合成和分子对接研究一些新的醇-氨酸分子杂交物作为抗菌剂
Jehan Y Al-Humaidi1, Sobhi M Gomha2, Fathy M Abdelrazek3
1Department of Chemistry, College of Science, Princess Nourah bint Abdulrahman University, P.O .BOX 84428, Riyadh 11671, Saudi Arabia.
Current organic synthesis
|August 11, 2023
概括
合成了新型的醇-氨酸杂交物,并对其抗菌活性进行了评估. 一些衍生品显示出对格拉姆阳性和格拉姆阴性细菌的显著有效性,提供了潜在的新抗菌剂.
科学领域:
- 药用化学 医学化学
- 有机合成 有机合成
- 发现抗微生物药物 发现抗微生物药物
背景情况:
- 耐药细菌和多抗药性疾病对全球健康构成重大挑战.
- 二醇和二醇的支架已经证明了抗菌性质.
研究的目的:
- 合成新型的提亚衍生物,其中包含氨酸部分.
- 评估合成的化合物作为潜在的抗菌剂.
- 通过分子对抗DNA旋转酶B的对接来研究它们的作用机制.
主要方法:
- 通过凝结反应合成 thiazole-coumarin 混合物.
- 中间体与替代的化和化的反应.
- 在体外抗菌活性测定.
- 分子对接研究针对DNA旋转酶B.
主要成果:
- 几种合成的化合物,包括10b,7和6b,表现出明显的抗菌活性,对抗阳性和阴性细菌.
- 化合物10b,7和6b对目标DNA旋转酶B的结合亲和力最强.
结论:
- 成功合成了一系列具有多种抗菌活性的新型 thiazole 衍生物.
- 合成方法是环保的,使用易于获得的原材料,避免危险的催化剂.
- 这些发现表明,这些化合物具有作为新抗菌剂的有前途潜力.
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