کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1373172 | 981891 | 2011 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Trisubstituted ureas as potent and selective mPGES-1 inhibitors
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Trisubstituted ureas as potent and selective mPGES-1 inhibitors Trisubstituted ureas as potent and selective mPGES-1 inhibitors](/preview/png/1373172.png)
چکیده انگلیسی
A novel series of trisubstituted ureas has been identified as potent and selective mPGES-1 inhibitors. These compounds are selective over other prostanoid enzymes such as PGF synthase and TX synthase. This series of inhibitors was developed by lead optimization of a hit from an internal HTS campaign. Lead compound 42 is potent in A549 cell assay (IC50 of 0.34 μM) and in human whole blood assay (IC50 of 2.1 μM). An efficient and versatile one-pot strategy for the formation of ureas, involving a reductive amination, was developed to generate these inhibitors.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 5, 1 March 2011, Pages 1488–1492
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 5, 1 March 2011, Pages 1488–1492
نویسندگان
Jean-François Chiasson, Louise Boulet, Christine Brideau, Anh Chau, David Claveau, Bernard Côté, Diane Ethier, André Giroux, Jocelyne Guay, Sébastien Guiral, Joseph Mancini, Frédéric Massé, Nathalie Méthot, Denis Riendeau, Patrick Roy, Joel Rubin,