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

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• 作者：Stella Cascioferro ; Benedetta Maggio ; Demetrio Raffa…
• 关键词：Phenylhydrazinylidene derivatives ; Antibiofilm agents ; Sortase A ; Antivirulence agents ; Bacterial adhesion
• 刊名：Medicinal Chemistry Research
• 出版年：2016
• 出版时间：May 2016
• 年：2016
• 卷：25
• 期：5
• 页码：870-878
• 全文大小：574 KB
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• 作者单位：Stella Cascioferro (1) (2)
  Benedetta Maggio (1)
  Demetrio Raffa (1)
  Maria Valeria Raimondi (1)
  Maria Grazia Cusimano (1)
  Domenico Schillaci (1)
  Barbara Manachini (1)
  Ainars Leonchiks (3)
  Giuseppe Daidone (1)
  
  1. Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche - Sezione di Chimica e Tecnologie Farmaceutiche, Università degli Studi di Palermo, Via Archirafi 32, 90123, Palermo, Italy
  2. IEMEST, Istituto Euromediterraneo di Scienza e Tecnologia, Via Emerico Amari, 123, 90139, Palermo, Italy
  3. Latvian Biomedical Research and Study Centre, Ratsupites 1, Riga, 1067, Latvia
  
• 刊物主题：Pharmacology/Toxicology; Biochemistry, general; Cell Biology;
• 出版者：Springer US
• ISSN：1554-8120

文摘

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).