Covalent inhibitors of PfGAPDH characterized by a 3-bromoisoxazoline warhead were developed, and their mode of interaction with the target enzyme was interpreted by means of molecular modeling studies: some of them displayed a submicromolar antiplasmodial activity against both chloroquine sensitive and resistant strains of Plasmodium falciparum, with good selectivity indices.
|Titolo:||Covalent Inhibitors of Plasmodium falciparum Glyceraldehyde 3-Phosphate Dehydrogenase with Antimalarial Activity in Vitro|
|Parole Chiave:||Glyceraldehyde 3-phosphate dehydrogenase; malaria; covalent inhibitor; 3-bromoisoxazoline|
|Settore Scientifico Disciplinare:||Settore CHIM/08 - Chimica Farmaceutica|
|Data di pubblicazione:||2019|
|Digital Object Identifier (DOI):||10.1021/acsmedchemlett.8b00592|
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