Lipophilic substituents at benzodioxane C (7) of 3-(benzodioxan-2-ylmethoxy)-2,6-difluorobenzamide improve the antibacterial activity against methicillin-resistant Staphylococcus aureus strains to MIC values in the range of 0.2-2.5 μg/mL, whereas hydrophilic substituents at the same position and modifications at the benzodioxane substructure, excepting for replacement with 2-cromanyl, are deleterious. Some of the lead compounds also exhibit good activity against Mtb. Parallel SARs to those of 3-(2-benzothiazol-2-ylmethoxy)-2,6-difluorobenzamide, well known FtsZ inhibitor, and cells alterations typical of FtsZ inhibition indicate such a protein as the target of these potent antibacterial benzodioxane-benzamides.

3-(Benzodioxan-2-ylmethoxy)-2,6-difluorobenzamides bearing hydrophobic substituents at the 7-position of the benzodioxane nucleus potently inhibit methicillin-resistant Sa and Mtb cell division / V. Straniero, M. Pallavicini, G. Chiodini, C. Zanotto, L. Volontè, A. Radaelli, C. Bolchi, L. Fumagalli, M. Sanguinetti, G. Menchinelli, G. Delogu, B. Battah, C. De Giuli Morghen, E. Valoti. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - 120(2016), pp. 227-243. [10.1016/j.ejmech.2016.03.068]

3-(Benzodioxan-2-ylmethoxy)-2,6-difluorobenzamides bearing hydrophobic substituents at the 7-position of the benzodioxane nucleus potently inhibit methicillin-resistant Sa and Mtb cell division

V. Straniero
Primo
;
M. Pallavicini
Secondo
;
G. Chiodini;C. Zanotto;A. Radaelli;C. Bolchi;L. Fumagalli;C. De Giuli Morghen
Penultimo
;
E. Valoti
2016

Abstract

Lipophilic substituents at benzodioxane C (7) of 3-(benzodioxan-2-ylmethoxy)-2,6-difluorobenzamide improve the antibacterial activity against methicillin-resistant Staphylococcus aureus strains to MIC values in the range of 0.2-2.5 μg/mL, whereas hydrophilic substituents at the same position and modifications at the benzodioxane substructure, excepting for replacement with 2-cromanyl, are deleterious. Some of the lead compounds also exhibit good activity against Mtb. Parallel SARs to those of 3-(2-benzothiazol-2-ylmethoxy)-2,6-difluorobenzamide, well known FtsZ inhibitor, and cells alterations typical of FtsZ inhibition indicate such a protein as the target of these potent antibacterial benzodioxane-benzamides.
FtsZ; Antibacterial activity; Benzodioxane; 2,6-Difluorobenzamide; Staphylococcus aureus; Mycobacterium tuberculosis; Methicillin resistance
Settore CHIM/08 - Chimica Farmaceutica
Settore BIO/19 - Microbiologia Generale
Settore MED/07 - Microbiologia e Microbiologia Clinica
Settore CHIM/06 - Chimica Organica
2016
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/417157
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