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.
No
English
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
Articolo
Esperti anonimi
Pubblicazione scientifica
2016
Elsevier
120
227
243
17
Pubblicato
Periodico con rilevanza internazionale
IF: 6.514 Quartile: Q1
scopus
Aderisco
info:eu-repo/semantics/article
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]
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Prodotti della ricerca::01 - Articolo su periodico
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262
Article (author)
no
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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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/417157
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