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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
Thu Dec 28 2017
Journal Name
Ibn Al- Haitham Journal For Pure And Applied Science
Microwave Preparation, Spectral Studies and Antimicrobial Activities Evaluation of Mn(II),Ni(II), Hg(II),Co(II) and Cu(II) Complexes with Schiff Base Ligand
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New Schiff base and their Mn(II),Co(II),Ni(II), Cu(II) and Hg(II) complexes formed by the condensation of O-phathaldehyde and ethylene diamine (2:1) to give ligand (L1) in the first step ,then the ligand (L1) with 2- aminophenol (1:2) to give ligand (L2) were prepared by classic addition through microwave method . These compounds (Ligands and complexes) have been diagnosed electronic spectra, FT-IR,1H-&13C-NMR (only ligand), magnetic susceptibility, elemental microanalysis and molar conductance measurements. Analytical values displayed that all the complexes appeared (metal: ligand) (1:1) ratio with the six chelation. All the compounds appear a high activity versus four types of bacteria such as; (Escherichia coli), (Sta

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Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Determination of Testosterone level as predictor for insulin resistance in young men with family history of type2 diabetes and hypertension.
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Background: Insulin resistance is associated with metabolic syndrome , type 2 diabetes and representing a risk factor for cardiovascular disease . This relationship may be modulated to some extent by age related changes in sex hormone status.. In particular, reduced total testosterone (TT) levels have been associated with insulin resistance and subsequent risk for developing type 2 diabetes. Aim of study: we examined whether low total testosterone level were associated with insulin resistance in young adult men. Methods: a total of 83 men (young adult men) divided into 2 group : (group1 ) 49 men with a risk factor for insu

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Publication Date
Sun Jun 01 2014
Journal Name
Alustath Journal For Human And Social Sciences
Obstacles to the application of electronic management in university libraries: the universities of Baghdad and Al-Mustansiriya as a model.
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The research aims to identify the obstacles facing the application of electronic management in our university libraries, including the central library of the University of Baghdad and the central library of Al-Mustansiriya University, the research sample, as they are among the main libraries that used electronic technologies in managing some of their work and in providing their services, and they have a website via the Internet. The research relied on the case study method to identify the obstacles by visiting the two libraries, interviewing their managers and employees responsible for the departments, and answering inquiries about the obstacles that prevent the application of electronic management in order to identify them and find appropr

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Publication Date
Thu Feb 16 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Combination of FDM 3D Printing and Compressed Tablet for Preparation of Baclofen as Gastro-Floating Drug Delivery System (Conference Paper )#
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This study aimed to develop an oral drug delivery system for gastro-retentive sustained drug release of baclofen by using a 3D printed capsular device since baclofen has a short half-life of 2.5 to 4 hours and has a narrow absorption window. Firstly sustained-release tablets of baclofen were formulated through the hot-melt extrusion of various thermoplastic polymers and direct compression of the extrudate, then a capsular device was designed and 3D printed to contain two air pockets to enable floating of the device and has four windows for drug release.

3D printing of the capsular device was done by an FDM printer using biodegradable PLA filament, and the sustained release tablets were inserted into the device to allow the medici

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Publication Date
Thu Apr 20 2023
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Evaluation of Adiponectin, Irisin, Vitamin D Levels and Their Relation in Iraqi Patients with Non alcoholic Fatty Liver Disease
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Non-alcoholic fatty liver disease (NAFLD) is one of chronic liver and defines by fat accumulation ≥5% in liver which can progresses to non-alcoholic steatohepatitis (NASH). NAFLD related to obesity as well as non obese individuals. Adiponectin is a cytokine secreted from adipose tissue involved NAFLD pathogenesis and liked with obesity. Irisin is a myokine, has a convenient effect against metabolic diseases such as obesity, disylipemia diabetes type 2 and reversed liver steatosis and may be related with NAFLD.  Vitamin D is one of the fat soluble vitamins and more precisely as a pro-hormone through its metabolite (1,25(OH)2 cholecalciferol) the major steroid hormone. After the skin exposure to the light, vitamin D undergoes to

