Artículo
Antimalarial activity of novel imidazoisoquinolinone derivatives correlates with heme binding affinity
Bollini, Mariela
; Casal, Juan José
; Asís, Silvia Elizabeth; Leal, Emilse Soledad
; Bruno, Ana María
Fecha de publicación:
03/2015
Editorial:
Birkhauser Boston Inc
Revista:
Medicinal Chemistry Research
ISSN:
1054-2523
Idioma:
Inglés
Tipo de recurso:
Artículo publicado
Clasificación temática:
Resumen
A series of novel imidazoisoquinolinone derivatives were synthesized and evaluated for in vitro antimalarial efficacy against chloroquine sensitive GHA strain of Plasmodium falciparum. Compounds 2, 4, 6, 9, and 17 revealed moderate to good activities in the micromolar range. Binding interaction between these active compounds and heme were determined and correlated with antimalarial activity. A good correlation (r = 0.98) was observed between antimalarial activity and the heme dissociation constants (K d). These suggest that antimalarial mode of action of this class of compounds appears to be similar to that of chloroquine and involves the inhibition of hemozoin formation.
Palabras clave:
Antiplasmodial
,
Hemozoin
,
Imidazoisoquinolinones
,
Malaria
,
Plasmodium Falciparum
Archivos asociados
Licencia
Identificadores
Colecciones
Articulos(OCA HOUSSAY)
Articulos de OFICINA DE COORDINACION ADMINISTRATIVA HOUSSAY
Articulos de OFICINA DE COORDINACION ADMINISTRATIVA HOUSSAY
Citación
Bollini, Mariela; Casal, Juan José; Asís, Silvia Elizabeth; Leal, Emilse Soledad; Bruno, Ana María; Antimalarial activity of novel imidazoisoquinolinone derivatives correlates with heme binding affinity; Birkhauser Boston Inc; Medicinal Chemistry Research; 24; 4; 3-2015; 1496-1503
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