Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 5, Issue 1, Pages 40-44Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml400315s
Keywords
Toxoplasma gondii; Cryptosporidium parvum; calcium-dependent protein kinase-1; enzyme inhibitor; selectivity
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Funding
- University of Washington Plein Endowment for Geriatric Pharmacy Research
- National Institute of Allergy and Infectious Diseases [T32AI007509]
- National Institute of General Medical Sciences of the National Institutes of Health [T32AI007509, R01AI089441, R01GM086858]
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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.
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