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

被引：30
|
作者：
Kessler, Ulrich [1 ]
Castagnolo, Daniele [2 ]
Pagano, Mafalda [2 ]
Deodato, Davide [2 ]
Bernardini, Martina [2 ]
Pilger, Beatrice [1 ]
Ranadheera, Charlene [1 ]
Botta, Maurizio [2 ,3 ]
机构：
[1] PiKe Pharma GmbH, Zurich, Switzerland
[2] Univ Siena, Dipartimento Biotecnol Chim & Farm, I-53100 Siena, Italy
[3] Temple Univ, Ctr Biotechnol, Coll Sci & Technol, Sbarro Inst Canc Res & Mol Med, Philadelphia, PA 19122 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 20期
关键词：
Antiviral agents; Influenza virus; Viral RNA polymerase; Benzofurazan; H1N1; ANTIVIRAL ACTIVITY; EMERGENCE;
D O I：
10.1016/j.bmcl.2013.08.048
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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. (C) 2013 Elsevier Ltd. All rights reserved.
引用
收藏
页码：5575 / 5577
页数：3
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