Synthesis and Biological Evaluation of Halogenated 2-Arylimino-3-arythiazolidine- 4-ones Containing Benzoic Acid Fragments as Antibacterial Agents
A series of halogenated 2-arylimino-3-ary-thiazolidine-4-ones containing (5-furan-2-yl)-benzoic acid or (5-thiophene-2-yl)-benzoic acid fragments were synthesized, and evaluated in vitro for their antibacterial activity, antibiofilm activity, erythrocyte hemolysis and cytotoxicity. Compounds (7c, 7f, 7i, 7n and 7p) exhibited excellent potency in inhibiting the growth of Staphylococcus epidermidis ATCC35984 (minimal inhibitory concentration (MIC): 0.8 μg/mL). The five compounds also presented promising antibiofilm activity against S. epidermidis ATCC35984 and none of them showed obvious hemolytic activity and cytotoxicity. Further antibacterial effects of the selected five compounds (7c, 7f, 7i, 7n and 7p) against clinical isolates (methicillin-resistant Staphylococcus epidermidis and methicillin-resistant Staphylococcus aureus) were investigated in comparison with methicillin and ampicillin.7p showed the most potent antibacterial activities among the synthesized compounds.
Keywords: 2-Arylimino-3-ary-thiazolidine-4-ones, Antibacterial activity, Antibifilm activity, Staphylococcus epidermidis,
Staphylococcus aureus, Methicillin-resistant isolates.
Rights & PermissionsPrintExport