Title: Discovery of dihydro-alkyloxy-benzyl-oxopyrimidines as promising anti-influenza virus agents
Authors: Yu, Mingyan ×
Liu, Ailin
Du, Guanhua
Naesens, Lieve
Vanderlinden, Evelien
De Clercq, Erik
Liu, Xinyong #
Issue Date: Oct-2011
Publisher: Blackwell Munksgaard
Series Title: Chemical Biology & Drug Design vol:78 issue:4 pages:596-602
Article number: 10.1111/j.1747-0285.2011.01180.x
Abstract: A series of novel dihydro-alkyloxy-benzyl-oxopyrimidine derivatives were synthesized and evaluated for their activity against influenza virus in Madin-Darby canine kidney cells. Four dihydro-alkyloxy-benzyl-oxopyrimidine derivatives (4a1, 4a2, 4a3, and 4d1) showed potent activity against influenza virus. Among them, compound 4a3 was the most promising lead with broad activity against influenza A (antiviral EC(50) values of 9 and 18 μm for the A/H1N1 and A/H3N2 subtype, respectively) and influenza B viruses (EC(50) : 33 μm). The antiviral mechanism of action of these dihydro-alkyloxy-benzyl-oxopyrimidine derivatives must be quite different from that of the currently approved anti-influenza virus drugs that target the viral M2 or neuraminidase proteins. The dihydro-alkyloxy-benzyl-oxopyrimidine derivatives represent a new avenue for further optimization and development of novel anti-influenza virus agents.
ISSN: 1747-0277
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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