3 research outputs found
The gatekeeper residue and beyond: homologous calcium-dependent protein kinases as drug development targets for veterinarian Apicomplexa parasites
Potent and Selective Inhibitors of CDPK1 from <i>T. gondii</i> and <i>C. parvum</i> Based on a 5‑Aminopyrazole-4-carboxamide Scaffold
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 <i>Toxoplasma gondii</i> and <i>Cryptosporidium parvum</i>. Compounds with low nanomolar inhibitory
potencies against the target enzymes were obtained. The most selective
inhibitors also exhibited submicromolar activities in <i>T. gondii</i> cell proliferation assays and were shown to be nontoxic to mammalian
cells