The purpose of this research is to prepare new vanillic acid derivatives with 1,2,4-triazole-3-thiol heterocyclic ring and evaluate their antimicrobial activity in a preliminary assessment. A multistep synthesis was established for the preparation of new vanillic acid-triazole conjugates. The intermediate of 4-(4-amino-5-mercapto-4H-1,2,4-triazol-3-yl)-2-methoxyphenol (4) reacts with different heterocyclic aldehydes (thiophene-2-carboxaldehyde, pyrrole-2-carboxaldehyde, thiophene-3-carboxaldehyde, and furfural ) in ethanol containing few drops of acetic acid yielded the corresponding 4-(4-(substituted amino)-5-mercapto-4H-1,2,4-1triazol-3-yl)-2-methoxy phenol derivatives (
The purpose of this research is to prepare new vanillic acid derivatives with 1,2,4-triazole-3-thiol heterocyclic ring and evaluate their antimicrobial activity in a preliminary assessment. A multistep synthesis was established for the preparation of new vanillic acid-triazole conjugates. The intermediate of 4-(4-amino-5-mercapto-4H-1,2,4-triazol-3-yl)-2-methoxyphenol (4) reacts with different heterocyclic aldehydes (thiophene-2-carboxaldehyde, pyrrole-2-carboxaldehyde, thiophene-3-carboxaldehyde, and furfural ) in ethanol containing few drops of acetic acid yielded the corresponding 4-(4-(substituted amino)-5-mercapto-4H-1,2,4-1triazol-3-yl)-2-methoxy phenol derivatives (5-8). These compounds were characterized spectroscopically by
... Show More1,3,4-oxadizole and pyrazole derivatives are very important scaffolds for medicinal chemistry. A literature survey revealed that they possess a wide spectrum of biological activities including anti-inflammatory and antitumor effects.
To describe the synthesis and evaluation of two classes of new niflumic acid (NF) derivatives, the 1,3,4-oxadizole derivatives (compounds 3 and (4A-E) and pyrazole derivatives (compounds 5 and 6), as EGFR tyrosine kinase inhibitors in silico and in vitro.
The designed compounds were synthesized using convent
To synthesize new hydrazone derivatives of naproxen with enhanced anti-inflammatory activity and devoid the ulcerogenic side effects. Hydrazones were synthesized by conjugation of naproxen hydrazide with seven natural and synthetic aldehyde and ketone by using glacial acetic acid as catalyst. The synthesis has been carried out following simple methodology in excellent isolated yields.The structure of the synthesized derivatives has been characterized by elemental microanalysis (CHN), FTIR Spectroscopy, and other physicochemical properties.The anti- inflammatory activity of the synthesized compounds was evaluated in vivo using the egg-white induced edema model in rats, and the results of the biological assay was found to be comparable to Nap
... Show MoreIn recent years , the interest in gold (III) species have gained more and more attention for cancer chemotherapy , this was stimulating by the possibility to develop new agents with mode of action and clinical profile different from the established platinum metalodrugs.
With this frame, recently new square planar Au(III) complexes (Au(L)(L')n); where L=SCH2COO- ; L'=HSCH2COO- had been synthesized with S/O – donor ligands.
In this article and by the aim to replace, one of (L') ligand by anion chloride ligand (which supposedly more relevant for the biodistribution of the compound than for its pharmacodynamic effects), new complex (Au(L')
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
... Show MoreAmaranthus viridis L. belongs to the Amaranthaceae family. It is a rich source of numerous phytochemicals and amino acids. The objective of this work was to optimize Ultrasound-Assisted Extraction (UAE) based on the extraction yield and Thin-Layer Chromatography (TLC) profile under different conditions, to compare the optimized UAE to the Soxhlet extraction method and evaluate the cytotoxic effects of the ethyl acetate fraction of the 80 % ethanolic extract on the SKGT-4 (human esophageal adenocarcinoma), AGS (human gastric adenocarcinoma) and A431 (human epidermoid carcinoma). A one-factor at a time experiment was carefully designed to assess the influence of the following factors on the extraction: time, frequency, solid-to-solven
... 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
All the prepared metal complexes of Pt (IV), Au(III), Rh (III), Co (II) and V(IV) with new ligand sodium [5-(p-nitro phenyl)-/4-phenyl-1,2,4-triazole-3-dithiocarbamato hydrazide] (TRZ.DTC) have been synthesized and characterized in solid state by using flame atomic absorption, elemental analysis C.H.N.S, FT-IR ,UV-Vis Spectroscopy, conductivity and magnetic susceptibility measurements. The nature of the complexes formed in ethanolic solution has been studied following the molar ratio method also was studied stability constant and found to be stable in molar ratio1:1 of VL (IV) and CoL(II) while Pt(IV), Au(III) and Rh(III) complexes stable in molar ratio 1:2 as well as the molar absorptivity for these complexes were calculated. From the prev
... Show More