کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1364958 | 981550 | 2008 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design and optimization of aniline-substituted tetrahydroquinoline C5a receptor antagonists
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Design and optimization of aniline-substituted tetrahydroquinoline C5a receptor antagonists Design and optimization of aniline-substituted tetrahydroquinoline C5a receptor antagonists](/preview/png/1364958.png)
چکیده انگلیسی
A series of aniline-substituted tetrahydroquinoline C5a receptor antagonists were discovered. A functionality requirement of ortho substitution on the aniline was revealed. Secondary anilines, in general, outperformed tertiary analogs in inhibition of C5a-induced calcium mobilization. Further enhancement of activity was realized in the presence of an ortho hydroxyalkyl side chain. The functional IC50 of selected analogs was optimized to the single-digit nanomolar level.
A series of aniline-substituted tetrahydroquinoline C5aR antagonists with distinct structure-activity relationships are presented.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 14, 15 July 2008, Pages 3852–3855
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 14, 15 July 2008, Pages 3852–3855
نویسندگان
Yong Gong, J. Kent Barbay, Mieke Buntinx, Jian Li, Jean Van Wauwe, Concha Claes, Guy Van Lommen, Pamela J. Hornby, Wei He,