In this research investigation, a total of eighteen diverse tetra- and penta-lateral cyclic compounds were synthesized. These included 1,3,4-thiadiazole, thiazolidin-4-one (via an alternative method), 1,2,4-triazole, carbothioamide, thiazole-4-one, azetidin-2-one, and oxazole. The synthesis procedure entailed a sequence of reactions. The thiazolidine-4-one 1 was obtained by reaction p-aminobenzoic acid with thiosemicarbazide, followed by treatment with p-tolualdehyde to produce Schiff base 2. Reaction Schiff base 2 with mercaptoacetic acid in dry benzene was carried out to produce thiazolidine-4-one 3. In another synthesis pathway, the esterification of p-nitro benzoic acid with ethanol in the presence of sulfuric acid was obtained to formation of compound 4. Compound 4 was subsequently reacted with thiosemicarbazide, yielding compound 5. Cyclization of compound 5 was then achieved using 4% sodium hydroxide solution. This formed the 1,2,4-triazole heterocycle, designated compound 6. Thiosemicarbazone 7-9 were prepared by reaction of thiosemicarbazide with different aldehydes. Additionally, 2-substituted-1,3-thiazolidine-4-one derivatives 10-12 were synthesized through the reaction of thiosemicarbazone with chloroacetic acid in the presence of anhydrous sodium acetate. The Oxazole derivative 15 was obtained through a series of reactions starting with the reaction of p-amino benzoic acid with ethyl chloroacetate, resulting in compound 13. Compound 13 was then treated with urea to obtain compound 14, followed by a reaction with 4-phenyl phenacyl bromide to yield the final product, the Oxazole derivative 15. The 2-aminooxadiazole derivative 16 was synthesized by reaction urea with 4-bromoacetophenone which was reacted with 4-bromobenzaldehyde to produce Schiff base derivative 17. Finally, β-lactam 18 is obtained through reaction Schiff base with chloroacetyl chloride in the presence of triethyl amine. FT-IR, 1H-NMR, and 13C-NMR spectroscopy were used to confirm their proposed structures. Moreover, the antibacterial and antifungal activities of certain synthesized compounds, specifically 2,3,6,11,13,15,17, and 18, were assessed against Staphylococcus aureus, Escherichia coli, and Candida albicans, demonstrating encouraging outcomes.Keywords: Antibacterial, antifungal activity, oxadaizole, heterocyclic derivatives, Oxazole.
In this contribution new oxazepine compounds containing azo group were preppared. In the firststep,4-(dimethylamino)-3-((4-methoxy phenyl) diazenyl) benzaldehyde [Z] was synthesised by using 4-methoxyaniline. The second step was the condensation reaction between aldehyde group of the azo compound [Z] and
different primary aromatic amines [4-hydroxyaniline, 4-chloroaniline and 4-amino- N-(pyrimidin-2-yl) benzenesulfonamide] to yield new azo Schiff bases compounds [A1-A3] respectively. In the final step, oxazepine compounds [B1-B3] and [B4-B6] were prepared from reaction imines compounds [A1-A3] with maleic anhydride and phathalic anhydride in dry benzene respectively. All these derivatives were c
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 s
... Show MoreDensities ρ and viscosities η for several concentrations of amino acids (Serine, Cysteine and Threonine) at different temperatures (298.15, 303.15 and 308.15K) have been measured. On the basis of these data, the apparent molal volumes v , partial molal volumes at infinite dilution v , slope Sv , Gibbs free energy of activation for viscous flow of solution ∆G1,2 and Jones – Dole Bcoefficients were calculated the nature of solute-solvent and solute-solute interactions have been discussed in terms of the values of v , v , Sv and B-coefficents
The research includes the preparation of several complexes of the internal transition elements lanthanide (Ln = La, Nd, Er, Gd, and Dy) containing the 4f shell, with Schiff bases resulting from condensation reactions between 4-antipyrinecarboxaldehyde and 2-aminobenzothiazoles. Schiff's base was identified using FTIR spectra, UV-vis spectroscopy, elemental microanalysis CHNSO, nuclear magnetic resonance, mass spectrometry, and TGA thermal analysis. The complexes were studied and identified with elemental microanalysis CHNSO, FTIR spectroscopy, UV-vis spectroscopy, TGA thermal analysis, conductivity measurement, and magnetic sensitivity. The result showed that these complexes were classified as homogeneous bidentate complexes with th
... Show MoreThe molecular structures of acetophenonylidine-4-aminopyridine (I), 2, 6-dihydroxyacetophenonlidine-4-aminopyridine (II), 2, 4, 6- trihydroxyaceto phenonylidine-4-aminopyridine (III) and 2, 6-dihydroxyacetophenonylidine-2-aminopyridine (IV) have been investigated by IR and UV-visible spectrophotometry. The IR data indicate that the hydroxyl groups of these Schiff bases exist as tautomeric mixtures of free and bonded with the azomethine groups. The electronic spectra, effect of polar and nonpolar solvents, and the effect of acidity and basicity on the electronic spectra were studied and discussed. Their charge-transfer (CT) complexes with chloranil in chloroform solvent were also investigated; these complexes absorb light at 398-533 nm. T
... Show MoreThis study includes isolation, purification, and identification of algae from the canal around Baghdad university Al-jadriah. Four unialgal cultures were obtained. These algal cultures included 3 species of cyanophyta ( Nostoc carneum, Westillopesis prolifica, Chroococcus turgidus), 1 species of chlorophyta (Chlorella vulgaris) . Different plants belonging to different families were collected and extracted for their oils which were Ricinus communis and Sesamum indicum (seeds), Matricaria chamomilla (flowers) .However, antialgal activity of the extracted oils were evaluated the isolated algae with 7 concentrations (0.09, 0.3, 0.5, 1, 10, 20 , 30) % using the agar wells diffusion method. Results showed that R. communis oil was more effecti
... Show MoreIn the present study, nickel oxide nanoparticles (NiO NPs) were evaluated as an antibacterial and anticancer agent. The nanoparticles of nikel oxide were synthesized using aloe vera leaves extract and characterized with AFM (showing an average diameter of 45.11 nm), XRD and FE-SEM analyses. Three different concentrations (125, 250 and 500 µg/ml) were prepared from the synthesized NiO NPs and investigated for their potential antibacterial activity against both Enterococcus faecalis (Gram-positive bacteria) and Acinobacter baumannii (Gram-negative bacteria). While cytotoxicity and apoptotic activity were measured on both MCF-7 and AMJ13 cancer cell lines by MTT and caspase-9 luminescence assays. The results showe
... Show MoreThe purpose of this research work is to synthesize conjugates of some NSAIDs with sulfamethoxazole as possible mutual prodrugs to overcome the local gastric irritation of NSAID with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo group that undergo reduction only by colonic bacterial azo reductaze enzyme to liberate the parent compound to act locally (treatment of inflammation and infections in colon)
The purpose of this research work is to synthesize conjugates of some NSAIDs with sulfamethoxazole as possible mutual prodrugs to overcome the local gastric irritation of NSAID with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo group that undergo reduction only by colonic bacterial azo reductaze enzyme to liberate the parent compound to act locally (treatment of inflammation and infections in colon).
Key words: Mutual prodrug, Ester linkage, Azo bond, Colon targeting