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Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi

Overview of attention for article published in Journal of Medicinal Chemistry, August 2017
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1 tweeter

Citations

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7 Dimensions

Readers on

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58 Mendeley
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Title
Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi
Published in
Journal of Medicinal Chemistry, August 2017
DOI 10.1021/acs.jmedchem.7b00463
Pubmed ID
Authors

Stephen Brand, Eun Jung Ko, Elisabet Viayna, Stephen Thompson, Daniel Spinks, Michael Thomas, Lars Sandberg, Amanda F. Francisco, Shiromani Jayawardhana, Victoria C. Smith, Chimed Jansen, Manu De Rycker, John Thomas, Lorna MacLean, Maria Osuna-Cabello, Jennifer Riley, Paul Scullion, Laste Stojanovski, Frederick R. C. Simeons, Ola Epemolu, Yoko Shishikura, Sabrinia D. Crouch, Tania S. Bakshi, Christopher J. Nixon, Iain H. Reid, Alan P. Hill, Tim Z. Underwood, Sean J. Hindley, Sharon A. Robinson, John M. Kelly, Jose M. Fiandor, Paul G. Wyatt, Maria Marco, Timothy J. Miles, Kevin D. Read, Ian H. Gilbert

Abstract

Chagas' disease, caused by the protozoan parasite Trypanosoma cruzi, is the most common cause of cardiac-related deaths in endemic regions of Latin America. There is an urgent need for new safer treatments because current standard therapeutic options, benznidazole and nifurtimox, have significant side effects and are only effective in the acute phase of the infection with limited efficacy in the chronic phase. Phenotypic high content screening against the intracellular parasite in infected VERO cells was used to identify a novel hit series of 5-amino-1,2,3-triazole-4-carboxamides (ATC). Optimization of the ATC series gave improvements in potency, aqueous solubility, and metabolic stability, which combined to give significant improvements in oral exposure. Mitigation of a potential Ames and hERG liability ultimately led to two promising compounds, one of which demonstrated significant suppression of parasite burden in a mouse model of Chagas' disease.

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

Geographical breakdown

Country Count As %
Unknown 58 100%

Demographic breakdown

Readers by professional status Count As %
Researcher 13 22%
Student > Master 12 21%
Student > Ph. D. Student 5 9%
Student > Doctoral Student 3 5%
Student > Postgraduate 3 5%
Other 9 16%
Unknown 13 22%
Readers by discipline Count As %
Chemistry 18 31%
Medicine and Dentistry 6 10%
Agricultural and Biological Sciences 6 10%
Biochemistry, Genetics and Molecular Biology 5 9%
Pharmacology, Toxicology and Pharmaceutical Science 4 7%
Other 4 7%
Unknown 15 26%

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 07 September 2017.
All research outputs
#7,303,825
of 11,727,438 outputs
Outputs from Journal of Medicinal Chemistry
#16,330
of 17,532 outputs
Outputs of similar age
#150,430
of 263,887 outputs
Outputs of similar age from Journal of Medicinal Chemistry
#40
of 79 outputs
Altmetric has tracked 11,727,438 research outputs across all sources so far. This one is in the 23rd percentile – i.e., 23% of other outputs scored the same or lower than it.
So far Altmetric has tracked 17,532 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 5.5. This one is in the 3rd percentile – i.e., 3% 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 263,887 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 33rd percentile – i.e., 33% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 79 others from the same source and published within six weeks on either side of this one. This one is in the 37th percentile – i.e., 37% of its contemporaries scored the same or lower than it.