Identification of entry inhibitors with 4-aminopiperidine scaffold targeting group 1 influenza A virus.
A549 Cells
Antiviral Agents
/ pharmacology
Humans
Influenza A Virus, H1N1 Subtype
/ drug effects
Influenza A Virus, H5N1 Subtype
/ drug effects
Influenza A virus
/ drug effects
Piperidines
/ pharmacology
Small Molecule Libraries
/ pharmacology
Structure-Activity Relationship
Virus Internalization
/ drug effects
Virus Replication
/ drug effects
Fusion inhibitor
Hemagglutinin
Influenza a viruses
Structure activity relationship
Virus entry
Journal
Antiviral research
ISSN: 1872-9096
Titre abrégé: Antiviral Res
Pays: Netherlands
ID NLM: 8109699
Informations de publication
Date de publication:
05 2020
05 2020
Historique:
received:
13
11
2019
revised:
20
03
2020
accepted:
22
03
2020
pubmed:
31
3
2020
medline:
2
4
2021
entrez:
31
3
2020
Statut:
ppublish
Résumé
Influenza A viruses (IAVs) cause seasonal flu and occasionally pandemics. The current therapeutics against IAVs target two viral proteins - neuraminidase (NA) and M2 ion-channel protein. However, M2 ion channel inhibitors (amantadine and rimantadine) are no longer recommended by CDC for use due to the emergence of high level of antiviral resistance among the circulating influenza viruses, and resistant strains to NA inhibitors (oseltamivir and zanamivir) have also been reported. Therefore, development of novel anti-influenza therapies is urgently needed. As one of the viral surface glycoproteins, hemagglutinin (HA) mediates critical virus entry steps including virus binding to host cells and virus-host membrane fusion, which makes it a potential target for anti-influenza drug development. In this study, we report the identification of compound CBS1116 with a 4-aminopiperidine scaffold from a chemical library screen as an entry inhibitor specifically targeting two group 1 influenza A viruses, A/Puerto Rico/8/34 (H1N1) and recombinant low pathogenic avian H5N1 virus (A/Vietnam/1203/04, VN04
Identifiants
pubmed: 32222293
pii: S0166-3542(19)30640-0
doi: 10.1016/j.antiviral.2020.104782
pmc: PMC7243365
mid: NIHMS1581692
pii:
doi:
Substances chimiques
4-aminopiperidine
0
Antiviral Agents
0
Piperidines
0
Small Molecule Libraries
0
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
104782Subventions
Organisme : NIAID NIH HHS
ID : R41 AI127031
Pays : United States
Informations de copyright
Copyright © 2020 Elsevier B.V. All rights reserved.
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