کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1362623 981492 2006 20 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Modelling, synthesis and biological evaluation of novel glucuronide-based probes of Vibrio cholerae sialidase
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Modelling, synthesis and biological evaluation of novel glucuronide-based probes of Vibrio cholerae sialidase
چکیده انگلیسی

The development of sialidase inhibitors is an area of continuing interest due to their potential use as therapeutic agents to combat viral and bacterial infections. Herein, we report our studies involving the sialidase from the pathogen Vibrio cholerae, through the modelling, synthesis and biological evaluation of mimetics of 5-acetamido-2,6-anhydro-3,5-dideoxy-d-glycero-d-galacto-non-2-enonic acid (Neu5Ac2en, 1), a naturally occurring sialidase inhibitor. These mimetics are O- and S-glycosides of N-acetyl-d-glucosaminuronic acid in which the aglycone portion effectively replaces the C-6 glycerol side chain of Neu5Ac2en (1). The choice of aglycones was aided by use of the X-ray crystal structure of V. cholerae sialidase complexed with Neu5Ac2en (1). All Neu5Ac2en mimetics tested were found to inhibit V. cholerae sialidase as determined using a standard fluorometric assay.

The synthesis and biological evaluation of a series of glucuronide-based Neu5Ac2en mimetics are presented.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 14, Issue 5, 1 March 2006, Pages 1518–1537
نویسندگان
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