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Synthesis and antibacterial activity of novel 2-(arylimino)thiazolidin-4-one and 2-(benzylidenehydrazono)-3-arylthiazolidin-4-one derivatives

El-Hossary, Ebaa M.; Nissan, Yassin M.; Edkins, Katharina; Bruhn, Heike

Synthesis and antibacterial activity of novel 2-(arylimino)thiazolidin-4-one and 2-(benzylidenehydrazono)-3-arylthiazolidin-4-one derivatives Thumbnail


Authors

Ebaa M. El-Hossary

Yassin M. Nissan

Katharina Edkins

Heike Bruhn



Abstract

The ongoing spread of multidrug-resistant bacteria demands an intensive search for new antibacterial agents. In the present study, a series of new 1,3-thiazolidin-4-ones has been synthesized and investigated for its in vitro antibacterial activity. The most potent antibacterial compound 4c was found to be active, at low micromolar range, against Staphylococcus aureus, Staphylococcus epidermidis, Enterococcus faecalis and the pneumonic plague causative agent Yersinia pestis with minimum inhibitory concentrations of 5 µM, 2.5 µM, 2.5 µM and 5 µM, respectively. Compound 4c showed the ability to kill E. faecalis JH212 strain with a minimum bactericidal concentration of 5 µM. Furthermore, compounds 9b and 10a inhibited the biofilm formation in S. epidermidis, where they showed 70% to 80% inhibition at a concentration of 40 µM.

Citation

El-Hossary, E. M., Nissan, Y. M., Edkins, K., & Bruhn, H. (2016). Synthesis and antibacterial activity of novel 2-(arylimino)thiazolidin-4-one and 2-(benzylidenehydrazono)-3-arylthiazolidin-4-one derivatives. Journal of Applied Pharmaceutical Science, 6(05), 007-017. https://doi.org/10.7324/japs.2016.60502

Journal Article Type Article
Acceptance Date Apr 8, 2016
Online Publication Date May 28, 2016
Publication Date May 28, 2016
Deposit Date Jun 9, 2016
Publicly Available Date Jun 10, 2016
Journal Journal of Applied Pharmaceutical Science
Publisher Journal of Applied Pharmaceutical Science
Peer Reviewed Peer Reviewed
Volume 6
Issue 05
Pages 007-017
DOI https://doi.org/10.7324/japs.2016.60502

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