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新型熊果酸苯并咪(噻)唑连苯酯合成及抗炎活性测定
引用本文:李财虎,杨聪玲,张宽,石万棋,李剑忠,李颖,尹述凡. 新型熊果酸苯并咪(噻)唑连苯酯合成及抗炎活性测定[J]. 有机化学, 2012, 32(1): 133-137
作者姓名:李财虎  杨聪玲  张宽  石万棋  李剑忠  李颖  尹述凡
作者单位: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610066
3. 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 Benzimidazole (Benzothiazole) Phenylursolate
Li,Caihu , Yang,Congling , Zhang,Kuan , Shi,Wanqi , Li,Jianzhong , Li,Ying , Yin,Shufan. Synthesis and Anti-inflammatory Activity of Novel Benzimidazole (Benzothiazole) Phenylursolate[J]. Chinese Journal of Organic Chemistry, 2012, 32(1): 133-137
Authors:Li  Caihu    Yang  Congling    Zhang  Kuan    Shi  Wanqi    Li  Jianzhong    Li  Ying    Yin  Shufan
Affiliation: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:ursolic acid  benzimidazole  benzothiazole  anti-inflammatory
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