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.
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.
authors.forename: Zhenyu
authors.initials: Z
authors.lastname: Li
authors.forename: Peng
authors.initials: P
authors.lastname: Zhan
authors.forename: Lieve
authors.initials: L
authors.lastname: Naesens
authors.forename: Evelien
authors.initials: E
authors.lastname: Vanderlinden
authors.forename: Ailin
authors.initials: A
authors.lastname: Liu
authors.forename: Guanhua
authors.initials: G
authors.lastname: Du
authors.forename: Erik
authors.initials: E
authors.lastname: De Clercq
authors.forename: Xinyong
authors.initials: X
authors.lastname: Liu
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001549:Benzamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001583:Benzoxazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D004285:Dogs; D053122:Influenza A Virus, H3N2 Subtype / Q000187:drug effects*; D009981:Influenza B virus / Q000187:drug effects; D053139:Oseltamivir / Q000494:pharmacology
chemical_list: D000998:Antiviral Agents; D001549:Benzamides; D001583:Benzoxazoles; C574248:N-(4-(5-(3,4-dimethoxybenzamido)benzo(d)oxazol-2-yl)phenyl)-3,4-dimethoxybenzamide; D053139:Oseltamivir