R75761, a lead compound for the development of antiviral drugs in late stage poliomyelitis eradication strategies and beyond

被引:6
|
作者
Thys, Bert [1 ]
De Palma, Armando M. [2 ]
Neyts, Johan [2 ]
Andries, Koen [3 ]
Vrijsen, Raf [1 ]
Rombaut, Bart [1 ]
机构
[1] Vrije Univ Brussel, Dept Pharmaceut Biotechnol & Mol Biol, B-1090 Brussels, Belgium
[2] Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Louvain, Belgium
[3] Johnson & Johnson Pharmaceut Res & Dev, B-2340 Beerse, Belgium
关键词
anti-poliovirus compound; polio eradication; pyridazinamine analogue; picornavirus; poliovirus;
D O I
10.1016/j.antiviral.2008.01.002
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
In this study the antiviral activity of a panel of 18 out of 240 pyridazinamine analogues was evaluated against the Sabin strains of the three poliovirus types. We found one compound, R75761 which had a comparable 50% effective concentration (EC(50)) value against all three poliovirus Sabin strains. Virus multiplication was reduced by 10(4.0)-fold, 10(6.2)-fold and 10(6.6)-fold for poliovirus type 1, type 2 and type 3, respectively. R75761 could be considered as a lead compound for development of anti-poliovirus drugs to be used during the late stage of poliovirus eradication and beyond. (C) 2008 Elsevier B.V. All rights reserved.
引用
收藏
页码:278 / 281
页数:4
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