1,2,3-Triazolyl-4-oxoquinolines: A feasible beginning for promising chemical structures to inhibit oseltamivir-resistant influenza A and B viruses | Health & Environmental Research Online (HERO)

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Citation
Tags

HERO ID

7221304

Reference Type

Journal Article

Title

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

Author(s)

Boechat, FdaC; Sacramento, CQ; Cunha, AC; Sagrillo, FS; Nogueira, CM; Fintelman-Rodrigues, N; Santos-Filho, O; Riscado, CS; Forezi, LdaS; Faro, LV; Brozeguini, L; Marques, IP; Ferreira, VF; Souza, TM; de Souza, MC; ,

Year

2015

Is Peer Reviewed?

Yes

Journal

Bioorganic & Medicinal Chemistry
ISSN: 0968-0896
EISSN: 1464-3391

Language

English

PMID

26643220

DOI

10.1016/j.bmc.2015.11.028

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.