کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1369902 | 981793 | 2014 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Switching cannabinoid response from CB2 agonists to FAAH inhibitors
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
A series of 3-carboxamido-5-aryl-isoxazoles designed as CB2 agonists were evaluated as FAAH inhibitors. The pharmacological results led to identify structure–activity relationships enabling to switch cannabinoid response from CB2 agonists to FAAH inhibitors. Two compounds were selected for their FAAH and/or CB2 activity, and evaluated in a colitis model for their anti-inflammatory activity. Results showed that compounds 10 and 11 inhibit the development of DSS-induced acute colitis in mice and then, are interesting leads to explore new drug candidates for IBD.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 5, 1 March 2014, Pages 1322–1326
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 5, 1 March 2014, Pages 1322–1326
نویسندگان
Aurélien Tourteau, Natascha Leleu-Chavain, Mathilde Body-Malapel, Virginie Andrzejak, Amélie Barczyk, Madjid Djouina, Benoit Rigo, Pierre Desreumaux, Philippe Chavatte, Régis Millet,