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Title: 1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus
Authors: Geisman, Alexander N
Valuev-Elliston, Vladimir T
Ozerov, Alexander A
Khandazhinskaya, Anastasia L
Chizhov, Alexander O
Kochetkov, Sergey N
Pannecouque, Christophe
Naesens, Lieve
Seley-Radtke, Katherine L ×
Novikov, Mikhail S #
Issue Date: Jun-2016
Publisher: Pergamon
Series Title: Bioorganic & Medicinal Chemistry vol:24 issue:11 pages:2476-85
Article number: 10.1016/j.bmc.2016.04.010
Abstract: A series of 1,6-bis[(benzyloxy)methyl]uracil derivatives combining structural features of both diphenyl ether and pyridone types of NNRTIs were synthesized. Target compounds were found to inhibit HIV-1 reverse transcriptase at micro- and submicromolar levels of concentrations and exhibited anti-HIV-1 activity in MT-4 cell culture, demonstrating resistance profile similar to first generation NNRTIs. The synthesized compounds also showed profound activity against influenza virus (H1N1) in MDCK cell culture without detectable cytotoxicity. The lead compound of this assay appeared to exceed rimantadine, amantadine, ribavirin and oseltamivir carboxylate in activity. The mechanism of action of 1,6-bis[(benzyloxy)methyl]uracils against influenza virus is currently under investigation.
URI: 
ISSN: 0968-0896
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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