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合成和生物评估的颗粒胺B及其结构类似物

Dario Matulja¹, Petra Grbčić², Gabrijela Matijević³

¹Department of Biotechnology, University of Rijeka, Radmile Matejčić 2, Rijeka, 51000, Croatia.

Current medicinal chemistry

|February 13, 2024

概括

研究人员合成了花胺B和类似物,评估了它们的抗氧化,抗菌和毒性作用. 侧链的修改显示影响有限,这表明内环功能化可改善生物活性.

科学领域:

海洋天然产品化学化学
药用化学医学化学
药物发现药物发现药物发现

背景情况:

从*Eunicella*珊瑚物种中分离出来的A和B颗粒胺,具有部分检查的生物活性.
试胺衍生物如颗粒胺B因其潜在的治疗应用而引起人们的兴趣.

研究的目的:

通过修改侧链来合成颗粒胺B (4b) 和12种结构类似物.
全面评估合成化合物的生物活性和毒性.

主要方法:

使用Sun和Fürstner程序合成颗粒胺B和类似物.
对抗氧化,抗增殖和抗菌性质的评估.
在斑马鱼 (*Danio rerio*) 模型中进行体内毒性评估.

主要成果:

化合物4i显示出最强的ABTS激素清除活性 (IC50 = 36 ± 2μM).
颗粒胺B (4b) 呈现出适度的抗菌活性对抗*细菌菌* (MIC = 125μM).
化合物4b和4i在斑马鱼中诱导了显著的发育异常,表明了毒性.

结论:

与颗粒胺B相比,侧链的修改并没有显著改变生物活性.
未来的研究应该专注于功能化内醇环以增强生物效应.
新的合成正在进行中,以探索用于改进药物候选者的英多尔核心修饰.

关键词:

颗粒胺 B 种类 N-脂肪酸乙衍生物的N-脂肪酸乙衍生物它是一种抗菌药物,具有抗菌作用.抗氧化剂是一种抗氧化剂.这是一种抗增殖药物.胚胎毒性胚胎毒性胚胎毒性

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