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有机化学
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有机化学 ›› 2011, Vol. 31 ›› Issue (12): 2106-2113. 上一篇    下一篇

研究论文

新型N-取代愈创兰烃薁-1-磺酰胺类衍生物的合成及抗胃溃疡活性研究

杨芳1，王海峰2，张露昀1，石万棋3，张萍3，李颖*,1，尹述凡*,1   

  1. (1四川大学化学学院 成都 610064)
    (2四川师范大学化学与材料科学学院 成都 610068)
    (3四川国康药业有限公司 成都 610059)
  • 收稿日期:2011-05-11 修回日期:2011-07-22 发布日期:2011-09-02
  • 通讯作者: 尹述凡 E-mail:chuandayouji217@163.com;;

Synthesis and Anti-Gastric Ulcer Activity of Novel N-Substituted Guaiazulene-1-sulfonamides Derivatives

Yang Fang1 Wang Haifeng2 Zhang Lu-yun1 ShiWanqi3 Zhang Ping3 Li Ying*,1 Yin Shufan*,1   

  1. (1 College of Chemistry, Sichuan University, Chengdu 610064)
    (2 Department of Chemistry and Materials, Sichuan Normal University, Chengdu 610068)
    (3 Sichuan Guokang Pharmaceutical Limited Company, Chengdu 610059)
  • Received:2011-05-11 Revised:2011-07-22 Published:2011-09-02

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以愈创兰烃薁、氨基酸甲酯盐酸盐、水合肼、芳香醛为原料, 合成了15种未见报道的新型N-取代愈创兰烃薁-1-磺酰胺类衍生物, 其结构经1H NMR, IR, HRMS确证. 初步生物活性测试结果表明, 部分化合物具有明显的抗胃溃疡活性.

关键词: 愈创兰烃薁, 薁磺酸钠, 磺酰胺, 抗胃溃疡, 合成

Fifteen novel N-substituted guaiazulenes-1-sulfonamides derivatives were designed and synthesized via guaiazulene, sodium 3,8-dimethyl-5-isopropylazulene-1-sulfonate, amino acid methyl ester hydro-chlorides, hydrazine hydrate and arylaldehydes. Their structures were confirmed by 1H NMR, IR and HRMS techniques, and anti-gastric ulcer activity was studied as well. The preliminary bioassay test indicated that some of the compounds had obvious anti-gastric ulcer activity.

Key words: guaiazulene, sodium guaiazulene-1-sulfonate, sulfonamide, anti-gastric ulcer, synthesis