Title: Synthesis and preliminary biologic evaluation of 5-substituted-2-(4-substituted phenyl)-1,3-benzoxazoles as a novel class of influenza virus A inhibitors
Authors: Li, Zhenyu ×
Zhan, Peng
Naesens, Lieve
Vanderlinden, Evelien
Liu, Ailin
Du, Guanhua
De Clercq, Erik
Liu, Xinyong #
Issue Date: Jun-2012
Publisher: Blackwell Munksgaard
Series Title: Chemical Biology & Drug Design vol:79 issue:6 pages:1018-1024
Article number: 10.1111/j.1747-0285.2012.01344.x
Abstract: The diversity-oriented chemistry synthesis together with the random screening approach has permitted the discovery and optimization of novel antiviral lead compounds. In this paper, a series of novel 5-substituted-2-(4-substituted phenyl)-1,3-benzoxazoles was synthesized and evaluated for their in vitro anti-influenza A virus and anti-influenza B virus activity. The activity was monitored by the MTS assay in the Madin-Darby canine kidney cells. Compound 7h showed excellent inhibitory activity and selective index against A/H3N2 (EC(50 ) = 37.03 μm, SI > 5), which were all higher than that of the reference drug oseltamivir (EC(50 ) > 59.00 μm, SI > 1). However, no compound displays inhibitory activity against influenza B virus.
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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