Isatin (1H-indole-2, 3-dione) and its analogs are an important class of heterocyclic compounds. N-benzyl isatins and Schiff bases of isatin analogs have been reported to demonstrate a variety of biological activities. This work illustrates the synthesis of new N-benzylisatin Schiff bases and studies their biological activity. Firstly, Isatin and its analogs; 5-methoxyisatin, 5-fluoroisatin reacted with benzyl iodide to obtain N-benzylated derivatives of isatins 2 (ac). Secondly, these compounds were reacted with different amines (sulphanilamide and 4-methyl sulphonyl aniline) separately, to obtain Schiff bases compounds 3 (ac) and 4 (ac), respectively. The synthesized compounds were characterized by using FT-IR and 1HNMR spectroscopy. The synthesized Schiff bases 3 (ac) and 4 (ac) were examined for their in vitro antimicrobial activity using different Gram-positive bacteria, Gram-negative bacteria, and Candida albicans as fungi. The obtained results were compared with standard drugs: amoxicillin, ciprofloxacin, and fluconazole. All the compounds show no antifungal activity at any concentrations used, while most of them show moderate antibacterial activity at concentration 5mg/mL toward most bacteria except Klebsiella pneumonia.
Phosphorus‐based Schiff base were synthesized by treating bis{3‐[2‐(4‐amino‐1.5‐dimethyl‐2‐phenyl‐pyrazol‐3‐ylideneamino)ethyl]‐indol‐1‐ylmethyl}‐phosphinic acid with paraformaldehyde and characterized as a novel antioxidant. Its corresponding complexes [(VO)2L(SO4)2], [Ni2LCl4], [Co2LCl4], [Cu2LCl4], [Zn2LCl4], [Cd2LCl4], [Hg2LCl4], [Pd2LCl4], and [PtL
... Show MoreNew Schiff base and their Mn(II),Co(II),Ni(II), Cu(II) and Hg(II) complexes formed by the condensation of O-phathaldehyde and ethylene diamine (2:1) to give ligand (L1) in the first step ,then the ligand (L1) with 2- aminophenol (1:2) to give ligand (L2) were prepared by classic addition through microwave method . These compounds (Ligands and complexes) have been diagnosed electronic spectra, FT-IR,1H-&13C-NMR (only ligand), magnetic susceptibility, elemental microanalysis and molar conductance measurements. Analytical values displayed that all the complexes appeared (metal: ligand) (1:1) ratio with the six chelation. All the compounds appear a high activity versus four types of bacteria such as; (Escherichia coli), (Sta
... Show MorePhenoxathiin was prepared by the reaction of diphenyl ether with sulfur in the presence of anhydrous aluminum chloride. This work comprised the synthesis of new phenoxathiin derivatives containing heterocyclic moieties. These heterocyclic compounds were synthesized in three groups. The first group was made up of 2-(oxoalken-1-yl) phenoxathiin derivatives (3a-3j) obtained from the reaction of 2-acetylphenoxathiin with different aromatic aldehyde in the presence of sodium hydroxide. The other two groups involved compounds produced from the reaction of (3a-3j) with hydrazine hydrate in acetic acid to get 2-(1-acetyl pyrazolin-3-yl) phenoxathiin derivatives (4a-4j), and phenyl hydrazine in the presence of piperidine to afford 2-(1-phenyl pyrazo
... Show MoreRecently, some prostate cancer patients have acquired resistance to the second -generation drugs (anzalutamide and apalutamide) prescribed for the treatment of this disease due to the emergence of the F876L mutation, which represents a challenge to modern medicine. In this study, a new series of 2-thiohydantoin derivatives were prepared through the reaction of different derivatives of maleimide (1c-4c) with isothiocyanate derivatives. The prepared compounds were diagnosed using FT-IR,1H-NMR ,13C-NMR, Mass spectra. The prepared series compounds has been studied against prostate cancer cells. The MTT assay was used to determine the activity of the prepared compounds against prostate cancer cells. The da
... Show MoreA series of new 4-(((4-(5-(Aryl)-1,3,4-oxadiazol-2-yl)benzyl)oxy)methyl)-2,6-dimethoxy phenol (6a-i) were synthesized from cyclization of 4-(((4-hydroxy-3,5-dimethoxy benzyl)oxy)methyl)benzohydrazide with substituted carboxylic acid in the presences of phosphorusoxy chloride.The resulting compounds were characterized by IR, 1H-NMR, 13C-NMR, and HRMS data. 2,2-Diphenyl-1-picrylhydrazide (DPPH) and ferric reducing antioxidant power (FRAP) assays were used to screen their antioxidant properties. Compounds 6i and 6h exhibited significant antioxidant ability in both assay. Furthermore, type of substituent and their position of the aryl attached 1,3,4-oxadiazole ring at position five are play an important roles in enhancing or declining the antio
... Show MoreThe New Schiff base ligand 4,4'-[(1,1'-Biphenyl)-4,4'-diyl,bis-(azo)-bis-[2-Salicylidene thiosemicarbazide](HL)(BASTSC)and its complexes with Co(II), Ni(II), and Cu(II) were prepared and characterized by elemental analysis, electronic, FTIR, magnetic susceptibility measurements. The analytical and spectral data showed, the stiochiometry of the complexes to be 1:1 (metal: ligand). FTIR spectral data showed that the ligand behaves as dibasic hexadentate molecule with (N, S, O) donor sequence towards metal ions. The octahedral geometry for Co(II), Ni(II), and Cu(II) complexes and non electrolyte behavior was suggested according to the analysis data.
Unregulated epigenetic modifications, including histone acetylation/deacetylation mediated by histone acetyltransferases (HATs) and histone deacetylases (HDACs), contribute to cancer progression. HDACs, often overexpressed in cancer, downregulate tumor suppressor genes, making them crucial targets for treatment. This work aimed to develop non‐hydroxamate benzoic acid–based HDAC inhibitors (HDACi) with comparable effect to the currently four FDA‐approved HDACi, which are known for their poor solubility, poor distribution, and significant side effects. All compounds were structurally verified using FTIR, 1HNMR, 13CNMR, and mass spectrometry. In silico ana
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
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