1. Synthesis and biofilm formation reduction of pyrazole-4-carboxamide derivatives in some Staphylococcus aureus strains
- Author
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Maria Grazia Cusimano, Fabiana Plescia, Demetrio Raffa, Domenico Schillaci, Giuseppe Daidone, Maria Valeria Raimondi, Benedetta Maggio, Barbara Manachini, Stella Cascioferro, Cascioferro, S., Maggio, B., Raffa, D., Raimondi, M., Cusimano, M., Schillaci, D., Manachini, B., Plescia, F., and Daidone, G.
- Subjects
0301 basic medicine ,Staphylococcus aureus ,medicine.drug_class ,030106 microbiology ,Carboxamide ,Moths ,N-phenyl-1H-pyrazole-4-carboxamide ,Pyrazole ,Settore BIO/19 - Microbiologia Generale ,medicine.disease_cause ,01 natural sciences ,Microbiology ,Structure-Activity Relationship ,03 medical and health sciences ,chemistry.chemical_compound ,Drug Discovery ,Inhibition of biofilm formation ,medicine ,Animals ,IC50 ,Pharmacology ,Wax ,Virulence ,biology ,010405 organic chemistry ,Drug Discovery3003 Pharmaceutical Science ,Anti-virulence ,Organic Chemistry ,Biofilm ,S. aureu ,General Medicine ,Staphylococcal Infections ,biology.organism_classification ,Settore CHIM/08 - Chimica Farmaceutica ,Anti-Bacterial Agents ,0104 chemical sciences ,Galleria mellonella ,Hydrazines ,Settore AGR/11 - Entomologia Generale E Applicata ,chemistry ,Biofilms ,Larva ,visual_art ,Wax moth larva model ,visual_art.visual_art_medium ,Pyrazoles ,Lead compound - 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.
- Published
- 2016