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

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

doi:10.1039/C9MD00511K

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

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

*^a

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^a Department of Chemistry and Biochemistry, Montclair State University, Montclair, NJ 07043, USA
E-mail: rotellad@montclair.edu

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.

RSC Medicinal Chemistry

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

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

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