Structure-activity relationship study of selective benzimidazole-based inhibitors of Cryptosporidium parvum IMPDH.

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.

DOI: 10.1016/j.bmcl.2012.01.029
050201520162017
Citations per Year

Citation Velocity: 14

Averaging 14 citations per year over the last 3 years.

Learn more about how we calculate this metric in our FAQ.

Cite this paper

@article{Kirubakaran2012StructureactivityRS, title={Structure-activity relationship study of selective benzimidazole-based inhibitors of Cryptosporidium parvum IMPDH.}, author={Sivapriya Kirubakaran and Suresh Kumar Gorla and Lisa Sharling and Minjia Zhang and Xiaoping Liu and Soumya S Ray and Iain S Macpherson and Boris Striepen and Lizbeth Hedstrom and Gregory D. Cuny}, journal={Bioorganic & medicinal chemistry letters}, year={2012}, volume={22 5}, pages={1985-8} }