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Phenoxazine nucleoside derivatives with a multiple activity against RNA and DNA viruses
- Source :
- European Journal of Medicinal Chemistry
- Publication Year :
- 2021
- Publisher :
- ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER, 2021.
-
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.<br />Graphical abstract Image 1
- Subjects :
- RNA viruses
Microbial Sensitivity Tests
medicine.disease_cause
Virus Replication
01 natural sciences
Antiviral Agents
Article
Madin Darby Canine Kidney Cells
03 medical and health sciences
chemistry.chemical_compound
Structure-Activity Relationship
Dogs
Cell Line, Tumor
Drug Discovery
Chlorocebus aethiops
Oxazines
medicine
Structure–activity relationship
Animals
Humans
Phenoxazine
Vero Cells
030304 developmental biology
Coronavirus
Pharmacology
0303 health sciences
Nucleoside analogue
Molecular Structure
010405 organic chemistry
Chemistry
SARS-CoV-2
Organic Chemistry
DNA Viruses
RNA
Nucleosides
General Medicine
Antivirals
Virology
0104 chemical sciences
Viral replication
Nucleoside analogs
DNA viruses
Nucleoside
DNA
medicine.drug
Subjects
Details
- Language :
- English
- Database :
- OpenAIRE
- Journal :
- European Journal of Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....aa16fb4d0619f7f9ca6148418439dee0