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Examination of the antimalarial potential of experimental aminoquinolines: poor in vitro effect does not preclude in vivo efficacy

Overview of attention for article published in International Journal of Antimicrobial Agents, September 2017
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Title
Examination of the antimalarial potential of experimental aminoquinolines: poor in vitro effect does not preclude in vivo efficacy
Published in
International Journal of Antimicrobial Agents, September 2017
DOI 10.1016/j.ijantimicag.2017.06.002
Pubmed ID
Authors

Jelena Srbljanović, Tijana Štajner, Jelena Konstantinović, Nataša Terzić-Jovanović, Aleksandra Uzelac, Branko Bobić, Bogdan A. Šolaja, Olgica Djurković-Djaković

Abstract

Malaria remains a major disease of the developing world and globally the most important parasitic disease causing significant morbidity and mortality. Because of widespread resistance to conventional antimalarials including chloroquine (CQ), new drugs are urgently needed. We here report on the antimalarial efficacy, both in vitro and in vivo, of a series of aminoquinoline derivatives with adamantane or benzothiophene as a carrier. In vitro efficacy was evaluated by an LDH assay in cultures of a CQ-sensitive (3D7) and a CQ-resistant (Dd2) strain of Plasmodium falciparum. Of a series of 26 screened compounds, those 12 that exerted a growth inhibition rate of at least 50% were further examined in vitro, to determine the IC50 values, and in vivo. This way, even the four compounds that exhibited high IC50 values, were evaluated in vivo, in a modified Thompson test, in C57BL/6 mice infected with the P. berghei ANKA strain. However, another three compounds were eventually excluded due to toxicity in mice. All nine compounds examined in vivo prolonged survival of treated vs. untreated mice, four of which afforded at least a 60% survival. Most notably, two of these, both with the adamantane carrier, afforded complete cure (100% survival and parasite clearance). One of these, interestingly, had no in vitro effect (against the CQR strain). Better in vivo than in vitro results suggest a role for the compound metabolites. The presented results point to adamantane as a carrier which enhances the antimalarial potential of aminoquinolines.

Twitter Demographics

The data shown below were collected from the profile of 1 tweeter who shared this research output. Click here to find out more about how the information was compiled.

Mendeley readers

The data shown below were compiled from readership statistics for 11 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 11 100%

Demographic breakdown

Readers by professional status Count As %
Researcher 3 27%
Student > Ph. D. Student 3 27%
Professor 1 9%
Student > Master 1 9%
Other 1 9%
Other 0 0%
Unknown 2 18%
Readers by discipline Count As %
Medicine and Dentistry 2 18%
Agricultural and Biological Sciences 1 9%
Immunology and Microbiology 1 9%
Chemistry 1 9%
Engineering 1 9%
Other 0 0%
Unknown 5 45%

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 03 July 2017.
All research outputs
#9,790,429
of 12,254,034 outputs
Outputs from International Journal of Antimicrobial Agents
#1,294
of 1,687 outputs
Outputs of similar age
#192,840
of 265,670 outputs
Outputs of similar age from International Journal of Antimicrobial Agents
#62
of 86 outputs
Altmetric has tracked 12,254,034 research outputs across all sources so far. This one is in the 11th percentile – i.e., 11% of other outputs scored the same or lower than it.
So far Altmetric has tracked 1,687 research outputs from this source. They receive a mean Attention Score of 4.0. This one is in the 13th percentile – i.e., 13% 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 265,670 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 15th percentile – i.e., 15% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 86 others from the same source and published within six weeks on either side of this one. This one is in the 12th percentile – i.e., 12% of its contemporaries scored the same or lower than it.