Schiff bases of Ceftizoxime sodium were synthesized in an attempt to improve the antimicrobial spectrum of Ceftizoxime. Aminothiazole ring of Ceftizoxime is linked directly through an imino group to different aromatic aldehydes reacted by nucleophilic addition using trimethylamine (TEA), as a catalyst and refluxed in methanol. The antimicrobial activity was evaluated for such Schiff bases using disc diffusion method. Molecular docking was conducted on certain penicillin-binding proteins (PBPs) and carboxypeptidases using 1- click docking software. Schiff bases of Ceftizoxime were prepared with reasonable yields and their chemical structures were confirmed by spectral analysis (FTIR, 1H-NMR) and elemental microanalysis (CHNS). The antibacterial evaluation of the new Schiff bases of Ceftizoxime showed better antibacterial activities when compared with Ceftizoxime sodium. Molecular docking has recorded lower docking scores of all Schiff bases in comparison with Ceftizoxime sodium. This means that they needed less energy of binding with PBPs and carboxypeptidases and hence have better bioactivities. This chemical modification may afford newer cephalosporins having Schiff bases at the aminothiazole ring of improved activities.
In this work, lanthanium (III) complexes were synthesized using by Schiff base ligand (L) derived from benzaldehyde and o-aminoaniline with five amino acids (AA) from glycine (Gly), L-alanine (Ala), L-valine (Val), L-asparagine (Asp) and DL- phenylalanine (Phe). The Schiff base ligand has been characterized by elemental analysis, (MASS, FTIR, 1HNMR, 13CNMR, UV-VIS) electronic spectra. The structures of the new complexes have been described of analysis of elements, molar conductivity, (UV-Vis electronic, FTIR, mass) spectra also magnetic moment. The molar conductivity values of the complexes indicat this every of complexes are electrolytes and other analytical studies reveal octahedral geometry for La (III) ion. The Schiff base ligand, five
... Show MoreThe Cu(II) was found using a quick and uncomplicated procedure that involved reacting it with a freshly synthesized ligand to create an orange complex that had an absorbance peak of 481.5 nm in an acidic solution. The best conditions for the formation of the complex were studied from the concentration of the ligand, medium, the eff ect of the addition sequence, the eff ect of temperature, and the time of complex formation. The results obtained are scatter plot extending from 0.1–9 ppm and a linear range from 0.1–7 ppm. Relative standard deviation (RSD%) for n = 8 is less than 0.5, recovery % (R%) within acceptable values, correlation coeffi cient (r) equal 0.9986, coeffi cient of determination (r2) equal to 0.9973, and percentage capita
... Show MoreAmoxicillin have been conjugated with metronidazole as possible mutual prodrug to get a wider spectrum of activity by acting on aerobic and anaerobic bacteria, have antifungal activity, to provide protection for beta lactam ring of amoxicillin and also to improve patient compliance as it given as a single dose therapy. The structures of the synthesized compound were confirmed and characterized using elemental microanalysis (CHN), IR and some physiochemical properties. Biological study was done by using disc diffusion method against different bacterial strains which are , Staphylococcus aureus , Salmonella typhie , Pseudomonas aeruginosa , E. coli , Klebsiella pneumonia and fungi ( Candida albicans) . using nutrien
... Show MoreIn this work we prepared some schiff bases by condensation urea and benzaldehyde or its derevative ( bromo benzaldehyde or hydroxy benzaldehyde ) as ( 1 : 1 ) mole ( urea : benzaldehyde or its substitution ) to prepare compounds ( A1 , B1 , C1 , D1 , E1 , F1 , G1 ) and ( 1 : 2 ) mole ( urea : benzaldehyde or its substitution ) to prepare compounds ( A2 , B2 , C2 , D2 , E1 , F2 , G2 ) . The prepared compounds identified spectroscopic by infrared spectroscopy FT-IR and Thin layer chromotography T.L.C . The force constant calculated from the wave number for the carbonyl stretching from FT-IR chart and by using the following equation K = 4?2C2?'2? The change in double bond order for carbonyl deteremined in according with some past re
