| 依布硒啉衍生物对白三烯B4生物合成抑制作用及其构效关系 |
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| 引用本文： | 郭颖,肖颖歆,郭宗儒,程桂芳.依布硒啉衍生物对白三烯B4生物合成抑制作用及其构效关系[J].药学学报,1999,34(9):652-654. |
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| 作者姓名： | 郭颖 肖颖歆 郭宗儒 程桂芳 |
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| 作者单位： | 中国医学科学院,中国协和医科大学药物研究所 |
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| 摘 要： | 目的：研究一系列依布硒啉衍生物对白三烯B4生物合成的影响，并探讨其构效关系。方法：高效液相色谱法测定白三烯B4。结果：依布硒啉的磺酰胺类似物以及N-芳香环取代的磺酰胺衍生物对白三烯B4生物合成具有抑制作用，其IC50在10-5～10-6 mol.L-1之间，并存在一定的构效关系。结论：磺酰胺基团上的酸性氢原子是关键因素，它的存在可以形成分子内氢键，从而使化合物具有活性。
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| 关 键 词： | 白三烯B4生物合成 有机硒化合物 依布硒啉 高效液相色谱法 构效关系 |
| 收稿时间： | 1998-12-05 |
INHIBITORY EFFECT AND STRUCTURE-ACTIVITY RELATIONSHIP OF EBSELEN DERIVATIVES ON LEUKOTRIENE B4 BIOSYNTHESIS |
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| Guo Ying,Xiao Yingxin,Guo Zongru and Cheng Guifang.INHIBITORY EFFECT AND STRUCTURE-ACTIVITY RELATIONSHIP OF EBSELEN DERIVATIVES ON LEUKOTRIENE B4 BIOSYNTHESIS[J].Acta Pharmaceutica Sinica,1999,34(9):652-654. |
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| Authors: | Guo Ying Xiao Yingxin Guo Zongru and Cheng Guifang |
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| Abstract: | AIM: A series of ebselen derivatives were synthesized for studying their effects on LTB4 biosynthesis. Preliminary analysis of structure-activity relationship(SAR) of these compounds were conducted. METHODS: High performance liquid chromatography(HPLC) was used to determine LTB4. RESULTS: Sulfonamide analogues of ebselen and N-aryl substituted derivatives of ebselen showed significant inhibitory effects on LTB4 biosynthesis with IC50 of 10-5 mol.L-1 to 10-6 mol.L-1.CONCLUSION: According to SAR, the presence of an acidic hydrogen atom on the sulfonamido group seemed to be a critical factor for the activity. In the absence of the hydrogen or loss of the ability to form intermolecular hydrogen bonding compounds would abolish the activity. |
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| Keywords: | LTB 4 biosynthesis seleno organic compounds ebselen HPLC structure activity relationship |
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