| N-烷基/芳基-N'-(4-芳基噻唑-2-基)-N"-糖基胍的合成及生物活性研究 |
| |
| 引用本文： | 史合方,曹玲华.N-烷基/芳基-N'-(4-芳基噻唑-2-基)-N"-糖基胍的合成及生物活性研究[J].有机化学,2005,25(9):1066-1070. |
| |
| 作者姓名： | 史合方 曹玲华 |
| |
| 作者单位： | [1]新疆大学化学化工学院,乌鲁木齐830046 [2]南开大学元素有机化学国家重点实验室,天津300071 |
| |
| 基金项目： | 国家自然科学基金（Nos.29962002.20462006）资助项目. |
| |
| 摘 要： | 2,3,4,6-四-O-乙酰基-β-D-吡喃葡萄糖基异硫氰酸酯(1)与2-氨基-4-取代苯基噻唑(2a～2b)反应, 生成糖基硫脲衍生物3a～3b, 再在伯胺存在下经氯化汞脱硫, 得到一系列新的N-烷基/芳基-N'-(4-芳基噻唑-2-基)-N"-糖基胍类化合物(4a～4e, 5a～5e). 所有新化合物的结构均经IR, 1H NMR, MS谱和元素分析证实, 所得产物均为β-构型. 生物活性测试结果表明, 化合物4b和5d对HIV-1 PR表现出了较高的抑制活性.
|
| 关 键 词： | 糖基异硫氰酸酯 糖基硫脲 糖基胍 生物活性 |
| 收稿时间： | 2004-9-6 |
| 修稿时间： | 2004年9月6日 |
Synthesis and Biological Activity of N-Alkyl/aryl-N'-(4-arylthiazol-2-yl)- N'-glycosyl Guanidines |
| |
| Shi GeFang;Cao LingHua.Synthesis and Biological Activity of N-Alkyl/aryl-N'-(4-arylthiazol-2-yl)- N'-glycosyl Guanidines[J].Chinese Journal of Organic Chemistry,2005,25(9):1066-1070. |
| |
| Authors: | Shi GeFang;Cao LingHua |
| |
| Institution: | (College of Chemistry and Chemical Engineering, Xinjiang University, Urumqi 830046)(State Key Laboratory of Elemento-Organic Chemistry, Nankai Univer-sity, Tianjin 300071) |
| |
| Abstract: | The reaction of 2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyl isothiocyanate (1) and 2-amino-4- arylthiazoles (2a～2b) gave glucosylthioureas 3a～3b, which then reacted with alkyl/aryl amine in the presence of HgCl2 to afford a series of new N-alkyl/aryl-N'-(4-arylthiazol-2-yl)-N'-glucosyl guanidines (4a～4e and 5a～5e). The structures of the new compounds were established on the basis of IR, 1H NMR and MS spectra and all compounds took β-configuration. The anti-HIV and antibacterial activities of these compounds have been evaluated. Compounds 4b and 5d showed anti-HIV activity. |
| |
| Keywords: | glucosyl isothiocyanate glucosylthiourea guanidinoglucoside biological activity |
| 本文献已被 维普 等数据库收录！ |
| 点击此处可从《有机化学》浏览原始摘要信息 |
| 点击此处可从《有机化学》下载免费的PDF全文 |
|
