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Bioorg Med Chem. 2013 Sep 1;21(17):5629-46. doi: 10.1016/j.bmc.2013.02.016. Epub 2013 Mar 5.

Acyclic phosph(on)ate inhibitors of Plasmodium falciparum hypoxanthine-guanine-xanthine phosphoribosyltransferase.

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  • 1Carbohydrate Chemistry, Industrial Research Ltd, Lower Hutt 5040, New Zealand.

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.

Copyright © 2013 Elsevier Ltd. All rights reserved.

KEYWORDS:

HGXPRTase; Malaria; Phosphoribosyltransferase; Protozoa; Purine salvage

PMID:
23810424
[PubMed - indexed for MEDLINE]
PMCID:
PMC3740065
Free PMC Article
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