874584-98-2Relevant academic research and scientific papers
Phthalazinone inhibitors of inosine-5′-monophosphate dehydrogenase from Cryptosporidium parvum
Johnson, Corey R.,Gorla, Suresh Kumar,Kavitha, Mandapati,Zhang, Minjia,Liu, Xiaoping,Striepen, Boris,Mead, Jan R.,Cuny, Gregory D.,Hedstrom, Lizbeth
, p. 1004 - 1007 (2013/03/13)
Cryptosporidium 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.
