Synthesis and antimicrobial evaluation of new halogenated 1,3-Thiazolidin-4-ones.
Bioorg Chem
; 95: 103517, 2020 01.
Article
en En
| MEDLINE
| ID: mdl-31884138
ABSTRACT
The ongoing prevalence of multidrug-resistant bacterial pathogens requires the development of new effective antibacterial agents. In this study, two series of halogenated 1,3-thiazolidin-4-ones were synthesized and characterized. All the synthesized thiazolidinone derivatives were evaluated for their antimicrobial activity. Biological screening of the tested compounds revealed the antibacterial activity of the chlorinated thiazolidinones 4a, 4b and 4c against Escherichia coli TolC-mutant, with MIC values of 16 µg/mL. A combination of a sub-inhibitory concentration of colistin (0.25 × MIC) with compounds 4a, 4b or 4c showed antibacterial activity against different Gram-negative bacteria (MICs = 4-16 µg/mL). Interestingly, compounds 4a, 4b and 4c were not cytotoxic to murine fibroblasts and Caco-2 cells. The chlorinated thiazolidinone derivative 16d demonstrated a bacteriostatic activity against a panel of pathogenic Gram-positive bacteria, including clinical isolates of methicillin and vancomycin-resistant Staphylococcus aureus, Listeria monocytogenes and multidrug-resistant Staphylococcus epidermidis (MICs = 8 - 64 µg/mL), with no cytotoxicity against both Caco-2 and L929 cells. Compound 16d was superior to vancomycin in disruption of the pre-formed MRSA biofilm. Furthermore, the three fluorinated thiazolidinone derivatives 26c, 30c and 33c showed a hindrance to hemolysin activity, without cytotoxicity against L929 cells.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Bacterias Gramnegativas
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Bacterias Grampositivas
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Antibacterianos
Tipo de estudio:
Risk_factors_studies
Límite:
Animals
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Humans
Idioma:
En
Revista:
Bioorg Chem
Año:
2020
Tipo del documento:
Article
País de afiliación:
Egipto