Discovery and synthesis of novel benzofurazan derivatives as inhibitors of influenza A virus

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• 作者：Ulrich Kessler ; Daniele Castagnolo ; Mafalda Pagano ; Davide Deodato ; Martina Bernardini ; Beatrice Pilger ; Charlene Ranadheera ; Maurizio Botta
• 关键词：Antiviral agents ; Influenza virus ; Viral RNA polymerase ; Benzofurazan ; H1N1
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2013
• 出版时间：15 October, 2013
• 年：2013
• 卷：23
• 期：20
• 页码：5575-5577
• 全文大小：607 K

文摘

The identification of a novel hit compound inhibitor of the protein-protein interaction between the influenza RNA-polymerase PA and PB1 subunits has been accomplished by means of high-throughput screening. A small family of structurally related molecules has been synthesized and biologically evaluated with most of the compounds showing micromolar potency of inhibition against viral replication.