Evidence map›Paper›PMID 21194954›Full record

ArticleBioorganic & medicinal chemistry2011

Syntheses, structures and antibiotic activities of LpxC inhibitors based on the diacetylene scaffold.

Xiaofei Liang, Chul-Jin Lee, Xin Chen, Hak Suk Chung, Daina Zeng, Christian R H Raetz, Yaoxian Li, Pei Zhou, Eric J Toone

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 papers.

0numbers the graph read from it
0cells of the map it votes in
35citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

35 citing papers in PubMed.

  1. Article
  2. Article
  3. Review
  4. Article
  5. Tetrahedron letters · 2021
    Article
  6. Review
  7. The Complex Structure of Protein AaLpxC fromMolecules (Basel, Switzerland) · 2021
    Article
  8. Article
  9. Structural basis of the UDP-diacylglucosamine pyrophosphohydrolase LpxH inhibition by sulfonyl piperazine antibiotics.Proceedings of the National Academy of Sciences of the United States of America · 2020
    Article
  10. Mutations ReducingAntimicrobial agents and chemotherapy · 2019
    Article
  11. Article
  12. Review
  13. Article
  14. Article
  15. Article
  16. Lipid A Has Significance for Optimal Growth ofFrontiers in cellular and infection microbiology · 2018
    Article
  17. Structure, inhibition, and regulation of essential lipid A enzymes.Biochimica et biophysica acta. Molecular and cell biology of lipids · 2017
    Review
  18. Article
  19. Article
  20. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

9 authors.

Xiaofei LiangDepartment of Chemistry, Jilin University, Changchun, PR China.
Chul-Jin Lee
Xin Chen
Hak Suk Chung
Daina Zeng
Christian R H Raetz
Yaoxian Li
Pei Zhou
Eric J Toone

Funding

BIOSYNTHESIS AND FUNCTION OF LIPOPOLYSACCHARIDESR01GM051310 · NIGMS · DUKE UNIVERSITY · PI ZHOU, PEI · 1994 to 2013
$8.1M
Structure and Mechanism of LpxC in Lipid A BiosynthesisR01AI055588 · NIAID · DUKE UNIVERSITY · PI ZHOU, PEI · 2003 to 2012
$3.0M
NIAID NIH HHS AI055588NIAID NIH HHS R01 AI055588NIGMS NIH HHS GM-51310NIGMS NIH HHS R01 GM051310
6 · The paper itself

Abstract

Compounds inhibiting LpxC in the lipid A biosynthetic pathway are promising leads for novel antibiotics against multidrug-resistant Gram-negative pathogens. We report the syntheses and structural and biochemical characterizations of LpxC inhibitors based on a diphenyl-diacetylene (1,4-diphenyl-1,3-butadiyne) threonyl-hydroxamate scaffold. These studies provide a molecular interpretation for the differential antibiotic activities of compounds with a substituted distal phenyl ring as well as the absolute stereochemical requirement at the C2, but not C3, position of the threonyl group.

Indexed as

AmidohydrolasesAmino Acid SequenceAnti-Bacterial AgentsBinding SitesComputer SimulationEnzyme InhibitorsEscherichia coliEscherichia coli ProteinsMicrobial Sensitivity TestsMolecular Sequence DataProtein Structure, TertiaryStructure-Activity RelationshipAmidohydrolasesAnti-Bacterial AgentsEnzyme InhibitorsEscherichia coli ProteinsUDP-3-O-acyl-N-acetylglucosamine deacetylase

Identifiers

PMID21194954
PMCPMC3035996

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Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.