The 3-aminoacetophenone and 4-aminoantipyrine were used as precursors to prepare new six ligands. The three new ligands (L1,L2 and L3) were synthesis by reacting one mole of 3-aminoacetophenone with one mole of (Acetyl chloride), (benzoyl chloride), (4-methoxybenzoyl chloride) and ammonium thiocyanat in acetone as a solvent, they are:- L1 (AAA) =[N-(3-acetylphenylcarbamothioyl)acetamide] L2 (BAA) =[N-(3-acetylphenylcarbamothioyl)benzamide] L3 (MAA) =[N-(3-acetylphenylcarbamothioyl)-4-methoxy benzamide] Also three new derivatives of 4-aminoantipyrine were synthesis by reacting one mole of 4-aminoantipyrine with one mole of (Acetyl chloride), (benzoyl chloride), (4-methoxybenzoyl chloride) and ammonium thiocyanat in acetone as solvent and the ligands are given: L4 (AAD) =[N-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-ylcarbamothioyl)acetamide] L5 (BAD) =[N-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-ylcarbamothioyl)benzamide] L6 (MAD) =[N-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-ylcarbamothioyl)-4-methoxybenzamide] These ligands were identified by FT-IR ,1H,13C-NMR,elemental analysis(C.H.N.S), electronic spectra, the molecular formula of there were concluded:- L1 (AAA) = C11H12O2N2S L2 (BAA) = C16H14O2N2S L3 (MAA) = C17H16O3N2S L4 (AAD) = C14H16N4O2S L5 (BAD) = C19H18O2N4S L6 (MAD) = C20H20O3N4S The ligands were reacted with some metal ions (M+2 =VO, Mn, Co, Ni, Cu, Zn, Cd , Hg and Pd), to give complexes with molecular formulas:- [M(AAA)2(H2O)2]Cl2 , [M(BAA)2(H2O)2]Cl2 , [M(MAA)2(H2O)2]Cl2, [M(AAD)2(H2O)2]Cl2 , [M(BAD)2(H2O)2]Cl2, [M(MAD)2(H2O)2]Cl2 Where (M+2 = Mn, Co, Ni, Cu, Zn, Cd , Hg and Pd) [VO(AAA)2]SO4 , [VO(BAA)2]SO4 , [VO(MAA)2]SO4, [VO(AAD)2]SO4 , [VO(BAD)2]SO4, [VO(MAD)2]SO4 The complexes were characterized by solubility, melting point and decomposition, FT-IR, electronic spectra, molar conductivity, magnetic susceptibility measurements, element microanalysis for some complexes and flame atomic absorption. From above results, one can conclude that complexes of (M+2 = Mn, Co, Ni, Cu, Zn, Cd, Hg and Pd) have an octahedral geometry while the square pyramid for complexes for(VO+2) The biological effects of ligands and some of their complexes have been investigated on two types of bacteria species Staphylococcus aureu a gram positive and Escherichia coli a gram negative In agricultural agar medium, the results exhibited all the compounds (expect Ni2+ with L1)have varsity anti bacterial activities
This study designed to prepare ultrafine apixaban (APX) o/w nanoemulsion (NE) based gel with droplet size below 50 nm as a good method for transdermal APX delivery without using permeation enhancer, alternatively, the formulation components itself act as permeation enhancer. APX, a potent oral anticoagulant drug that selectively and directly inhibit coagulation factor Xa, was selected as a good candidate for transdermal delivery as it displays poor water solubility (0.028 mg/mL) and low bioavailability (50%). APX-NE gel was prepared using triacetin, triton-x-100 and carbitol as oil phase, surfactant and cosurfactant respectively, while Carbopol 940 used as a gelling agent. Ex vivo permeation of APX-NE gel through human stratum c
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The study aimed to identify the degree of teaching competencies and job satisfaction of the teachers of physical education in the province of Baghdad, and then find the relationship between them. Use the descriptive approach in the style of associative relationships, the research community represented by teachers of physical education in the departments of education Karh (first, second, third) in the province of Baghdad. (522) teachers and (324) school principals distributed in (324) medium within the administrative configurations of these directorates for the academic year (2016 - 2017). The measure (teaching competencies) included (47) words distributed across seven areas. And the measure of (job satisfaction) included (15) words. After t
... Show MoreBacterial strains were isolated from oil-contaminated soil, in 2018, these isolates were identified, and with the aim of finding out the ability of these isolates to degrede the oil compounds, the color change of medium which added to it isolates was read by the method of Pacto Bushnell Hans. Then the change in the petroleum compounds was read by gas chromatography, for the most effective isolates.
The nine isolated bacterial showed different degrees of color change, and the isolates (Pseudomonas, Bacillus, Micrococcus) outperformed the color change amount (78, 78, 77) %, respectively, compared to the control, and the three isolates together showed the best color change of 90.7. % Compared to the control, and the
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Polycyclicacetal was prepared from the reaction of PEG with aldehyde derived from Erythro-ascorbic acid (pentulosono-ɣ-lactone-2,3-enedianisoate).All these compounds were characterized by Thin Layer Chromatography (TLC) and FTIR spectra and aldehyde was also characterized by (U.V-Vis), 1HNMR, 13CNMR, and mass spectra.The inhibitory effect of prepared polymer on the activity of human serum AcetylCholinesterase has been studied in vitro. The polymer showed a remarkable activity at low concentration (4.7x10-3 – 4.7x10-8M).
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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)
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
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Tetradentate complexes type [M (HL) 2] were prepared from the reaction of 2-hydroxy -1, 2-diphynel-ethanone oxime [H2L] and KOH with ( Mn II, Fe II, Co II, Ni II , Cu II and Hg II ), in methanol with (2:1) metal: ligand ratio. The general formula for Cu II and Mn II complexes are [M (HL) 2 Cl.H2O] K, for Co II [Co (HL) 2. H2O] and [M (HL) 2] for the rest of complexes. All compounds were characterised by spectroscopic methods, I.R, U.V-Vis, H.P.L.C, atomic absorption and conductivity measurements chloride content. From the data of these measurements, the proposed molecular structures for Fe II and Hg II complexes are tetrahedrals, while Mn II and Cu II complexes are octahedrals, Ni II complex adopting square planar structure and the complex
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