Zhang Z.,University of Washington |
Ojo K.K.,University of Washington |
Vidadala R.,University of Washington |
Huang W.,University of Washington |
And 18 more authors.
ACS Medicinal Chemistry Letters
5-Aminopyrazole-4-carboxamide was used as an alternative scaffold to substitute for the pyrazolopyrimidine of a known "bumped kinase inhibitor" to create selective inhibitors of calcium-dependent protein kinase-1 from both Toxoplasma gondii and Cryptosporidium parvum. Compounds with low nanomolar inhibitory potencies against the target enzymes were obtained. The most selective inhibitors also exhibited submicromolar activities in T. gondii cell proliferation assays and were shown to be nontoxic to mammalian cells. © 2013 American Chemical Society. Source