顺-1,8-对烷二胺双酰胺杂环类衍生物的合成及抑菌活性研究

Synthesis and Antibacterial Activity of Bis-alkanoyl-amines Heterocyclic Derivatives of cis-1,8-p-Menthane Diamine

以二氯甲烷为溶剂,含杂环羧酸先经酰氯化,再与顺-1,8-对烷二胺在常温下通过亲核加成-消除反应合成8个相应的双酰胺杂环类衍生物B1~B8,产率为53%~100%。产物结构通过FT-IR、ESI^+-MS和~1H NMR等表征手段进行确证。进一步对产物进行抑菌活性测定,结果表明部分产物对金黄色葡萄球菌和白色念珠菌具有一定的抑菌活性,其中化合物B8对金黄色葡萄球菌和白色念珠菌表现出良好的抑菌效果,最小抑菌浓度(MIC)值均为56.25 mg/L。

Using dichloroacetonitrile as solvent, Eight bis-alkanoyl-amines heterocyclic derivatives B1 - 118 were synthesized through nucleophilic addition-elimination reaction of carboxylic acid chloride containing heterocycle and c/s-l, 8-p-menthane diamine. And the yields of derivatives were 53% - 100%. The structures of the products were characterized by FF-IR, ESI ＋ - MS, L H NMR and 13C NMR. The antibacterial activities were determined, and the resuhs showed that some products had excellent antibacterial activities against Staphylococcus aureus and Candida albicans. The minimum inhibitory concentration （MIC） of compound B8 against S. aureus and C. albicans were both 56. 25 mg/L.