کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1372614 981872 2009 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype
چکیده انگلیسی

This Letter describes the discovery and SAR of three novel series of mGluR5 non-competitive antagonists/negative allosteric modulators (NAMs) not based on manipulation of an MPEP/MTEP chemotype. This work demonstrates fundamentally new mGluR5 NAM chemotypes with submicromolar potencies, and the first example of a mode of pharmacology ‘switch’ to provide PAMs with a non-MPEP scaffold.

This Letter describes the discovery and SAR of three novel series of mGluR5 non-competitive antagonists/negative allosteric modulators (NAMs) not based on manipulation of an MPEP/MTEP chemotype. This work demonstrates fundamentally new mGluR5 NAM chemotypes with submicromolar potencies, and the first example of a mode of pharmacology ‘switch’ to provide PAMs with a non-MPEP scaffold.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 12, 15 June 2009, Pages 3209–3213
نویسندگان
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