TY - JOUR
T1 - A new class of phenylhydrazinylidene derivatives as inhibitors of Staphylococcus aureus biofilm formation
AU - Cascioferro, Stella Maria
AU - Raimondi, Maria Valeria
AU - Maggio, Benedetta
AU - Raffa, Demetrio
AU - Cusimano, Maria Grazia
AU - Daidone, Giuseppe
AU - Manachini, Barbara Rosy Ines
AU - Schillaci, Domenico
AU - Cascioferro, Stella
AU - Leonchiks, Ainars
PY - 2016
Y1 - 2016
N2 - 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).
AB - 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).
UR - http://hdl.handle.net/10447/179978
UR - http://www.springerlink.com/content/1054-2523
M3 - Article
VL - 25
SP - 870
EP - 878
JO - Medicinal Chemistry Research
JF - Medicinal Chemistry Research
SN - 1054-2523
ER -