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Synthesis, Molecular Docking Study and Cytotoxicity Evaluation of some Quinazolinone Derivatives as Nonclassical Antifolates and Potential Cytotoxic Agents
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Abstract

A series of new 4(3H)-quinazolinone derivatives (S1-S4) were synthesized and characterized   by FTIR,1HNMR and 13CNMR .Their cytotoxic activity against a set of human cancer cell lines MCF-7 (breast) and A549 (lung) was evaluated using MTT assay. To detect their selectivity toward cancer cells, the compounds were also tested against epithelial cells derived from normal human fibroblast (NHF). Methotrexate (MTX) was used as a reference for comparison . All the tested compounds exhibited toxicity against the normal cells lower than cancer cells. All the tested compounds displayed higher cytotoxicity against lung cancer cell line (A549) than MTX with the most potent one is compound S2 (IC50: 5.73 µM). Among the tested compounds, compound S1 exhibited the highest antitumor activity against MCF-7cell line (IC50: 3.38 µM) compared to MTX (IC50: 27.32 µM). The binding modes of the synthesized compounds with the target proteins (DHFR and TS) were investigated by molecular docking studies using GOLD software.

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Publication Date
Sun Dec 06 2015
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Study the Biological Activity of New Morpholine Derivative
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A new series of morpholine derivative were prepared by reacting the morpholine with ethyl chloro acetate in the presence triethylamine as an catalyst and benzene as a solvent gave the ethyl morpholin-4-ylacetate reaction with hydrazine hydrate and ethanol as a solvent gave the 2-(morpholin-4-yl)acetohydrazide gave series of Schiff base were prepared by reacting 2-(morpholin-4- yl)acetohydrazide with different aromatic aldehydes and ketons . The new series of (3-9 )were synthesis by reaction of Schiff base (10-14) with chloroacetyl chloride, triethyl amine as an catalyst and 1,4dioxane as a solvent .The chemical structures of the synthesis compound were identified by spectral methods their [ IR ,1H-NMR and 13C-NMR ].The synthesised compoun

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Publication Date
Sun Nov 01 2020
Journal Name
Chemosphere
Sorption and degradation of ranitidine in soil: Leaching potential assessment
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Publication Date
Fri Mar 31 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Effect of Metformin and Antioxidant Agents on Hirsutism in Women with Polycystic Ovary Syndrome
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Forty six Iraqi women with PCOS were involved in this study . They were treated with metformin alone and with antioxidant agents (vitamin E or C).It was found that all patients who treated with metformin or with combination of metformin with antioxidant agents showed significant decrease in hirsutism score. The treatment of metformin with antioxidant agents is of great benefit in treatment of hirsutism in PCOS due to that there was no worsening effect after treatment. This may indicate that antioxidant agents may participate in alleviation of hirsutism so it can be said that oxidative stress may play an important role in developing of hirsutism in PCOS.   

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Publication Date
Wed Feb 01 2023
Journal Name
Health Science Reports
Diagnostic potential of salivary interleukin‐17, RANKL, and OPG to differentiate between periodontal health and disease and discriminate stable and unstable periodontitis: A case‐control study
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Abstract<sec><title>Background and Aims

Limitations of the conventional diagnostic techniques urged researchers to seek novel methods to predict, diagnose, and monitor periodontal disease. Use of the biomarkers available in oral fluids could be a revolutionary surrogate for the manual probing/diagnostic radiograph. Several salivary biomarkers have the potential to accurately discriminate periodontal health and disease. This study aimed to determine the diagnostic sensitivity and specificity of salivary interleukin (IL)‐17, receptor activator of nuclear factor‐κB ligand (RANKL), osteoprotegerin (OPG), RANKL/OPG for differentiating (1) periodontal health from disease and (2) stable a

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Publication Date
Wed Nov 01 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization, and Preliminary Evaluation of Antimicrobial activity of Imines derived from Vanillic Acid Conjugated to Heterocyclic
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The purpose of this research is to prepare new vanillic acid derivatives with 1,2,4-triazole-3-thiol heterocyclic ring and evaluate their antimicrobial activity in a preliminary assessment. A multistep synthesis was established for the preparation of new vanillic acid-triazole conjugates. The intermediate of 4-(4-amino-5-mercapto-4H-1,2,4-triazol-3-yl)-2-methoxyphenol (4) reacts with different heterocyclic aldehydes (thiophene-2-carboxaldehyde, pyrrole-2-carboxaldehyde, thiophene-3-carboxaldehyde, and furfural ) in ethanol containing few drops of acetic acid yielded the corresponding 4-(4-(substituted amino)-5-mercapto-4H-1,2,4-1triazol-3-yl)-2-methoxy phenol derivatives (

