Background: Isoxazoles are an important class of five-membered unsaturated heterocyclic compounds. They show several applications in diverse areas such as pharmaceuticals, agrochemistry and industry. Isoxazoles are also found in natural sources showing insecticidal, plant growth regulation and pigment functions. Current study was conducted for synthesis of twenty five new Isoxazole derivatives and to evaluate the in vitro antibacterial activities of these derivatives. Methods: Benzaldoxime and their substituted [I] ae were prepared via addition-elimination reactions between aromatic aldehyde and hydroxylamine hydrochloride. In a second step, para-or meta-substituted benzaldoximes [I] ae were reacted with N-chlorosucceinimide in DMF to yield the para-or meta-substituted benzhydroxamic chlorides [II] ae. On the other hand D-fructose was converted to 2, 3: 4, 5-di-O-isopropylidene-D-fructopyranose [III] using dry acetone and sulfuric acid as a catalyst. Results and Conclusions: The reaction of compound [III] with propargyl bromide in DMF yielded the terminal alkyne [IV]. The esterification reaction of hydroxyl groups of compounds [VI] ae with different acid chloride in mixture THF and DMF using triethylamine as a catalyst give new compounds [VII] ae,[VIII] ae and [IX] ae. All synthesized compounds were identified by FTIR and most of them were characterized by 1H NMR, 13C NMR, and HRMS. Also the synthesized compounds showed variable antimicrobial activities in vitro against Escherichia coli, Bacillus substilis,
The purpose of this research was to prepare, characterize, and evaluate the new antimicrobial peptide KSL peptide encapsulated in poly(D,L-lactide-co-glycolide) (PLGA)composite microspheres. KSL was loaded in poly(acryloyl hydroxyethyl) starch (acHES) micropar-ticles, and then the peptide-containing microparticles were encapsulated in the PLGA matrix by a solvent extraction /evaporation method.
KSL-loaded PLGA microspheres were also prepared without the starch hydrogel microparticle microspheres for comparison study. KSL peptide microspheres were characterized for drug content, surface morphology, microspheres size determination, polymers stability , in vitro microspheres degradation and in vitro release. KSL peptide
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This contribution provides an atomistic understanding into the impact of W, Nb, and Mo co-substitution at Hf-site of cubic HfO2 lattice to produce Hf1−xTMxO2 system at x = 25%. The calculations have been performed under the framework of density functional theory supported by Habbured parameter (DFT+U). Structural analysis demonstrates that the recorded lattice constants is in good coherence with the previously published results. For the lattice parameters, contraction by 1.33% comparing with the host system has been reported. Furthermore, the doping effect of TM on the band gap leads to its reduction in the resulting Hf0.75TM0.25O2 configurations. The partial density of states (PDOS) indicate that hybridization through localized electroni
... Show MoreThis contribution provides an atomistic understanding into the impact of W, Nb, and Mo co-substitution at Hf-site of cubic HfO2 lattice to produce Hf1−xTMxO2 system at x = 25%. The calculations have been performed under the framework of density functional theory supported by Habbured parameter (DFT+U). Structural analysis demonstrates that the recorded lattice constants is in good coherence with the previously published results. For the lattice parameters, contraction by 1.33% comparing with the host system has been reported. Furthermore, the doping effect of TM on the band gap leads to its reduction in the resulting Hf0.75TM0.25O2 configurations. The partial density of states (PDOS) indicate that hybridization through localized electroni
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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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Implementations of Transition Metal complexes of shiff Base Derived Ampyrone
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Alizarin is one of the popularly used and wide separated compounds with a chemical name (1,2- dihydroxy-9,10-anthraquinone) which belong to the anthraquinones family that contain three aromatic conjugated rings and in the central rings it contains two ketonic groups.1
Previously, many empirical models have been used to predict corrosion rates under different CO2 corrosion parameters conditions. Most of these models did not predict the corrosion rate exactly, besides it determined effects of variables by holding some variables constant and changing the values of other variables to obtain the regression model. As a result the experiments will be large and cost too much. In this paper response surface methodology (RSM) was proposed to optimize the experiments and reduce the experimental running. The experiments studied effects of temperature (40 – 60 °C), pH (3-5), acetic acid (HAc) concentration (1000-3000 ppm) and rotation speed (1000-1500 rpm) on CO2 corrosion performance of t
... Show MoreIn this work, two graphene oxide (GO) samples were prepared using the Hummers method with graphite (g) and KMnO4 (g) ratios of 1:3 (GO3) and 1:6 (GO6). The effect of oxidation degree on the structural, electrical, and dielectric properties of the GO samples was investigated. The structures of the GO samples were studied using various techniques, including X-ray diffraction (XRD), Fourier transform infrared (FT-IR) spectroscopy, scanning electron microscopy (SEM), and energy-dispersive X-ray spectroscopy (EDXS). XRD analysis revealed an increase in the interlayer spacing and a decrease in the number of layers of the samples with increasing oxidant content. The two GO samples have giant permittivity values of ~105 in the low-frequency
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