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.

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.. - In: ACS MEDICINAL CHEMISTRY LETTERS. - ISSN 1948-5875. - 10:4(2019), pp. 590-595. [10.1021/acsmedchemlett.8b00592]

Covalent Inhibitors of Plasmodium falciparum Glyceraldehyde 3-Phosphate Dehydrogenase with Antimalarial Activity in Vitro

Bruno S.;Margiotta M.;Mozzarelli A.;Persico M.;Paladino A.;
2019

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.
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.. - In: ACS MEDICINAL CHEMISTRY LETTERS. - ISSN 1948-5875. - 10:4(2019), pp. 590-595. [10.1021/acsmedchemlett.8b00592]
File in questo prodotto:
Non ci sono file associati a questo prodotto.

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11381/2870796
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 7
  • ???jsp.display-item.citation.isi??? 8
social impact