calcium-dependent protein kinase 1 (CDPK1) is a promising target for drug development against cryptosporidiosis. We report a series of low-nanomolar CDPK1 5-aminopyrazole-4-carboxamide (AC) scaffold inhibitors that also potently inhibit growth Correlation between anti-CDPK1 and growth inhibition, as previously reported for pyrazolopyrimidines, was not apparent. Nonetheless, lead AC compounds exhibited a substantial reduction of parasite burden in the neonatal mouse cryptosporidiosis model when dosed at 25 mg/kg.
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| http://dx.doi.org/10.1128/AAC.00020-17 | DOI Listing |
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