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作者机构：Key Laboratory of Drug Targeting and Drug Delivery Systems West China School of Pharmacy Sichuan University Chengdu 610041 China
出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)
年 卷 期：2011年第22卷第7期
页 面：831-834页
核心收录：
学科分类：0710[理学-生物学] 1007[医学-药学(可授医学、理学学位)] 07[理学] 08[工学] 09[农学] 071007[理学-遗传学] 0901[农学-作物学] 0836[工学-生物工程] 090102[农学-作物遗传育种] 10[医学]
基 金：supported by the National Natural Science Foundation of China(No.81072532)
主 题：Liposome ligands Brain target GLUTt transporter Tegafur Synthesis
摘 要：A series of glucose-cholesterol derivatives 8a-8e as ligands for brain targeting liposomes were synthesized. The preparation of compound 6 involved temporary protection of glucose with chlorotrimethylsilicane and hexamethyldisilazane followed by selectively hydrolyzed. The known cholesteryl tosylate 1 were coupled to ethylene glycols to afford alcohol 2a-2e. Substitution and deprotection of alcohol 2a-2e furnished the acids 4a-4e, which was condensed with compound 6 to get compounds 7a-7e, and then was deprotected in tetrahydrofuran with TFA to obtain the title compounds. As a model drug, tegafur was entrapped by liposomes coupled with 8b, and preliminary in vivo evaluation shown 8b could enhance the ability of liposomes delivering tegafur across the blood brain barrier.
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