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Antimalarials with Benzothiophene Moieties as Aminoquinoline Partners

Overview of attention for article published in Molecules, February 2017
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Title
Antimalarials with Benzothiophene Moieties as Aminoquinoline Partners
Published in
Molecules, February 2017
DOI 10.3390/molecules22030343
Pubmed ID
Authors

Jelena Konstantinović, Milica Videnović, Jelena Srbljanović, Olgica Djurković-Djaković, Katarina Bogojević, Richard Sciotti, Bogdan Šolaja

Abstract

Malaria is a severe and life-threatening disease caused by Plasmodium parasites that are spread to humans through bites of infected Anopheles mosquitoes. Here, we report on the efficacy of aminoquinolines coupled to benzothiophene and thiophene rings in inhibiting Plasmodium falciparum parasite growth. Synthesized compounds were evaluated for their antimalarial activity and toxicity, in vitro and in mice. Benzothiophenes presented in this paper showed improved activities against a chloroquine susceptible (CQS) strain, with potencies of IC50 = 6 nM, and cured 5/5 Plasmodium berghei infected mice when dosed orally at 160 mg/kg/day × 3 days. In the benzothiophene series, the examined antiplasmodials were more active against the CQS strain D6, than against strains chloroquine resistant (CQR) W2 and multidrug-resistant (MDR) TM91C235. For the thiophene series, a very interesting feature was revealed: hypersensitivity to the CQR strains, resistance index (RI) of <1. This is in sharp contrast to chloroquine, indicating that further development of the series would provide us with more potent antimalarials against CQR strains.

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 14 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 14 100%

Demographic breakdown

Readers by professional status Count As %
Other 3 21%
Student > Ph. D. Student 3 21%
Student > Master 2 14%
Professor 1 7%
Student > Bachelor 1 7%
Other 1 7%
Unknown 3 21%
Readers by discipline Count As %
Chemistry 3 21%
Pharmacology, Toxicology and Pharmaceutical Science 2 14%
Agricultural and Biological Sciences 1 7%
Medicine and Dentistry 1 7%
Unknown 7 50%

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 02 March 2017.
All research outputs
#7,922,311
of 9,138,320 outputs
Outputs from Molecules
#3,393
of 4,634 outputs
Outputs of similar age
#214,815
of 253,872 outputs
Outputs of similar age from Molecules
#420
of 431 outputs
Altmetric has tracked 9,138,320 research outputs across all sources so far. This one is in the 1st percentile – i.e., 1% of other outputs scored the same or lower than it.
So far Altmetric has tracked 4,634 research outputs from this source. They receive a mean Attention Score of 2.1. This one is in the 1st percentile – i.e., 1% 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 253,872 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 1st percentile – i.e., 1% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 431 others from the same source and published within six weeks on either side of this one. This one is in the 1st percentile – i.e., 1% of its contemporaries scored the same or lower than it.