tetano
Editor, Senior Moderator
Arch Pharm (Weinheim). 2019 Sep 18:e1900028. doi: 10.1002/ardp.201900028. [Epub ahead of print]
[h=1]Novel N-(1-thia-4-azaspiro[4.5]decan-4-yl)carboxamide derivatives as potent and selective influenza virus fusion inhibitors.[/h] G?ktaş F[SUP]1[/SUP], ?zbil M[SUP]2[/SUP], Cesur N[SUP]1[/SUP], Vanderlinden E[SUP]3[/SUP], Naesens L[SUP]3[/SUP], Cesur Z[SUP]1[/SUP].
[h=3]Author information[/h] 1 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Istanbul University, Istanbul, Turkey. 2 Department of Molecular Biology and Genetics, Istanbul Arel University, Istanbul, Turkey. 3 Department of Microbiology, Immunology and Transplantation, Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, KU Leuven, Leuven, Belgium.
[h=3]Abstract[/h] Hemagglutinin is the surface protein of the influenza virus that mediates both binding and penetration of the virus into host cells. We here report on the synthesis and structure-activity relationship of some novel N-(1-thia-4-azaspiro[4.5]decan-4-yl)-carboxamide compounds carrying the 5-chloro-2-methoxybenzamide structure, designed as influenza virus fusion inhibitors. The carboxamides (1a-h, 2a-h) have a similar backbone structure as the fusion inhibitors that we reported on previously. Compounds 2b and 2d displayed inhibitory activity against influenza A/H3N2 virus replication (average antiviral EC[SUB]50[/SUB] : 2.1 ?M for 2b and 3.4 ?M for 2d). Data obtained in the hemolysis inhibition assay supported that these compounds act as inhibitors of the influenza virus hemagglutinin-mediated fusion process.
? 2019 Deutsche Pharmazeutische Gesellschaft.
[h=4]KEYWORDS:[/h] antiviral activity; cycloaddition; influenza virus; structure elucidation; synthesis
PMID: 31531897 DOI: 10.1002/ardp.201900028
[h=1]Novel N-(1-thia-4-azaspiro[4.5]decan-4-yl)carboxamide derivatives as potent and selective influenza virus fusion inhibitors.[/h] G?ktaş F[SUP]1[/SUP], ?zbil M[SUP]2[/SUP], Cesur N[SUP]1[/SUP], Vanderlinden E[SUP]3[/SUP], Naesens L[SUP]3[/SUP], Cesur Z[SUP]1[/SUP].
[h=3]Author information[/h] 1 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Istanbul University, Istanbul, Turkey. 2 Department of Molecular Biology and Genetics, Istanbul Arel University, Istanbul, Turkey. 3 Department of Microbiology, Immunology and Transplantation, Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, KU Leuven, Leuven, Belgium.
[h=3]Abstract[/h] Hemagglutinin is the surface protein of the influenza virus that mediates both binding and penetration of the virus into host cells. We here report on the synthesis and structure-activity relationship of some novel N-(1-thia-4-azaspiro[4.5]decan-4-yl)-carboxamide compounds carrying the 5-chloro-2-methoxybenzamide structure, designed as influenza virus fusion inhibitors. The carboxamides (1a-h, 2a-h) have a similar backbone structure as the fusion inhibitors that we reported on previously. Compounds 2b and 2d displayed inhibitory activity against influenza A/H3N2 virus replication (average antiviral EC[SUB]50[/SUB] : 2.1 ?M for 2b and 3.4 ?M for 2d). Data obtained in the hemolysis inhibition assay supported that these compounds act as inhibitors of the influenza virus hemagglutinin-mediated fusion process.
? 2019 Deutsche Pharmazeutische Gesellschaft.
[h=4]KEYWORDS:[/h] antiviral activity; cycloaddition; influenza virus; structure elucidation; synthesis
PMID: 31531897 DOI: 10.1002/ardp.201900028