Naeem Razaq, Amina Asghar, Amna Mumtaz, Samiah H. Al-Mijalli, Mehr un Nisa, Tauheeda Riaz, Munawar Iqbal, Bilal Shahid
{"title":"合成具有生物活性的头孢泊肟和香草醛基雪夫碱金属配合物,并进行详细的生物学评价。","authors":"Naeem Razaq, Amina Asghar, Amna Mumtaz, Samiah H. Al-Mijalli, Mehr un Nisa, Tauheeda Riaz, Munawar Iqbal, Bilal Shahid","doi":"10.1007/s10534-024-00601-5","DOIUrl":null,"url":null,"abstract":"<div><p>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, <sup>1</sup>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 <i>in-vitro</i> 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 <i>in-vitro</i> 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) <i>in-vitro</i> 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. <i>Patch Dock</i>, 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 <b>2b</b> 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.</p></div>","PeriodicalId":491,"journal":{"name":"Biometals","volume":"37 5","pages":"1201 - 1224"},"PeriodicalIF":4.1000,"publicationDate":"2024-06-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis of biologically active cefpodoxime and vanillin-based schiff base metal complexes with the detailed biological evaluations\",\"authors\":\"Naeem Razaq, Amina Asghar, Amna Mumtaz, Samiah H. 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Synthesis of biologically active cefpodoxime and vanillin-based schiff base metal complexes with the detailed biological evaluations
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, 1H-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.
期刊介绍:
BioMetals is the only established journal to feature the important role of metal ions in chemistry, biology, biochemistry, environmental science, and medicine. BioMetals is an international, multidisciplinary journal singularly devoted to the rapid publication of the fundamental advances of both basic and applied research in this field. BioMetals offers a forum for innovative research and clinical results on the structure and function of:
- metal ions
- metal chelates,
- siderophores,
- metal-containing proteins
- biominerals in all biosystems.
- BioMetals rapidly publishes original articles and reviews.
BioMetals is a journal for metals researchers who practice in medicine, biochemistry, pharmacology, toxicology, microbiology, cell biology, chemistry, and plant physiology who are based academic, industrial and government laboratories.