微生物学微生物学
药用化学医学化学
药物发现药物发现药物发现

背景情况:

抗生素耐药性是一个日益增长的全球健康威胁,由滥用和过度使用现有的药物,如氨基糖化物 (AMG) 驱动.
迫切需要新型抗菌剂,有效对抗多药耐药 (MDR) 细菌菌株.
现有的AMG抗生素由于获得的细菌耐药性而面临限制.

研究的目的:

通过将氨基甘油酸与抗微生物结合,开发新的混合抗微生物化合物.
评估这些杂交物对抗耐药细菌菌株的疗效.
评估合成化合物的安全性,特别是溶血活性.

主要方法:

用点击化学 (triazole链接器) 和二硫化物桥梁形成 (细胞质裂变) 将2-deoxystreptamine aminoglycosides (neomycin 和 amikacin) 与阿诺林及其衍生物结合在一起.
通过二硫化物桥梁合成阿诺林衍生物的同位二次体.
对包括耐药菌株在内的格拉姆阳性和格拉姆阴性细菌的抗菌和杀菌活性的评估.
使用绵羊红血红细胞评估溶血活性.

主要成果:

与单个成分或简单组合相比,合成的AMG杂交体显示出显著增强的抗菌和杀菌活性.
这些化合物特别有效地对抗了耐尼奥米或阿米卡的细菌菌株.
新型合物和二硫化二元体表现出低血解活性,这表明安全性概况有利.

结论:

氨基甘油酸与抗菌的混合化是克服细菌耐药性的可行策略.
开发的AMG-联体和二聚体代表了开发针对MDR细菌的新疗法的有希望的候选人.
低血溶性活性表明临床应用的潜力.

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