Design, synthesis and biological activity evaluation of novel 2,6-difluorobenzamide derivatives through FtsZ inhibition.

doi:10.1016/j.bmcl.2016.12.081

Paper

DOI: 10.1016/j.bmcl.2016.12.081

Design, synthesis and biological activity evaluation of novel 2,6-difluorobenzamide derivatives through FtsZ inhibition.

Published Feb 15, 2017 · Fangchao Bi, Liwei Guo, Yinhu Wang

Bioorganic & medicinal chemistry letters

Q2 SJR score

Citations

Influential Citations

Full textSemantic Scholar

Abstract

Abstract hidden due to publisher request; this does not indicate any issues with the research. Click the full text link above to read the abstract and view the original source.

In Vitro Study

Study Snapshot

Novel 2,6-difluorobenzamide derivatives show promising antibacterial activity against Bacillus subtilis and Staphylococcus aureus, with potent cell division inhibitory activity.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Sign up to use Study Snapshot

Consensus is limited without an account. Create an account or sign in to get more searches and use the Study Snapshot.

Create an account

Full text analysis coming soon...

References

DOI: 10.1016/j.ejmech.2015.04.048

Design, synthesis and antibacterial activity of cinnamaldehyde derivatives as inhibitors of the bacterial cell division protein FtsZ.

Cinnamaldehyde derivatives show promising antibacterial activity against Staphylococcus aureus, with compounds 3, 8 and 10 showing particularly strong cell division inhibitory activity.

2015·60citations·Xin Li et al.·European journal of medicinal chemistry

European journal of medicinal chemistry

DOI: 10.1016/j.ejmech.2014.09.100

Benzodioxane-benzamides as new bacterial cell division inhibitors.

Chiral 2,6-difluorobenzamides with 1,4-benzodioxane-2-methyl residue at the 3-position are potent antistaphylococcal compounds.

2015·44citations·G. Chiodini et al.·European journal of medicinal chemistry

European journal of medicinal chemistry

DOI: 10.1107/S0907444912022640

Structural reorganization of the bacterial cell-division protein FtsZ from Staphylococcus aureus.

The bacterial cell-division protein FtsZ from Staphylococcus aureus undergoes conformational changes, showing similarities to eukaryotic tubulin, and is a potential target for antibacterial drugs.

2012·159citations·T. Matsui et al.·Acta crystallographica. Section D, Biological crystallography

Acta crystallographica. Section D, Biological crystallography

DOI: 10.1021/ja303564a

Mechanism of action of the cell-division inhibitor PC190723: modulation of FtsZ assembly cooperativity.

PC190723 inhibits cell division by negatively modulating FtsZ assembly cooperativity in Staphylococcus aureus, enabling polymer assembly at lower concentrations without a defined critical concentration.

2012·115citations·N. Elsen et al.·Journal of the American Chemical Society

Journal of the American Chemical Society

DOI: 10.1016/j.bmcl.2011.10.034

Exploration of in vitro time point quantitative evaluation of newly synthesized benzimidazole and benzothiazole derivatives as potential antibacterial agents.

Newly synthesized benzimidazole and benzothiazole derivatives show moderate to good antibacterial activity against various bacteria, with some showing complete bactericidal activity within 24 hours compared to ciprofloxacin.

2011·70citations·P. Bandyopadhyay et al.·Bioorganic & medicinal chemistry letters

Bioorganic & medicinal chemistry letters

DOI: 10.1016/j.mib.2011.08.002

The antibiotic R&D pipeline: an update.

New antibiotics are urgently needed to combat multidrug-resistant bacteria, but current research efforts are mainly based on modifications of existing drugs, with only four new chemical classes approved for clinical use.

2011·97citations·D. Jabes·Current opinion in microbiology

Current opinion in microbiology

DOI: 10.1021/jm1012006

Novel trisubstituted benzimidazoles, targeting Mtb FtsZ, as a new class of antitubercular agents.

Novel trisubstituted benzimidazoles show promising antitubercular activity against Mtb H37Rv and clinical strains, with potential for use in antitubercular drug discovery.

2011·158citations·Kunal Kumar et al.·Journal of medicinal chemistry

Journal of medicinal chemistry

DOI: 10.1128/MMBR.00021-10

FtsZ in Bacterial Cytokinesis: Cytoskeleton and Force Generator All in One

FtsZ, a bacterial homolog of tubulin, serves as both a cytoskeletal framework and force generator in bacterial cytokinesis, with potential antibacterial drug targets.

2010·599citations·H. Erickson et al.·Microbiology and Molecular Biology Reviews

Microbiology and Molecular Biology Reviews

DOI: 10.1021/jm9016366

Creating an Antibacterial with in Vivo Efficacy: Synthesis and Characterization of Potent Inhibitors of the Bacterial Cell Division Protein FtsZ with Improved Pharmaceutical Properties

Potent antistaphylococcal compounds with improved pharmaceutical properties were identified by exploring structure-activity relationships of FtsZ inhibitors.

2010·93citations·D. Haydon et al.·Journal of Medicinal Chemistry

Journal of Medicinal Chemistry

Citations

DOI: 10.1016/j.molstruc.2023.137365

New naphthoquinone thiazole hybrids as carbonic anhydrase and cholinesterase inhibitors: Synthesis, crystal structure, molecular docking, and acid dissociation constant

New 1,4-naphthoquinone thiazole hybrids show potential as effective and safe inhibitors of carbonic anhydrase and cholinesterase enzymes, making them suitable lead agents for glaucoma and Alzheimer's disease.

2023·19citations·Cagla Efeoglu et al.·Journal of Molecular Structure

Journal of Molecular Structure

DOI: 10.1016/j.ejmech.2023.115930

New broad-spectrum and potent antibacterial agents with dual-targeting mechanism: Promoting FtsZ polymerization and disrupting bacterial membranes.

MA220607 is a promising new antibacterial agent with a dual-targeting mechanism, effectively killing both Gram-positive and Gram-negative bacteria and blocking biofilm formation.

2023·4citations·Yangchun Ma et al.·European journal of medicinal chemistry

European journal of medicinal chemistry

DOI: 10.3389/fmicb.2022.967949

Cinnamaldehyde derivatives act as antimicrobial agents against Acinetobacter baumannii through the inhibition of cell division

Cinnamaldehyde derivatives, particularly 4-bromophenyl-substituted 4, show promising antimicrobial activity against Acinetobacter baumannii, inhibiting cell division and targeting the FtsZ protein.

2022·8citations·Wern Chern Chai et al.·Frontiers in Microbiology

Frontiers in Microbiology

DOI: 10.3389/fnhum.2022.790006

Fatigue Across the Lifespan in Men and Women: State vs. Trait

Older individuals report less fatigue during task performance, with middle frontal areas playing a different role in combating fatigue in younger individuals compared to older individuals.

2022·21citations·G. Wylie et al.·Frontiers in Human Neuroscience

Frontiers in Human Neuroscience

DOI: 10.1016/j.jmgm.2022.108189

Exploration of the inhibitory mechanism of PC190723 on FtsZ protein by molecular dynamics simulation.

PC190723 inhibits FtsZ protein by increasing its high-affinity conformational stability, disrupting its normal assembly, and providing new ideas for developing new antibacterial agents.

2022·5citations·Yangchun Ma et al.·Journal of molecular graphics & modelling

Journal of molecular graphics & modelling