کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1371719 981853 2010 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
5-Functionalized indazoles as glucocorticoid receptor agonists
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
5-Functionalized indazoles as glucocorticoid receptor agonists
چکیده انگلیسی

An indazole based series of glucocorticoid receptor agonists is reported. The SAR exploration of this scaffold yielded compounds with nanomolar affinity for the glucocorticoid receptor with indications of selectivity for the preferred transrepression mechanism; in vivo efficacy was observed in the mouse LPS induced TNFα model for compound 28.

An indazole based series of glucocorticoid receptor (GR) agonists is reported and the SAR disclosed. The series yielded potent compounds for the GR with indications of selectivity for the preferred transrepression mechanism.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 10, 15 May 2010, Pages 3017–3020
نویسندگان
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