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Chin. J. Org. Chem. ›› 2011, Vol. 31 ›› Issue (12): 2106-2113. Previous Articles     Next Articles

Full Papers

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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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