Key result
A new class of Michael acceptor-containing irreversible inhibitors demonstrated antiviral activity against HRV-14 infected H1-HeLa cells with EC50 values ranging from 1.94 to 0.15 microM.
Effect estimate: EC50 1.94 to 0.15 microM
A newly discovered class of Michael acceptor-containing irreversible inhibitors demonstrates potent in vitro antiviral activity against human rhinovirus 14.
Supports preclinical development of these HRV inhibitors; leaves open in vivo efficacy and clinical translation.
Utilizing the tools of parallel synthesis and structure-based design, a new class of Michael acceptor-containing, irreversible inhibitors of human rhinovirus 3C protease (HRV 3CP) was discovered. These inhibitors are shown to inhibit HRV-14 3CP with rates of inactivation ranging from 886 to 31 400 M(-1) sec(-1). These inhibitors exhibit antiviral activity when tested against HRV-14 infected H1-HeLa cells, with EC(50) values ranging from 1.94 to 0.15 microM. No cytotoxicity was observed at the limits of the assay concentration. A crystal structure of one of the more potent inhibitors covalently bound to HRV-2 3CP is detailed. These compounds were also tested against HRV serotypes other than type 14 and were found to have highly variable activities.
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Johnson et al. (2002) studied Human rhinovirus infection. Michael acceptor-containing irreversible inhibitors of HRV 3CP was evaluated on Antiviral activity against HRV-14 infected H1-HeLa cells (EC50 1.94 to 0.15 microM). A new class of Michael acceptor-containing irreversible inhibitors demonstrated antiviral activity against HRV-14 infected H1-HeLa cells with EC50 values ranging from 1.94 to 0.15 microM.
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