title: Synthesis and biofilm formation reduction of pyrazole-4-carboxamide derivatives in some Staphylococcus aureus strains.
abstract: The ability of several N-phenyl-1H-pyrazole-4-carboxamide derivatives and other pyrazoles opportunely modified at the positions 3, 4 and 5, to reduce the formation of the biofilm in some Staphylococcus aureus strains (ATCC 29213, ATCC 25923 and ATCC 6538) were investigated. All the tested compounds were able, although to a different extent, to reduce the biofilm formation of the three bacterial strains considered. Among these, the 1-(2,5-dichlorophenyl)-5-methyl-N-phenyl-1H-pyrazole-4-carboxamide 14 resulted as the best inhibitor of biofilm formation showing an IC50 ranging from 2.3 to 32 μM, against all the three strains of S. aureus. Compound 14 also shows a good protective effect in vivo by improving the survival of wax moth larva (Galleria mellonella) infected with S. aureus ATCC 29213. These findings indicate that 14d is a potential lead compound for the development of new anti-virulence agents against S. aureus infections.
authors.affiliation: Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche, Via Archirafi, 32, 90123, Palermo, Italy; IEMEST, Istituto Euromediterraneo di Scienza e Tecnologia, via Emerico Amari, 123, 90139, Palermo, Italy.
authors.forename: Stella
authors.initials: S
authors.lastname: Cascioferro
authors.affiliation: Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche, Via Archirafi, 32, 90123, Palermo, Italy. Electronic address: benedetta.maggio@unipa.it.
authors.forename: Benedetta
authors.initials: B
authors.lastname: Maggio
authors.affiliation: Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche, Via Archirafi, 32, 90123, Palermo, Italy. Electronic address: demetrio.raffa@unipa.it.
authors.forename: Demetrio
authors.initials: D
authors.lastname: Raffa
authors.affiliation: Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche, Via Archirafi, 32, 90123, Palermo, Italy.
authors.forename: Maria Valeria
authors.initials: MV
authors.lastname: Raimondi
authors.affiliation: Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche, Via Archirafi, 32, 90123, Palermo, Italy.
authors.forename: Maria Grazia
authors.initials: MG
authors.lastname: Cusimano
authors.affiliation: Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche, Via Archirafi, 32, 90123, Palermo, Italy.
authors.forename: Domenico
authors.initials: D
authors.lastname: Schillaci
authors.affiliation: Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche, Via Archirafi, 32, 90123, Palermo, Italy.
authors.forename: Barbara
authors.initials: B
authors.lastname: Manachini
authors.affiliation: Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche, Via Archirafi, 32, 90123, Palermo, Italy.
authors.forename: Fabiana
authors.initials: F
authors.lastname: Plescia
authors.affiliation: Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche, Via Archirafi, 32, 90123, Palermo, Italy.
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Daidone
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology; D018441:Biofilms / Q000187:drug effects*; D006834:Hydrazines / Q000138:chemical synthesis / Q000494:pharmacology*; D007814:Larva / Q000187:drug effects; D009036:Moths / Q000382:microbiology; D011720:Pyrazoles / Q000138:chemical synthesis / Q000494:pharmacology*; D013203:Staphylococcal Infections / Q000188:drug therapy*; D013211:Staphylococcus aureus / Q000187:drug effects* / Q000502:physiology; D013329:Structure-Activity Relationship; D014774:Virulence / Q000187:drug effects
chemical_list: C000614243:2-((2-(2,5-dichlorophenyl)hydrazinyl)methylene)-3-oxo-N-phenylbutanamide; D000900:Anti-Bacterial Agents; D006834:Hydrazines; D011720:Pyrazoles
keywords: Anti-virulence; Inhibition of biofilm formation; N-phenyl-1H-pyrazole-4-carboxamides; S. aureus; Wax moth larva model