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合成三氨酸附加的迪司皮罗利丁氧醇及其抗菌性评价

Sruthi Sudheendran Leena¹, Abdul Akhir², Deepanshi Saxena²

¹Department of Chemistry, University of Kerala Kariavattom Trivandrum-695581 India anideepthi@gmail.com.

RSC medicinal chemistry

|June 26, 2023

概括

研究人员合成了新型的三氨酸附加的迪斯皮罗利丁氧醇. 化合物5b表现出强大的抗菌活性对黄金葡萄球菌,包括耐药菌株.

科学领域:

药用化学医学化学
有机合成有机合成
抗菌研究抗菌研究

背景情况:

特里普坦林和奥克辛多尔支架以它们的生物活动而闻名.
开发新的抗菌剂对于对抗日益增长的抗菌素耐药性至关重要.
迪斯皮罗利丁氧辛醇是异环化合物的有前途的类别.

研究的目的:

为了合成新型的三氨酸附加的迪斯皮罗利丁氧醇.
评估这些合成化合物的体外抗菌活性.
为了识别强大的抗菌剂对抗具有挑战性的病原体.

主要方法:

通过 [3 + 2] 循环添加合成十六种三氨酸附加的迪斯皮罗利丁氧学.
使用三氨酸衍生的亚甲化物和异化物作为关键反应剂.
在体外对ESKAPE病原体和耐药菌株 (MRSA/VRSA) 的抗菌评估.

主要成果:

成功合成了16种目标化合物.
鉴定替代的dsipyrrolidine oxindole 5b作为一种高强度的抗菌剂.
化合物5b的最低抑制度 (MIC) 低,为0.125μg mL−1对黄金葡萄球菌 (Staphylococcus aureus) ATCC 29213.3.
化合物5b表现出良好的选择性指数.

结论:

合成的三丁林附加的迪西罗皮罗利丁氧醇是有效的抗菌剂.
化合物5b是一种有前途的分子,用于进一步开发对抗金黄色葡萄球菌感染.
这项研究为抗击细菌感染提供了具有重大潜力的新型异环化合物.

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