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EnglishA FRET-based random screening assay was used to generate hit compounds as sortase A inhibitors that allowed us to identify ethyl 3-oxo-2-(2-phenylhydrazinylidene)butanoate as an example of a new class of sortase A inhibitors. Other analogues were generated by changing the ethoxycarbonyl function for a carboxy, cyano or amide group, or introducing substituents in the phenyl ring of the ester and acid derivatives. The most active derivative found was 3-oxo-2-(2-(3,4dichlorophenyl)hydrazinylidene)butanoic acid (2b), showing an IC50 value of 50 μM. For a preliminary assessment of their antivirulence properties the new derivatives were tested for their antibiofilm activity. The most active compound resulted 2a, which showed inhibition of about 60% against S. aureus ATCC 29213, S. aureus ATCC 25923, S. aureus ATCC 6538 and S. epidermidis RP62A at a screening concentration of 100 μM.
Maggio, B., Raffa, D., Raimondi, M., Cascioferro, S., Plescia, F., Schillaci, D., et al. (2016). Discovery of a new class of sortase a transpeptidase inhibitors to tackle gram-positive pathogens: 2-(2-phenylhydrazinylidene)alkanoic acids and related derivatives. MOLECULES, 21(2) [10.3390/molecules21020241].
| Data di pubblicazione: | 2016 | |
| Titolo: | Discovery of a new class of sortase a transpeptidase inhibitors to tackle gram-positive pathogens: 2-(2-phenylhydrazinylidene)alkanoic acids and related derivatives | |
| Autori: | ||
| Citazione: | Maggio, B., Raffa, D., Raimondi, M., Cascioferro, S., Plescia, F., Schillaci, D., et al. (2016). Discovery of a new class of sortase a transpeptidase inhibitors to tackle gram-positive pathogens: 2-(2-phenylhydrazinylidene)alkanoic acids and related derivatives. MOLECULES, 21(2) [10.3390/molecules21020241]. | |
| Rivista: | ||
| Digital Object Identifier (DOI): | http://dx.doi.org/10.3390/molecules21020241 | |
| Abstract: | A FRET-based random screening assay was used to generate hit compounds as sortase A inhibitors that allowed us to identify ethyl 3-oxo-2-(2-phenylhydrazinylidene)butanoate as an example of a new class of sortase A inhibitors. Other analogues were generated by changing the ethoxycarbonyl function for a carboxy, cyano or amide group, or introducing substituents in the phenyl ring of the ester and acid derivatives. The most active derivative found was 3-oxo-2-(2-(3,4dichlorophenyl)hydrazinylidene)butanoic acid (2b), showing an IC50 value of 50 μM. For a preliminary assessment of their antivirulence properties the new derivatives were tested for their antibiofilm activity. The most active compound resulted 2a, which showed inhibition of about 60% against S. aureus ATCC 29213, S. aureus ATCC 25923, S. aureus ATCC 6538 and S. epidermidis RP62A at a screening concentration of 100 μM. | |
| URL: | http://www.mdpi.com/1420-3049/21/2/241/pdf | |
| Settore Scientifico Disciplinare: | Settore CHIM/08 - Chimica Farmaceutica Settore BIO/19 - Microbiologia Generale | |
| Appare nelle tipologie: | 1.01 Articolo in rivista |
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