Benzodioxane-benzamides As New Bacterial Cell Division Inhibitors

Overview

Journal Eur J Med Chem

Specialty Chemistry

Date 2014 Dec 3

PMID 25462242

Citations 10

Authors

Giuseppe Chiodini

Marco Pallavicini

Carlo Zanotto

Massimiliano Bissa

Antonia Radaelli

Valentina Straniero

Cristiano Bolchi

Laura Fumagalli

Paola Ruggeri

Carlo De Giuli Morghen

Ermanno Valoti

Affiliations

Soon will be listed here.

Abstract

A SAR study was performed on 3-substituted 2,6-difluorobenzamides, known inhibitors of the essential bacterial cell division protein FtsZ, through a series of modifications first of 2,6-difluoro-3-nonyloxybenzamide and then of its 3-pyridothiazolylmethoxy analogue PC190723. The study led to the identification of chiral 2,6-difluorobenzamides bearing 1,4-benzodioxane-2-methyl residue at the 3-position as potent antistaphylococcal compounds.

Citing Articles

Targeting Bacterial Cell Division with Benzodioxane-Benzamide FtsZ Inhibitors as a Novel Strategy to Fight Gram-Positive Ovococcal Pathogens.

Furlan B, Sobrinos-Sanguino M, Sammartino M, Monterroso B, Zorrilla S, Lanzini A Int J Mol Sci. 2025; 26(2).

PMID: 39859428 PMC: 11765573. DOI: 10.3390/ijms26020714.

A FtsZ Inhibitor That Can Utilize Siderophore-Ferric Iron Uptake Transporter Systems for Activity against Gram-Negative Bacterial Pathogens.

Bryan E, Qiao Q, Wang Y, Roberge J, LaVoie E, Pilch D Antibiotics (Basel). 2024; 13(3).

PMID: 38534644 PMC: 10967458. DOI: 10.3390/antibiotics13030209.

Benzodioxane-Benzamides as FtsZ Inhibitors: Effects of Linker's Functionalization on Gram-Positive Antimicrobial Activity.

Suigo L, Margolin W, Ulzurrun E, Hrast Rambaher M, Zanotto C, Sebastian-Perez V Antibiotics (Basel). 2023; 12(12).

PMID: 38136746 PMC: 10740499. DOI: 10.3390/antibiotics12121712.

Structural and Antibacterial Characterization of a New Benzamide FtsZ Inhibitor with Superior Bactericidal Activity and In Vivo Efficacy Against Multidrug-Resistant .

Bryan E, Ferrer-Gonzalez E, Sagong H, Fujita J, Mark L, Kaul M ACS Chem Biol. 2023; 18(3):629-642.

PMID: 36854145 PMC: 10274580. DOI: 10.1021/acschembio.2c00934.

Structural Variations in the Central Heterocyclic Scaffold of Tripartite 2,6-Difluorobenzamides: Influence on Their Antibacterial Activity against MDR .

Barbier T, Badiou C, Davy F, Queneau Y, Dumitrescu O, Lina G Molecules. 2022; 27(19).

PMID: 36235156 PMC: 9573484. DOI: 10.3390/molecules27196619.