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EnglishLipophilic 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]
| Autori: | ||
| Titolo: | 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 | |
| Digital Object Identifier (DOI): | http://dx.doi.org/10.1016/j.ejmech.2016.03.068 | |
| Data di pubblicazione: | 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. | |
| Lingua: | Inglese | |
| Rivista: | ||
| Citazione: | 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] | |
| Appare nelle tipologie: | Articolo in rivista, Nota a sentenza |
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