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.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Boechat Fda C,Sacramento CQ,Cunha AC,Sagrillo FS,Nogueira CM,Fintelman-Rodrigues N,Santos-Filho O,Riscado CS,Forezi Lda S,Faro LV,Brozeguini L,Marques IP,Ferreira VF,Souza TM,de Souza MCdoi
10.1016/j.bmc.2015.11.028subject
Has Abstractpub_date
2015-12-15 00:00:00pages
7777-84issue
24eissn
0968-0896issn
1464-3391pii
S0968-0896(15)30153-Xjournal_volume
23pub_type
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