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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 08 2025
Journal Name
Egyptian Journal Of Veterinary Sciences
Histological and Histochemical Study of the Esophagus Before and After Crop in the Guinea Fowl (Numida meleagris)
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Publication Date
Mon Apr 29 2024
Journal Name
Journal Of The College Of Basic Education
Detection Of Biofilm Formation By Beta- Lactam Resistance Klebsiella Pneumoniae Isolated From Clinical Specimens And Aquatic Samples
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Publication Date
Sun Dec 01 2013
Journal Name
Journal Of International Academic Research For Multidisciplinary
SYNTHESIS AND LIQUID CRYSTALLINE BEHAVIOUR OF NEW SERIES CONTAINING 1, 3-OXAZEPINE AND 1, 3-THIAZOLE RINGS
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The synthesis and properties of two new series of compounds having 1,3-Oxazepineand 1,3-thiazole rings connected through azo linkage are reported. These compounds weresynthesized by the reaction of phthalic anhydride with Schiff bases. The molecular structuresof these compounds were verified by elemental analysis, FTIR and 1HNMR spectroscopy.The mesomorphic behaviors of these compounds were studied by optical polarizedmicroscopy (OPM) and differential scanning calorimetry (DSC). All compounds of the twoseries show liquid crystalline properties. The influence of the central oxazepine and thiazolerings and the terminal substituents on the type and temperature range of the mesomorphousproperties of these compounds has been elucidated

Publication Date
Thu Jan 21 2021
Journal Name
Iop Conf. Series: Materials Science And Engineering
Synthesis, spectroscopic study, biological activity and dyeing application of curcumin - Schiff base with various metal ions complexes
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A tetradentate (N2O2) Schiff base (H2Ldfm) was successfully synthesized via condensation of curcumin / diferuloylmethane (dfm) and L-leucine amino acid (HL). There were three different methods that used for synthesizing H2Ldfm; (refluxing, grading, and fusion). Ten different metal complexes were also successfully synthesized by combination of the Schiff base (H2Ldfm) and 1,10-phenanthroline (phen) ligand to form a hexadentate (N4O2) mixed ligands (Ldfm , phen) with ten different metal salts (M) where{ M= Al(III), Mn(II), Fe(III), Co(II), Ni(II), Cu(II), Ag(I), Cd(II), Hg(II), and Pb(II)}. The molar ratio of reactants was (1:1:1) (M: H2Ldfm : phen). The new Schiff base and its new complexes were characterized by different physicochemical tec

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Publication Date
Wed Jul 10 2019
Journal Name
Proceedings Of The Institution Of Mechanical Engineers, Part H: Journal Of Engineering In Medicine
The speed, reflection and intensity of waves propagating in flexible tubes with aneurysm and stenosis: Experimental investigation
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A localized stenosis or aneurysm is a discontinuity that presents the pulse wave produced by the contracting heart with a reflection site. However, neither wave speed ( c) in these discontinuities nor the size of reflection in relation to the size of the discontinuity has been adequately studied before. Therefore, the aim of this work is to study the propagation of waves traversing flexible tubes in the presence of aneurysm and stenosis in vitro. We manufactured different sized four stenosis and four aneurysm silicone sections, connected one at a time to a flexible ‘mother’ tube, at the inlet of which a single semi-sinusoidal wave was generated. Pressure and velocity were measured simultaneously 25 cm downstream the inlet of th

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Publication Date
Wed Feb 22 2023
Journal Name
Iraqi Journal Of Science
Novel Study of Cyproheptadine Hydrochloride Precipitate Formed by Potassium hexacyanoferrate and Sodium nitroprusside using Atomic Force Microscopy
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Atomic Force Microscope is an efficient tool to study the topography of precipitate. A study using Continuous Flow Injection via the use of Ayah 6SX1-T-2D Solar cell CFI Analyser . It was found that Cyproheptadine –HCl form precipitates of different quality using a precipitating agent's potassium hexacyanoferrate (III) and sodium nitroprusside. The formed precipitates are collected as they are formed in the usual sequence of forming the precipitate via the continuous flow .The precipitates are collected and dried under normal atmospheric pressure. The precipitates are subjected to atomic force microscope scanning to study the variation and differences of these precipitates relating them to the kind of response to both precipitates give

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Publication Date
Sun Sep 04 2016
Journal Name
Baghdad Science Journal
Synthesizing, Characterizing and Studying the Biological Activity of Some New Schiff-Bases Derivatives Containing the Monosaccharide Moiety
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A new series of ?-D-glucose as Schiff bases derivatives is synthesized and characterized with studying their bioactivity. Hydroxyl groups at C (1,2&5,6) sugar moiety are converted into acetal form through a reaction with dry acetone using phosphoric acid and anhydrous zinc chloride as catalysts producing 1,2:5,6-di-O-isopropyledine ?-D-glucofuranose(I). The five memberd ring acetal of C(5,6) is hydrolyzed with acetic acid (65%)and a reaction of the new product with sodium periodate is carried on to get an aldehyde moiety which is used to produce a new series of Schiff bases through reacting with different amino compounds such as 4-amino antipyrene . The suggested chemical structures of the prepared compounds are confirmed by using UV., FT

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Publication Date
Sat Jan 31 2026
Journal Name
Journal Of Baghdad College Of Dentistry
Early detection of periodontitis among young adult cigarette smokers and non-smokers using cone beam computed tomography
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Background: Periodontitis is an inflammatory disease that affects the supporting tissues of the teeth; Smoking is an important risk factor for periodontitis induces alveolar bone loss and cause an imbalance between bone resorption and bone deposition. The purpose of this study is to detect and compare the presence of incipient periodontitis among young smokers and non-smokers by measuring the distance between cement-enamel junction and alveolar crest (CEJ-Ac) using Cone Beam Computed Tomography (CBCT). Material and methods: The total sample composed of fifty two participants, thirty one smokers and twenty one non-smokers (age range 14-22 years). Periodontal parameters: plaque index (PLI), gingival index (GI) were recorded for all teeth exc

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Publication Date
Mon Feb 25 2019
Journal Name
Oriental Journal Of Chemistry
Viscosity and Density Studies of Drugs in Aqueous Solution and in Aqueous Threonine Solution at 298.15 K
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Publication Date
Thu Oct 01 2015
Journal Name
Journal Of The Faculty Of Medicine Baghdad
Effect of 1,3-Oxazepine Derivative on Alkaline Phosphatase and Lactate Dehydrogenase Activity in Healthy Iraqi Females Serum
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Background: Heterocyclic compounds and its derivatives have biological activities and used as analgesic, anti-helminthic, antituberculer, antifungal, antiviral, anticancer and inhibitor of some enzymes. Oxazepine (benzodiazepine) derivative used in relief of psychoneuroses characterized by anxiety and tension. Alkaline phosphatase (ALP) hydrolyzes phosphate monoesters, while Lactate dehydrogenase (LDH) catalyses oxidation of L-lactate to pyruvate utilizing NAD+Objective: The study was carried out to know of the impact of 1,3-oxazepine derivative on the ALP and LDH enzyme activity on human serum in vitro.Methods: The study included the effect of synthesized 1,3-oxazepine divertive [(Z)-3-(5-mercapto-1-3,4-Thiadizol-2-yl)-2-(4-nitroph

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