Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


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

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


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.

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Article Details

Year: 2013
Page: [928 - 934]
Pages: 7
DOI: 10.2174/15701808113109990031
Price: $58