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)
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Benzothiophene piperazine and piperidine urea inhibitors of fatty acid amide hydrolase (FAAH)
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
نویسندگان
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