Inhibitory effect of thiosemicarbazone derivatives on Junin virus replication in vitro
The inhibitory effect of several thiosemicarbazones (TSCs), synthesized from aromatic ketones and terpenones, and their heterocyclic thiadiazoline (TDZ) derivatives, was investigated against Junin virus (JUNV), an arenavirus agent of Argentine haemorrhagic fever. From the 25 compounds tested, six co...
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2003
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| Acceso en línea: | https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_09563202_v14_n2_p99_Garcia http://hdl.handle.net/20.500.12110/paper_09563202_v14_n2_p99_Garcia |
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paper:paper_09563202_v14_n2_p99_Garcia2023-06-08T15:56:00Z Inhibitory effect of thiosemicarbazone derivatives on Junin virus replication in vitro Antiviral Arenavirus Haemorrhagic fever Junin virus Thiosemicarbazone derivatives 1 tetralone derivative ketone terpenoid thiazolidine derivative thiosemicarbazone animal cell antiviral activity Arenavirus article cyclization hemorrhagic fever Junin virus nonhuman priority journal protein expression structure activity relation virion virus infection virus inhibition virus replication The inhibitory effect of several thiosemicarbazones (TSCs), synthesized from aromatic ketones and terpenones, and their heterocyclic thiadiazoline (TDZ) derivatives, was investigated against Junin virus (JUNV), an arenavirus agent of Argentine haemorrhagic fever. From the 25 compounds tested, six compounds belonging to the TSC group were found to be selective inhibitors of JUNV, with EC 50 values determined by a virus yield inhibition assay in the range 3.4-12.5 μM, and selectivity indices greater than 10. By contrast, most of the TDZs obtained by heterocyclization of the TSCs were not active against JUNV. No conclusive structure-activity relationships could be established but systematically higher activity was associated to TSCs derived from aromatic ketones. The mode of action of one of the most active compound, the 3,4-dihydronaphtalen-1(2H)one thiosemicarbazone (tetralone thiosemicarbazone), was studied further. This TSC lacked virucidal effects on JUNV virions. Results from time of addition experiments and viral protein expression assays suggest that tetralone thiosemicarbazone inhibited a late stage in the replicative cycle of JUNV. 2003 https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_09563202_v14_n2_p99_Garcia http://hdl.handle.net/20.500.12110/paper_09563202_v14_n2_p99_Garcia |
| institution |
Universidad de Buenos Aires |
| institution_str |
I-28 |
| repository_str |
R-134 |
| collection |
Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) |
| topic |
Antiviral Arenavirus Haemorrhagic fever Junin virus Thiosemicarbazone derivatives 1 tetralone derivative ketone terpenoid thiazolidine derivative thiosemicarbazone animal cell antiviral activity Arenavirus article cyclization hemorrhagic fever Junin virus nonhuman priority journal protein expression structure activity relation virion virus infection virus inhibition virus replication |
| spellingShingle |
Antiviral Arenavirus Haemorrhagic fever Junin virus Thiosemicarbazone derivatives 1 tetralone derivative ketone terpenoid thiazolidine derivative thiosemicarbazone animal cell antiviral activity Arenavirus article cyclization hemorrhagic fever Junin virus nonhuman priority journal protein expression structure activity relation virion virus infection virus inhibition virus replication Inhibitory effect of thiosemicarbazone derivatives on Junin virus replication in vitro |
| topic_facet |
Antiviral Arenavirus Haemorrhagic fever Junin virus Thiosemicarbazone derivatives 1 tetralone derivative ketone terpenoid thiazolidine derivative thiosemicarbazone animal cell antiviral activity Arenavirus article cyclization hemorrhagic fever Junin virus nonhuman priority journal protein expression structure activity relation virion virus infection virus inhibition virus replication |
| description |
The inhibitory effect of several thiosemicarbazones (TSCs), synthesized from aromatic ketones and terpenones, and their heterocyclic thiadiazoline (TDZ) derivatives, was investigated against Junin virus (JUNV), an arenavirus agent of Argentine haemorrhagic fever. From the 25 compounds tested, six compounds belonging to the TSC group were found to be selective inhibitors of JUNV, with EC 50 values determined by a virus yield inhibition assay in the range 3.4-12.5 μM, and selectivity indices greater than 10. By contrast, most of the TDZs obtained by heterocyclization of the TSCs were not active against JUNV. No conclusive structure-activity relationships could be established but systematically higher activity was associated to TSCs derived from aromatic ketones. The mode of action of one of the most active compound, the 3,4-dihydronaphtalen-1(2H)one thiosemicarbazone (tetralone thiosemicarbazone), was studied further. This TSC lacked virucidal effects on JUNV virions. Results from time of addition experiments and viral protein expression assays suggest that tetralone thiosemicarbazone inhibited a late stage in the replicative cycle of JUNV. |
| title |
Inhibitory effect of thiosemicarbazone derivatives on Junin virus replication in vitro |
| title_short |
Inhibitory effect of thiosemicarbazone derivatives on Junin virus replication in vitro |
| title_full |
Inhibitory effect of thiosemicarbazone derivatives on Junin virus replication in vitro |
| title_fullStr |
Inhibitory effect of thiosemicarbazone derivatives on Junin virus replication in vitro |
| title_full_unstemmed |
Inhibitory effect of thiosemicarbazone derivatives on Junin virus replication in vitro |
| title_sort |
inhibitory effect of thiosemicarbazone derivatives on junin virus replication in vitro |
| publishDate |
2003 |
| url |
https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_09563202_v14_n2_p99_Garcia http://hdl.handle.net/20.500.12110/paper_09563202_v14_n2_p99_Garcia |
| _version_ |
1768542229043871744 |