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New class of hantaan virus inhibitors based on conjugation of the isoindole fragment to (+)-camphor or (-)-fenchone hydrazonesv
- Source :
- Bioorganicmedicinal chemistry letters. 40
- Publication Year :
- 2020
-
Abstract
- This work presents the design and synthesis of camphor, fenchone, and norcamphor N-acylhydrazone derivatives as a new class of inhibitors of the Hantaan virus, which causes haemorrhagic fever with renal syndrome (HFRS). A cytopathic model was developed for testing chemotherapeutics against the Hantaan virus, strain 76–118. In addition, a study of the antiviral activity was carried out using a pseudoviral system. It was found that the hit compound possesses significant activity (IC50 = 7.6 ± 2 µM) along with low toxicity (CC50 > 1000 µM). Using molecular docking procedures, the binding with Hantavirus nucleoprotein was evaluated and the correlation between the structure of the synthesised compounds and the antiviral activity was established.
- Subjects :
- Clinical Biochemistry
Pharmaceutical Science
Microbial Sensitivity Tests
Norcamphor
Isoindoles
Biochemistry
Antiviral Agents
Madin Darby Canine Kidney Cells
chemistry.chemical_compound
Camphor
Dogs
Drug Discovery
Animals
Humans
Molecular Biology
Hantaan virus
Hantavirus
Camphanes
Strain (chemistry)
Viral Core Proteins
Organic Chemistry
Hydrazones
virus diseases
Virology
Norbornanes
Fenchone
Nucleoprotein
Molecular Docking Simulation
HEK293 Cells
chemistry
Drug Design
Molecular Medicine
Capsid Proteins
Isoindole
Protein Binding
Subjects
Details
- ISSN :
- 14643405
- Volume :
- 40
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....5da4e7aecb709e0cd64c4597c1a1963b