Objective: Synthesis, Characterization of formazan derivatives and studies the antioxidant activity of prepared compounds and molecular docking. Methods: In this study, formazan compounds (III–XIV) were produced by combining Schiff base compounds (I), (II) with diazonium salts resulting from reactions of different aromatic amines with sodium nitrate in the presence of Con.HCl at 0–5°C. When isonicotinic acid hydrazide reacts with (N,N-dimethylbenzaldehyde, 4-hydroxy-3-methoxybenzaldehyde) in the presence glacial acetic acid as a solvent Schiff base compounds are created. Results: The prepared compounds were identified by FT-IR, 1H NMR, 13C NMR, then the antioxidant activity of the derivatives and molecular docking were studied. Discussion: Formazan derivatives showed antioxidant activity compound (XIV) has a high antioxidant according to the IC50 value. The low value of it means the strength of the compound as an antioxidant and vice versa. The molecular docking was studied by GOLD Suite, showed perfect position prediction performance and excellent results for virtual screening by examining the contact interactions between the active binding sites of the GABA-AT protein and the target molecules. Conclusions: The prepared derivatives showed good activity as antioxidants (III–XIV) when compared to ascorbic acid. The final compounds and reference drugs were ranked based on their PLP fitness. PLP fitness of the docked compounds on GABA-AT was found in the range of 57.71 to 95.91. GOLD software also gives the distance of hydrogen bonding between our ligands and a target protein as well as all bonds length was ≤3 Å.
Starting from 4, - Dimercaptobiphenyl, a variety of phenolic Schiff bases (methylolic, etheric, epoxy) derivatives have been synthesized. All proposed structure were supported by FTIR, 1H-NMR, 13C-NMR Elemental analysis all analysis were performed in center of consultation in Jordan Universty.
Objectives: Six different Schiff bases were synthesized from ampicillin and amoxicillin with isatin, 5-bromoisatin, and 5-nitroisatin. Methods: Ampicillin and Amoxicillin are linked directly through their α-amino groups to the acyl side chain with isatin and isatin derivatives by nucleophilic addition using glacial acetic acid as a catalyst. Results: chemical structures of these Schiff bases were confirmed using FTIR, 1H NMR and elemental microanalysis. The antibacterial activity was evaluated by measuring minimum inhibitory concentration (MIC) values and showed various degrees of antibacterial activities when compared with parent drugs. Compounds 1a and 2b, which are the Schiff bases of ampicillin and amoxicillin with isatin, showed very
... Show MoreThe researchers aimed to develop a novel azo ligand as a continuation of their prior investigations. They synthesized the ligand, identified as N-(3-acetyl-2- hydroxy-5-methyl-phenyl)N-(4-carboxy-cyclohexylmethyl)-diazonium salt, and proceeded to synthesize a series of chelate complexes with Ru+3, Rh+3, Pd+2, Pt+4, and Au+3 ions. Characterization of these compounds includes advanced techniques including elemental analysis, UV-Vis spectroscopy, FT-IR spectroscopy, LC-Mass spectrometry, NMR spectroscopy plus thermal analysis, conductivity measurements, magnetic quantification using TGA and DSC are used to further clarify the and synthesized complexes have been developed.Analysis revealed that the complexes formed with Ru+3, Rh+3, Pt+4, and Au
... Show MoreNew series of imidazole[1,2-a]pyridine-sulfonamides was designed and synthesized from 2-aminopyridine, which was reacted with p-bromo phenacyl bromide in the present of MgO to produce the corresponding imidazole[1,2-a]pyridine, which was then reacted with chlorosulfonic acid to produce 2-(4-bromophenyl)imidazole[1,2-a]pyridine-3-sulfonyl chloride [2]. Following that, treatment of (2) with different amines using the grand method to generate imidazole [1,2-a] pyridine sulfonamides. All the synthesized compounds have been characterized by FTIR, 1HNMR and 13CNMR and C.H.N analysis. The DFT, POM analysis and molecular docking were carried out on for all final compounds to investigate drug like attributes, and the results revealed showed that the
