摘要
以达克罗宁为先导化合物,通过烷基链改造和生物电子等排原理进行结构优化,共设计出12个类似化合物。在实验过程中,以4-羟基苯甲酸为起始原料,经酰氯化、酰胺化、醚键化、N-烷基化等4步合成目标产物,其目标分子结构经~1H NMR、^(13)C NMR、MS和元素分析法进行表征。通过角膜反射实验对各目标分子进行了生物活性研究,结果表明,各目标分子都具有良好的生物活性,其中化合物1l的生物活性最好。
Dyclonine as lead compounds, the use of alkyl chain transformation and biological electronic principle, structure optimization, the 12 similar compounds had been designed. In the process of ex- periment, with 4-hydroxy benzoic acid as the starting material, via acyl chlorination, amidation, ether bond and N-alkylation four steps such as synthesis of target products, its target molecules structure byl H NMR, 13C NMR, MS and elemental analysis were characterized. Using corneal reflex experiment to the study of biological activity of the target molecules, results showed that each target molecules had good biological activity, biological activity of compounds 11 of the best.
出处
《贵州师范大学学报（自然科学版）》
CAS
2017年第6期93-98,共6页
Journal of Guizhou Normal University：Natural Sciences
基金
重庆市社会民生科技创新专项(No.cstc2015shmszx80060)
活性物质生物技术教育部工程研究中心开放基金项目(No.20150408
AS201605)
关键词
先导化合物
结构优化
表征
生物活性
lead compounds
structure optimization
characterized
biological activity
