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Rational modifications on a benzylidene-acrylohydrazide antiviral scaffold, synthesis and evaluation of bioactivity against Chikungunya virus.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2018 Apr 10; Vol. 149, pp. 56-68. Date of Electronic Publication: 2018 Feb 23. - Publication Year :
- 2018
-
Abstract
- Chikungunya virus is a re-emerging arbovirus transmitted to humans by Aedes mosquitoes, responsible for an acute febrile illness associated with painful and debilitating arthralgia, which can persist for several months or become chronic. Over the past few years, infection with this virus has spread worldwide with a previously unknown virulence. No specific antiviral treatments nor vaccines are currently available against this important pathogen. Starting from the structure of a class of selective anti-CHIKV agents previously identified in our research group, different modifications to this scaffold were rationally designed, and 69 novel small-molecule derivatives were synthesised and evaluated for their inhibition of Chikungunya virus replication in Vero cells. Further structure-activity relationships associated with this class of antiviral agents were elucidated for the original scaffolds, and novel antiviral compounds with EC <subscript>50</subscript> values in the low micromolar range were identified. This work provides the foundation for further investigation of these new structures as antivirals against Chikungunya virus.<br /> (Copyright © 2018 Elsevier Masson SAS. All rights reserved.)
- Subjects :
- Animals
Antiviral Agents chemistry
Benzylidene Compounds pharmacology
Chlorocebus aethiops
Humans
Hydrazines pharmacology
Structure-Activity Relationship
Vero Cells
Virus Replication drug effects
Antiviral Agents chemical synthesis
Benzylidene Compounds chemical synthesis
Chikungunya virus drug effects
Hydrazines chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 149
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 29499487
- Full Text :
- https://doi.org/10.1016/j.ejmech.2018.02.054