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

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.

SUBMITTER: Mahmood SU

PROVIDER: S-EPMC7536641 | biostudies-literature | 2020 Jan

REPOSITORIES: biostudies-literature

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

Mahmood Shams Ul SU Cheng Huimin H Tummalapalli Sreedhar R SR Chakrasali Ramappa R Yadav Bheemanaboina Rammohan R RR Kreiss Tamara T Chojnowski Agnieska A Eck Tyler T Siekierka John J JJ Rotella David P DP

RSC medicinal chemistry 20191216 1

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. ...[more]

PMID: 33479608

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