In the current work, aromatic amines and alkyl halides have been converted to the corresponding azides 2a‒d and 4a-d by the reaction with sodium nitrite and sodium azide respectively for amines and sodium azide for halides. Then, dipropargyl ether derivative of D-mannose 8 has been synthesized from diacetone mannose that has been obtained by the treatment of D-mannose (5) with dry acetone in the presence of sulfuric acid. Then, aldol condensation has been used to prepare diol 7 from the mannose diacetonide 6. The reaction of compound 7 with propargyl bromide in alkaline media has been afforded dipropargyl derivative 8. In a parallel step, both dialkyne with aromatic and aliphatic azide have been coupled to produce 1,2,3-triazole derivatives 9a‒d in the presence of Cu(I) salts. All synthesized compounds have been characterized by 1D and 2D NMR spectra alongside with HRMS data. The antibacterial activity against both gram-positive and gram-negative has been tested. Moreover, the anticancer activity has also been evaluated against AMJ13 cell line.
Antibiotic resistance increment is a major problem for the human society nowadays which encourages the efforts to look for new therapeutic alternatives from natural defenses. Synergistic antibacterial activity of epidermin and staphylolysin LasA A against Staphylococcus aureus (Staph aureus), Escherichia coli (E. coli) and Pseudomonas aeruginosa (Ps. aeruginosa) was evaluated. The antibacterial activities of epidermin from Staphylococcus epidermidis (Staph epidermidis) and Staphylolysin (LasA) from Ps. aeruginosa using the agar well diffusion assay were evaluated, and then using the micro dilution method to evaluate the minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC). The checkerboard method and fract
... Show More A series of N- benzoyl - 2 – alkyl -1- ( 2- thio – 1,3,4- thiadiazole -5- yl ) , have been synthesized from DL- α– amino acids , The methyl and sulfon thio ethers of these compounds were also prepared , representative samples of the prepared compounds were characterized from their IR- spectrum and elemental analysis .
This study was conducted to investigate the antibacterial activity of green synthesized copper oxide nanoparticles (CuO NPs) using Aloe vera. Initially, bacteria were collected from clinical samples of patients having otitis media infection and the isolates were identified at the species level following biochemical tests. Copper oxide nanoparticles were prepared by green synthesis using Aloe vera leaves and characterized using UV- visible spectroscopy at 260 nm peak. The shape and size were determined by using transmission electron microscopy (TEM) and the dimensions of the particles were more precisely determined by using scanning electron microscopy (SEM) and x-ray diffraction (XRD). Different concentrations of nanopa
... Show MoreA new series of Sulfamethoxazole derivatives was prepared and examined for antifibrinolytic and antimicrobial activities. Sulfamethoxazole derivatives bear heterocyclic moieties such as 1,3,4-thiadiazine {3}, pyrazolidine-3,5-diol {4} 6-hydroxy-1,3,4-thiadiazinane-2-thione {5} and [(3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-4-yl)diazenyl] {8}. Their structures were elucidated by spectral methods (FT-IR, H1-NMR). Physical properties are also determined for all compound derivatives. Recently prepared compounds were tested for their antimicrobial activity in the laboratory. Each screened compound showed good tendency to moderate antimicrobial activity.
Phenoxathiin 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 MoreSeveral new derivatives of 1, 2, 4-triazoles linked to phthalimide moiety were synthesized through following multisteps. The first step involved preparation of 2, 2-diphthalimidyl ethanoic acid [2] via reaction of two moles of phthalimide with dichloroacetic acid. Treatment of the resulted imide with ethanol in the second step afforded 2, 2-diphthalimidyl ester [3] which inturn was introduced in reaction with hydrazine hydrate in the third step, producing the corresponding hydrazide derivative [4]. The synthesized hydazide was introduced in different synthetic paths including treatment with carbon disulfide in alkaline solution then with hydrazine hydrate to afford the new 1, 2, 4-triazole [10]. Reaction of compound [10] with different alde
... Show MoreSeveral new derivatives of 1, 2, 4-triazoles linked to phthalimide moiety were synthesized through following multisteps. The first step involved preparation of 2, 2-diphthalimidyl ethanoic acid [2] via reaction of two moles of phthalimide with dichloroacetic acid. Treatment of the resulted imide with ethanol in the second step afforded 2,2-diphthalimidyl ester[3] which inturn was introduced in reaction with hydrazine hydrate in the third step ,producing the corresponding hydrazide derivative[4] .The synthesized hydazide was introduced in different synthetic paths including treatment with carbon disulfide in alkaline solution then with hydrazine hydrate to afford the new 1,2,4-triazole[10] .Reaction of com
... Show MoreThis study was designed to show the inhibitory effect of different concentrations of alcoholic extract of Borage officinalis on the Monoamine oxidase (MAO) and Acetylcholinesterase (AChE) enzymes in human serum. The results obtained from the study exhibited that alcoholic extract of Borage officinalis caused inhibition to enzymes activity with all concentrations of the extract. The results also showed that when the concentration of the extract was (0.001 mg/ml), the percentage of inhibition was (4.3% with MAO and 15.2% with AChE) and this percentage increases until reaching up to (74.7% with MAO and 84.18% with AChE) when the concentration of the extract was (0.1 mg/ml). From the kinetic parameters, studies found that alcoholic extract o
... Show MoreLevofloxacin belongs to the fluoroquinolone family; it is a potent broad-spectrum bactericidal agent. The pharmacophore required for significant antibacterial activity is the C-3 carboxylic acid group and the 4-pyridine ring with the C-4 carbonyl group, into which binding to the DNA bases occur. In this work, we tried to show that by masking the carboxyl group through amide formation using certain amines to form levofloxacin carboxamides, an interesting activity is kept. Levofloxacin carboxamides on the C-3 group were prepared, followed by the formation of their copper complexes. The target compounds were characterized by FT-IR, elemental analysis. The antimicrobial activity of the target compounds was evaluated and showed satisfactory resu
... Show MoreThe present work involved synthesis of new thiozolidinone derivatives,These derivatives could be divided into three type of compounds; quinolin-2-one[V]a,b ,Schiff bases[VI]a,b and imide compounds[VII]a-d. The reaction p-Hydroxyacetophenone with thiosemicarbazide led to formation thiosemicarbazon compound [II], the reacted of thiosemicarbazone with chloro acetic acid in CH3CO2Na led to yield 4- thiazelidinone compound[III] in addition, thiosemicarbazide was POCl3 to [III] give [IV] compound used intermediates to synthesis new compounds of reacted with two type of coumarin in glacial acetic acid to give quinolin-2-one[V]a,b, The later compound refluxing with different benzaldehyde in dry benzene and glacial acetic acid give Schiff bases[VI]a
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