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Synthesis and evaluation of new tyrosyl-tRNA synthetase inhibitors as antibacterial agents based on a N2-(arylacetyl)glycinanilide scaffold

Overview of attention for article published in European Journal of Medicinal Chemistry, August 2015
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Title
Synthesis and evaluation of new tyrosyl-tRNA synthetase inhibitors as antibacterial agents based on a N2-(arylacetyl)glycinanilide scaffold
Published in
European Journal of Medicinal Chemistry, August 2015
DOI 10.1016/j.ejmech.2015.08.025
Pubmed ID
Authors

Zhu-Ping Xiao, Wei Wei, Peng-Fei Wang, Wei-Kang Shi, Na Zhu, Me-Qun Xie, Yu-Wen Sun, Ling-Xia Li, Yong-Xiang Xie, Liang-Song Zhu, Nian Tang, Hui Ouyang, Xian-Hui Li, Guang-Cheng Wang, Hai-Liang Zhu

Abstract

Tyrosyl-tRNA synthetase (TyrRS), an essential enzyme in bacterial protein biosynthesis, is an attractive therapeutic target for finding novel antibacterial agents, and a series of N2-(arylacetyl)glycinanilides has been herein synthesized and identified as TyrRS inhibitors. These efforts yielded several compounds, with IC50 in the low micromolar range against TyrRS from Staphylococcus aureus. Out of the obtained compounds, 3ap is the most active and exhibits excellent activity against both Gram-positive (S. aureus) and Gram-negative (Escherichia coli and Pseudomonas aeruginosa) bacterial strains. In comparison with the parent scaffold 3-arylfuran-2(5H)-one, N2-(arylacetyl)glycinanilide significantly improved the potency against Gram-negative bacterial strains, indicating that this scaffold offers a significant potential for developing new antibacterial drugs.

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

Mendeley readers

The data shown below were compiled from readership statistics for 21 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
United States 1 5%
Unknown 20 95%

Demographic breakdown

Readers by professional status Count As %
Researcher 3 14%
Student > Ph. D. Student 3 14%
Student > Master 2 10%
Lecturer 1 5%
Other 1 5%
Other 3 14%
Unknown 8 38%
Readers by discipline Count As %
Chemistry 6 29%
Biochemistry, Genetics and Molecular Biology 4 19%
Pharmacology, Toxicology and Pharmaceutical Science 1 5%
Medicine and Dentistry 1 5%
Computer Science 1 5%
Other 0 0%
Unknown 8 38%
Attention Score in Context

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 01 September 2015.
All research outputs
#17,286,379
of 25,374,917 outputs
Outputs from European Journal of Medicinal Chemistry
#4,632
of 6,651 outputs
Outputs of similar age
#165,941
of 276,630 outputs
Outputs of similar age from European Journal of Medicinal Chemistry
#55
of 78 outputs
Altmetric has tracked 25,374,917 research outputs across all sources so far. This one is in the 21st percentile – i.e., 21% of other outputs scored the same or lower than it.
So far Altmetric has tracked 6,651 research outputs from this source. They receive a mean Attention Score of 4.1. This one is in the 23rd percentile – i.e., 23% 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 276,630 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 31st percentile – i.e., 31% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 78 others from the same source and published within six weeks on either side of this one. This one is in the 28th percentile – i.e., 28% of its contemporaries scored the same or lower than it.