Transition state analogue inhibitors of protozoan nucleoside hydrolases.
Bioorg Med Chem
; 7(11): 2599-606, 1999 Nov.
Article
en En
| MEDLINE
| ID: mdl-10632070
Protozoan parasites are unable to synthesize purines de novo and must rely on purine salvage pathways for their requirements. Nucleoside hydrolases, which are not found in mammals, function as key enzymes in purine salvage in protozoa. Inhibition of these enzymes may disrupt purine supply and specific inhibitors are potential therapeutic agents for the control of protozoan infections. A series of 1,4-dideoxy-1,4-imino-D-ribitols bearing C-bonded aromatic substituents at C-1 have been synthesized, following carbanion additions to the imine 2, and tested as potential nucleoside hydrolase inhibitors. Nucleoside analogues 8, 11, 14, 17, 20, 24-26, 28 exhibit Ki values in the range 0.2-22 microM against two representative isozymes of protozoan nucleoside hydrolases.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Inhibidores Enzimáticos
/
N-Glicosil Hidrolasas
Límite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
1999
Tipo del documento:
Article
País de afiliación:
Nueva Zelanda
Pais de publicación:
Reino Unido