R75761，一种用于晚期脊髓灰质炎根除策略及后续抗病毒药物研发的先导化合物。

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

作者信息

Thys Bert, De Palma Armando M, Neyts Johan, Andries Koen, Vrijsen Raf, Rombaut Bart

机构信息

Department of Pharmaceutical Biotechnology and Molecular Biology, Vrije Universiteit Brussel, Laarbeeklaan 103, B-1090 Brussels, Belgium.

出版信息

Antiviral Res. 2008 Jun;78(3):278-81. doi: 10.1016/j.antiviral.2008.01.002. Epub 2008 Feb 4.

DOI:10.1016/j.antiviral.2008.01.002

PMID:18294707

Abstract

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 (EC50) 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.

摘要

在本研究中，对240种哒嗪胺类似物中的18种进行了抗病毒活性评估，以检测其对三种脊髓灰质炎病毒型别（Sabin株）的作用。我们发现一种化合物R75761，它对所有三种脊髓灰质炎病毒Sabin株的50%有效浓度（EC50）值相当。对于1型、2型和3型脊髓灰质炎病毒，病毒增殖分别降低了10(4.0)倍、10(6.2)倍和10(6.6)倍。R75761可被视为开发用于脊髓灰质炎病毒根除后期及以后阶段的抗脊髓灰质炎病毒药物的先导化合物。