C1-NH2-芳香基小诺霉素衍生物的合成

摘要

Objective To find new antibacterial agents.Methods In this paper, novel compounds: 1-N-(4methylbenzyl)micronomicin, 1-N-(4-methoxylbenzyl)micronomicin, 1-N-(2-furyl-methylene)micronomicin and 1-N(2-thienylmethylene)micronomicin, were obtained by arylation of amino group at C l-position of micronomicin.The structure of these compounds were determined by elemental analysis, IR, MS, 1H-NMR, 13C-NMR, and their bioactivities and acute toxicity were screened in vitro.Results Four derivatives showed less activity in vitro than micronomicin, while 1-N-(2-furylmethylene)micronomicin was found to be less toxicity than micronomicin.Conclusion The results played positive revalation role and had reference value for future work.%目的 发现新的抗菌药物.方法 本文对小诺霉素的C1-NH进行芳香化修饰,得到4个新衍生物[即:1-N-(4-甲基苄基)小诺霉素,1-N-(4-甲氧基苄基)小诺霉素,1-N-(2-呋喃基亚甲基)小诺霉素,1-N-(2-噻吩基亚甲基)小诺霉素].所有衍生物的结构经元素分析、IR、MS、H-NMR和C-NMR所确证,并进行了体外活性及急性毒性测试.结果 新衍生物活性不及小诺霉素,1-N-(2-呋喃基亚甲基)小诺霉素的急性毒性低于小诺霉素.结论 对以后相关工作具有启示作用和一定的参考价值.