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Benzodioxane‐Benzamides as Antibacterial Agents: Computational and SAR Studies to Evaluate the Influence of the 7‐Substitution in FtsZ Interaction
Author(s) -
Straniero Valentina,
SebastiánPérez Victor,
Hrast Martina,
Zanotto Carlo,
Casiraghi Andrea,
Suigo Lorenzo,
Zdovc Irena,
Radaelli Antonia,
De Giuli Morghen Carlo,
Valoti Ermanno
Publication year - 2020
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201900537
Subject(s) - ftsz , escherichia coli , antimicrobial , bacteria , bacterial cell structure , staphylococcus aureus , chemistry , computational biology , antibacterial activity , microbiology and biotechnology , biology , combinatorial chemistry , biochemistry , genetics , gene
FtsZ is a crucial prokaryotic protein involved in bacterial cell replication. It recently arose as a promising target in the search for antimicrobial agents able to fight antimicrobial resistance. In this work, going on with our structure‐activity relationship (SAR) study, we developed variously 7‐substituted 1,4‐benzodioxane compounds, linked to the 2,6‐difluorobenzamide by a methylenoxy bridge. Compounds exhibit promising antibacterial activities not only against multidrug‐resistant Staphylococcus aureus , but also on mutated Escherichia coli strains, thus enlarging their spectrum of action toward Gram‐negative bacteria as well. Computational studies elucidated, through a validated FtsZ binding protocol, the structural features of new promising derivatives as FtsZ inhibitors.