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SAR studies of 9-norbornylpurines as Coxsackievirus B3 inhibitors

M. Sála, AM. De Palma, H. Hřebabecký, M. Dejmek, M. Dračínský, P. Leyssen, J. Neyts, H. Mertlíková-Kaiserová, R. Nencka,

. 2011 ; 21 (14) : 4271-5. [pub] 20110527

Language English Country England, Great Britain

Document type Journal Article, Research Support, Non-U.S. Gov't

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-(bicyclo[2.2.1]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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