Fe (III), Co (II), Ni (II), Cu (II), Y (III), Zr (IV), La (III), and U (VI) interact with Gat‐o‐phdn Schiff base (4E,4′E)‐4,4′‐(1,2‐phenylenebis (azaneylylidene))bis(1‐cyclopropyl‐6‐fluoro‐8‐methoxy‐7‐(3‐methylpiperazin‐1‐yl)‐1,4‐dihydroquinoline‐3‐carboxylic acid to produce cationic mononuclear complexes. The isolated solid complexes were characterized with physicochemical, spectroscopic techniques (FT‐IR, UV–Vis and 1H NMR), mass spectrometry, and thermogravimetric analyses. The infrared data indicated that Gat‐o‐phdn acting as tetradentate ligand chelated to the metal ions through the carboxylate oxygen and the nitrogen of azomethine group. The metal ions complete the coordination number with water molecules. The mechanism of the thermal decomposition was detected, and the kinetic parameters of the dissociation steps were evaluated using Coats–Redfern (CR) and Horowitz–Metzger (HM) methods. Bond lengths, bond angles, total energy, heat of formation, dipole moment, and the lowest energy model structures have been determined using density functional theory (DFT) calculations. The synthesized ligand and its complexes were screened for antimicrobial activities against two Gram‐positive bacteria, two Gram‐negative bacteria, and two fungi. The Cu (II) complex was very highly significant against Staphylococcus aureus compared with free Gat‐o‐phdn and references standard control. Also, it showed the highest antibacterial effects compared with all complexes.
A new Schiff base, (N,N \ -phenylene-(bis-1-ethyl-6-fluoro-7-(piperazine-1-yl)quinolone-3-carboxylic acid) and (Nor-o-phdn.2H 2 O), and its derived complexes with nickel (II), cobalt (II), copper (II), iron (III), yttrium (III), lanthanum (III), zirconium (IV) and uranium (VI) were synthesised and distinguished by different tools such as elemental analyses, magnetic properties, molar conductivity, spectroscopic methods (UV-Vis., IR and 1 H-NMR), mass spectrometry and thermogravimetric analysis. Depending on the spectroscopic data, Schiff base Nor-o-phdn.2H 2 O is coordinated to metal centres as a potentially tetradentate ligand via N 2 O 2 atoms. UV-Vis. and magnetic data suggest an octahedral-geometry for all mentioned complexes. Thermogravimetric
Fluoroquinolones emerged as one of potent therapeutic agents, targeting DNA‐signalling pathways. Thus, efforts were spent to create novel quinolones for optimizing their antimicrobial and anticancer properties. Therefore, the new compound N,N′‐phenylene (bis1‐cyclopropyl‐7‐(4‐ethylpiperazin‐1‐yl)‐6‐fluoro‐1,4‐dihydroquinoline‐3‐carboxylic acid) (H2Enro‐o‐phdn) in addition to its related chelates‐contained metals were synthesised and described by spectroscopic, physical methods and thermal analyses. The reaction between H2Enro‐o‐phdn and trivalent La(III), Y(III), and Fe(III) and tetravalent Zr(IV) chloride with molar ratio 1:1 (M:H2Enro‐o‐phdn) yielded the production of chelates. The infrared results elucidate the binding mode of H2Enro‐o‐phdn by means of azomethine nitrogen and carboxylato oxygen atoms as tetradentate. The thermal analyses assured the proposed formula as well as existence of coordinated and latticed H2O molecules. Kinetic parameters for investigated metal complexes were quantified utilisation Horowitz–Metzger in addition to Coats–Redfern methods. Regarding antibacterial efficacy, Y(III) and Fe(III) complexes showed a robust inhibitory activity towards negative‐gram stained (Escherichia coli and Salmonella typhi) and positive‐Gram stained (Staphylococcus aureus and “spore‐forming” Bacillus cereus) strains. Then, we further tested the cytotoxicity of the complexes against the survival of colon‐cancer cells line (CT26). In this regard, in the descending order, Fe(III) > Zr(IV) > La(III) complexes possessed a powerful antitumour activity with IC50 values 6.38, 5.36, and 4.03 μM, respectively, compared with the anticancer drug‐reference cisplatin (16.77 μM). To understand the precise mechanism behind the tumour cell death, Western‐blotting analysis was conducted, to monitor the changes in levels of pro‐apoptotic “P53” protein after drug‐treatment. Results indicated that H2Enro‐o‐phdn with higher covalency metals, like La(III) and Zr(IV) complexes, had the highest upregulation of P53 expression in a threefold to fourfold compared cisplatin, paving the way for a novel P53‐based colon‐cancer therapies.
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