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Cephalothin as a Carrier of 6-Mercaptopurine for Targeting Cancer Tissues
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A lower extracellular pH is one of the few well-documented physiological differences between tumour and normal tissues. On the other hand, elevated glutathione (GSH) level has been detected in many tumours compared with healthy surrounding tissues. The compound II: 3-(9H-purin-6-yl-thio) carbonothionyl methyl-8-oxo-7-(2-thiophen-2-yl) acetamido-5-thia-1-azabicyclo-4-octo-ene-carboxylic acid was a cephalothin derivative contain 6-mercaptopurine (6-MP). Compound II react with general base catalysis in slightly acidic pH or with sulfhydryl nucleophiles to release the chemotherapeutic drug 6-MP. The generation of compound II was accomplished following multistep reaction procedures. The structure of compound II and its intermediate was confirmed by their melting point, infrared spectroscopy, CHN and NMR analysis. The hydrolysis of compound II in aqueous buffer solution of pH 6 and in the presence of GSH at pH 7.4 was studied. The partition coefficient (PC) of compound II was also determined. Compound II has acceptable rate of hydrolysis at slightly acidic medium pH 6 (t1/2 = 56.34 min.) and 80% of compound II had been converted to 6-MP within 30 min in the presence of GSH. And the compound has acceptable stability at pH 7.4(t0.5=639.65 min.) and the rate of hydrolysis was effected by change the buffer concentration.  This compound can selectively deliver 6-MP into the tumour tissues which have acidic pH or elevated GSH level. Compound II had an improved PC value of 12.23 compared to 1.22 for free drug 6-MP confirming higher lipophilicity.

Key words: 6-mercaptopurine, cancer, prodrug, targeting

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Publication Date
Wed Jan 01 2020
Journal Name
Colloids And Surfaces A: Physicochemical And Engineering Aspects
Studies on membrane stability and extraction of ciprofloxacin from aqueous solution using pickering emulsion liquid membrane stabilized by magnetic nano-Fe2O3
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Publication Date
Mon Jul 01 2024
Journal Name
Ecological Engineering & Environmental Technology
Elimination of Methyl Orange Dye with Three Dimensional Electro-Fenton and Sono-Electro-Fenton Systems Utilizing Copper Foam and Activated Carbon
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This study deals with the elimination of methyl orange (MO) from an aqueous solution by utilizing the 3D electroFenton process in a batch reactor with an anode of porous graphite and a cathode of copper foam in the presence of granular activated carbon (GAC) as a third pole, besides, employing response surface methodology (RSM) in combination with Box-Behnk Design (BBD) for studying the effects of operational conditions, such as current density (3–8 mA/cm2), electrolysis time (10–20 min), and the amount of GAC (1–3 g) on the removal efficiency beside to their interaction. The model was veiled since the value of R2 was high (>0.98) and the current density had the greatest influence on the response. The best removal efficiency (MO Re%)

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Publication Date
Sun Sep 06 2015
Journal Name
Baghdad Science Journal
Measurement of radon gas concentration in water and soil samples in AL-Najaf governorate by using nuclear track detector (CR-39)
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The radon gas concentration in environmental samples soil and water of selected regions in Al-Najaf governorate was measured by using alpha-emitters registrations which are emitted form radon gas in (CR-39) nuclear track detector. The first part is concerned with the determination of radon gas concentration in soil samples, results of measurements indicate that the highest average radon concentration in soil samples was found in (Al-Moalmen) region which was (100.0±7.0 Bq/m3), while the lowest average radon concentration was found in (Al-Askary) region which was (38.5±4.7 Bq/m3), with an average value of (64.23±14.9 Bq/m3) ,the results show that the radon gas concentrations in soil is below the allowed limit from (ICRP) agency which is (

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Publication Date
Mon Mar 29 2021
Journal Name
Journal Of Engineering
Extracting Four Solar Model Electrical Parameters of Mono-Crystalline Silicon (mc-Si) and Thin Film (CIGS) Solar Modules using Different Methods
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Experimental measurements were done for characterizing current-voltage and power-voltage of two types of photovoltaic (PV) solar modules; monocrystalline silicon (mc-Si) and copper indium gallium di-selenide (CIGS). The conversion efficiency depends on many factors, such as irradiation and temperature. The assembling measures as a rule cause contrast in electrical boundaries, even in cells of a similar kind. Additionally, if the misfortunes because of cell associations in a module are considered, it is hard to track down two indistinguishable photovoltaic modules. This way, just the I-V, and P-V bends' trial estimation permit knowing the electrical boundaries of a photovoltaic gadget with accuracy. This measure

