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
Articolo
Data di Pubblicazione:
2016
Citazione:
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]
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.
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
FtsZ; Antibacterial activity; Benzodioxane; 2,6-Difluorobenzamide; Staphylococcus aureus; Mycobacterium tuberculosis; Methicillin resistance
Elenco autori:
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
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