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环维黄杨星D磺酰化衍生物的合成及耐缺氧活性的研究
引用本文:郭彩红,窦后松,郜宁,肖佩玉,李颖,尹述凡. 环维黄杨星D磺酰化衍生物的合成及耐缺氧活性的研究[J]. 华西药学杂志, 2006, 21(6): 511-514
作者姓名:郭彩红  窦后松  郜宁  肖佩玉  李颖  尹述凡
作者单位:四川大学化学学院,四川,成都,610064;四川川大华西药业股份有限公司,四川,成都,610041;广州中心附属第三医院,广东,广州,510630
摘    要:目的寻找更多具有治疗心脑血管疾病的潜在药物。方法通过磺酰化反应将不同取代的磺酰氯中间体连接到环维黄杨星D上,合成得到目标产物,并对其进行耐缺氧活性的研究。结果和结论共合成了7个环维黄杨星D磺酰化衍生物,其结构经IR、MS1、HNMR和高分辨质谱(HRMS)确证,且化合物2 a~2g均具有良好的药理活性,其中化合物2 e、2g作用最强,超过现有临床药物黄杨宁片。

关 键 词:环维黄杨星D  磺酰化  结构修饰  合成  耐缺氧活性
文章编号:1006-0103(2006)06-0511-04
收稿时间:2006-04-01
修稿时间:2006-04-01

Synthesis and effects of sulfonamide derivatives of Cyclovirobuxine D on oxygen-deficient endurance in mice
GUO Cai-hong,DOU Hou-song,GAO Ning,XIAO Pei-yu,LI Ying,YIN Shu-fan. Synthesis and effects of sulfonamide derivatives of Cyclovirobuxine D on oxygen-deficient endurance in mice[J]. West China Journal of Pharmaceutical Sciences, 2006, 21(6): 511-514
Authors:GUO Cai-hong  DOU Hou-song  GAO Ning  XIAO Pei-yu  LI Ying  YIN Shu-fan
Affiliation:1. College of Chemistry, Sichuan University, Chengdu 610064, China; 2. Sichuan Chuanda West China Pharmaceuitical Co. , Lid, Chengdu 610041, China ; 3. The Third Affiliated Hospital of Sun Yat - sen University, Guangzhou 510630, China
Abstract:OBJECTIVE To obtain more potential agents for the treatment of cardiovascular diseases.METHODS The target compounds were synthesized from the corresponding sulfonic acid chloride and Cyclovirobuxine D by sulfonamide acylation.RESULTS and CONCLUSION The structures of all compounds synthesized were determined by IR,MS,()~1HNMR and HRMS.Their effects on oxygen-deficient endurance in mice were primarily evaluated.The results indicated that all compounds possess efficiency on oxygen-defecient endurance,especially that compounds 2e,2g were more active than clinical drug Cyclovirobuxinel tablet.These seven new compounds can promote the treatment capability of cardiovascular diseases.
Keywords:Cyclovirobuxine D  Sulfonamide  Structural modification  Synthesis  Oxygen-deficient endurance
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