The compound 3-[4Ì„-(4Ë-methoxy benzoyloxy) benzylideneamino]-2-thioxo-imidazolidine-4-one [III] was prepared from the cyclization of thiosemicarbazone [II] with
ethyl α -chloroacetate in the presence of fused sodium acetate. Treatment the later compound
with acetic anhydride yielded the corresponding 1-Acetyl-3-[ 4Ì„- (4Ë- methoxy benzoyloxy)
benzylideneamino] – 2 – thioxo -imidazolidine-4-one [IV]. 1,3-Oxazepine derivatives [V]a-d
and [VI]a-d are obtained from the reaction of compounds[III] and [IV] with different acid
anhydrides, in dry benzene. The FTIR and
1
HNMR spectroscopy are indicated a good
evidence for the formation of the synthesized compounds. Some of the synthesized
compounds have been screened against E.coli , Staph. aureus , Psenudomonsaeruginosa and
Bascillus cereus . They exhibited moderate to weak antibacterial activity unless compound
[V]d did not show any biological activity
Secnidazole was linked with ciprofloxacin as mutual prodrugs to get antibiotics with broader spectrum of activity, improved physicochemical properties and given by single dose to improve patient’s compliance. Furthermore, they provide structural modifications to overcome bacterial adaptation. The structures of the synthesized compounds were confirmed using FT-IR, mass spectrometry, elemental microanalysis (CHNO) and some physiochemical properties. This modification was led to an increase in Log P values for Mutual I (Log P 1.114) and Mutual II (Log P 1.97) compared with its values for Secnidazole (Log P -0.373) and ciprofloxacin (Log P -0.832). The solubility of prodrugs had been determined in different media, Mutual II showed 1
... Show MoreIn :the _pr sent _paper we report ths. ynthesis ·of a new li:ga!!d..
[f4LJ [{'2 {1-'[(2-hyd•:0xy-.ben:zy1i.den·e)..,bxcJrazanci}:etby-l }benzerieÂ
J,5 t;rtiol .aad its complexes ·w-ith '('Mlif(1 J Fev 1 ), ed(J'l), and. :f.::I:g 01>-)
The ligand \VS preP..ated rin tWo steps' • fp I t}Je nrst stea -soJutiQil Qf
-saUcyla[deeyeq. ip methatt:oJ . re3ctcd lU1der reflux
... Show MoreIntroduction: Biocides are commonly used for disinfection in a variety of contexts. They are generally used to avoid infection by controlling biofilm on medical equipment. However, the literature lacks information on the effect of biocide on efflux pump gene expression. Objective: To determine the influence of biocide on biofilm development and efflux pump acrA and ramA gene expression. Methodology: The microtiter plate method was used to identify biofilm development in 80 isolates of K. pneumoniae. The minimal inhibitory concentrations (MIC) of three biocides (quaternary ammonium compound (QAC), chlorohexidine digluconate, and chloroxylenol) were estimated. The effect of QAC on the intensity and viability of biofilms was investigated as we
... Show MoreObjective: The aim of this study was to develop a bioadhesive gel of gatifloxacin for the treatment of periodontal diseases.Methods: Periodontal gels of gatifloxacin were prepared using different hydrophilic polymers such as carbopol 940 (CP 940), carboxymethyl cellulose (CMC) and hydroxypropylmethyl cellulose (HPMC) in varied concentrations, either alone or as a combination. The prepared gels were evaluated for their physical appearance, pH, drug content, viscosity, bioadhesiveness and in vitro drug release profile. The influence of the type and the concentration of polymer on the drug release as well as on viscosity and mucoadhesiveness of prepared gels were investigated.Results: The prepared gels showed acceptable physical proper
... Show MoreIn this research, the preparation of a chemically activated carbon from date stones by using electric and microwave assisted K2CO3 activation was studied. The effect of radiation power, radiation time, and impregnation ratio on the yield and Iodine number on the activated carbons was investigated. The activated carbon characterizations were examined by its surface area, pore structure analysis, bulk density, moisture content, ash content, iodine number, FTIR, and scanning electron microscopy (SEM). The adsorption capacity was also studied by adsorption of fluoroquinolones antibiotics, CIP, NOR, and LEVO, by the prepared activated carbon.
... Show MoreEndoglucanase produced from Aspergillus flavus was purified by several steps including precipitation with 25 % ammonium sulphate followed by Ion –exchange chromatography, the obtained specific activity was 377.35 U/ mg protein, with a yield of 51.32 % .This step was followed by gel filtration chromatography (Sepharose -6B), when a value of specific activity was 400 U/ mg protein, with a yield of 48 %. Certain properties of this purified enzyme were investigated, the optimum pH of activity was 7 and the pH of its stability was 4.5, while the temperature stability was 40 °C for 60 min. The enzyme retained 100% of its original activity after incubation at 40 °C for 60 min; the optimum temperature for enzyme activity was 40 °C.
Abstract
The present investigation aimed to formulate a liquid self-microemulsifying drug delivery system (SMEDDS) of tacrolimus to enhance its oral bioavailability by improving its dispersibility and dissolution rate. Four liquid SMEDDS were prepared using maisine CC as oil phase, labrasol ALF as surfactant and transcutol HP as co-surfactant based on the solubility studies of tacrolimus in these components. The phase behavior of the components and the area of microemulsion were evaluated using pseudoternary phase diagrams. The formulations were also assessed for thermodynamic stability, robustness to dilution, self-emulsification time, drug content, globule size and polydispersity index. The prepared SMEDDS formulations exhibi
... Show MoreThis study aims to formulate azithromycin oleogel to locally treat skin infections such as acne vulgaris and skin wound infection. Providing a form of azithromycin that can be administered topically is highly desired to prevent unwanted systemic complications including diarrhea, nausea, and abdominal pain. Additionally, it will avoid first pass metabolism, improves patient acceptance, provides an alternative in nauseated patients, decreases the dose by direct contact with the pathological site, and provides a noninvasive and convenient mode of administration. Furthermore, for treating wound infections, the gel will act as a scaffold biomaterial for wound closure besides its antibacterial effect. Herein, we propose the use of grapeseed oil-b
... Show MoreOil from Brassca campestris (local variety) was extracted with hexane using Soxhlet. The extracted oil was characterized and its antimicrobial activity was determined as well. The content of extracted oil was 40% with 0.5% of volatile oil .Oil was immiscible with polar solvent such as ethanol, acetone and water, while it was easily miscible with chloroform due to its hydrophobicity. The result of organoleptic tests revealed that the oil is clear yellow in color and odorless with acceptable taste. The oil was stable at 4 -25 C? for a month. Refractive index (RI) of oil was 1.4723 with density of 0.914, [both at 4-25 C?]. Boiling point 386 C?. Infra red spectroscopy (IR) indicated the presence of different chemical groups (C=C
... Show MoreIn context of this paper we prepare high purity powder ZnO nanostructures by chemical method at low temperature solution and study the effect off annealing at high temperature, ZnO nanoparticles have been successfully synthesized by chemical method at 0Cᵒ solution. In this method, suddenly reaction is occurred between zinc acetate solution and sodium hydroxide solution at 0Cᵒ, annealing temperature of powder product surfactant plays an important role in morphological changes. The nanostructures have been characterized by X-ray diffraction (XRD), Scanning Electron Microscope (SEM), differential scanning calorimetry(DSC) and UV-visible .analysis Effect of annealing temperatures on the morphology , structure and optical properties is di
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