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1,3,4-氧化基化合物的增强抗菌活性,这些化合物限制金黄色葡萄球菌 (Staphylococcus aureus) 独立于LtaS功能的生长

Edward J A Douglas¹, Brandon Marshall², Arwa Alghamadi²

¹Department of Life Sciences, University of Bath, Bath BA2 7AY, U.K.

ACS infectious diseases

|October 13, 2023

概括

化合物1771的新衍生物显示出对抗多药耐药细菌的增强抗菌活性. 这些化合物向脂铁醇酸 (LTA) 生物合成,为新型抗生素开发提供了有前途的途径.

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:

脂铁醇酸 (LTA) 生物合成途径是新型抗菌疗法的关键目标.
化合物1771是一种1,3,4氧沙,此前已被确定为有效对抗格拉姆阳性病原体的LTA抑制剂.

研究的目的:

为了合成和评估化合物1771的新衍生物,提高了抗菌活性.
研究这些化合物的作用机制并确定这些化合物的特定分子标.

主要方法:

六种1771衍生物的合成,包括添加五硫替代剂.
对抗多药耐药*金黄色葡萄球菌*菌株的抗菌素敏感性测试.
哺乳动物细胞毒性评估.
涉及删除和过度表达假定LTA合成酶 (LtaS) 基因的分子技术.
分子对接研究,分析与LtaS的化合物相互作用.

主要成果:

化合物13是一种新型衍生物,与化合物1771相比,其活性增加了16至32倍.
化合物13对哺乳动物细胞的毒性概况得到了改善.
无论是删除还是过度表达LtaS都没有影响菌株对1771或13化合物的敏感性.
过度表达LtaS增加了刚果红色的最小抑制度 (MIC),这是一个已知的LtaS抑制剂.
接姿势表明了LtaS以外的其他分子目标的潜力.
化合物1771和13在外部膜透后,独立于LtaS,对抗阴性细菌表现出抗菌活性.

结论:

五硫替代剂显著增强了1771衍生物的抗菌活性.
化合物1771和13的作用机制似乎独立于LtaS,这表明了替代或额外的点.
这些化合物代表了开发新抗生素的有希望的线索,这些抗生素有效地对抗多抗药性格兰正和潜在的格兰阴性病原体.

关键词:

一,三,四氧沙醇黄金葡萄球菌黄金葡萄球菌抗微生物耐药性抗微生物耐药性发现药物的发现.利波泰可酸抑制剂的使用

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