6533b86ffe1ef96bd12cd481
RESEARCH PRODUCT
A new class of phenylhydrazinylidene derivatives as inhibitors of Staphylococcus aureus biofilm formation
Maria Grazia CusimanoBenedetta MaggioAinars LeonchiksGiuseppe DaidoneBarbara ManachiniStella CascioferroMaria Valeria RaimondiDemetrio RaffaDomenico Schillacisubject
0301 basic medicinemedicine.drug_class030106 microbiologyAntibioticsBacterial adhesionAntibiofilm agentSettore BIO/19 - Microbiologia Generalemedicine.disease_causeMicrobiologyAntivirulence agent03 medical and health sciencesAntibiotic resistanceIn vivomedicineGeneral Pharmacology Toxicology and PharmaceuticsbiologyChemistrySortase AOrganic ChemistryBiofilmPhenylhydrazinylidene derivativebiochemical phenomena metabolism and nutritionbiology.organism_classificationSettore CHIM/08 - Chimica FarmaceuticaGalleria mellonellaSettore AGR/11 - Entomologia Generale E Applicata030104 developmental biologyMechanism of actionBiochemistryStaphylococcus aureusPharmacology Toxicology and Pharmaceutics (all)Sortase Amedicine.symptomdescription
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).
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2016-02-24 | Medicinal Chemistry Research |