Phthalazinone inhibitors of inosine-5?-monophosphate dehydrogenase from Cryptosporidium parvum

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dc.contributor.authorJohnson, Corey R.
dc.contributor.authorGorla, Suresh K.
dc.contributor.authorKavitha, Mandapati
dc.contributor.authorZhang, Minjia
dc.contributor.authorLiu, Xiaoping
dc.contributor.authorStriepen, Boris
dc.contributor.authorMead, Jan R.
dc.contributor.authorCuny, Gregory D.
dc.contributor.authorHedstrom, Lizbeth
dc.date.accessioned2020-03-10T17:31:09Z
dc.date.available2020-03-10T17:31:09Z
dc.date.issued2014-02
dc.description.abstractCryptosporidium 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.
dc.identifier.citationCopyright 2013 Bioorganic and Medicinal Chemistry Letters. This is a post-print version of a published paper that is available at: https://www.sciencedirect.com/science/article/pii/S0960894X12016319. Recommended citation: Johnson, Corey R., Suresh Kumar Gorla, Mandapati Kavitha, Minjia Zhang, Xiaoping Liu, Boris Striepen, Jan R. Mead, Gregory D. Cuny, and Lizbeth Hedstrom. "Phthalazinone inhibitors of inosine-5?-monophosphate dehydrogenase from Cryptosporidium parvum." Bioorganic & medicinal chemistry letters 23, no. 4 (2013): 1004-1007. doi: 10.1016/j.bmcl.2012.12.037. This item has been deposited in accordance with publisher copyright and licensing terms and with the author's permission.
dc.identifier.urihttps://hdl.handle.net/10657/5941
dc.language.isoen_US
dc.publisherBioorganic and Medicinal Chemistry Letters
dc.subjectIMPDH
dc.subjectIMP dehydrogenase
dc.subjectcryptosporidiosis
dc.subjectAntiparasitic
dc.titlePhthalazinone inhibitors of inosine-5?-monophosphate dehydrogenase from Cryptosporidium parvum
dc.typeArticle

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