کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1373933 | 981909 | 2009 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Benzothiophene piperazine and piperidine urea inhibitors of fatty acid amide hydrolase (FAAH)
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
The synthesis and structure–activity relationships (SAR) of a series of benzothiophene piperazine and piperidine urea FAAH inhibitors is described. These compounds inhibit FAAH by covalently modifying the enzyme’s active site serine nucleophile. Activity-based protein profiling (ABPP) revealed that these urea inhibitors were completely selective for FAAH relative to other mammalian serine hydrolases. Several compounds showed in vivo activity in a rat complete Freund’s adjuvant (CFA) model of inflammatory pain.
The synthesis and SAR of a series of benzothiophene piperazine and piperidine urea FAAH inhibitors is described.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 10, 15 May 2009, Pages 2865–2869
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 10, 15 May 2009, Pages 2865–2869
نویسندگان
Douglas S. Johnson, Kay Ahn, Suzanne Kesten, Scott E. Lazerwith, Yuntao Song, Mark Morris, Lorraine Fay, Tracy Gregory, Cory Stiff, James B. Dunbar Jr., Marya Liimatta, David Beidler, Sarah Smith, Tyzoon K. Nomanbhoy, Benjamin F. Cravatt,