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Molecules 2016, 21(5), 568; doi:10.3390/molecules21050568

Design, Synthesis, Antimicrobial Evaluation and Molecular Modeling Study of 1,2,4-Triazole-Based 4-Thiazolidinones

1
Department of Pharmacognosy and Pharmaceutical Chemistry, College of Pharmacy, Taibah University, Al-Madinah, Al-Munawarah 30001, Saudi Arabia
2
Department of Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt
3
Pharmaceutical Chemistry, Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar University, Cairo 11884, Egypt
4
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt
5
Department of Pharmaceutics, College of Pharmacy, King Saud University, P. O. Box 2457, Riyadh 11451, Saudi Arabia
6
Department of Microbiology and Immunology, Faculty of Pharmacy, Al-Azhar University, Nasr City, Cairo 11884, Egypt
*
Author to whom correspondence should be addressed.
Academic Editor: Peter J. Rutledge
Received: 17 March 2016 / Revised: 17 April 2016 / Accepted: 22 April 2016 / Published: 30 April 2016
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [4164 KB, uploaded 30 April 2016]   |  

Abstract

A series of 3-(2H-1,2,4-triazol-5-yl)-1,3-thiazolidin-4-one derivatives (7cl) was designed and synthesized. Their structures have been elucidated based on analytical and spectral data. They were evaluated for their antibacterial and antifungal activities. Compound 7h showed the highest activity against all tested strains, except P. vulgaris, with MIC 8 μg/mL and 4 μg/mL against S. aureus and C. albicans, respectively. Furthermore, Compounds 7c, 7h, and 7j demonstrated moderate anti-mycobacterium activity. The binding mode of the synthesized thiazolidinones to bacterial MurB enzyme was also studied. Good interactions between the docked compounds to the MurB active site were observed primarily with Asn83, Arg310, Arg188 and Ser82 amino acid residues. View Full-Text
Keywords: 4-thiazolidinones; 1,2,4-triazoles; antibacterial agents; antifungal agents; molecular docking 4-thiazolidinones; 1,2,4-triazoles; antibacterial agents; antifungal agents; molecular docking
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MDPI and ACS Style

Ahmed, S.; Zayed, M.F.; El-Messery, S.M.; Al-Agamy, M.H.; Abdel-Rahman, H.M. Design, Synthesis, Antimicrobial Evaluation and Molecular Modeling Study of 1,2,4-Triazole-Based 4-Thiazolidinones. Molecules 2016, 21, 568.

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