Sammanfattning

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 mu M IC50 values in the Thermotoga maritima test system. Promisingly, the compounds retained activity against Plasmodium falciparum mPPase in membranes and inhibited parasite growth.

Originalspråkengelska
TidskriftACS Medicinal Chemistry Letters
Volym11
Utgåva4
Sidor (från-till)605-610
Antal sidor6
ISSN1948-5875
DOI
StatusPublicerad - 9 apr 2020
MoE-publikationstypA1 Tidskriftsartikel-refererad

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