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
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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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
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 10, 15 May 2010, Pages 3017–3020
نویسندگان
Mei Bai, Grant Carr, Russell J. DeOrazio, Thomas D. Friedrich, Svetlana Dobritsa, Kevin Fitzpatrick, Peter R. Guzzo, Douglas B. Kitchen, Michael A. Lynch, Denise Peace, Mohammed Sajad, Alexander Usyatinsky, Mark A. Wolf,