کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1379598 982032 2005 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Discovery and structure–activity relationships of novel sulfonamides as potent PTP1B inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Discovery and structure–activity relationships of novel sulfonamides as potent PTP1B inhibitors
چکیده انگلیسی

A series of novel sulfonamides containing a single difluoromethylene-phosphonate group were discovered to be potent inhibitors of protein tyrosine phosphatase 1B. Structure–activity relationships around the scaffold were investigated, leading to the identification of compounds with IC50 or Ki values in the low nanomolar range. These sulfonamide-based inhibitors exhibit 100 and 30 times higher inhibitory activity than the corresponding tertiary amines and carboxamides, respectively.

A series of novel sulfonamides containing a single DFMP group were discovered to be potent inhibitors of PTP1B. Investigation of SAR led to the identification of compounds with IC50 or Ki values in the low nanomolar range.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 19, 1 October 2005, Pages 4336–4341
نویسندگان
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