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.
Schiff bases are versatile compounds synthesized from the condensation of primary amino compounds with aldehydes or ketones. The high thermal of many Schiff base and their complexes were useful attributes for their application as catalysts in reactions involving at high temperatures. This thermal behavior of Schiff bases and their complexes was evaluated by TGA/DTG and DTA curves with 10 mass losses related to dehydration and decomposition. This review summarizes the developments in the last decade for thermal analysis of Schiff bases. Therefore, synthesis of Schiff bases and their complexes are reviewe
Reducing of ethyl 4-((2-hydroxy-3-methoxybenzylidene)amino)benzoate (1) afford ethyl 4-((2-hydroxy-3-methoxybenzyl)amino)benzoate (2). Reaction of this compound with Vilsmeier reagent affords novel 2-chloro-[1,3] benzoxazine ring (3). The corresponding acid hydrazide of compound 3 was synthesized from reaction of compound (3) with hydrazine hydrate. Newly series of hydrazones (5a–i) were synthesized from reaction of acid hydrazide with various aryl aldehydes. Antibacterial activity of the hydrazones was secerned utilizing gram-negative and gram-positive bacteria. Compound (5b) and (5c) exhibited significant antibacterial ability against both gram-negative and gram-positive bacteria, while the compounds (5a) showed mild antibacteri
... Show MoreReducing of ethyl 4-((2-hydroxy-3-methoxybenzylidene)amino)benzoate (1) afford ethyl 4-((2-hydroxy-3-methoxybenzyl) amino)benzoate (2). Reaction of this compound with Vilsmeier reagent affords novel 2-chloro-[1,3] benzoxazine ring (3). The corresponding acid hydrazide of compound 3 was synthesized from reaction of compound (3) with hydrazine hydrate. Newly series of hydrazones(5a–i) were synthesized from reaction of acid hydrazide with various aryl aldehydes. Antibacterial activity of the hydrazones wassecerned utilizing gram-negative and gram-positive bacteria. Compound (5b) and (5c) exhibited significant antibacterial ability against both gram-negative and gram-positive bacteria, while the compounds(5a) showed mild antibacterial activit
... Show More4-chloro and 4- nitro substituted phenol and aniline incorporated to a carboxylic group of naproxen a well-known non-steroidal anti-inflammatory drug (NSAID) to increase bulkiness were synthesized for evaluation as a potential anti-inflammatory agents with expected COX-2 selectivity. In vivo acute anti-inflammatory activity of these compounds (I-IV) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (2.5 mg/Kg) of naproxen. All tested compounds produced a significant reduction in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, compounds I and IV might show higher effect comparable to that of naproxen and to that of compounds II & III whic
... Show More4-aminobenzenesulfonamide conjugates of ibuprofen (compound 10) and indomethacin (compound 11) have been designed and synthesized by the reaction of sulfanilamide (compound 7) with 2-(4-isobutylphenyl) propanoic acid (ibuprofen) and 2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)acetic acid (indomethacin) for the evaluation as potential anti-inflammatory agents with expected selectivity against COX-2 enzyme. In vivo acute anti-inflammatory activity of the synthesized final compounds (10 and 11) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (10mg/Kg) of ibuprofen and (2mg/kg) of indomethacin. The tested compounds pr
... Show MoreIn this research we prepared shiff bases unilateral claw( benzyl imine aniline ) and Bilateral claw ( benzayal-2-imine phenol ) in high purity reach to 98% , which it's prepared from aromatic amine with aldehydes, it's solid,thermosetting, not dissolved in water in general. Diagnosed prepared article by using infra red spectroscopy (IR) which shows azomethen grop at 1640cm-1 At this diagnosis we suggest tetra headral mechanism in this Circumstances For a reaction.
Trimethoprim derivative Schiff bases are versatile ligands synthesized with carbonyl groups from the condensation of primary amines (amino acids). Because of their broad range of biological activity, these compounds are very important in the medical and pharmaceutical fields. Biological activities such as antibacterial, antifungal and antitumor activity are often seen. Transition metal complexes derived from biological activity Schiff base ligands have been commonly used.
Reaction of  p-fluoro benzoic acid with the thiosemicarbazide and salcialdehyde gave the new bidentate ligand .The prepared ligand Identified by FT-I.R and U.V-Visible spectcopic technique .Treatment of the prepared   ligand   with following metal ions  M=Tb(III),Eu(III),Nd(III) and La(III) ,in ethanol with a (1:1) M:L ratio and at pH=7 yielded series of neutral complexes as the general formula  [M LCl (H O ]. The prepared complexes were characterized using (FT-IR, UV-Vis) spectra , melting point, molar conductivity measurements . chloride ion content were also evolution by (mhor method) . The proposed structure of the complexes using program , chem office 3D(2004) .
A group of amino derivatives [4-aminobenzenesulfonamide,4-amino-N¹ methylbenzenesulfonamide, or N¹-(4-aminophenylsulfonyl)acetamide] bound to carboxyl group of mefenamic acid a well known nonsteroidal anti-inflammatory drugs (NSAIDs) were designed and synthesized for evaluation as a potential anti-inflammatory agent. In vivo acute anti-inflammatory activity of the final compounds (9, 10 and 11) was evaluated in rat using egg-white induced edema model of inflammation in a dose equivalent to (7.5mg/Kg) of mefenamic acid. All tested compounds produced a significant reduction in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the 4-amino-N-methylbenzenesulfonamide derivative (c
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