Acyclic phosph(on)ate inhibitors of Plasmodium falciparum hypoxanthine-guanine-xanthine phosphoribosyltransferase.
Bioorg Med Chem
; 21(17): 5629-46, 2013 Sep 01.
Article
en En
| MEDLINE
| ID: mdl-23810424
ABSTRACT
The pathogenic protozoa responsible for malaria lack enzymes for the de novo synthesis of purines and rely on purine salvage from the host. In Plasmodium falciparum (Pf), hypoxanthine-guanine-xanthine phosphoribosyltransferase (HGXPRT) converts hypoxanthine to inosine monophosphate and is essential for purine salvage making the enzyme an anti-malarial drug target. We have synthesized a number of simple acyclic aza-C-nucleosides and shown that some are potent inhibitors of Pf HGXPRT while showing excellent selectivity for the Pf versus the human enzyme.
Palabras clave
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Pentosiltransferasa
/
Plasmodium falciparum
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Inhibidores Enzimáticos
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Antimaláricos
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Nucleósidos
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2013
Tipo del documento:
Article
País de afiliación:
Nueva Zelanda