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.

Straniero, V., Pallavicini, M., Chiodini, G., Zanotto, C., Volontè, L., Radaelli, A., Bolchi, C., Fumagalli, L., Sanguinetti, M., Menchinelli, G., Delogu, G., Battah, B., De Giuli Morghen, C., Valoti, E., 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, <<EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY>>, 2016; 120 (May): 227-243. [doi:10.1016/j.ejmech.2016.03.068] [http://hdl.handle.net/10807/80014]

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

Sanguinetti, Maurizio;Menchinelli, Giulia;Delogu, Giovanni;
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.
Inglese
Straniero, V., Pallavicini, M., Chiodini, G., Zanotto, C., Volontè, L., Radaelli, A., Bolchi, C., Fumagalli, L., Sanguinetti, M., Menchinelli, G., Delogu, G., Battah, B., De Giuli Morghen, C., Valoti, E., 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, <<EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY>>, 2016; 120 (May): 227-243. [doi:10.1016/j.ejmech.2016.03.068] [http://hdl.handle.net/10807/80014]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10807/80014
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