Synthesis and antibacterial study of unsaturated Mannich ketones
Several Mannich ketones of 2-arylmethylenecycloalkanones were synthesised using the classical acid-catalysed Mannich reaction. Antibacterial activity of these new water-soluble compounds was reported against Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus, Staphylococcus saprophyticu...
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Veröffentlicht in: | European journal of medicinal chemistry 2001-09, Vol.36 (9), p.705-717 |
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Hauptverfasser: | , , , , , , , |
Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | Several Mannich ketones of 2-arylmethylenecycloalkanones were synthesised using the classical acid-catalysed Mannich reaction. Antibacterial activity of these new water-soluble compounds was reported against
Pseudomonas aeruginosa,
Escherichia coli,
Staphylococcus aureus,
Staphylococcus saprophyticus,
Micrococcus luteus and
Bacillus subtilis standard strains. Human cell line cytotoxicity of our new compounds was evaluated against HeLa cell lines. Some compounds showed low cytotoxicity (41.52 nM
mL
−1 for
14 and 46.60 nM
mL
−1 for
18) and proved to be efficient antibacterial agents against the Gram-positive strains. Minimum inhibitory concentrations varied from 1.56 to 100 μg
mL
−1. The mechanism of action was examined, too. |
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ISSN: | 0223-5234 1768-3254 |
DOI: | 10.1016/S0223-5234(01)01264-8 |