... Show MoreSynthesis of 2-mercaptobenzothiazole (A1) is performed from the reaction of o-aminothiophenol and carbon disulfide CS2 in ethanol under basic condition. Compound (A1) is reacted with chloro acetyl chloride to give compound (A2). Hydrazide acid compound (A3) is obtained from the reaction of compound (A2) with hydrazine hydrate in ethanol under reflux in the presence of glacial acetic acid .The reaction of hydrazide acid compound (A3) with ethyl acetoacetate gives pyrazole compound (A4). The new hydrazone compound (A5) was prepared from the reaction of compound (A3) with benzaldehyde. Reaction of compound
... Show MoreA new tridentate ligand has been synthesized derived from phenyl(pyridin-3-yl)methanone. Three coordinated metal complexes were prepared by complexation of the new ligand with Cu(II), Ni(II) and Zn(II) metal salts. The new Schiff base “benzyl -2-[phenyl(pyridin-3-yl)methylidene]hydrazinecarbodithioate” and the new metal complexes were characterized using various physico-chemical and spectroscopic techniques. From the analysis results, the expected structure to the metal complexes are octahedral in geometry for Cu(II) complex, square planner for Ni(II) and tetrahedral for Zn(II) complex. The new compounds are expected to show strong bioactivity against bacteria and cancer cells.
This study includes synthesis of some nitrogenous heterocyclic compounds linked to amino acid esters or heterocyclic amines that may have a potential activity as antimicrobial and/or cytotoxic. Quinolines are an important group of organic compounds that possess useful biological activity as antibacterial, antifungal and antitumor .8-Hydroxyquinoline (8-HQ) and numerous of its derivatives exhibit potent activities against fungi and bacteria which make them good candidates for the treatment of many parasitic and microbial infection diseases.
These pharmacological properties of quinolones aroused our interest in synthesizing several new compounds featuring heterocyclic rings of the quinoline derivatives linke
... Show MoreA new mixed ligand complexes have been prepared between 8- hydroxy quinoline and o-hydroxybenzylidene-1-phenyl-2,3-dimethyl-4-amino-3-pyrazolin-5-on with Mn(II),Fe(II),Co(II),Ni(II) and Cu(II) ions . the prepared complexes were isolated and characterized by (FT-IR)and (UV-Vis) spectroscopy. Elemental analysis (C.H.N) Flame atomic absorption technique . in addition to magnetic susceptibility and conductivity measurement.
Aim: To evaluate the cytotoxic activity of newly synthesized a series of novel HDAC inhibitors comprising sulfonamide as zinc binding group and Isatin derivatives as cap group joined by mono amide linker as required to act as HDAC inhibitors. Materials and Methods: The utilization of sulfonamide as zinc binding group joined by N-alkylation reaction with ethyl-bromo hexanoate as linker group that joined by amide reaction with Isatin derivatives as cap groups which known to possess antitumor activity in the designed of new histone deacetylase inhibitors and using the docking and MTT assay to evaluate the compounds. Results: Four compounds have been synthesized and characterized successfully by ART-FTIR, NMR and ESI-Ms. the compounds w
... Show MoreA new series of metal ions complexes of VO(II), Cr(III), Mn(II), Zn(II), Cd(II) and Ce(III) have been synthesized from the Schiff bases (4-chlorobenzylidene)-urea amine (L1) and (4-bromobenzylidene)-urea amine (L2). Structural features were obtained from their elemental microanalyses, magnetic susceptibility, molar conductance, FT-IR, UV–Vis, LC-Mass and 1HNMR spectral studies. The UV–Vis, magnetic susceptibility and molar conductance data of the complexes suggest a tetrahedral geometry around the central metal ion except, VOII complexes that has square pyramidal geometry, but CrIII and CeIII octahedral geometry. The biological activity for the ligand (L1) and its Vanadium and Cadmium complexes were studied. Structural geometries of com
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