Structure-guided design and biosynthesis of a novel FR-900098 analogue as a potent Plasmodium falciparum 1-deoxy-D-xylulose-5-phosphate reductoisomerase (Dxr) inhibitor.
Chem Commun (Camb)
; 51(13): 2526-8, 2015 Feb 14.
Article
em En
| MEDLINE
| ID: mdl-25567100
ABSTRACT
We report here the enzymatic biosynthesis of FR-900098 analogues and establish an in vivo platform for the biosynthesis of an N-propionyl derivative FR-900098P. FR-900098P is found to be a significantly more potent inhibitor of Plasmodium falciparum 1-deoxy-D-xylulose 5-phosphate reductoisomerase (PfDxr) than the parent compound, and thus a more promising antimalarial drug candidate.
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Base de dados:
MEDLINE
Assunto principal:
Plasmodium falciparum
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Desenho de Fármacos
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Aldose-Cetose Isomerases
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Fosfomicina
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Antimaláricos
Idioma:
En
Ano de publicação:
2015
Tipo de documento:
Article