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

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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.

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

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Supplementary files

Article information


Submitted
28 Oct 2019
Accepted
26 Nov 2019
First published
16 Dec 2019

RSC Med. Chem., 2020, Advance Article
Article type
Research Article

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

S. U. Mahmood, H. Cheng, S. R. Tummalapalli, R. Chakrasali, R. R. Yadav Bheemanaboina, T. Kreiss, A. Chojnowski, T. Eck, J. J. Siekierka and D. P. Rotella, RSC Med. Chem., 2020, Advance Article , DOI: 10.1039/C9MD00511K

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