A new Schiff base [I] was prepared by refluxing Amoxicillin trihydrate and 4-Hydroxy- 3,5-dimethoxybenzaldehyde in aqueous methanol solution using glacial acetic acid as a catalyst. The new 1,3-oxazepine derivative [II] was obtained by Diels- Alder reaction of Schiff base [I] with phthalic anhydride in dry benzene. The reaction of Schiff base [I] with thioglycolic acid in dry benzene led to the formation of thiazolidin-4-one derivative [III]. While the imidazolidin-4-one [IV] derivative was produced by reacting the mentioned Schiff base [I] with glycine and triethylamine in ethanol for 9 hrs. Tetrazole derivative [V] was synthesized by refluxing Schiff base [I] with sodium azide in dimethylformamid DMF. The structure of synthesized compounds[I-V] was characterized by their melting points, elemental analysis CHN-S and by their spectral data; FTIR and 1H NMR spectroscopy. Two cancer cell lines include: (RD) human pelvic rhabdomyosarcoma and (L20B) the mice intestines carcinoma cell line (which expresses the genes for human cellular receptor for Polio viruses) were used in this study. The cytotoxic effect of different concentrations of all the synthesized compounds for 48 hrs was examined. All compounds except [IV] and [V] showed less than 50% inhibition for (L20B), while these compounds exhibit inhibition more than 50% inhibition for (RD).
The compounds 3-[4̄-(4˭-methoxybenzoyloxy) benzylideneamino]-2-thioxo-imidazolidine-4-one(3)aand 4-(1-(5-oxo- 2-thioxoimidazolidin-1-ylimino)ethyl)phenyl acetate(3)b were prepared from the reaction of aromatic aldehyde or ketone(1)a,bwith thiosemicarbazide to give aryl thiosemicarbazones(2)a,b ,followed by cyclization with ethylchloroacetate in the presence of fused sodium acetate. Treatment the compounds(3)a,bwith 4- hydroxybenzenediazoniumchloride yielded the correspondings4-((4-((4-hydroxyphenyl)diazenyl)-5-oxo-2- thioxoimidazolidin-1-ylimino)methyl)phenyl 4-methoxybenzoate(4)aand4-(1-(4-((4-hydroxyphenyl)diazenyl)-5-oxo-2- thioxoimidazolidin-1-ylimino)ethyl)phenyl acetate(4)b.The new 2-thioxo-imidazolidin-4-one with esters (5-7)a,b sy
... Show MoreObjective: 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. D
... Show MoreA new 5‐fluorouracil–naproxen conjugate is synthesized as a mutual prodrug for targeting cancer tissues. The structure of the target compound and their intermediate are characterized by their melting point, IR, 1H NMR, 13C NMR, and elemental microanalysis. The cytotoxic activity is preliminarily evaluated using nonsmall lung cancer CRL‐2049, human breast cancer CAL‐51, and one type of normal cell line; rat embryo fibroblast cell line. The synthesized compound shows a good cytotoxic effect at the cancer cell and no significant effect at rat embryo fibroblast cell line.
Most drugs undergo some metabolism in the liver before excretion by the kidneys or bile. Thus, it is not surprising that liver injury may be provoked due to its exposure to various drugs and compounds. Drug-induced cholestatic liver injury may occur particularly under conditions of increased drug concentrations, genetic alterations in expression of enzymes or transporters. Additionally, the drug-induced cholestasis can be caused by direct toxic effects of drugs or their metabolites on different hepatic cell types or through an immune-mediated process. Amoxicillin/ clavulanic acid, an antibiotic that is therapeutically utilized for the treatment of a number of bacterial infections. Omega-3 fatty acids are unsaturated fatty acids that have ro
... Show MoreSome new 2,5-disubsituted-1,3,4-oxadiazole derivatives with azo group were synthesized by known reactions sequence . The structure of the synthesized compounds were confirmed by physical and spectral means .
Background: Leukemia is a cancer of blood cells which treated by different anticancer agents, Plants nowadays considered a new source for the development of new anticancer agent. Euphorbia Lathyris use in folklore to treat skin cancer. Objective Euphorbia lathyris seeds phytochemically investigated then examined its cytotoxic activity against leukemia cells. Materials and Methods: Euphorbia lathyris seed was extracted by maceration with different organic solvents (petroleum ether, chloroform and methanol), each organic extract submitted to phytochemical investigation and evaluated its cytotoxic activity on Leukemic blood with three different doses (50,100 and 150 µg mL¯1) and three different intervals. The data were evaluated by two-way a
... Show MoreKamil, S.H. 2024. Effects of Aqueous and Alcoholic Extracts of Lemongrass, Cymbopogon citratus on Some Biological Aspects of the Fig Moth, Ephestia cautella. Arab Journal of Plant Protection, 42(3): 377-381. https://doi.org/10.22268/AJPP-001245 This study evaluated the effects of aqueous and ethanolic extracts of lemongrass on the third instar larvae of the date moth Ephestia cautella Walker (Lepidoptera: Pyralidae). The results obtained showed that there were toxic effects of aqueous extract, which produced the highest mortality rate of 43.35% at 5% concentration72 hours after treatment, whereas the lowest mortality rate of 17% was obtained at 0.5% concentration, 72 hours after treatment. The LC50 was 0.082%. The results indicated
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