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Publication Date
Mon Mar 04 2024
Journal Name
Journal Of Emergency Medicine, Trauma And Acute Care
Cone beam computed tomography (CBCT) evaluation of ridge shape and bone density in Iraqi sample pre-dental implant insertion
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One of the critical factors for dental implant success is accurate clinical and radiological assessment. Cone-beam computed tomography systems (CBCT) allow surgeons to determine the quality and quantity before surgery, aiding in treatment planning. This study highlights the importance of such an assessment Materials and Methods A total of 40 patients were referred to CBCT scanning for pre-dental implant assessment in the Oral and Maxillofacial Radiology department at Al-Shaheed Gazi Al Hariri Hospital from 2021 to 2022. The patients were between 18 and 50 years old. All data were analyzed with on-demand 3D software (Kavo OP 3D: Cone Beam 3D imaging Germany). Results: Regarding the ridge shape: In the upper anterior and posterior regions, th

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Publication Date
Fri Jun 30 2023
Journal Name
Azerbaijan Pharmaceutical And Pharmacotherapy J
Evaluation of Nurses’ Practices and Perceived Barriers Related to Pain Assessment in Critically Ill Patients at Baghdad Teaching Hospitals
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Introduction: Inadequate pain assessment and management is a problem in hospitalized patients that impairs their wellbeing. Intensive care unit nurses’ pain practices are affected by several barriers and enablers. Objectives: The objectives of this study were to determine the level of nurses’ practices and perceived barriers related to pain assessment in critically ill patients. Methodology: A cross-sectional design study was used. Purposive sampling technique was employed, including 100 nurses recruited from 8 intensive care units in Baghdad city, Iraq. The study was conducted from September 1st to October 20th, 2022. The pain assessment and management for critically ill patients survey was used to collect data. Descriptive sta

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Publication Date
Fri Jun 30 2017
Journal Name
Journal Of Engineering
Performance Evaluation of a PID and a Fuzzy PID Controllers Designed for Controlling a Simulated Quadcopter Rotational Dynamics Model
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This work is concerned with designing two types of controllers, a PID and a Fuzzy PID, to be used
for flying and stabilizing a quadcopter. The designed controllers have been tuned, tested, and
compared using two performance indices which are the Integral Square Error (ISE) and the Integral
Absolute Error (IAE), and also some response characteristics like the rise time, overshoot, settling
time, and the steady state error. To try and test the controllers, a quadcopter mathematical model has
been developed. The model concentrated on the rotational dynamics of the quadcopter, i.e. the roll,
pitch, and yaw variables. The work has been simulated with “MATLAB”. To make testing the
simulated model and the controllers m

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Publication Date
Mon Jan 01 2024
Journal Name
International Journal Of Clinical And Diagnostic Pathology
Evaluation of transferrin saturation and serum ferritin in assessing body iron status in patients with end stage renal disease
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The study aimed to evaluate the benefits of transferrin saturation percentage (TSAT) and serum ferritin in assessing body iron status, which can influence erythropoietin treatment in patients with ESRD. Forty end-stage renal disease patients on regular hemodialysis participated in this study. Clinical data were obtained. Serum iron, total iron binding capacity, transferrin saturation, ferritin, albumin, creatinine, and C-reactive protein were investigated. Thirty healthy people were enrolled as a control group. ESRD patients had a mean age of 45.1±13.9 years, with 60% being males. They exhibited significantly lower hematocrit (25.3±6.5%), and higher platelet (285.7±148.1x10^9/L) and WBC (9.4±3.1x10^9/L) counts compared to healthy contro

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Publication Date
Mon Sep 28 2026
Journal Name
Journal Of Baghdad College Of Dentistry
The Effect of Pores in Dual Nano Hydroxyapatite Coating on Thermally Oxidized Commercial Pure Titanium: Mechanical and Histological Evaluation
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Background:In this study,TiO2 layer was thermally grown as a diffusion barrier on CP Ti substrate prior to electrophoretic deposition of HA coatings, to improve the coating’s compatibility also macro and micro pores in nano Hydroxyapatite dual coatings were created and their effect on the bond strength between the bone and implant was evaluated. Materials and methods: Electrophoretic Deposition technique (EPD) was used to obtain coatings for each one of four types of Hydroxyapatite(HA)on CP Ti screws (micro HA, nano HA, dual nano HA with micro pores, dual nano HA with macro pores) where carbon particles used as fugitive material to be removed by thermal treatment to create porosity.For examination of the changes occurred on the subs

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