In the struggle against the emergence of the antibiotic resistance, new molecules targeting biofilm formation could be useful as adjuvant of conventional antibiotics. This study focused on a new class of 2-phenylhydrazinylidene derivatives as antivirulence agents. The compound 12e showed interesting activities against biofilm formation of all tested Staphylococcus aureus strains with IC50 ranging from 1.7 to 43 μM; compounds 12f and 13a resulted strong inhibitors of S. aureus ATCC 6538 and ATCC 29213 biofilm formation with IC50 of 0.9 and 0.8 μM, respectively. A preliminary study on the mechanism of action was carried on evaluating the inhibition of sortase A transpeptidase. Compound 12e resulted not to be toxic at 1 mg/ml by using an in vivo model (the wax moth larva model, Galleria mellonella).

Cascioferro, S., Maggio, B., Raffa, D., Raimondi, M., Cusimano, M., Schillaci, D., et al. (2016). A new class of phenylhydrazinylidene derivatives as inhibitors of Staphylococcus aureus biofilm formation. MEDICINAL CHEMISTRY RESEARCH, 25(5), 870-878 [10.1007/s00044-016-1535-9].

A new class of phenylhydrazinylidene derivatives as inhibitors of Staphylococcus aureus biofilm formation

CASCIOFERRO, Stella Maria;MAGGIO, Benedetta;RAFFA, Demetrio;RAIMONDI, Maria Valeria;CUSIMANO, Maria Grazia;SCHILLACI, Domenico;MANACHINI, Barbara Rosy Ines;DAIDONE, Giuseppe
2016-01-01

Abstract

In the struggle against the emergence of the antibiotic resistance, new molecules targeting biofilm formation could be useful as adjuvant of conventional antibiotics. This study focused on a new class of 2-phenylhydrazinylidene derivatives as antivirulence agents. The compound 12e showed interesting activities against biofilm formation of all tested Staphylococcus aureus strains with IC50 ranging from 1.7 to 43 μM; compounds 12f and 13a resulted strong inhibitors of S. aureus ATCC 6538 and ATCC 29213 biofilm formation with IC50 of 0.9 and 0.8 μM, respectively. A preliminary study on the mechanism of action was carried on evaluating the inhibition of sortase A transpeptidase. Compound 12e resulted not to be toxic at 1 mg/ml by using an in vivo model (the wax moth larva model, Galleria mellonella).
2016
Settore CHIM/08 - Chimica Farmaceutica
Settore BIO/19 - Microbiologia Generale
Settore AGR/11 - Entomologia Generale E Applicata
Cascioferro, S., Maggio, B., Raffa, D., Raimondi, M., Cusimano, M., Schillaci, D., et al. (2016). A new class of phenylhydrazinylidene derivatives as inhibitors of Staphylococcus aureus biofilm formation. MEDICINAL CHEMISTRY RESEARCH, 25(5), 870-878 [10.1007/s00044-016-1535-9].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10447/179978
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