کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10595130 981858 2013 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Discovery and SAR of a novel series of GIRK1/2 and GIRK1/4 activators
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Discovery and SAR of a novel series of GIRK1/2 and GIRK1/4 activators
چکیده انگلیسی
This Letter describes a novel series of GIRK activators identified through an HTS campaign. The HTS lead was a potent and efficacious dual GIRK1/2 and GIRK1/4 activator. Further chemical optimization through both iterative parallel synthesis and fragment library efforts identified dual GIRK1/2 and GIRK1/4 activators as well as the first examples of selective GIRK1/4 activators. Importantly, these compounds were inactive on GIRK2 and other non-GIRK1 containing GIRK channels, and SAR proved shallow.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 18, 15 September 2013, Pages 5195-5198
نویسندگان
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