新型熊果酸苯并咪(噻)唑连苯酯合成及抗炎活性测定有机化学.pdfVIP

DOI: 10.6023/cjoc1104011 研究论文 有机化学 Chinese Journal of Organic Chemistry ARTICLE 新型熊果酸苯并咪(噻)唑连苯酯合成及抗炎活性测定 李财虎a 杨聪玲b 张 宽a 石万棋c 李剑忠b 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 610066) (c 四川国康药业有限公司 成都 610041) 摘要 以熊果酸、取代苯甲醛和邻苯二胺或邻氨基苯硫酚为原料, 合成了一系列熊果酸苯并咪(噻) 唑连苯酯衍生物 4a～4h, 8 个新化合物均未见文献报道, 其结构经 1H NMR, IR 和 HRMS 加以确认, 并对 4a～4h 进行药理活性筛选, 结 果表明, 化合物 4d (150 mg•kg－1), 4g (150 mg•kg－1)等具有良好抗炎活性. 关键词 熊果酸; 苯并咪唑; 苯并噻唑; 抗炎 Synthesis and Anti-inflammatory Activity of Novel Benzimida- zole (Benzothiazole) Phenylursolate Li, Caihua Yang, Conglingb Zhang, Kuana Shi, Wanqic Li, Jianzhongb Li, Ying*,a Yin, Shufan*,a a ( Faculty of Chemistry Sichuan University, Chengdu 610064) (b College of Chemical and Material Science, Sichuan Normal University, Chengdu 610066) c ( Sichuan Guokang Pharmaceutical Co., Ltd, Chengdu 610041) Abstract A novel series of the benzimidazole or benzothiazole phenyl ester derivatives of ursolic acid 4a～4h were prepared via ursolic acid, substituted benzaldehyde, and o-phenylendiamine or 2-aminothiophenol. The compounds were structurally confirmed by 1H NMR, IR and HRMS techniques. The preliminary bioassay test demonstrated that compounds 4d and 4g had potent anti-inflammatory activity. Keywords urso