| 第 51 卷第 4 期 |  | Vol. 51 No. 4 | | 2021 年 8 月 | Aug 2021 |
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所屬欄目：醫藥及中間體
雙脫氫樅基酰胺化合物的合成與體外抑菌活性 |
| 伍 勇1，黃春花1，徐 靜1，毛曉雪2，劉孝禎1
（1. 四川衛生康復職業(yè)學(xué)院 藥學(xué)系，四川 自貢 643000；2. 自貢市第四人民醫院 檢驗科，四川 自貢 643000） |
| 摘 要：以脫氫樅酸為原料，在二氯甲烷溶劑中與二氯亞砜制備脫氫樅酰氯，再以無(wú)水碳酸鈉作縛酸劑，脫氫樅酰氯與脫氫樅胺在四氫呋喃溶劑中回流生成雙脫氫樅基酰胺化合物，收率46.3％。產(chǎn)物結構經(jīng)核磁共振氫譜、碳譜及紅外光譜確證。采用瓊脂二倍稀釋法對產(chǎn)物進(jìn)行金黃色葡萄球菌、糞腸球菌、肺炎鏈球菌、銅綠假單胞菌、大腸埃希菌和陰溝腸桿菌6個(gè)菌種的體外抑菌活性實(shí)驗，結果表明雙脫氫樅基酰胺化合物對6個(gè)菌種的體外最低抑菌濃度（MIC）為8~128 μg／mL，其中，對肺炎鏈球菌、陰溝腸桿菌的最低抑菌濃度（MIC）均為8 μg／mL。 |
| 關(guān)鍵詞：脫氫樅酸；脫氫樅胺；酰胺；合成；體外抑菌活性 |
| 中圖分類(lèi)號：O621.3 文獻標識碼：A 文章編號：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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基金項目：自貢市重點(diǎn)科技計劃資助項目（2018CZ30），四川衛生康復職業(yè)學(xué)院重點(diǎn)項目（CWKY-2018Z-03）。
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作者簡(jiǎn)介：伍 勇（1975—），男，四川榮縣人，副教授，碩士，主要從事天然產(chǎn)物化學(xué)研究（E-mail：wuyongrx@163.com）。
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收稿日期：2021-06-21
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