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.
A new Schiff base (4-chlorophenyl)(phenyl methanimine (6R,7R)-3-methyl-8-oxo-7-(2-phenylpropanamido)-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate=HL=C29H24ClN3O4S) has been synthesized from β-lactam antibiotic (cephalexin mono hydrate (CephH)=(C16H19N3O5S.H2O) and 4- chlorobenzophenone. Metal mixed ligand complexes of the Schiff base were prepared from chloride salt of Fe(II), Co(II), Ni(II), Cu(II), Zn(II) and Cd(II), in 50% (v/v) ethanol – water medium in aqueous ethanol(1:1) and Saccharin(C7H5NO3S) containing sodium hydroxide. Several physical tools in particular; IR, C:H:N , 1H NMR,13C NMR for ligand, melting point, molar conductance, magnetic moment. and determination of the percentage of the metal in the complexes by flame(AAS
... Show MoreThis research includes synthesis of new heterocyclic derivatives of N-benzyl-5-bromoisatin. New 1, 2, 4-triazole, oxazoline and thiazoline derivatives of [N-benzyl-5-bromo-3-(Ethyliminoacetate)-indole-2-one] (2) have been synthesized. The preparation process started by the reaction of 5-bromoisatin with sodium hydride in dimethylformamide (DMF) at 0°C, gave suspension of sodium salt of 5-bromoisatin and subsequent reaction with benzylchloride to give N-benzyl-5-bromoisatin (1). Compound (1) reacted with ethylglycinate (Schiff base) obtained the intermediate compound (2) which reacted with different reagents in two ways. The first way, compound (2) reacted with (hydrazine hydrate, semicarbazide, phenylsemicarbazide and thiosemicarbazide)
... Show MoreIn study of effective bioactive compounds, we have synthesized the Co((ІІ), Mn(ІІ), Fe(ІІ), Cu(ІІ), Ni(ІІ), and Zn(ІІ) complexes of the Schiff base derived from trimethoprim and2'-amino-4-chlorobenzophenone and characterized by spectroscopic (NMR, IR, Mass, UV–vis,), analytical, TGA studies and magnetic data .The solution electronic spectral study suggests the stoichiometry of the synthesized complexes and Elemental analysis detected the square planer and octahedral geometry of the compounds. The prepared metal complexes presented promoted efficiency versus the screened bacterial (Escherichia Coli and Staphylococcus aureus) antibacterial efficacy against (Staphylococcus aureus, Salmonella spp., E. coli, Vibrio spp., Pseud
... Show MoreThis study including synthesis of some new Schiff bases compounds [1‐6] from the reaction of Sulfamethoxazole drug with some aromatic aldehydes in classical Schiff base method then treatment Schiff bases with succinic anhydride to get oxazepines rings [7-11]These derivatives were characterized by melting point, FT‐IR, 1H NMR and mass spectra. Some of synthesized compounds were evaluated in vitro for their antibacterial activities against three kinds of pathogenic strains Staphylococcus aureus, Escherichia coli
A new series of 5-methoxy-2-mercapto benzimidazole derivatives were synthesized by the reaction of 5-methoxy- 2-mercaptobenzimidazole with chloroacetic acid and affords 2-((5-methoxy-1H-benzo[d]imidazol-2-yl)thio) acetic acid (1),which on cyclization with acetic anhydride and pyridine gives 7- methoxybenzo[4,5]imidazo[2,1-b]thiazol- 3(2H)-one(2), which on condensation with different aryl aldehydes in the presence of anhydrous sodium acetate in glacial acetic acid, furnishes a arylidene thiazolidinone. The purity of the synthesized compounds was confirmed by melting point and TLC.The structures were established by different spectral analysis such as FTIR,1HNMR, and CHN analysis. The newly synthesized compounds (3a-d) were in vivo evaluated f
... Show More
(4)
Heterogeneous organic compounds play an important role in our daily life as they contribute in many medical and industrial fields and are in continuous development as a result of the preparation of new derivatives with different properties. From this premise, the goal of this work appears, which is preparation of (four, five, six, and seven) membered ring systems derived from furfural, by its reaction with different aromatic aldehydes, and record their antioxidant activity by using free radical scavenging method of DPPH radicals. The new ring systems are synthesized by reacting the prepared Schiff-bases with different ring closure agents (chloroacetyl chloride, mercaptoaceticacid, anthranilic acid, and phthalic anhydride), the prep
... Show More
(9)
(3)
The Ligand 6,6--(1,2-benzenediazo) bis (3-aminobenzoicacid) derived from o-phenylenediamine and 3-aminobenzoicacid was synthesized. The prepared ligand was identified by Microelemental Analysis, 1HNMR, FT-IR and UV-Vis spectroscopic techniques. Treatment of the ligand with the following metal ions (CoII, NiII, CuII and ZnII ) in aqueous ethanol with a 1:1 M:L ratio and at optimum pH. Characterization of these compounds has been done on the basis of elemental analysis, electronic data, FT-IR and UV-Vis, as well as magnetic susceptibility and conductivity measurements. The nature of the complexes formed were studied following the mole ratio and continuous variation methods, Beer's law obeyed over a concentration range (1×10-4 - 3×10-4 M). H
... Show MoreThe preparation, spectroscopic characterisation of complexes derived from the mixed ligands with CdII, ZnII and CoII metal ions with Schiff base, Dithiocarbamates (DTCs) and 8-Hydroxyquinoline are reported. The compounds that prepared have been defined via; chloride content, F.T-IR, UV-Vis 1H-NMR spectroscopy and C.H.N.S, as well as conductance and magnetic susceptibility.All data which collected from such methods specified complexes with 6 coordinates in solution and solid states. The biologicalactivity that is related to all the prepared compounds which were screened for their antimicrobial activitiesagainst (G+ and (G-)). The data that collected from biological activity indicate that complexes will have extra activity against such tested
... Show MoreThe preparation, spectroscopic characterisation of complexes derived from the mixed ligands with CdII, ZnII and CoII metal ions with Schiff base, Dithiocarbamates (DTCs) and 8-Hydroxyquinoline are reported. The compounds that prepared have been defined via; chloride content, F.T-IR, UV-Vis 1H-NMR spectroscopy and C.H.N.S, as well as conductance and magnetic susceptibility.All data which collected from such methods specified complexes with 6 coordinates in solution and solid states. The biologicalactivity that is related to all the prepared compounds which were screened for their antimicrobial activitiesagainst (G+ and (G- )). The data that collected from biological activity indicate that complexes will have extra activity against such teste
... Show MoreNew Schiff-base ligands bearing tetrazole moiety and their polymeric metal complexes with Co(II), Ni(II) and Cd(II) ions are reported. Ligands were prepared in a multiple-step reaction. The reaction of sodium 2,6- diformylphenolate and cyclohexane-1,3-dione with 5-amino-2-fluorobenzonitrile resulted in the isolation of two precursors sodium 2,6-bis((E)-(3-cyano-4-fluorophenylimino)methyl)-4-methylphenolate 1 and 5,5'- (1E,1'E)-cyclohexane-1,3-diylidenebis- (azan-1-yl-1-ylidene)bis(2-fluorobenzonitrile) 2, respectively. The reaction of precursors with azide gave the required ligands; sodium 2,6-bis((E)-(4-fluoro-3-(1H-tetrazol-5- yl)phenylimino)methyl)-4-methylphenolate (NaL) and (N, N'E, N, N'E)-N, N'-(cyclohexane-1,3-diylidene)bis(4- fluor
... Show More