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有机化学.pdfVIP

2011 年第 31 卷 有 机 化 学 Vol. 31, 2011 第 12 期, 2106～2113 Chinese Journal of Organic Chemistry No. 12, 2106～2113 ·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 a 王海峰 b 张露昀 a 石万棋 c 张 萍 c 李 颖*,a 尹述凡*,a (a 四川大学化学学院 成都 610064) (b 四川师范大学化学与材料科学学院 成都 610068) (c 四川国康药业有限公司 成都 610059) 摘要 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- 1 磺酰胺类衍生物, 其结构经 H 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 Synthesis and Anti-Gastric Ulcer Activity of Novel N-Substituted Guaiazulene-1-sulfonamides Derivatives Yang, Fanga Wang, Haifengb Zhang, Luyuna Shi,Wanqic Zhang, Pingc Li, Ying*,a Yin, Shufan*,a (a College of Chemistry, Sichuan University, Chengdu 610064) (b Department of Chemistry and Materials, Sichuan Normal University, Chengdu 610068) (c Sichuan Guokang Pharmaceutical Limited Company, Chengdu 610059) Abstract Fifteen novel N-substituted guaiazulenes-1-sulfonamides derivatives were designed and synthe- sized via guaiazulene, sodium 3,8-dimethyl-5-isopropylazulene-1-sulfonate, amino acid methyl ester hydro- 1 chlorides, hydrazine hydrate and arylaldehydes. Their structures were confirmed by H NMR, IR and HRMS techniques, and anti-gastric ulcer activity was studied as well.