| Autor: |
Thibaut, Barbier, Alexia, Barbry, Jérémy, Magand, Cédric, Badiou, Floriane, Davy, Anne, Baudouin, Yves, Queneau, Oana, Dumitrescu, Gérard, Lina, Laurent, Soulère |
| Rok vydání: |
2021 |
| Předmět: |
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| Zdroj: |
Biomolecules |
| ISSN: |
2218-273X |
| Popis: |
The benzo[b]thiophene nucleus and the acylhydrazone functional group were combined to prepare three new series of compounds for screening against Staphylococcus aureus. The reaction of substituted benzo[b]thiophene-2-carboxylic hydrazide and various aromatic or heteroaromatic aldehydes led to a collection of 26 final products with extensive structural diversification on the aromatic ring and on position 6 of the benzo[b]thiophene nucleus. The screening lead to the identification of eight hits, including (E)-6-chloro-N’-(pyridin-2-ylmethylene)benzo[b]thiophene-2-carbohydrazide (II.b), a non-cytotoxic derivative showing a minimal inhibitory concentration of 4 µg/mL on three S. aureus strains, among which were a reference classical strain and two clinically isolated strains resistant to methicillin and daptomycin, respectively. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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