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X Demographics
Mendeley readers
Attention Score in Context
| Title |
Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy
|
|---|---|
| Published in |
Journal of Medicinal Chemistry, September 2016
|
| DOI | 10.1021/acs.jmedchem.6b00723 |
| Pubmed ID | |
| Authors |
Beatriz Baragaña, Neil R. Norcross, Caroline Wilson, Achim Porzelle, Irene Hallyburton, Raffaella Grimaldi, Maria Osuna-Cabello, Suzanne Norval, Jennifer Riley, Laste Stojanovski, Frederick R. C. Simeons, Paul G. Wyatt, Michael J. Delves, Stephan Meister, Sandra Duffy, Vicky M. Avery, Elizabeth A. Winzeler, Robert E. Sinden, Sergio Wittlin, Julie A. Frearson, David W. Gray, Alan H. Fairlamb, David Waterson, Simon F. Campbell, Paul Willis, Kevin D. Read, Ian H. Gilbert |
| Abstract |
The antiplasmodial activity, DMPK properties, and efficacy of a series of quinoline-4-carboxamides are described. This series was identified from a phenotypic screen against the blood stage of Plasmodium falciparum (3D7) and displayed moderate potency but with suboptimal physicochemical properties and poor microsomal stability. The screening hit (1, EC50 = 120 nM) was optimized to lead molecules with low nanomolar in vitro potency. Improvement of the pharmacokinetic profile led to several compounds showing excellent oral efficacy in the P. berghei malaria mouse model with ED90 values below 1 mg/kg when dosed orally for 4 days. The favorable potency, selectivity, DMPK properties, and efficacy coupled with a novel mechanism of action, inhibition of translation elongation factor 2 (PfEF2), led to progression of 2 (DDD107498) to preclinical development. |
X Demographics
The data shown below were collected from the profiles of 3 X users who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Switzerland | 1 | 33% |
| Unknown | 2 | 67% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 2 | 67% |
| Practitioners (doctors, other healthcare professionals) | 1 | 33% |
Mendeley readers
The data shown below were compiled from readership statistics for 111 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Switzerland | 1 | <1% |
| Brazil | 1 | <1% |
| Unknown | 109 | 98% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 23 | 21% |
| Student > Master | 15 | 14% |
| Researcher | 10 | 9% |
| Student > Bachelor | 9 | 8% |
| Other | 8 | 7% |
| Other | 12 | 11% |
| Unknown | 34 | 31% |
| Readers by discipline | Count | As % |
|---|---|---|
| Chemistry | 39 | 35% |
| Pharmacology, Toxicology and Pharmaceutical Science | 13 | 12% |
| Biochemistry, Genetics and Molecular Biology | 8 | 7% |
| Medicine and Dentistry | 4 | 4% |
| Agricultural and Biological Sciences | 2 | 2% |
| Other | 7 | 6% |
| Unknown | 38 | 34% |
Attention Score in Context
This research output has an Altmetric Attention Score of 5. 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 12 August 2021.
All research outputs
#6,128,512
of 23,079,238 outputs
Outputs from Journal of Medicinal Chemistry
#11,890
of 22,164 outputs
Outputs of similar age
#93,116
of 326,368 outputs
Outputs of similar age from Journal of Medicinal Chemistry
#65
of 155 outputs
Altmetric has tracked 23,079,238 research outputs across all sources so far. This one has received more attention than most of these and is in the 73rd percentile.
So far Altmetric has tracked 22,164 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 6.7. This one is in the 46th percentile – i.e., 46% 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 326,368 tracked outputs that were published within six weeks on either side of this one in any source. This one has gotten more attention than average, scoring higher than 71% of its contemporaries.
We're also able to compare this research output to 155 others from the same source and published within six weeks on either side of this one. This one has gotten more attention than average, scoring higher than 57% of its contemporaries.