Harnessing the antibacterial activity of new thiosemicarbazone and their corresponding acetylthiazole compounds

Document Type : Original Article

Authors

1 Department of Chemistry, Faculty of Science, Mansoura University, 35516 Mansoura, Egypt

2 Chemistry Department, Faculty of Science, Mansoura University

3 Applied Organic Chemistry Department, Chemical Industries Research Institute, National Research Centre, Dokki, Giza, 12622 Egypt

Abstract

The escalating prevalence of bacteria resistant to antibiotics has created a significant worldwide health challenge, necessitating the urgent development of innovative antimicrobial medications. Our research focuses on the synthesis of thiosemicarbazone derivatives 2a and 2b by condensation of 3-(benzofuryl)-1-phenyl-pyrazole-4-carbaldehyde derivatives 1a and 1b with thiosemicarbazide. Thiosemicarbazone compounds 2a and 2b were cyclized when subjected to reflux with 3-chloroacetylacetone in ethanol and triethylamine to produce the corresponding 5-acetyl-4-methylthiazole compounds 3a and 3b, respectively. The chemical structures of 5-acetylthiazoles 3a and 3b were supported by compatible spectral analyses. The antibacterial properties of thiosemicarbazones 2a-b and their corresponding 5-acetylthiazole compounds 3a-b were assessed in E. coli and S. aureus. The results were compared those with of the reference antibiotic Gentamycin. Additionally, the compounds were tested against the fungus Candida albicans and compared to Ketoconazole. 5-Acetylthiazole compound 3b exhibited significant activity against Candida albicans and slightly less potent inhibition of Staphylococcus aureus. To understand the ligand interaction with protein receptors available in the RCSB Protein Data Bank (PDB ID 2FZD), human aldose reductase complexed with tolrestat at 1.08 A resolution.

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