1. Synthesis of biologically active cefpodoxime and vanillin-based schiff base metal complexes with the detailed biological evaluations.
- Author
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Razaq N, Asghar A, Mumtaz A, Al-Mijalli SH, Nisa MU, Riaz T, Iqbal M, and Shahid B
- Subjects
- Molecular Docking Simulation, Gram-Negative Bacteria drug effects, Molecular Structure, Gram-Positive Bacteria drug effects, Antioxidants pharmacology, Antioxidants chemistry, Antioxidants chemical synthesis, Schiff Bases chemistry, Schiff Bases pharmacology, Schiff Bases chemical synthesis, Anti-Bacterial Agents pharmacology, Anti-Bacterial Agents chemical synthesis, Anti-Bacterial Agents chemistry, Benzaldehydes chemistry, Benzaldehydes pharmacology, Coordination Complexes pharmacology, Coordination Complexes chemistry, Coordination Complexes chemical synthesis, Microbial Sensitivity Tests, Ceftizoxime pharmacology, Ceftizoxime chemistry, Ceftizoxime analogs & derivatives, Ceftizoxime chemical synthesis
- Abstract
Schiff bases of existing antimicrobial drugs are an area, which is still to be comprehensively explored to improve drug efficiency against consistently resisting bacterial species. In this study, we have targeted a new and eco-friendly method of condensation reaction that allows the "green synthesis" as well as improved biological efficacy. The transition metal complexes of cefpodoxime with well-enhanced biological activities were synthesized. The condensation reaction product of cefpodoxime and vanillin was further reacted with suitable metal salts of [Mn (II), Cu (II), Fe (II), Zn (II), and Ni (II)] with 1:2 molar ratio (metal: ligand). The characterization of all the products were carried out by using UV-Visible, elemental analyzer, FTIR,
1 H-NMR, ICP-OES, and LC-MS. Electronic data obtained by UV-Visible proved the octahedral geometry of metal complexes. The biological activities Schiff base ligand and its transition metal complexes were tested by using in-vitro anti-bacterial analysis against various Gram-negative, as well as Gram-positive bacterial strains. Proteinase and protein denaturation inhibition assays were utilized to evaluate the products in-vitro anti-inflammatory activities. The in vitro antioxidant activity of the ligand and its complexes was evaluated by utilizing the 2,2-diphenyl-1-picrylhydrazyl (DPPH) in-vitro method. The final results proved metal complexes to be more effective against bacterial microorganisms as compared to respective parent drug as well as their free ligands. Patch Dock, a molecular docking tool, was used to dock complexes 1a-5e with the crystal structure of GlcN-6-P synthase (ID: 1MOQ). According to the docking results, complex 2b exhibited a highest score (8,882; ACE = -580.43 kcal/mol) that is well correlated with a high inhibition as compared to other complexes which corresponds to the antibacterial screening outcomes., (© 2024. The Author(s), under exclusive licence to Springer Nature B.V.)- Published
- 2024
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