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, novel compounds of hydrazones derived from (2,4-dinitrophenyl) hydrazine were synthesized. Benzamides derivatives and sulfonamides derivatives were prepared from p-amino benzaldehyde. Then these compounds were condensed with (2,4-dinitrophenyl) hydrazine through Imine bond formation to give hydrazones compounds. The compounds were characterized using FT-IR (IR Affinity-1) spectrometer, and 1HNMR analyses. The majority of the compounds have a moderate antimicrobial activity against “Gram-positive bacteria staphylococcus Aureus, and staphylococcus epidermidis, Gram-negative bacteria Escherichia coli, and Klebsiella pneumoniae, and fungi species Candida albicans” using concentrations of 250 µg\ml.
In this work, a series of new maleimides linked to substituted benzothiazole moiety were synthesized. Synthesis of these new cyclic imides were performed via three steps, the first one involved preparation of a series of 2-aminobenzothiazole substituted with different substituents via reaction of different primary aromatic amines with ammonium thiocyanate and bromine in glacial acetic acid. The prepared 2- amino benzothiozoles were introduced in the second step in reaction with maleic anhydride producing a series of N-(substituted benzothiazole-2-yl) maleamic acids.The resulted maleamic acids were dehydrated in the third step via treatment with acetic anhydride and anhydrous sodium acetate to afford a series of the desirable N-(substitu
... Show MoreThe new Schiff base (L) “4‐[(2,4‐dimethoxy‐benzylidene)‐amino]‐1,5‐dimethyl‐2‐phenyl‐1,2‐dihydro‐pyrazol‐3‐one” was synthesized from 2,4‐dimethoxy‐benzaldehyde and 4‐amino‐1,5‐dimethyl‐2‐phenyl‐1,2‐dihydropyrazol‐3‐one, and the geometry of Schiff base was characterized and determined by proton nuclear magnetic resonance (1H‐NMR), mass, Fourier transform infrared (FT‐IR), and ultraviolet‐visible (UV‐vis) spectroscopy. Schiff complexes of Ni(II), Pd(II), Pt(IV), Zn(II), Cd(II), and Mg(II) have been prepared by reaction of ion metals with as‐prepared Schiff base. The results showed that synthesized complexes offered 1:2 m
In the present study a series of some four-,five-and seven-membered heterocyclic compounds have been synthesized by the reaetion of Schiff bases (1a,b) with chloroacetyl chloride, sodium azide, thioglycolic acid or various anhydrides to give azetidinone (2a,b), tetrazole (3a,b), thiazolidinone (4a,b) and 1,3-oxazepine derivatives (5-8a,b) respectively. Schiff bases (1a,b)were prepared from the reaction of p-toluidine with aromatic aldehydes. All synthesized compounds were characterized by physical properties and spectral data.
By unusual method for separating two isomers of a substituted nitro-coumarin using a soxhlet extractor and in controlling temperature to get a selective nitration reaction, several new Schiff base coumarins were synthesized from nitro coumarins as starting material, which were reduced by Fe in glacial acetic acid to produce corresponding amino coumarin derivatives. Then the latter was reacted with different aromatic aldehydes to produce the desired Schiff bases derivatives. After characterization by Fourier transform infrared (FT-IR), Proton nuclear magnetic resonance (1HNMR) and Carbon-13 nuclear magnetic resonance (C-NMR), all these compounds were evaluated as potential Antimicrobial and Antioxidant Agents.
Abstract Organic compounds with pyrazole cores have a variety of uses, notably in the pharmaceutical and agrochemical sectors. The interest in creating pyrazole compounds, examining their many features, and looking for potential uses is growing. Our work has concert with synthesis of chalcones and pyrazolines, then finally pyrazoline-aniline derivatives and evaluation their anti-inflammatory, antibacterial and antifungal activities
The new Schiff base 1‐[(2‐{1‐[(dicyclohexylamino)‐methyl]‐1H‐indol‐3‐yl}‐ethylimino)‐methyl]naphthalen‐2‐ol (HL) was prepared from 1‐{[2‐(1H‐Indol‐3‐yl)‐ethylimino] methyl}‐naphthalen‐2‐ol and dicyclohexyl amine. From this Schiff base, monomeric complexes [M (L)n (H2O)2 Cl2] with M = Cr, Fe, Mn, Cd, and Hg were synthesized and characterized based on elemental analysis (EA), FT‐IR, mass(MS), UV‐visible, thermal analysis, magnetic moment, and molar conductance. The results showed that the geometrical structural were octahedral geometries for the Cr(III) and Fe(III) complex
The new Schiff base 1‐[(2‐{1‐[(dicyclohexylamino)‐methyl]‐1H‐indol‐3‐yl}‐ethylimino)‐methyl]naphthalen‐2‐ol (HL) was prepared from 1‐{[2‐(1H‐Indol‐3‐yl)‐ethylimino] methyl}‐naphthalen‐2‐ol and dicyclohexyl amine. From this Schiff base, monomeric complexes [M (L)n (H2O)2 Cl2] with M = Cr, Fe, Mn, Cd, and Hg were synthesized and characterized based on elemental analysis (EA), FT‐IR, mass(MS), UV‐visible, thermal analysis, magnetic moment, and molar conductance. The results showed that the geometrical structural were octahedral geometries for the Cr(III) and Fe(III) complex