Journal of Medicinal Chemistry p. 2688 - 2703 (2016)
Update date:2022-08-15
Topics:
Trist, Iuni M. L.
Nannetti, Giulio
Tintori, Cristina
Fallacara, Anna Lucia
Deodato, Davide
Mercorelli, Beatrice
Palù, Giorgio
Wijtmans, Maikel
Gospodova, Tzveta
Edink, Ewald
Verheij, Mark
De Esch, Iwan
Viteva, Lilia
Loregian, Arianna
Botta, Maurizio
Influenza is an infectious disease that represents an important public health burden, with high impact on the global morbidity, mortality, and economy. The poor protection and the need of annual updating of the anti-influenza vaccine, added to the rapid emergence of viral strains resistant to current therapy make the need for antiviral drugs with novel mechanisms of action compelling. In this regard, the viral RNA polymerase is an attractive target that allows the design of selective compounds with reduced risk of resistance. In previous studies we showed that the inhibition of the polymerase acidic protein-basic protein 1 (PA-PB1) interaction is a promising strategy for the development of anti-influenza agents. Starting from the previously identified 3-cyano-4,6-diphenyl-pyridines, we chemically modified this scaffold and explored its structure-activity relationships. Noncytotoxic compounds with both the ability of disrupting the PA-PB1 interaction and antiviral activity were identified, and their mechanism of target binding was clarified with molecular modeling simulations.
View Moreqingdao goldenchem imp and exp co.,ltd.
Contact:532-55579246
Address:no.62 ,haier road laoshan distirct
Xuzhou Tianrun Chemical Co.,Ltd
website:http://www.tianrunchem.cn
Contact:86-516-83832636
Address:fuxing road
website:http://www.simagchem.com
Contact:+86-592-2680277
Address:21/F Hualong Office Building,No.6 Hubin East Road, Xiamen,China
Henan zhongda Biological Engineering Co., Ltd
Contact:86-28-18109029985
Address:shenzhou road,xuedian industrial estate,zhengzhou city,henan province CHN
Jiande City Silibase Silicone New Material Manufacture Co., Ltd.
Contact:15967177856
Address:Genglou Industrial Development Area
Doi:10.1016/j.catcom.2015.09.012
(2016)Doi:10.1039/b921016d
(2010)Doi:10.1016/j.tetlet.2020.151772
(2020)Doi:10.1002/ejoc.201800300
(2018)Doi:10.1016/j.apcata.2016.11.033
(2017)Doi:10.1021/ja00200a060
(1989)