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1,2,3-Triazolyl-4-oxoquinolines: A feasible beginning for promising chemical structures to inhibit oseltamivir-resistant influenza A and B viruses

2015; Elsevier BV; Volume: 23; Issue: 24 Linguagem: Inglês

10.1016/j.bmc.2015.11.028

1464-3391

Fernanda da Costa Santos Boechat, Carolina Q. Sacramento, Anna C. Cunha, Fernanda S. Sagrillo, Christiane Mapheu Nogueira, Natália Fintelman-Rodrigues, Osvaldo A. Santos‐Filho, Cecília S. Riscado, Luana da Silva Magalhães Forezi, Letícia V. Faro, Leonardo Brozeguini, Isakelly P. Marques, Vı́tor F. Ferreira, Thiago Moreno L. Souza, Maria Cecília B. V. de Souza,

Click Chemistry and Applications

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 0.2 μM 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.