Design, synthesis and preliminary bio-evaluation of glucose–cholesterol derivatives as ligands for brain targeting liposomes
Design, synthesis and preliminary bio-evaluation of glucose–cholesterol derivatives as ligands for brain targeting liposomes
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DOI：
10.1016/j.cclet.2010.12.056
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发表时间：
2011-07
影响因子：
9.1
通讯作者：
Fan Lei;Wei Fan;Xiankun Li;Shanshan Wang;Li Hai;Yong Wu
中科院分区：
文献类型：
--
作者：
Fan Lei;Wei Fan;Xiankun Li;Shanshan Wang;Li Hai;Yong Wu
A series of glucose–cholesterol derivatives8a–8eas ligands for brain targeting liposomes were synthesized. The preparation of compound6involved temporary protection of glucose with chlorotrimethylsilicane and hexamethyldisilazane followed by selectively hydrolyzed. The known cholesteryl tosylate1were coupled to ethylene glycols to afford alcohol2a–2e. Substitution and deprotection of alcohol2a–2efurnished the acids4a–4e, which was condensed with compound6to get compounds7a–7e, and then was deprotected in tetrahydrofuran with TFA to obtain the title compounds. As a model drug, tegafur was entrapped by liposomes coupled with8b, and preliminaryin vivoevaluation shown8bcould enhance the ability of liposomes delivering tegafur across the blood brain barrier.
