Covalent Inhibitors of Plasmodium falciparum Glyceraldehyde 3-Phosphate Dehydrogenase with Antimalarial Activity in Vitro
- Cullia G.
- Bruno S.
- Parapini S.
- Margiotta M.
- Tamborini L.
- Pinto A.
- Galbiati A.
- Mozzarelli A.
- Persico M.
- Paladino A.
- Fattorusso C.
- Taramelli D.
- Conti P.
Publication date
January 2019
DOI Publisher
American Chemical Society (ACS)Abstract
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
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