合成和生物评估新型aminoguanidine衍生物作为潜在的抗菌剂
Xueqian Bai1, Jinghan Wang1, Feitong Jiao1
1Jilin Medical University, Jilin, Jilin Province, 132013, People's Republic of China.
Scientific reports
|November 6, 2024
概括
具有1,2,4-triazol部分的新型aminoguanidine衍生物显示出强大的抗菌活性. 化合物5f有效地向具有低毒性的细菌,包括耐药菌株,为新的杀菌剂提供了有希望的支架.
科学领域:
- 药用化学 医学化学
- 微生物学 微生物学
- 药物发现 药物发现 药物发现
背景情况:
- 抗生素耐药性的增加需要开发新的抗菌剂.
- 氨基瓜尼丁衍生物和1,2,4-triazol部分因其潜在的生物活性而得到认可.
研究的目的:
- 为了合成和评估新型的aminoguanidine衍生物,包括1,2,4-triazol部分作为潜在的抗菌剂.
- 识别具有针对广泛细菌菌株和低毒性强效活性的化合物.
主要方法:
- 合成两系列含有1,2,4-三环的阿米诺瓜尼丁衍生物.
- 在体外对各种细菌菌株进行抗菌活性测试,包括多药耐药 (MDR) 病原体.
- 确定最小抑制度 (MIC) 和细胞毒性测定.
- 作用研究的机制包括膜透性和传输电子显微镜 (TEM).
主要成果:
- 所有合成的化合物都表现出显著的体外抗菌活性.
- 化合物5f对黄金葡萄球菌,大肠杆菌,表皮葡萄球菌,细菌菌和白菌有强烈的活性,MIC值在2-8μg/mL之间.
- 化合物5f对Hela细胞 (>100μM) 具有低毒性,并且有效透细菌膜,导致细胞死亡.
- 在使用5f化合物治疗后,TEM研究揭示了不规则的细菌细胞形态.
结论:
- 与1,2,4-triazol部分功能化的aminoguanidine衍生物代表了开发新的杀菌剂的有希望的化合物类别.
- 化合物5f是一种强大的抗菌候选物,具有良好的毒性概况和破坏膜的作用机制.
- 对这些支架的进一步调查可能会导致针对细菌感染的有效治疗,包括由MDR菌株引起的细菌感染.
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