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Synthesis and Preliminary Biologic Evaluation of 5‐Substituted‐2‐(4‐substituted phenyl)‐1,3‐Benzoxazoles as A Novel Class of Influenza Virus A Inhibitors
Author(s) -
Li Zhenyu,
Zhan Peng,
Naesens Lieve,
Vanderlinden Evelien,
Liu Ailin,
Du Guanhua,
De Clercq Erik,
Liu Xinyong
Publication year - 2012
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2012.01344.x
Subject(s) - virus , in vitro , oseltamivir , chemistry , influenza a virus , lead compound , virology , combinatorial chemistry , stereochemistry , biochemistry , biology , covid-19 , medicine , disease , pathology , infectious disease (medical specialty)
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 μ m , SI > 5), which were all higher than that of the reference drug oseltamivir (EC 50 > 59.00 μ m , SI > 1). However, no compound displays inhibitory activity against influenza B virus.