... Show MoreA series of coumarin derivatives linked to amino acid ester side chains were synthesized and evaluated of their antibacterial and antifungal activity. The coumarin derivatives was alkylated by the ethyl bromoacetate and then using potassium carbonate to get alkylated hymecromone. Conventional solution method for amide bond formation was used as a coupling method between the carboxy-protected amino acids with acetic acid side chain of coumarin derivatives. The DCC/ HOBt coupling reagents were used for peptide bond formation. The proposed analogues were successfully synthesized and their structural formulas were consistent with the proposed struct
... Show MoreIn this paper a new series of morpholine derivatives was prepared by reacting the morpholine with ethyl chloro acetate in the presence triethylamine as a catalyst in benzene gave morpholin-N-ethyl acetate(1) which reacted with hydrazine hydrate in ethanol, and gave morpholin-N-ethyl acetohydrazide (2) . Morpholin-N-aceto semithiocarbazide (3) were prepared by reacting compound(2) with ammonium thiocyanate , concentrated hydrochloric acid and ethanol as a solvent .Compound (3) reacted with sodium hydroxide and hydrochloric acid to give 5-(morpholin-N-methylene)-1H-1,2,4-triazole-3-thiol (4) .The new series of 1,2,4-triazol derivatives (5-8) was synthesized by reaction of compound(4) with formaldehyde , DMF as a solvent and different
... Show MoreThis work contain many steps starting from esterification of isophthalic acid to yield diester compound [I] which was converted to their acid hydrazide [II], then the later compound reacted with ethylacetoacetate to yield pyrazol-5-one compound [III]. Afterword added acetyl chloride to give the compound [IV], thereaction of this compound with theiosemicarbazide ledto produce a new carbothioamide compound [V], Which was reacted with ethyl chloro acetate to yield thethioxoimidazolidin compound [VI]. The condensation reaction of this compound with different substituted aldehyde give new alkene derivatives[VII]a-d. The synthesized compounds were characterized by melting points , FT-IR ,1H-NMR and Mass spectroscopy .
الوصف Mixed ligand complexes of Cu (II), Co (II) and Zn (II) with 2-((4-(1-(4-chlorophenylimino) ethyl) phenylimino) methyl) phenol (L) and histidine (His) have been prepared and diagnosed by ¹H and13 C NMR, FT-IR and electronic spectral data, thermal gravimetric, molar conductance and metal analysis measurements. The ligand (L) shows a bidentate nature and the coordination occurs through N and O atoms of imine group and phenol group respectively whereas (His) behave as tridentate ligand, coordinating through the-NH2 group and carboxylate oxygen group and N atoms of imidazole ring. The analytical studies for three complexes have shown octahedral structure. The anticancer activity was screened against human cancer cell such Follicular
... Show MoreA first step in this research was to synthesize Schiff's bases(1-3)using an Amoxcilline intensification reaction with different aromatic aldehydes in absolute ethanol. In benzene and refluxing conditions,Schiff's bases were cyclized with succinic and Phthalic anhydride to give a new sequence of 1,3-oxazepine derivatives(4-6) and (7-9),respectively.The last step,cyclization reactions with sodium azide in THF solvent resulted in the formation of [10 and 11], which are supposed to be biologically significant.FT.IR, 1H-NMR and 13C-NMR (for compound 4,7,9, and 11),as well as melting points reported, were used to characterize these prepared compounds ,Bacillus (G+), Staphylococcus (G+), and E.Coli (G-)were screened against these compounds. . To i
... Show MoreIn this research, Schiff bases derived from the reaction of anthrone with different heterocyclic amines have been described. The resulted Schiff base compounds were reacted with various nucleophiles in order to obtain new heterocyclic derivatives. Chemical structures of all products were confirmed by IR, 1H-, 13C-NMR spectral data and elemental analysis. All synthesized compounds were in vitro tested against a standard strain of pathogenic microorganism including Gram +ve bacteria (Staphylococcus aureus), Gram –ve bacteria (Escherichia coli), and fungi (Candida albicans).