SAR studies of 9-norbornylpurines as Coxsackievirus B3 inhibitors |
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Authors: | Sála Michal De Palma Armando M Hřebabecký Hubert Dejmek Milan Dračínský Martin Leyssen Pieter Neyts Johan Mertlíková-Kaiserová Helena Nencka Radim |
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Institution: | a Gilead Sciences & IOCB Research Centre, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v.v.i, Flemingovo nám. 2, 166 10 Prague 6, Czech Republic b Rega Institute for Medical Research, Minderbroedersstraat 10, BE-3000, Leuven, Belgium |
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Abstract: | Coxsackievirus and related enteroviruses are important human pathogens that cause various diseases with clinical manifestations ranging from trivial flu-like syndromes to dangerous or even fatal diseases such as myocarditis, meningitis and encephalitis. Here, we report on our continuous SAR study focused on 9-(bicyclo2.2.1]hept-2-yl)-9H-purines as anti-enteroviral inhibitors. The purine moiety was modified at positions 2, 6 and 8. Several analogues inhibited Coxsackievirus B3 as well as other enteroviruses at low-micromolar concentrations. The 6-chloropurine derivative was confirmed as the most active compound in this series. |
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Keywords: | Coxsackievirus Norbornane Antiviral Purine Picornaviruses |
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