Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 16, Pages 5264-5267Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.06.050
Keywords
Cryptosporidium parvum; Toxoplasma gondii; Calcium-dependent protein kinase-1; Enzyme inhibitor; Selectivity
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Funding
- National Institutes of Health [R01AI089441, R01GM086858]
- training grant from the National Institute of Allergy and Infectious Diseases [T32AI007509]
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Calcium-dependent protein kinase-1 (CDPK1) from Cryptosporidium parvum (CpCDPK1) and Toxoplasma gondii (TgCDPK1) have become attractive targets for discovering selective inhibitors to combat infections caused by these protozoa. We used structure-based design to improve a series of benzoylbenzimidazole-based compounds in terms of solubility, selectivity, and potency against CpCDPK1 and TgCDPK1. The best inhibitors show inhibitory potencies below 50 nM and selectivity well above 200-fold over two human kinases with small gatekeeper residues. (c) 2012 Elsevier Ltd. All rights reserved.
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