Synthesis and Biological Evaluation of Benzo[ b ]thiophene Acylhydrazones as Antimicrobial Agents against Multidrug-Resistant Staphylococcus aureus

The benzo[ ]thiophene nucleus and the acylhydrazone functional group were combined to prepare three new series of compounds for screening against . The reaction of substituted benzo[ ]thiophene-2-carboxylic hydrazide and various aromatic or heteroaromatic aldehydes led to a collection of 26 final pr...

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Bibliographic Details
Published in:Biomolecules (Basel, Switzerland) Switzerland), 2022-01, Vol.12 (1), p.131
Main Authors: Barbier, Thibaut, Barbry, Alexia, Magand, Jérémy, Badiou, Cédric, Davy, Floriane, Baudouin, Anne, Queneau, Yves, Dumitrescu, Oana, Lina, Gérard, Soulère, Laurent
Format: Article
Language:English
Subjects:
Acids
acylhydrazone
Aldehydes
Anti-Bacterial Agents - chemistry
Anti-Infective Agents
antibacterial
Antibiotics
Antimicrobial agents
benzothiophene
Chemical Sciences
Chromatography
Cytotoxicity
Daptomycin
Drug resistance
Medicinal Chemistry
Methicillin
Methicillin-Resistant Staphylococcus aureus
Microbial Sensitivity Tests
MRSA
Multidrug resistance
Multidrug resistant organisms
NMR
Nuclear magnetic resonance
Pathogens
Staphylococcus aureus
Staphylococcus infections
Thiophenes - pharmacology
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Summary:The benzo[ ]thiophene nucleus and the acylhydrazone functional group were combined to prepare three new series of compounds for screening against . The reaction of substituted benzo[ ]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[ ]thiophene nucleus. The screening lead to the identification of eight hits, including ( )-6-chloro- '-(pyridin-2-ylmethylene)benzo[ ]thiophene-2-carbohydrazide ( ), a non-cytotoxic derivative showing a minimal inhibitory concentration of 4 µg/mL on three strains, among which were a reference classical strain and two clinically isolated strains resistant to methicillin and daptomycin, respectively.
ISSN:2218-273X
2218-273X
DOI:10.3390/biom12010131