Synthesis and Biological Evaluation of Halogenated 2-Arylimino-3-arythiazolidine- 4-ones Containing Benzoic Acid Fragments as Antibacterial Agents

Title:Synthesis and Biological Evaluation of Halogenated 2-Arylimino-3-arythiazolidine- 4-ones Containing Benzoic Acid Fragments as Antibacterial Agents

Volume: 10 Issue: 10

Author(s): Jie Zhang, Likang Zheng, Huayong Liu, Dan Zhao, Di Qu and Shiqing Han

Affiliation:

Keywords: 2-Arylimino-3-ary-thiazolidine-4-ones, Antibacterial activity, Antibifilm activity, Staphylococcus epidermidis, Staphylococcus aureus, Methicillin-resistant isolates.

Abstract: 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.

Cite this article as:

Zhang Jie, Zheng Likang, Liu Huayong, Zhao Dan, Qu Di and Han Shiqing, Synthesis and Biological Evaluation of Halogenated 2-Arylimino-3-arythiazolidine- 4-ones Containing Benzoic Acid Fragments as Antibacterial Agents, Letters in Drug Design & Discovery 2013; 10 (10) . https://dx.doi.org/10.2174/15701808113109990031