| 一氧化氮供体型3-丁基苯酞衍生物的合成及抗血小板活性 |
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| 引用本文： | 闵真立, 张奕华, 庄佩, 季晖, 赖宜生, 彭司勋. 一氧化氮供体型3-丁基苯酞衍生物的合成及抗血小板活性[J]. 中国药科大学学报, 2008, 39(5): 392-397. |
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| 作者姓名： | 闵真立 张奕华 庄佩 季晖 赖宜生 彭司勋 |
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| 作者单位： | 1.中国药科大学新药研究中心;2.中国药科大学药理学教研室 |
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| 摘 要： | 目的:研究一氧化氮(NO)供体型3-丁基苯酞衍生物的合成和生物活性,寻找新型抗脑缺血药物。方法:使用不同的连接基团将3-丁基苯酞的开环衍生物2-(1-乙酰氧戊基)苯甲酸与一氧化氮供体连接,合成了目标化合物6a-6c、10a-10c和12a-12c,同时测定它们在体外释放NO的量。结果:合成了9个未见文献报道的目标化合物,其结构均经IR、1HNMR、MS和元素分析确证。它们均有一定的抗血小板活性且有不同程度的NO释放,其中化合物10b活性最强,明显优于阿司匹林和3-丁基苯酞(P
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| 关 键 词： | NO供体 3-丁基苯酞 合成 抗血小板活性 |
Synthesis and anti-platelet activities of nitric oxide-releasing derivatives of 3-butylphthalide |
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| MIN Zhen-li. Synthesis and anti-platelet activities of nitric oxide-releasing derivatives of 3-butylphthalide[J]. Journal of China Pharmaceutical University, 2008, 39(5): 392-397 |
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| Authors: | MIN Zhen-li |
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| Affiliation: | MIN Zhen-li1,ZHANG Yi-hua1,ZHUANG Pei2,JI Hui2,LAI Yi-sheng1,PENG Si-xun11Center of Drug Discovery,2Department of Pharmacology,China Pharmaceutical University,Nanjing 210009,China |
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| Abstract: | Aim:To study the synthesis and anti-platelet activities of nitric oxide-releasing derivatives of 3-butylphthalide and search for novel anti-ischemia agents.Methods:Compounds 6a-6c,10a-10c and 12a-12c were synthesized by connecting a NO-donating moiety to 2-(1-acetoxypentyl) benzoic acid,the ring-opening form of 3-butylphthalide,through different linkers.Results:Nine compounds were synthesized and their structures were determined by IR,1H NMR,MS and elemental analysis.All these compounds exhibited anti-plate... |
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| Keywords: | nitric oxide donor 3-butylphthalide synthesis anti-platelet activity |
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