Discovery of isoxazolyl-based inhibitors of Plasmodium falciparum cGMP-dependent protein kinase

Literature Information

Publication Date 2019-12-16
DOI 10.1039/C9MD00511K
Impact Factor 0
Authors

Shams Ul Mahmood, Huimin Cheng, Sreedhar R. Tummalapalli, Ramappa Chakrasali, Rammohan R. Yadav Bheemanaboina, Tamara Kreiss, Agnieska Chojnowski, Tyler Eck, John J. Siekierka, David P. Rotella


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Abstract

The cGMP-dependent protein kinase in Plasmodium falciparum (PfPKG) plays multiple roles in the life cycle of the parasite. As a result, this enzyme is a potential target for new antimalarial agents. Existing inhbitors, while potent and active in malaria models are not optimal. This communication describes initial optimization of a structurally distinct class of PfPKG inhibitors.

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