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Publication Date
Sun Sep 22 2019
Journal Name
Baghdad Science Journal
A Molecular and Biochemical Study for Cholesteryl Ester Transfer Protein (CETP) Taq1B in Iraqi Patients with Hyperlipidemia
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Cholesteryl ester transfer protein gene contains some single nucleotide polymorphisms, which have been associated with serum high-density lipoprotein concentration and other lipoproteins. This study is done for determining of cholesteryl ester transfer protein polymorphism and evaluate its effect on serum lipid profile concentrations in some hyperlipidemic patients compared with healthy subjects in Salah Al-din governorate-Iraq. Blood samples were taken from (90) patients suffering from hyperlipidemia, and (70) samples that were apparently healthy controls.  Serum lipid concentrations were measured by enzymatic assays. The polymorphism was genotyped using polymerase chain reaction restriction fragment length polymorphism analysis.&n

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Publication Date
Sun Feb 10 2019
Journal Name
Drug Invention Today
Design, characterization, and in vitro evaluation of zaltoprofen solid dispersion as a hollow-type rectal suppository
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Aim: The present study aims to improve the poor water solubility of zaltoprofen which is a non-steroidal anti-inflammatory drug (NSAIDs) with a potent analgesic effect using solid dispersion then formulate it as a hollow type suppository to be more convenient for geriatric patients. Materials and Method: Zaltoprofen solid dispersions were prepared by solvent evaporation technique in different zaltoprofen: Soluplus® ratios. Results: Among the formulations tested, zaltoprofen solid dispersion preparation using 1:5 (zaltoprofen: Soluplus®) ratio showed the highest solubility and selected for further investigation. Solid dispersion characterization was evaluated by differential scanning calorimetry (DSC), X-ray diffraction study (XRD) and Fou

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Publication Date
Sun Dec 02 2018
Journal Name
Journal Of The College Of Education For Women
Nutritional and Evaluation properties of natural orange juice enriched by coconut milk as kids' nutritional drink
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Coconut milk is considered as a natural drink that enhances the immunity and it is enriched by calcium, iron, magnesium and vitamin (C) and it is also safe drink for kids and bacterial anti-oxdant, and it may be used in the natural juices instead of the whole milk (cow milk) which is added to some juices. This study aimed to determine the nutritrnal value and the sensory evaluation properties of the natural orange juice enriched by canned coconut milk                                                 &nb

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Publication Date
Wed Mar 29 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Development and in vitro Evaluation of Bioadhesive Vaginal Tablet using Econazole Nitrate as a Model Drug
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         In this study, a bioadhesive dosage form of eoconazole nitrate for vaginal delivery was designed using a combination of bioadhesive polymers: Carbopol 941 p and sodium carboxymethylcellulose or methylcellulose in different ratios. The bioadhesive strength was evaluated by measuring the force required to detach the tablet from sheep vaginal mucosal membrane. It was found that the bioadhesive force was directly proportional to Carbopol 941 p content in the different formulae. The formulae were tested for their swelling behavior using agar gel plate method. The results showed that formulae containing a combination of Carbopol 941 p and sodium carboxymethylcellulose had greater swelling index

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Publication Date
Sun Mar 05 2017
Journal Name
Baghdad Science Journal
Synthesis of Some Mixed ligands Complexes of (2-hydroxy benzaldine)-4-amino Antipyrine and 1,10-phenanthroline and Studying their antibacterial activity
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Complexes from the ligand (2-hydroxy benzaldine)-4-aminoantipyrine with some transition metal ions V(l?),Cr(lll),Fe(lll) and Co(ll) were prepared in the presence of the co-ligand 1,10-phenanthroline in alcoholic medium. These compounds were characterized by the available techniques: FT-IR ,UV-Visible ,magnetic susceptibility, Flame atomic absorption technique as well as elemental analysis and conductivity mesurments .From these spectral studies, a square pyramidal structure proposed for V(IV) complex and an octahedral geometry for Cr(III),Fe(III) and Co(II) complexes. The biological activity of the ligands and their complexes were evaluated by a gar plate diffusion technique against three human pathogenic bacterial strains: Pseudomonas ae

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