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.
Newly acid hydrazide was synthesized from ethyl 2-(2,3-dimethoxyphenoxy) acetate (2), which is cyclized to the corresponding 4-amino-1,2,4-triazole (3). Five newly azo derivatives (4a-e) were synthesized from this 1,2,4-triazole by converting the amine group to diazonium salt then reacted with various substituent phenol,as well three newly imine derivatives (5a-c) were synthesized from reacting the amine group of compound (3) with three aryl aldehyde. The thermal electro conductivity of these compounds was tested at 30, 50, 75 and 100 áµ’C. compound 4a showed interesting electro conductivity at 75áµ’C as well 5a at 75áµ’C while 5b showed significant conductivity at 100 áµ’C
Small ring heterocycles containing nitrogen and sulfur have been under investigation for a long time because of their important medicinal properties. Among the wide range of heterocycles explored to develop pharmaceutically important molecules, thiadiazoles had played an important role in medicinal chemistry. A survey of literature had shown that compounds having thiadiazole nucleus possess a broad range of biological activities such as anti-inflammatory (1), antibacterial (2), and antifungal activities (3). Thiazine-4-one and their derivatives are import classes of compounds in organic and medicinal chemistry. The thiazine-4-one ring system is a core structure in various synthetic pharmaceutical agents, displaying a broad spectrum of biolo
... Show MoreThe complexes of Schiff base of 4-aminoantipyrine and 1,10-phenanthroline with metal ions Mn (II), Cu (II), Ni (II) and Cd (II) were prepared in ethanolic solution, these complexes were characterized by Infrared , electronic spectra, molar conductance, Atomic Absorption ,microanalysis elemental and magnetic moment measurements. From these studies the tetrahedral geometry structure for the prepared complexes were suggested.The prepared ligand of 4-aminoantipyrine was characterized by using Gc-mass spectrometer .
Both traditional and novel techniques were employed in this work for magnetic shielding evaluation to shed new light on the magnetic and aromaticity properties of benzene and 12 [n]paracyclophanes with n = 3–14. Density functional theory (DFT) with the B3LYP functional and all-electron Jorge-ATZP and x2c-TZVPPall-s basis sets was utilized for geometry optimization and magnetic shielding calculations, respectively. Additionally, the 6-311+G(d,p) basis set was incorporated for the purpose of comparing the magnetic shielding results. In addition to traditional evaluations such as NICS/NICSzz-Scan, and 2D-3D σiso(r)/σzz(r) maps, two new techniques were implemented: bendable grids (BGs) and cylindrical grids (CGs) of ghost atoms (Bqs). BGs a
... Show MoreThis search include the synthesis of some new 1,3-oxazepine derivatives have been prepared, starting from reaction of L-ascorbic acid with dry acetone in presence of dry hydrogen chloride afforded the acetal (I). Treatment of the latter with p-nitrobenzoyl chloride in dry pyridine yielded the ester (II) which was dissolved in (65%) acetic acid in absolute ethanol yielded the glycol (III). The reaction of the glycol (III) with sodium periodate in distilled water at room temperature produced the aldehyde (IV). The compound (V) [2-amino-5-mercapato-1,3,4-thiadiazole] was prepared through the reaction of thiosemicarbazide with carbon disulphide (CS2) in entity of anhydrous (Na2CO3) in (abs. ethanol ). Compound (VI) [2-(5-mercapto-1,3,4-thiadiaz
... Show MoreThe multi-dentate Schiff base ligand (H2L), where H2L=2,2'-(((1,3,5,6)-1-(3-((l1-oxidaneyl)-l5-methyl)-4-hydroxyphenyl)-7-(4-hydroxy-3-methoxyphenyl)hepta-1,6-di ene-3,5-diylidene)bis(azaneylylidene))bis(3-(4-hydroxyphenyl)propanoic acid), has been prepared from curcumin and L- Tyrosine amino acid. The synthesized Schiff base ligand (H2L) and the second ligand 1,10-phenanthroline (phen) are used to prepare the new complexes [Al(L)(phen)]Cl, K[Ag(L)(phen)] and [Pb(L)(phen)]. The synthesized compounds are characterized by magnetic susceptibility measurements, micro elemental analysis (C.H.N), mass spectrometry, molar conductance, FT-infrared, UV-visible, atomic absorption (AA), 13C-NMR, and 1H-NMR spectral studies. The characterization of the
... Show More(E)-2-(benzo[d]thiazol-2-yliazenyl)-4-methoxyaniline was synthesized by reaction the diazonium salt of 2-aminobenzothiazole with 4-methoxyaniline. Identified of the ligand by spectral techniques (UV-Vis, FTIR,1HNMR and LC-Mass) and microelemental analysis (C.H.N.S.O) are used to produce of the azo ligand. Complexes of (Co2+, Ni2+, Cu2+ and Zn2+) were synthesized and identified using atomic absorption of flame, elemental analysis, infrared and UV-Vis spectral process as well conductivity and magnetic quantifications. Nature of compounds produced have been studied followed the mole ratio and continuous contrast methods, Beer's law followed during a concentration scope (1×10-4-3×10-4 mole/L). height molar absorptivity of compound solutions h
... Show More