Structure-activity relationship study of selective benzimidazole-based inhibitors of Cryptosporidium parvum IMPDH |
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Authors: | Kirubakaran Sivapriya Gorla Suresh Kumar Sharling Lisa Zhang Minjia Liu Xiaoping Ray Soumya S Macpherson Iain S Striepen Boris Hedstrom Lizbeth Cuny Gregory D |
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Institution: | Department of Biology, Brandeis University, MS009, 415 South Street, Waltham, MA 02454, USA. |
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Abstract: | Cryptosporidium parasites are important waterborne pathogens of both humans and animals. The Cryptosporidium parvum and Cryptosporidium hominis genomes indicate that the only route to guanine nucleotides is via inosine 5'-monophosphate dehydrogenase (IMPDH). Thus the inhibition of the parasite IMPDH presents a potential strategy for treating Cryptosporidium infections. A selective benzimidazole-based inhibitor of C. parvum IMPDH (CpIMPDH) was previously identified in a high throughput screen. Here we report a structure-activity relationship study of benzimidazole-based compounds that resulted in potent and selective inhibitors of CpIMPDH. Several compounds display potent antiparasitic activity in vitro. |
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