微生物衍生具有抗菌素潜在的抗菌素
Pengchao Zhao1, Pu Hou1, Zhishen Zhang1
1College of Medical Technology and Engineering, Henan University of Science and Technology, Luoyang, 471023, China.
European journal of medicinal chemistry
|July 24, 2024
概括
新型抗结核,包括RiPP和NRP,对抗耐药结核菌株表现出广泛的活性. 化学修饰可以提高它们的效力,为这种主要传染病提供有前途的新治疗途径.
科学领域:
- 微生物学 微生物学
- 药理学 药理学是指药理学的学科.
- 自然产品 化学 化学
背景情况:
- 结核病 (TB) 是全球主要的死亡原因,由多药耐药菌株加剧.
- 迫切需要发现新的抗结核病药物来对抗耐药性Mycobacterium结核病.
- 微生物衍生,特别是RiPPs和NRPs,正在成为有前途的抗菌菌剂.
研究的目的:
- 审查具有抗菌菌活性的天然核糖体合成和翻译后修饰 (RiPPs) 和非核糖体 (NRPs).
- 为了确定治疗耐药结核病的有前途的候选人.
- 探索结构-活性关系,以优化抗结核病的疗效.
主要方法:
- 关于微生物衍生的抗菌素的综合文献综述.
- 对非耐药和耐药菌根菌的体外活性光谱的分析.
- 确定96个RiPP和NRP家族的细胞内点和化学修饰策略.
主要成果:
- 96个天然的RiPP和NRP家族在体外表现出广泛的抗各种真菌菌的活性.
- 确定了22种抗菌素的细胞内标.
- 38个家族的化学修饰显示出改善抗结核病特性的潜力.
结论:
- 微生物RiPP和NRP是开发新型抗结核病药物的宝贵资源.
- 结构-活性关系研究强调了提高抗耐药结核病效的关键修改.
- 对这些和它们的标进行进一步的研究可能会导致结核病的有效新疗法.
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