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The effect of novel [3-fluoro-(2-phosphonoethoxy)propyl]purines on the inhibition of Plasmodium falciparum, Plasmodium vivax and human hypoxanthine–guanine–(xanthine) phosphoribosyltransferases

Overview of attention for article published in European Journal of Medicinal Chemistry, June 2013
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Title
The effect of novel [3-fluoro-(2-phosphonoethoxy)propyl]purines on the inhibition of Plasmodium falciparum, Plasmodium vivax and human hypoxanthine–guanine–(xanthine) phosphoribosyltransferases
Published in
European Journal of Medicinal Chemistry, June 2013
DOI 10.1016/j.ejmech.2013.06.032
Pubmed ID
Authors

Ondřej Baszczyňski, Dana Hocková, Zlatko Janeba, Antonín Holý, Petr Jansa, Martin Dračínský, Dianne T. Keough, Luke W. Guddat

Abstract

Protozoan parasites from the Plasmodiidae family are the causative agents of malaria. Inhibition of hypoxanthine-guanine-(xanthine) phosphoribosyltransferase (HG(X)PRT) has been suggested as a target for development of new anti-malarial therapeutics. Acyclic nucleoside phosphonates (ANPs) are potent and selective inhibitors of plasmodial HG(X)PRTs. A new series of ANPs, based on the chemical structure and inhibitory activity of three ANPs, 2-(phosphonoethoxy)ethyl with either guanine or hypoxanthine as the base (PEEG and PEEHx) and 3-hydroxy-2-(phosphonomethoxy)propyl with guanine as the base (HPMPG), were prepared. These compounds are stereoisomers of 3-fluoro-(2-phosphonoethoxy)propyl (FPEPs) and 3-fluoro-(2-phosphonomethoxy)propyl (FPMPs) analogues. Both the (R)- and (S)-isomers of these fluorinated derivatives have higher Ki values (by 10- to 1000-fold) for human HGPRT and Plasmodium falciparum HGXPRT than the non-fluorinated ANPs. Possible explanations for these changes in affinity are proposed based on docking studies using the known crystal structures of human HGPRT in complex with PEEG.

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Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 19 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 19 100%

Demographic breakdown

Readers by professional status Count As %
Student > Master 5 26%
Student > Ph. D. Student 4 21%
Student > Bachelor 3 16%
Researcher 2 11%
Unspecified 1 5%
Other 3 16%
Unknown 1 5%
Readers by discipline Count As %
Chemistry 11 58%
Biochemistry, Genetics and Molecular Biology 3 16%
Environmental Science 2 11%
Agricultural and Biological Sciences 1 5%
Unspecified 1 5%
Other 0 0%
Unknown 1 5%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 27 August 2014.
All research outputs
#20,656,820
of 25,374,917 outputs
Outputs from European Journal of Medicinal Chemistry
#5,243
of 6,651 outputs
Outputs of similar age
#159,367
of 209,401 outputs
Outputs of similar age from European Journal of Medicinal Chemistry
#41
of 48 outputs
Altmetric has tracked 25,374,917 research outputs across all sources so far. This one is in the 10th percentile – i.e., 10% of other outputs scored the same or lower than it.
So far Altmetric has tracked 6,651 research outputs from this source. They receive a mean Attention Score of 4.1. This one is in the 14th percentile – i.e., 14% of its peers scored the same or lower than it.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 209,401 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 11th percentile – i.e., 11% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 48 others from the same source and published within six weeks on either side of this one. This one is in the 8th percentile – i.e., 8% of its contemporaries scored the same or lower than it.