Oseltamivir analogs with potent anti-influenza virus activity.
Journal
Drug discovery today
ISSN: 1878-5832
Titre abrégé: Drug Discov Today
Pays: England
ID NLM: 9604391
Informations de publication
Date de publication:
08 2020
08 2020
Historique:
received:
19
02
2020
revised:
09
05
2020
accepted:
08
06
2020
pubmed:
20
6
2020
medline:
10
9
2021
entrez:
20
6
2020
Statut:
ppublish
Résumé
Influenza A and B viruses cause seasonal worldwide influenza epidemics each winter, and are a major public health concern and cause of morbidity and mortality. A substantial reduction in influenza-related deaths can be attributed to both vaccination and administration of oseltamivir (OS), which is approved for oral administration and inhibits viral neuraminidase (NA), a transmembrane protein. OS carboxylate (OSC), the active form of OS, is formed by the action of endogenous esterase, which targets NA and is shown to significantly reduce influenza-related deaths. However, the development of resistance in various viral variants, including H3N2 and H5N1, has raised concern about the effectiveness of OS. This comprehensive review covers a range of OS analogs shown to be effective against influenza virus, comparing different types of substituent group that contribute to the activity and bioavailability of these compounds.
Identifiants
pubmed: 32554062
pii: S1359-6446(20)30229-4
doi: 10.1016/j.drudis.2020.06.004
pii:
doi:
Substances chimiques
Antiviral Agents
0
Oseltamivir
20O93L6F9H
Neuraminidase
EC 3.2.1.18
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
1389-1402Informations de copyright
Copyright © 2020 Elsevier Ltd. All rights reserved.