Design,synthesis, and biological evaluation of novel coxsackievirus B3 inhibitors |
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| Authors: | Michal Šála Armando M De Palma Hubert Hřebabecký Radim Nencka Martin Dračínský Pieter Leyssen Johan Neyts Antonín Holý |
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| Institution: | 1. Gilead Sciences & IOCB Research Centre, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v.v.i, 166 10 Prague 6, Czech Republic;2. Rega Institute for Medical Research, Minderbroedersstraat 10, BE-3000 Leuven, Belgium |
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| Abstract: | The synthesis and SAR study of a novel class of coxsackievirus B3 (CVB3) inhibitors are reported. These compounds could be considered as the 6-chloropurines substituted at position 9 with variously substituted bicyclic scaffolds (bicyclo2.2.1]heptane/ene—norbornane or norbornene). The synthesis and biological evaluation of 31 target compounds are described. Several of the analogues inhibited CVB3 in the low micromolar range (0.66–2 μM). Minimal or no cytotoxicity was observed. |
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