作为潜在的抗菌剂的基基诺:合成和特性
Evgeniy S Izmest'ev1, Svetlana V Pestova1, Alena I Kolesnikova2
1Institute of Chemistry, FRC Komi Science Center Ural Branch of the Russian Academy of Sciences, 48, Pervomaiskaya St., 167000, Syktyvkar, Russian Federation.
ChemMedChem
|October 24, 2023
概括
研究人员合成了新型的烯 - 诺基诺结合物,发现结合物的存在和长度对于抗黄球菌的抗菌活性至关重要. 一些衍生品对抗抗甲素耐药菌株和具有低毒性的Candida albicans表现出强烈的活性.
科学领域:
- 药用化学 医学化学
- 抗微生物药物发现发现
- 有机合成 有机合成
背景情况:
- 诺基诺是面临耐药性的广谱抗生素.
- 烯是具有多种生物活动的天然化合物.
- 将药物与其他分子结合在一起可以提高疗效或改变性质.
研究的目的:
- 为了合成和表征新的烯-化诺类结合物.
- 评估这些结合物的抗微生物和抗真菌活性.
- 调查结构-活动关系和作用机制.
主要方法:
- 含有烯的西普罗夫洛克萨辛和诺夫洛克萨辛合物的化学合成.
- 苏微稀释试验用于确定针对S. aureus (MSSA,MRSA),P. aeruginosa和C. albicans的最小抑制度 (MIC).
- 用S. aureus DNA旋转酶对诺的分子对接研究.
- 使用牛初级肺细胞进行细胞毒性测定.
主要成果:
- 对黄金菌的抗菌活性取决于烯和诺基诺片段之间的连接器,随着长度的增加而减少.
- 齐普罗夫洛克萨衍生物与坎普霍林和2 - - 异-2--硫) 乙烯替代剂显示出对MSSA的高活性 (MIC分别为1和0.5μg/mL).
- 乙二二-硫) 乙烯基基普罗夫洛克萨辛衍生物对MRSA (MIC 8μg/mL) 具有显著的活性.
- 一种坎佛10-硫胺基普罗夫洛克萨衍生物对C. albicans表现出强大的抗真菌活性 (MIC 8μg/mL).
- 大多数活性化合物对牛肺细胞没有显著的毒性.
- 对接研究为观察到的抗菌活性提供了洞察力.
结论:
- 烯 - 诺基诺结合物代表了开发新抗菌剂的有希望的战略.
- 链接器的设计对于优化抗菌疗效至关重要.
- 这些新型化合物表现出广泛的活性和有利的安全概况,需要进一步调查.
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