Phenoxazine nucleoside derivatives with a multiple activity against RNA and DNA viruses.
Eur J Med Chem
; 220: 113467, 2021 Aug 05.
Article
in English
| MEDLINE | ID: covidwho-1184952
ABSTRACT
Emerging and re-emerging viruses periodically cause outbreaks and epidemics all over the world, eventually leading to global events such as the current pandemic of the novel SARS-CoV-2 coronavirus infection COVID-19. Therefore, an urgent need for novel antivirals is crystal clear. Here we present the synthesis and evaluation of an antiviral activity of phenoxazine-based nucleoside analogs divided into three groups (1) 8-alkoxy-substituted, (2) acyclic, and (3) carbocyclic. The antiviral activity was assessed against a structurally and phylogenetically diverse panel of RNA and DNA viruses from 25 species. Four compounds (11a-c, 12c) inhibited 4 DNA/RNA viruses with EC50 ≤ 20 µM. Toxicity of the compounds for the cell lines used for virus cultivation was negligible in most cases. In addition, previously reported and newly synthesized phenoxazine derivatives were evaluated against SARS-CoV-2, and some of them showed promising inhibition of reproduction with EC50 values in low micromolar range, although accompanied by commensurate cytotoxicity.
Keywords
Full text:
Available
Collection:
International databases
Database:
MEDLINE
Main subject:
Antiviral Agents
/
Oxazines
/
DNA Viruses
/
SARS-CoV-2
/
Nucleosides
Type of study:
Experimental Studies
/
Randomized controlled trials
Limits:
Animals
/
Humans
Language:
English
Journal:
Eur J Med Chem
Year:
2021
Document Type:
Article
Affiliation country:
J.ejmech.2021.113467
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