Research Article | Volume: 6, Issue: 5, May, 2016

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

Ebaa M. El-Hossary ,  ,  Yassin M. Nissan,  Katharina Edkins,  Heike Bruhn   
Ebaa M. El-Hossary1 , 2, Yassin M. Nissan3, Katharina Edkins4, Heike Bruhn5

1Institute of Pharmacy & Food Chemistry, University of Würzburg, Am Hubland, 97074 Würzburg, Germany.

2Permanent address: National Centre for Radiation Research & Technology, Egyptian Atomic Energy Authority, Ahmed El-Zomor St.

3El-Zohoor Dist., Cairo, Egypt. 3Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt.

4School of Medicine, Pharmacy and Health, Durham University, Stockton-on-Tees, United Kingdom.

5Institute for Molecular Infection Biology, SFB 630, Würzburg University, Josef-Schneider-Str. 2, Bau 15, 97080 Würzburg, Germany.

Open Access   

Published:  May 28, 2016

DOI: 10.7324/JAPS.2016.60502
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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.


Keyword:     13-Thiazolidin-4-oneAntibacterial activityMinimum inhibitory concentration Minimum bactericidal concentrationBiofilm formation.

Citation:

El-Hossary EM, Nissan YM, Edkins K, Bruhn H. Synthesis and antibacterial activity of novel 2-(arylimino)thiazolidin-4-one and 2- (benzylidenehydrazono)-3-arylthiazolidin-4-one derivatives. J App Pharm Sci, 2016; 6 (05): 007-017.

Copyright:The Author(s). This is an open access article distributed under the Creative Commons Attribution Non-Commercial License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
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