Anti-viral agents against Coxsackievirus B3 (CVB3) were developed with a strategy to inhibit 3C protease (CVB3 3Cpro), a well known target for the development of therapeutic agents for CVB3 mediated myocarditis or pericarditis. Hetero-aromatic group substituted peptidomimetic analogs with a Michael acceptor were synthesized and evaluated for the inhibitory activity against CVB3 3Cpro and antiviral effects. The substitutions of heteraromatic groups generally increase the inhibitory activity of CVB3 3Cpro. The potent protease inhibitors (9c and e ) with quinoline groups with IC50 values 130~ 280 nM also significantly inhibited the CVB3 mediated cell cytotoxicity. The binding mode of one of the potent inhibitor (9e ) was explored by a molecular docking study.

Development of anticoxackievirus agents targeting 3C protease

243rd National Meeting (2012)

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