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Chem Biol Drug Des. 2012 Jan 27. doi: 10.1111/j.1747-0285.2012.01344.x. [Epub ahead of print]
Synthesis and preliminary biological evaluation of 5-substituted-2-(4-substituted phenyl)-1,3-benzoxazoles as a novel class of influenza virus A inhibitors.
Li Z, Zhan P, Naesens L, Vanderlinden E, Liu A, Du G, De Clercq E, Liu X.
Source
Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, 250012, Jinan, Shandong, P.R.China. Rega Institute for Medical Research, Katholieke Universiteit Leuven, B-3000 Leuven, Belgium Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China.
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 (IFV-A) and anti-influenza B virus (IFV-B) activity. The activity was monitored by the MTS assay in the Madin-Darby canine kidney (MDCK) 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. ? 2012 John Wiley & Sons A/S.
? 2012 John Wiley & Sons A/S.
PMID:
22284752
[PubMed - as supplied by publisher]
Synthesis and preliminary biological evaluation of 5-substituted-2-(4-substituted phenyl)-1,3-benzoxazoles as a novel class of influenza virus A inhibitors.
Li Z, Zhan P, Naesens L, Vanderlinden E, Liu A, Du G, De Clercq E, Liu X.
Source
Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, 250012, Jinan, Shandong, P.R.China. Rega Institute for Medical Research, Katholieke Universiteit Leuven, B-3000 Leuven, Belgium Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China.
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 (IFV-A) and anti-influenza B virus (IFV-B) activity. The activity was monitored by the MTS assay in the Madin-Darby canine kidney (MDCK) 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. ? 2012 John Wiley & Sons A/S.
? 2012 John Wiley & Sons A/S.
PMID:
22284752
[PubMed - as supplied by publisher]
