Structure-based drug design of potent pyrazole derivatives against Rhinovirus replication
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Da Costa L., Scheers E., Coluccia A., Casulli A., Roche M., Di Giorgio C., Neyts J., Terme T., Cirilli R., La Regina G., Silvestri R., Mirabelli C., Vanelle P.
ISSN: 0022-2623
Rhinoviruses (RVs) have been linked to exacerbations of many pulmonary diseases, thus increasing morbidity and/or mortality in subjects at risk. Unfortunately, the wide variety of RV genotypes constitutes a major hindrance for the development of Rhinovirus replication inhibitors. In the current investigation, we have developed a novel series of pyrazole derivatives that potently inhibit the Rhinovirus replication. Compounds 10e and 10h behave as early stage inhibitors of Rhinovirus infection with a broad-spectrum activity against RV-A and RV-B species (EC50