Discovery of novel dengue virus NS5 methyltransferase non-nucleoside inhibitors by fragment-based drug design

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• 作者：Fatiha Benmansour^a ; ^b ; ^c ; Iuni Trist^d ; Bruno Coutard^a ; ^b ; Etienne Decroly^a ; ^b ; Gilles Querat^e ; Andrea Brancale^d ; Karine Barral^a ; ^b ; ^c ; ^{karine.barral@inserm.fr}
• 关键词：Phenyl [(phenylcarbamoyl)amino]benzene-1-sulfonate derivatives ; N-Phenyl-[(phenylcarbamoyl)amino]benzene-1-sulfonamide derivatives ; Fragment-linking strategy ; Dengue virus ; NS5 methyltransferase inhibitors ; Antiviral activity
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：865-880
• 全文大小：2801 K
• 卷排序：125

文摘

A fragment-based drug design approach on dengue virus methyltransferase. Optimization of new non-nucleosidique methyltransferase inhibitors by fragment-linking. Synthesis of Phenyl [(phenylcarbamoyl)amino]benzene-1-sulfonate and -sulfonamide derivatives. Crystal structures of dengue virus methyltransferase in complex with new inhibitors. Validation of dengue virus and West Nile virus methyltransferases inhibition.