کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10596030 | 981892 | 2013 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis of acylated glycoconjugates as templates to investigate in vitro biopharmaceutical properties
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
کلمات کلیدی
HSACYP450CuAACC log PHLMs - HLM هاAzide - آزیدhuman serum albumin - آلبومین سرم انسانیEsterase - استرسMetabolic stability - ثبات متابولیکCytochrome P450 - سیتوکروم پی۴۵۰Click chemistry - شیمی کلیکHuman Liver Microsomes - میکروسومهای کبدی انسانیProdrug - پروتئینCarbohydrate - کربوهیدراتcarboxylesterase - کربوکسی استراز
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A series of novel glycopyranosyl azides were synthesised wherein the carbohydrate moiety was peracylated with four acetyl, propionyl, butanoyl, pentanoyl (valeryl) or 3-methylbutanoyl (isovaleryl) ester linked groups. A panel of glycoconjugates was synthesised from these glycopyranosyl azides using copper-catalysed azide-alkyne cycloaddition. The in vitro metabolic stability, plasma stability and plasma protein binding was then measured to establish the impact of the different acyl group when presented on a common scaffold. The acetyl, propionyl and butanoyl esters exhibited metabolism consistent with esterase processing, and various mono-, di- and tri-acylated hydrolysis products as well as the fully hydrolysed compound were detected. In contrast, the pentanoyl and 3-methylbutanoyl esters were stable.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 2, 15 January 2013, Pages 455-459
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 2, 15 January 2013, Pages 455-459
نویسندگان
Cindy J. Carroux, Janina Moeker, Josephine Motte, Marie Lopez, Laurent F. Bornaghi, Kasiram Katneni, Eileen Ryan, Julia Morizzi, David M. Shackleford, Susan A. Charman, Sally-Ann Poulsen,