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

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 des...

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Published inRSC medicinal chemistry Vol. 11; no. 1; pp. 98 - 11
Main Authors Mahmood, Shams Ul, Cheng, Huimin, Tummalapalli, Sreedhar R, Chakrasali, Ramappa, Yadav Bheemanaboina, Rammohan R, Kreiss, Tamara, Chojnowski, Agnieska, Eck, Tyler, Siekierka, John J, Rotella, David P
Format Journal Article
LanguageEnglish
Published 29.01.2020
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Summary: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. The cGMP-dependent protein kinase in Plasmodium falciparum (PfPKG) plays multiple roles in the life cycle of the parasite.
Bibliography:10.1039/c9md00511k
Electronic supplementary information (ESI) available: General procedures and compound characterization is available. NMR and mass spectral data on all tested compounds as well as general synthetic procedures and biological evaluation. See DOI
ISSN:2632-8682
DOI:10.1039/c9md00511k