R75761, a lead compound for the development of antiviral drugs in late stage poliomyelitis eradication strategies and beyond.
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.
Thys
Bert
B
Department of Pharmaceutical Biotechnology and Molecular Biology, Vrije Universiteit Brussel, Laarbeeklaan 103, B-1090 Brussels, Belgium. bert.thys@vub.ac.be
De Palma
Armando M
AM
Neyts
Johan
J
Andries
Koen
K
Vrijsen
Raf
R
Rombaut
Bart
B
D000998:Antiviral Agents / Q000494:pharmacology*; D003588:Cytopathogenic Effect, Viral / Q000187:drug effects; D006367:HeLa Cells; D006801:Humans; D011051:Poliomyelitis / Q000188:drug therapy / Q000517:prevention & control* / Q000821:virology; D017955:Poliovirus / Q000145:classification / Q000187:drug effects* / Q000502:physiology; D011055:Poliovirus Vaccine, Oral; D011724:Pyridazines / Q000737:chemistry / Q000494:pharmacology*; D014779:Virus Replication / Q000187:drug effects
D000998:Antiviral Agents; D011055:Poliovirus Vaccine, Oral; D011724:Pyridazines