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Design, synthesis and biological evaluation of novel aryldiketo acids with enhanced antibacterial activity against multidrug resistant bacterial strains

Overview of attention for article published in European Journal of Medicinal Chemistry, January 2018
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Mentioned by

twitter
2 tweeters

Citations

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4 Dimensions

Readers on

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23 Mendeley
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Title
Design, synthesis and biological evaluation of novel aryldiketo acids with enhanced antibacterial activity against multidrug resistant bacterial strains
Published in
European Journal of Medicinal Chemistry, January 2018
DOI 10.1016/j.ejmech.2017.10.045
Pubmed ID
Authors

Ilija N. Cvijetić, Tatjana Ž. Verbić, Pedro Ernesto de Resende, Paul Stapleton, Simon Gibbons, Ivan O. Juranić, Branko J. Drakulić, Mire Zloh

Abstract

Antimicrobial resistance (AMR) is a major health problem worldwide, because of ability of bacteria, fungi and viruses to evade known therapeutic agents used in treatment of infections. Aryldiketo acids (ADK) have shown antimicrobial activity against several resistant strains including Gram-positive Staphylococcus aureus bacteria. Our previous studies revealed that ADK analogues having bulky alkyl group in ortho position on a phenyl ring have up to ten times better activity than norfloxacin against the same strains. Rational modifications of analogues by introduction of hydrophobic substituents on the aromatic ring has led to more than tenfold increase in antibacterial activity against multidrug resistant Gram positive strains. To elucidate a potential mechanism of action for this potentially novel class of antimicrobials, several bacterial enzymes were identified as putative targets according to literature data and pharmacophoric similarity searches for potent ADK analogues. Among the seven bacterial targets chosen, the strongest favorable binding interactions were observed between most active analogue and S. aureus dehydrosqualene synthase and DNA gyrase. Furthermore, the docking results in combination with literature data suggest that these novel molecules could also target several other bacterial enzymes, including prenyl-transferases and methionine aminopeptidase. These results and our statistically significant 3D QSAR model could be used to guide the further design of more potent derivatives as well as in virtual screening for novel antibacterial agents.

Twitter Demographics

The data shown below were collected from the profiles of 2 tweeters 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 23 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 23 100%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 6 26%
Researcher 4 17%
Professor 3 13%
Student > Doctoral Student 2 9%
Student > Master 2 9%
Other 3 13%
Unknown 3 13%
Readers by discipline Count As %
Chemistry 7 30%
Medicine and Dentistry 3 13%
Immunology and Microbiology 1 4%
Computer Science 1 4%
Agricultural and Biological Sciences 1 4%
Other 4 17%
Unknown 6 26%

Attention Score in Context

This research output has an Altmetric Attention Score of 2. 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 13 November 2018.
All research outputs
#8,303,069
of 13,777,184 outputs
Outputs from European Journal of Medicinal Chemistry
#2,145
of 3,508 outputs
Outputs of similar age
#207,123
of 393,086 outputs
Outputs of similar age from European Journal of Medicinal Chemistry
#30
of 160 outputs
Altmetric has tracked 13,777,184 research outputs across all sources so far. This one is in the 37th percentile – i.e., 37% of other outputs scored the same or lower than it.
So far Altmetric has tracked 3,508 research outputs from this source. They receive a mean Attention Score of 3.2. This one is in the 36th percentile – i.e., 36% 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 393,086 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 43rd percentile – i.e., 43% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 160 others from the same source and published within six weeks on either side of this one. This one has done well, scoring higher than 75% of its contemporaries.