کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1376642 | 981962 | 2008 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Non-acidic pyrazole EP1 receptor antagonists with in vivo analgesic efficacy
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Replacement of the carboxylic acid group in a series of previously described methylene-linked pyrazole EP1 receptor antagonists led to the discovery of amide, reversed amide and carbamate derivatives. Two compounds, 10a and 10b, were identified as brain penetrant compounds and both demonstrated efficacy in the CFA model of inflammatory pain.
This paper details the characterization of a series of amides, reversed amides and carbamates as EP1 antagonists which culminated in the identification of the two carbamate derivatives 10a and 10b. Both compounds were found to display potent analgesic activity in vivo and to penetrate the central nervous system.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 11, 1 June 2008, Pages 3392–3399
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 11, 1 June 2008, Pages 3392–3399
نویسندگان
Adrian Hall, Andy Billinton, Susan H. Brown, Nicholas M. Clayton, Anita Chowdhury, Gerard M.P. Giblin, Paul Goldsmith, Thomas G. Hayhow, David N. Hurst, Ian R. Kilford, Alan Naylor, Barry Passingham, Lisa Winyard,