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Publication Date
Mon Nov 01 2021
Journal Name
Iop Conference Series: Earth And Environmental Science
Treatability influence of municipal sewage effluent on surface water quality assessment based on Nemerow pollution index using an artificial neural network
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Abstract<p>Assessing water quality provides a scientific foundation for the development and management of water resources. The objective of the research is to evaluate the impact treated effluent from North Rustumiyia wastewater treatment plant (WWTP) on the quality of Diyala river. The model of the artificial neural network (ANN) and factor analysis (FA) based on Nemerow pollution index (NPI). To define important water quality parameters for North Al-Rustumiyia for the line(F2), the Nemerow Pollution Index was introduced. The most important parameters of assessment of water variation quality of wastewater were the parameter used in the model: biochemical oxygen demand (BOD), chemical oxygen dem</p> ... Show More
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Publication Date
Sun Sep 03 2017
Journal Name
Baghdad Science Journal
Polymorphism study of MTHFR 677C?T and its correlation with oxidative stress and their influence on female infertility in Erbil – Iraq
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This research includes a study of Methylenetetrahydrofolate reductase gene’s allele 677C?T and its correlation with oxidative stress and their impact on female infertility. Fifty infertile women with the range age (23-42) years and twenty five fertile women with the range age (22-39) years as control group living in Erbil city were selected. The serum level of Malondialdehyde (MDA), superoxide dismutase (SOD), prolactin hormone (PRL), Luteinizing hormone (LH), Thyroid stimulating hormone (TSH), Triiodothyronine hormone (T3), and Thyroxine hormone (T4) were measured, also a body mass index (BMI) was calculated. A restriction enzyme (Hinf1) was used to improve the mutation in DNA bands of infertile women. The results showed significant inc

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Publication Date
Thu Nov 08 2018
Journal Name
Chemistry – A European Journal
Magnetic Shielding, Aromaticity, Antiaromaticity and Bonding in the Low‐Lying Electronic States of S <sub>2</sub> N <sub>2</sub>
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Aromaticity, antiaromaticity and chemical bonding in the ground (S0), first singlet excited (S1) and lowest triplet (T1) electronic states of disulfur dinitride, S2N2, were investigated by analysing the isotropic magnetic shielding, σiso(r), in the space surrounding the molecule for each electronic state. The σiso(r) values were calculated by state-optimized CASSCF/cc-pVTZ wave functions with 22 electrons in 16 orbitals constructed from gauge-including atomic orbitals (GIAOs). The S1 and T1 electronic states were confirmed as 11Au and 13B3u, respectively, through linear response CC3/aug-cc-pVTZ calculations of the vertical excitation energies for eight singlet (S1–S8) and eight triplet (T1–T8) electronic states. The aromaticities of S

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Publication Date
Mon Sep 30 2024
Journal Name
Open Veterinary Journal
Crude aqueous Proteus mirabilis extract with quorum sensing inhibitory activity can increase the susceptibility of multidrug resistant Pseudomonas aeruginosa to antimicrobials
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Background: Suppression of quorum sensing (QS) that regulates many virulence factors, including antimicrobial resistance, in bacteria may subject the pathogenic microbes to the harmful consequences of the antibiotics, increasing their susceptibility to such drugs. Aim: The current study aimed to make an aqueous crude extract from the soil Proteus mirabilis isolate with the use of the gas chromatography-mass spectrometry (GC-MS) technique for its analysis, and then, study the impact of the extract on clinical isolates of Pseudomonas aeruginosa. Methods: Preparation of crude extracts from P. mirabilis (both organic and aqueous), which were then analyzed by GC-MS to detect the bioactive ingredients. Furthermore, the extract’s capability to i

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Publication Date
Tue Oct 25 2022
Journal Name
Aip Conference Proceedings
The structural properties of mawsoniteCu6Fe2 S8Sn[CFTS] thin films effected by violet laser irradiation deposited via semi-computerized spray pyrolysis technique
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Publication Date
Tue Feb 01 2022
Journal Name
Baghdad Science Journal
Evaluation of Amygdalin (B17) and Cucurbita pepo (Pumpkin seed) Activity Against Blastocystis from Diarrheic Patients in Baghdad, Iraq: in Vitro Study
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Blastocystis is a ubiquitous human and animal protozoa that inhabit the gastrointestinal tract. Metronidazole is considered the standard drug for the treatment of Blastocystis infection; however, there is growing evidence of treatment failure, hazardous side effects, and appearance of strains resistant to metronidazole. In the last era, many studies have been implicated in the quest for new treatments for Blastocystis infection, especially natural products. Attention has been focused on the effect of Amygdalin (B17) and pumpkin seed on eradicating parasitic infections. The current work was built up to explore the in vitro efficacy of two natural compounds, Amygdalin (B17) and pumpkin seeds against

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