Browsing by Author "Mead, Jan R."
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Item Phthalazinone inhibitors of inosine-5?-monophosphate dehydrogenase from Cryptosporidium parvum(Bioorganic and Medicinal Chemistry Letters, 2014-02) Johnson, Corey R.; Gorla, Suresh K.; Kavitha, Mandapati; Zhang, Minjia; Liu, Xiaoping; Striepen, Boris; Mead, Jan R.; Cuny, Gregory D.; Hedstrom, LizbethCryptosporidium parvum (Cp) is a potential biowarfare agent and major cause of diarrhea and malnutrition. This protozoan parasite relies on inosine 5?-monophosphate dehydrogenase (IMPDH) for the production of guanine nucleotides. A CpIMPDH-selective N-aryl-3,4-dihydro-3-methyl-4-oxo-1-phthalazineacetamide inhibitor was previously identified in a high throughput screening campaign. Herein we report a structure–activity relationship study for the phthalazinone-based series that resulted in the discovery of benzofuranamide analogs that exhibit low nanomolar inhibition of CpIMPDH. In addition, the antiparasitic activity of select analogs in a Toxoplasma gondii model of C. parvum infection is also presented.