| Literature DB >> 26643220 |
Fernanda da C S Boechat1, Carolina Q Sacramento2, Anna C Cunha1, Fernanda S Sagrillo1, Christiane M Nogueira1, Natalia Fintelman-Rodrigues2, Osvaldo Santos-Filho3, Cecília S Riscado1, Luana da S M Forezi1, Letícia V Faro1, Leonardo Brozeguini1, Isakelly P Marques1, Vitor F Ferreira1, Thiago Moreno L Souza2, Maria Cecília B V de Souza4.
Abstract
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 EC50 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.Entities:
Keywords: 1,2,3-Triazole; 4-Oxoquinoline; Antiviral resistance; Influenza viruses; Neuraminidase inhibitors; Oseltamivir carboxylate
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Year: 2015 PMID： 26643220 DOI： 10.1016/j.bmc.2015.11.028
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641