作为潜在的抗微生物剂,新型的纳-硫酸盐结合物与酸化连接剂:设计,合成和分子对接模拟
Asmaa F Kassem1,2, Sherif S Ragab3, Mohamed A Omar2
1Department of Chemistry, College of Science and Humanities in Al-Kharj, Prince Sattam Bin Abdulaziz University Al-Kharj 11942 Saudi Arabia.
RSC advances
|January 14, 2025
概括
新的quinazolinone衍生物对细菌和真菌表现出强大的抗菌活性. 化合物5k有效地抑制生物膜的形成,并在药物开发中表现出有希望的物理化学特性.
科学领域:
- 药用化学 医学化学
- 微生物学 微生物学
- 分子生物学分子生物学
背景情况:
- 抗微生物耐药性需要开发新的治疗药物.
- 基纳佐利诺支架以其多样化的生物活动而闻名.
研究的目的:
- 为了合成和表征新型quinazolinone-alkanesulfonate衍生物.
- 评估这些化合物的抗微生物,抗菌膜和机械性质.
主要方法:
- 通过一种硫酸乙酸酸酸 (5a-r) 的合成.通过一种硫酸乙酸酸酸酸酸酸链接剂.
- 抗微生物敏感性测试 (MIC),抗菌膜测试,脂质过氧化测试,聚焦激光扫描显微镜 (CLSM) 和分子对接研究.
- 对格拉姆阳性细菌 (Bacillus subtilis,Staphylococcus aureus),格拉姆阴性细菌 (Pseudomonas aeruginosa,Klebsiella pneumonia,Salmonella Typhimurium) 和Candida albicans进行评估. 这种细菌可以与其他细菌相比较.
主要成果:
- 化合物5a-r表现出显著的杀菌和杀菌活性.
- 衍生品5g和5k对Candida albicans和Staphylococcus aureus具有显著的有效性.
- 化合物5k有效抑制生物膜形成 (63.9%) 和诱导脂质过氧化,CLSM证实细胞活力降低.
- 分子对接表明强烈地与DNA回旋酶结合,与观察到的抗微生物作用相关.
结论:
- 这种新型的quinazolinone-alkanesulfonates具有显著的抗微生物和抗菌膜潜力.
- 化合物5k是作为抗菌药物的进一步开发的一个有希望的候选者.
- 作用机制包括准DNA回旋酶并诱导氧化应激.
相关概念视频
Aryldiazonium Salts to Azo Dyes: Diazo Coupling
2.9K
The reaction of weakly electrophilic aryldiazonium (also called arenediazonium) salts with highly activated aromatic compounds leads to the formation of products with an —N=N— link, called an azo linkage. This reaction, presented in Figure 1, is known as diazo coupling and occurs without the loss of the nitrogen atoms of the aryldiazonium salt. Highly activated aromatic compounds such as phenols or arylamines favor the diazo coupling reaction. The coupling generally occurs at the...
2.9K
Structure-Activity Relationships and Drug Design
493
Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence...
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence...
493
Combined Effects of Drugs: Synergism
3.7K
Synergism is a useful mechanism where combining two or more drugs is more effective than each constituent used alone. Such combinations are also called supra-additive interactions. The drugs collectively enhance the final therapeutic effect by acting on different targets. Another advantage is that the low dose of each constituent drug is sufficient to achieve the desired effect. This helps reduce the duration of therapy and lower the adverse effects of these drugs.
Such synergistic combinations...
Such synergistic combinations...
3.7K


