| 唾液酸8,9-二硫酸酯衍生物的合成及唾液酸酶抑制活性 |
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| 引用本文： | 李文姬,崔浩,李绍顺. 唾液酸8,9-二硫酸酯衍生物的合成及唾液酸酶抑制活性[J]. 第二军医大学学报, 2000, 21(1): 56-58 |
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| 作者姓名： | 李文姬 崔浩 李绍顺 |
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| 作者单位： | 1. 第二军医大学基础医学部药理学教研室,上海,200433
2. 军事医学科学院放射医学研究所 |
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| 基金项目： | 国家自然科学基金!资助项目（39570837） |
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| 摘 要： | 目的；合成２－去氧－２，３－去氧－Ｎ－乙酰神经氨酸８，９－二硫酸酯衍生物，并探讨其与唾液酸酶抑制活笥的关系。方法：在对４，７－二羟基保护后，用三氧化硫三甲胺「ＳＯ３．Ｎ（ＣＨ３）３」对８，９－二羟基进行硫酸酯化，并对化合物（３），（４），（５），（６）进行初步唾液酸酶抑制活性试验。结果和结论；合成了４个结构全新的唾液酸８，９－二硫酸氧基衍生物，其结构均得到＾１ＨＮＭＲ，ＭＳ确证；合成的唾液酸硫酸酯
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| 关 键 词： | 唾液酸衍生物 硫酸酯化 唾液酸 酶活性 |
| 文章编号： | 0258-879X(2000)01-0056-03 |
| 修稿时间： | 1999-08-23 |
Synthesis of 8,9-disulfates derivatives from sialic acid and sialidase inhibitory activi-ties |
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| LI Wen-Ji,CUI Hao,LI Shao-Shun. Synthesis of 8,9-disulfates derivatives from sialic acid and sialidase inhibitory activi-ties[J]. Former Academic Journal of Second Military Medical University, 2000, 21(1): 56-58 |
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| Authors: | LI Wen-Ji CUI Hao LI Shao-Shun |
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| Affiliation: | LI Wen-Ji(Department of Pharmacology, Department of Basic Medicine, Second Military MedicalUniversity, Shanghai 200433, China)LI Shao-Shun(Department of Pharmacology, Department of Basic Medicine, Second MilitaryMedical University, Shanghai 200433, China)CUI Hao(Institute of Radiant Medicine, Academic Military Medical Sciences) |
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| Abstract: | Objective:To synthesize 2 deoxy 2,3 dehydro N acetyl 8,9 O disulfoneuraminic acid and investigate the relationship between the sulfate group in the sialic acid derivatives and their sialidase inhibitory activities. Methods: The title compound was synthesized by sulfation using sulfur trioxide trimethyl amine complex after protecting 4,7 dihydroxyl groups with acetic anhydride. Results and Conclusion: The 4 derivatives of 2 deoxy 2,3 dehydro N acetyl 8,9 O disulfoneuraminic acid were synthesized. Their structures were confirmed by 1HNMR and MS spectrum. The behavior of compounds (3), (4), (5), (6) towards sialidase had been investigated. All of these sulfated derivatives of sialic acid possessed potent sialidase inhibitory activities. This suggested that the sulfate group in the compounds might enhance their antiviral activities. |
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| Keywords: | sialic acid derivatives sulfation sialidase activity |
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