Article ; Online: Synthesis and anti-coronavirus activity of a series of 1-thia-4-azaspiro[4.5]decan-3-one derivatives.
2019 Volume 352, Issue 6, Page(s) e1800330
Abstract: A series of 1-thia-4-azaspiro[4.5]decan-3-ones bearing an amide group at C-4 and various ... active compound was N-(2-methyl-8-tert-butyl-3-oxo-1-thia-4-azaspiro[4.5]decan-4-yl)-3-phenylpropanamide ... substitutions at C-2 and C-8 were synthesized and evaluated against human coronavirus and influenza virus ...
| Abstract | A series of 1-thia-4-azaspiro[4.5]decan-3-ones bearing an amide group at C-4 and various substitutions at C-2 and C-8 were synthesized and evaluated against human coronavirus and influenza virus. Compounds 7m, 7n, 8k, 8l, 8m, 8n, and 8p were found to inhibit human coronavirus 229E replication. The most active compound was N-(2-methyl-8-tert-butyl-3-oxo-1-thia-4-azaspiro[4.5]decan-4-yl)-3-phenylpropanamide (8n), with an EC |
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| MeSH term(s) | Animals ; Antiviral Agents/chemical synthesis ; Antiviral Agents/chemistry ; Antiviral Agents/pharmacology ; Aza Compounds/chemical synthesis ; Aza Compounds/chemistry ; Aza Compounds/pharmacology ; Coronavirus/drug effects ; Cytopathogenic Effect, Viral/drug effects ; Dogs ; Drug Design ; Fibroblasts/drug effects ; Fibroblasts/virology ; Humans ; Madin Darby Canine Kidney Cells ; Molecular Structure ; Spiro Compounds/chemical synthesis ; Spiro Compounds/chemistry ; Spiro Compounds/pharmacology ; Structure-Activity Relationship ; Virus Replication/drug effects | |||||
| Chemical Substances | Antiviral Agents ; Aza Compounds ; Spiro Compounds | |||||
| Keywords | covid19 | |||||
| Language | English | |||||
| Publishing date | 2019-05-09 | |||||
| Publishing country | Germany | |||||
| Document type | Journal Article | |||||
| ZDB-ID | 6381-2 | |||||
| ISSN | 1521-4184 ; 0365-6233 ; 1437-1014 | |||||
| ISSN (online) | 1521-4184 | |||||
| ISSN | 0365-6233 ; 1437-1014 | |||||
| DOI | 10.1002/ardp.201800330 | |||||
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| Database | MEDical Literature Analysis and Retrieval System OnLINE |
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