tetano
Editor, Senior Moderator
Bioorg Med Chem. 2015 Nov 26. pii: S0968-0896(15)30153-X. doi: 10.1016/j.bmc.2015.11.028. [Epub ahead of print]
[h=1]1,2,3-Triazolyl-4-oxoquinolines: A feasible beginning for promising chemical structures to inhibit oseltamivir-resistant influenza A and B viruses.[/h] Boechat FD[SUP]1[/SUP], Sacramento CQ[SUP]2[/SUP], Cunha AC[SUP]1[/SUP], Sagrillo FS[SUP]1[/SUP], Nogueira CM[SUP]1[/SUP], Fintelman-Rodrigues N[SUP]2[/SUP], Santos-Filho O[SUP]3[/SUP], Riscado CS[SUP]1[/SUP], Forezi LD[SUP]1[/SUP], Faro LV[SUP]1[/SUP], Brozeguini L[SUP]1[/SUP], Marques IP[SUP]1[/SUP], Ferreira VF[SUP]1[/SUP], Souza TM[SUP]2[/SUP], de Souza MC[SUP]4[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] We described the synthesis of a new congener series of 1,2,3-triazolyl-4-oxoquinolines and evaluated their ability to inhibit oseltamivir (OST)-resistant influenza strains. Oxoquinoline derivative 1i was the most potent compound within this series, inhibiting 94% of wild-type (WT) influenza neuraminidase (NA) activity. Compound 1i inhibited influenza virus replication with an EC[SUB]50[/SUB] of 0.2μM with less cytotoxicity than OST, and also inhibited different OST-resistant NAs. These results suggest that 1,2,3-triazolyl-4-oxoquinolines represent promising lead molecules for further anti-influenza drug design.
Published by Elsevier Ltd.
[h=4]KEYWORDS:[/h] 1,2,3-Triazole; 4-Oxoquinoline; Antiviral resistance; Influenza viruses; Neuraminidase inhibitors; Oseltamivir carboxylate
PMID: 26643220 [PubMed - as supplied by publisher]
[h=1]1,2,3-Triazolyl-4-oxoquinolines: A feasible beginning for promising chemical structures to inhibit oseltamivir-resistant influenza A and B viruses.[/h] Boechat FD[SUP]1[/SUP], Sacramento CQ[SUP]2[/SUP], Cunha AC[SUP]1[/SUP], Sagrillo FS[SUP]1[/SUP], Nogueira CM[SUP]1[/SUP], Fintelman-Rodrigues N[SUP]2[/SUP], Santos-Filho O[SUP]3[/SUP], Riscado CS[SUP]1[/SUP], Forezi LD[SUP]1[/SUP], Faro LV[SUP]1[/SUP], Brozeguini L[SUP]1[/SUP], Marques IP[SUP]1[/SUP], Ferreira VF[SUP]1[/SUP], Souza TM[SUP]2[/SUP], de Souza MC[SUP]4[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] We described the synthesis of a new congener series of 1,2,3-triazolyl-4-oxoquinolines and evaluated their ability to inhibit oseltamivir (OST)-resistant influenza strains. Oxoquinoline derivative 1i was the most potent compound within this series, inhibiting 94% of wild-type (WT) influenza neuraminidase (NA) activity. Compound 1i inhibited influenza virus replication with an EC[SUB]50[/SUB] of 0.2μM with less cytotoxicity than OST, and also inhibited different OST-resistant NAs. These results suggest that 1,2,3-triazolyl-4-oxoquinolines represent promising lead molecules for further anti-influenza drug design.
Published by Elsevier Ltd.
[h=4]KEYWORDS:[/h] 1,2,3-Triazole; 4-Oxoquinoline; Antiviral resistance; Influenza viruses; Neuraminidase inhibitors; Oseltamivir carboxylate
PMID: 26643220 [PubMed - as supplied by publisher]
