尿素衍生物:合成,生物评估,以及在研究中作为抗菌和抗癌剂
Nasrin S Munia1, Mohammed M Alanazi2, Youness El Bakri3
1Laboratory of Carbohydrate and Nucleoside Chemistry (LCNC), Department of Chemistry, Faculty of Science, University of Chittagong, Chittagong 4331, Bangladesh.
Medicina (Kaunas, Lithuania)
|June 28, 2023
概括
新的尿素衍生物显示出强大的抗微生物和抗癌特性. 这些改性核酸相似物对真菌病原体和癌细胞有效,具有低毒性,为新药开发提供了潜力.
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:
- 核糖类类似物是已确立的抗病毒和抗癌药物.
- 关于它们的抗菌和抗真菌作用的研究有限.
- 氨酸,一种pyrimidine核酸盐,作为一种新型抗菌药物开发的支架.
研究的目的:
- 合成和描述新的尿素衍生物.
- 评估它们在体外对细菌和真菌的抗微生物活性.
- 评估它们的抗癌潜力和安全性.
主要方法:
- 尿素衍生物的化学合成与阿利法和芳香修饰.
- 用光谱 (NMR,FTIR,MS),元素和物理化学分析进行表征.
- 在体外抗菌试验,细胞毒性测试,对EAC细胞的抗增殖试验.
- 分子对接,分子动力学模拟和结构-活性关系 (SAR) 分析.
- 在ADMET属性的形预测.
主要成果:
- 合成的尿素衍生物在体外表现出显著的抗菌活性,特别是对真菌植物病原体.
- 化合物6 (2',3'-di-O-cinnamoyl-5'-O-palmitoyluridine) 显示出对埃里希克瘤细胞具有有前途的抗癌活性.
- 分子对接和动力学模拟支持衍生物与细菌点的结合相互作用.
- SAR研究发现了有效的乙链和芳香基对抗微生物活性.
- 预测的药理动力学特性 (ADMET) 是有利的.
结论:
- 合成的尿素衍生物具有显著的抗微生物和抗癌潜力.
- 这些化合物代表了开发新治疗剂的有希望的候选者.
- 需要对它们的药用进行进一步的研究.
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