胍基木吡喃糖苷的合成及其抗HIV蛋白酶活性  

Synthesis of Guanidinoxylopyranosides and Their Anti-HIV PR Activity

作　　者：曹玲华[1] 连召斌[1] 

机构地区：[1]新疆大学化学化工学院

出　　处：《化学学报》2007年第4期349-354,共6页Acta Chimica Sinica

基　　金：国家自然科学基金(Nos.29962002;20462006)资助项目.

摘　　要：2,3,4-三-O-乙酰基-β-D-木吡喃糖基异硫氰酸酯1与2-氨基-4/6-取代-苯并噻唑2a～2e反应,生成糖基硫脲衍生物3a～3e,再在伯胺存在下经氯化汞脱硫,得到一系列新的胍基木吡喃糖苷类化合物4a～4e,5a～5e,6a～6e,7a～7e,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4c,5b,6b～6d,7b等对HIV-1蛋白酶表现出了较高的抑制活性.The reaction of 2,3,4-tri-O-acetyl-β-D-xylopyranosyl isothiocyanate 1 and 2-amino-4/6-substituted benzothiazoles 2a～2e gave xylopyranosylthioureas 3a～3e, which then reacted with alkyl/aryl amine in the presence of HgCl2 to afford a series of new guanidinoxylopyranosides （4a～4e, 5a～5e, 6a～6e and 7a～7e）. The structures of the new compounds were established on the basis of elemental analyses, IR, ^1H NMR and mass spectral data and all compounds took β-configuration. The biological activities of these compounds have been evaluated. Compounds 4c, 5b, 6b～6d and 7b showed anti-HIV-1 PR activity.

关 键 词：木吡喃糖基异硫氰酸酯 木吡喃糖基硫脲 胍基木吡喃糖苷 生物活性 

分 类 号：R914[医药卫生—药物化学]