کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1255672 | 971435 | 2011 | 4 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: 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](/preview/png/1255672.png)
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.
Journal: Chinese Chemical Letters - Volume 22, Issue 7, July 2011, Pages 831–834