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X Demographics
Mendeley readers
Attention Score in Context
| Title |
Trisubstituted Pyrimidines as Efficacious and Fast-Acting Antimalarials
|
|---|---|
| Published in |
Journal of Medicinal Chemistry, June 2016
|
| DOI | 10.1021/acs.jmedchem.6b00028 |
| Pubmed ID | |
| Authors |
Neil R. Norcross, Beatriz Baragaña, Caroline Wilson, Irene Hallyburton, Maria Osuna-Cabello, Suzanne Norval, Jennifer Riley, Laste Stojanovski, Frederick R. C. Simeons, Achim Porzelle, Raffaella Grimaldi, Sergio Wittlin, Sandra Duffy, Vicky M. Avery, Stephan Meister, Laura Sanz, Belén Jiménez-Díaz, Iñigo Angulo-Barturen, Santiago Ferrer, María Santos Martínez, Francisco Javier Gamo, Julie A. Frearson, David W. Gray, Alan H. Fairlamb, Elizabeth A. Winzeler, David Waterson, Simon F. Campbell, Paul Willis, Kevin D. Read, Ian H. Gilbert |
| Abstract |
In this paper we describe the optimization of a phenotypic hit against Plasmodium falciparum, based on a trisubstituted pyrimidine scaffold. This led to compounds with good pharmacokinetics and oral activity in a P. berghei mouse model of malaria. The most promising compound (13) showed a reduction in parasitemia of 96% when dosed at 30 mg/kg orally once a day for 4 days in the P. berghei mouse model of malaria. It also demonstrated a rapid rate of clearance of the erythrocytic stage of P. falciparum in the SCID mouse model with an ED90 of 11.7 mg/kg when dosed orally. Unfortunately, the compound is a potent inhibitor of cytochrome P450 enzymes, probably due to a 4-pyridyl substituent. Nevertheless, this is a lead molecule with a potentially useful antimalarial profile, which could either be further optimized or be used for target hunting. |
X Demographics
The data shown below were collected from the profiles of 10 X users who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| United Kingdom | 2 | 20% |
| France | 1 | 10% |
| Switzerland | 1 | 10% |
| Unknown | 6 | 60% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 5 | 50% |
| Scientists | 3 | 30% |
| Science communicators (journalists, bloggers, editors) | 1 | 10% |
| Practitioners (doctors, other healthcare professionals) | 1 | 10% |
Mendeley readers
The data shown below were compiled from readership statistics for 43 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 43 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Researcher | 10 | 23% |
| Student > Ph. D. Student | 9 | 21% |
| Other | 5 | 12% |
| Student > Doctoral Student | 3 | 7% |
| Professor > Associate Professor | 3 | 7% |
| Other | 7 | 16% |
| Unknown | 6 | 14% |
| Readers by discipline | Count | As % |
|---|---|---|
| Chemistry | 17 | 40% |
| Biochemistry, Genetics and Molecular Biology | 3 | 7% |
| Medicine and Dentistry | 2 | 5% |
| Unspecified | 2 | 5% |
| Pharmacology, Toxicology and Pharmaceutical Science | 2 | 5% |
| Other | 7 | 16% |
| Unknown | 10 | 23% |
Attention Score in Context
This research output has an Altmetric Attention Score of 14. 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 17 November 2022.
All research outputs
#2,257,344
of 23,770,218 outputs
Outputs from Journal of Medicinal Chemistry
#1,441
of 22,446 outputs
Outputs of similar age
#41,942
of 355,805 outputs
Outputs of similar age from Journal of Medicinal Chemistry
#19
of 167 outputs
Altmetric has tracked 23,770,218 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 22,446 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 6.8. This one has done particularly well, scoring higher than 93% 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 355,805 tracked outputs that were published within six weeks on either side of this one in any source. This one has done well, scoring higher than 88% of its contemporaries.
We're also able to compare this research output to 167 others from the same source and published within six weeks on either side of this one. This one has done well, scoring higher than 88% of its contemporaries.