| Literature DB >> 34260245 |
Kris White1,2, Matthew Esparza3, Jue Liang4, Prasanna Bhat3, Jacinth Naidoo4, Briana L McGovern1,2, Michael A P Williams1,2, Busola R Alabi3, Jerry Shay3, Hanspeter Niederstrasser4, Bruce Posner4, Adolfo García-Sastre1,2,5,6, Joseph Ready4, Beatriz M A Fontoura3.
Abstract
Influenza viruses cause approximately half a million deaths every year worldwide. Vaccines are available but partially effective, and the number of antiviral medications is limited. Thus, it is crucial to develop therapeutic strategies to counteract this major pathogen. Influenza viruses enter the host cell via their hemagglutinin (HA) proteins. The HA subtypes of influenza A virus are phylogenetically classified into groups 1 and 2. Here, we identified an inhibitor of the HA protein, a tertiary aryl sulfonamide, that prevents influenza virus entry and replication. This compound shows potent antiviral activity against diverse H1N1, H5N1, and H3N2 influenza viruses encoding HA proteins from both groups 1 and 2. Synthesis of derivatives of this aryl sulfonamide identified moieties important for antiviral activity. This compound may be considered as a lead for drug development with the intent to be used alone or in combination with other influenza A virus antivirals to enhance pan-subtype efficacy.Entities:
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Year: 2021 PMID： 34260245 PMCID： PMC8900595 DOI： 10.1021/acs.jmedchem.1c00304
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 8.039