| 第 51 卷第 4 期 |  | Vol. 51 No. 4 | | 2021 年 8 月 | Aug 2021 |
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所属栏目：医药及中间体
双脱氢枞基酰胺化合物的合成与体外抑菌活性 |
| 伍 勇1，黄春花1，徐 静1，毛晓雪2，刘孝祯1
（1. 四川卫生康复职业学院 药学系，四川 自贡 643000；2. 自贡市第四人民医院 检验科，四川 自贡 643000） |
| 摘 要：以脱氢枞酸为原料，在二氯甲烷溶剂中与二氯亚砜制备脱氢枞酰氯，再以无水碳酸钠作缚酸剂，脱氢枞酰氯与脱氢枞胺在四氢呋喃溶剂中回流生成双脱氢枞基酰胺化合物，收率46.3％。产物结构经核磁共振氢谱、碳谱及红外光谱确证。采用琼脂二倍稀释法对产物进行金黄色葡萄球菌、粪肠球菌、肺炎链球菌、铜绿假单胞菌、大肠埃希菌和阴沟肠杆菌6个菌种的体外抑菌活性实验，结果表明双脱氢枞基酰胺化合物对6个菌种的体外最低抑菌浓度（MIC）为8~128 μg／mL，其中，对肺炎链球菌、阴沟肠杆菌的最低抑菌浓度（MIC）均为8 μg／mL。 |
| 关键词：脱氢枞酸；脱氢枞胺；酰胺；合成；体外抑菌活性 |
| 中图分类号：O621.3 文献标识码：A 文章编号：1009-9212（2021）04-0017-03 |
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| Synthesis and in Vitro Antibacterial Activity of Didehydroabietyl Amide Compound |
| WU Yong1, HUANG Chun-hua1, XU Jing1, MAO Xiao-xue2, LIU Xiao-zhen1
(1. Department of Pharmacy, Sichuan Vocational College of Health and Rehabilitation, Zigong 643000, China; 2. Department of Laboratory Medicine, Zigong Fourth People's Hospital, ZiGong 643000, China) |
| Abstract：Dehydroabietyl chloride was synthesized through acylation of dehydroabietyl acid using dichlorosulfoxide, anhydrous sodium carbonate as acid binding agent and dichloromethane as solvent. Didehydroabityl amide was synthesized from the reaction between dehydroabietyl chloride and dehydroabietylamine in tetrahydrofuran solvent. A yield of 46.3% was obtained; and the structure of the product was confirmed by 1H NMR, 13C NMR and IR. The in vitro antibacterial activity of the product were tested according to the agar double dilution method for six strains including Staphylococcus aureus, Enterococcus faecalis, Streptococcus pneumoniae, Pseudomonas aeruginosa, Escherichia coli and Enterobacter cloacae. The results showed that the minimum inhibitory concentrations (MIC) of didehydroabityl amide against six strains were 8~128 μg/mL, among which, the MIC of the compound against Streptococcus pneumoniae and Enterobacter cloacae were 8 μg/mL. |
| Key words：dehydroabietic acid; dehydroabietylamine;amide; synthesis; in vitro antibacterial activity |
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基金项目：自贡市重点科技计划资助项目（2018CZ30），四川卫生康复职业学院重点项目（CWKY-2018Z-03）。
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作者简介：伍 勇（1975—），男，四川荣县人，副教授，硕士，主要从事天然产物化学研究（E-mail：wuyongrx@163.com）。
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收稿日期：2021-06-21
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