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- W3005771010 abstract "Membrane-bound pyrophosphatases (mPPases) regulate energy homeostasis in pathogenic protozoan parasites and lack human homologues, which makes them promising targets in e.g. malaria. Yet only few nonphosphorus inhibitors have been reported so far. Here, we explore an isoxazole fragment hit, leading to the discovery of small mPPase inhibitors with 6–10 μM IC50 values in the Thermotoga maritima test system. Promisingly, the compounds retained activity against Plasmodium falciparum mPPase in membranes and inhibited parasite growth." @default.
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- W3005771010 date "2020-02-17" @default.
- W3005771010 modified "2023-10-16" @default.
- W3005771010 title "Discovery of Membrane-Bound Pyrophosphatase Inhibitors Derived from an Isoxazole Fragment" @default.
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- W3005771010 doi "https://doi.org/10.1021/acsmedchemlett.9b00537" @default.
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