Synthesis and antibacterial study of unsaturated Mannich ketones

Several Mannich ketones of 2-arylmethylenecycloalkanones were synthesised u sing the classical acid-catalysed Mannich reaction. Antibacterial activity of these new water-soluble compounds was reported against Pseudomonas aerug inosa, Escherichia coli, Staphylococcus aureus, Staphylococcus saprophyticu s, Micrococcus luteus and Bacillus subtilis standard strains. Human cell li ne 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 n M mL(-1) for 18) and proved to be efficient antibacterial agents against th e Gram-positive strains. Minimum inhibitory concentrations varied from 1.56 to 100 mug mL(-1). The mechanism of action was examined, too. (C) 2001 Edi tions scientifiques et medicales Elsevier SAS.