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Discovery and preliminary structure–activity relationship analysis of 1,14-sperminediphenylacetamides as potent and selective antimalarial lead compounds

Overview of attention for article published in Bioorganic & Medicinal Chemistry Letters, November 2012
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About this Attention Score

  • In the top 25% of all research outputs scored by Altmetric
  • High Attention Score compared to outputs of the same age (92nd percentile)
  • High Attention Score compared to outputs of the same age and source (96th percentile)

Mentioned by

blogs
1 blog
patent
5 patents
googleplus
1 Google+ user

Citations

dimensions_citation
21 Dimensions

Readers on

mendeley
37 Mendeley
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Title
Discovery and preliminary structure–activity relationship analysis of 1,14-sperminediphenylacetamides as potent and selective antimalarial lead compounds
Published in
Bioorganic & Medicinal Chemistry Letters, November 2012
DOI 10.1016/j.bmcl.2012.11.072
Pubmed ID
Authors

Lydia P.P. Liew, Marcel Kaiser, Brent R. Copp

Abstract

Screening of synthesized and isolated marine natural products for in vitro activity against four parasitic protozoa has identified the ascidian metabolite 1,14-sperminedihomovanillamide (orthidine F, 1) as being a non-toxic, moderate growth inhibitor of Plasmodium falciparum (IC(50) 0.89 μM). Preliminary structure-activity relationship investigation identified essentiality of the spermine polyamine core and the requirement for 1,14-disubstitution for potent activity. One analogue, 1,14-spermine-di-(2-hydroxyphenylacetamide) (3), exhibited two orders of magnitude increased anti-P. f activity (IC(50) 8.6 nM) with no detectable in vitro toxicity. The ease of synthesis of phenylacetamido-polyamines, coupled with potent nM levels of activity towards dual drug resistant strains of P. falciparum makes this compound class of interest in the development of new antimalarial therapeutics.

Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 37 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
United Kingdom 1 3%
Unknown 36 97%

Demographic breakdown

Readers by professional status Count As %
Researcher 9 24%
Student > Ph. D. Student 6 16%
Student > Master 6 16%
Student > Doctoral Student 4 11%
Student > Bachelor 2 5%
Other 3 8%
Unknown 7 19%
Readers by discipline Count As %
Chemistry 15 41%
Medicine and Dentistry 4 11%
Pharmacology, Toxicology and Pharmaceutical Science 3 8%
Social Sciences 2 5%
Agricultural and Biological Sciences 2 5%
Other 3 8%
Unknown 8 22%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 15. 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 31 August 2021.
All research outputs
#2,330,078
of 25,374,917 outputs
Outputs from Bioorganic & Medicinal Chemistry Letters
#177
of 13,778 outputs
Outputs of similar age
#21,055
of 285,955 outputs
Outputs of similar age from Bioorganic & Medicinal Chemistry Letters
#2
of 139 outputs
Altmetric has tracked 25,374,917 research outputs across all sources so far. Compared to these this one has done particularly well and is in the 90th percentile: it's in the top 10% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 13,778 research outputs from this source. They receive a mean Attention Score of 4.9. This one has done particularly well, scoring higher than 98% of its peers.
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 285,955 tracked outputs that were published within six weeks on either side of this one in any source. This one has done particularly well, scoring higher than 92% of its contemporaries.
We're also able to compare this research output to 139 others from the same source and published within six weeks on either side of this one. This one has done particularly well, scoring higher than 96% of its contemporaries.