↓ Skip to main content

Synthesis and Kinetic Testing of Tetrahydropyrimidine‐2‐thione and Pyrrole Derivatives as Inhibitors of the Metallo‐β‐lactamase from Klebsiella pneumonia and Pseudomonas aeruginosa

Overview of attention for article published in Chemical Biology & Drug Design, July 2012
Altmetric Badge

About this Attention Score

  • In the top 25% of all research outputs scored by Altmetric
  • High Attention Score compared to outputs of the same age (80th percentile)
  • High Attention Score compared to outputs of the same age and source (82nd percentile)

Mentioned by

twitter
1 X user
patent
3 patents

Citations

dimensions_citation
43 Dimensions

Readers on

mendeley
32 Mendeley
You are seeing a free-to-access but limited selection of the activity Altmetric has collected about this research output. Click here to find out more.
Title
Synthesis and Kinetic Testing of Tetrahydropyrimidine‐2‐thione and Pyrrole Derivatives as Inhibitors of the Metallo‐β‐lactamase from Klebsiella pneumonia and Pseudomonas aeruginosa
Published in
Chemical Biology & Drug Design, July 2012
DOI 10.1111/j.1747-0285.2012.01440.x
Pubmed ID
Authors

Waleed M. Hussein, Samar S. Fatahala, Zainab M. Mohamed, Ross P. McGeary, Gerhard Schenk, David L. Ollis, Mosaad S. Mohamed

Abstract

Metallo-β-lactamases (MBLs), produced by an increasing number of bacterial pathogens, facilitate the hydrolysis of many commonly used β-lactam antibiotics. There are no clinically useful antagonists against MBLs. Two sets of tetrahydropyrimidine-2-thione and pyrrole derivatives were synthesized and assayed for their inhibitory effects on the catalytic activity of the IMP-1 MBL from Pseudomonas aeruginosa and Klebsiella pneumoniae. Nine compounds tested (1a, 3b, 5c, 6b, 7a, 8a, 11c, 13a, and 16a) showed micromolar inhibition constants (K(i) values range from ∼20-80 μM). Compounds 1c, 2b, and 15a showed only weak inhibition. In silico docking was employed to investigate the binding mode of each enantiomer of the strongest inhibitor, 5c (K(i) = 19 ± 9 μM), as well as 7a (K(i) =21 ± 10 μM), the strongest inhibitor of the pyrrole series, in the active site of IMP-1.

X Demographics

X Demographics

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

Geographical breakdown

Country Count As %
Unknown 32 100%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 7 22%
Student > Bachelor 4 13%
Lecturer > Senior Lecturer 4 13%
Researcher 4 13%
Student > Master 3 9%
Other 6 19%
Unknown 4 13%
Readers by discipline Count As %
Chemistry 8 25%
Biochemistry, Genetics and Molecular Biology 4 13%
Immunology and Microbiology 4 13%
Agricultural and Biological Sciences 3 9%
Pharmacology, Toxicology and Pharmaceutical Science 2 6%
Other 5 16%
Unknown 6 19%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 7. 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 24 October 2023.
All research outputs
#5,017,065
of 24,585,562 outputs
Outputs from Chemical Biology & Drug Design
#229
of 1,511 outputs
Outputs of similar age
#32,674
of 167,664 outputs
Outputs of similar age from Chemical Biology & Drug Design
#7
of 46 outputs
Altmetric has tracked 24,585,562 research outputs across all sources so far. Compared to these this one has done well and is in the 79th percentile: it's in the top 25% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 1,511 research outputs from this source. They receive a mean Attention Score of 3.1. This one has done well, scoring higher than 83% 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 167,664 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 80% of its contemporaries.
We're also able to compare this research output to 46 others from the same source and published within six weeks on either side of this one. This one has done well, scoring higher than 82% of its contemporaries.