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bijps-1639
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
Sat May 13 2023
Journal Name
Journal Of Population Therapeutics And Clinical Pharmacology
Synthesis, Characterization of Schiff's and Mannich bases of 5-Fluoroisatin and Preliminary Antimicrobial Evaluation
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With the aim of developing potential antimicrobials, a series of new 5-fluoroisatin derivatives incorporated with different secondary amines (piperidine, morpholine, pyrrolidine, dimethylamine, and diphenylamine) for monomer, and (piperazine) in case of dimer Mannich bases, separately in presence of formaldehyde to obtain Mannich bases of 5-fluoroisatin derivatives, which then each Mannich derivatives reacts with phenylhydrazine to form Schiff bases as final products. The resulting compounds were characterized by two spectroscopic analyses; (Fourier- transform infrared) FT-IR and proton nuclear magnetic resonance spectroscopy (¹H-NMR). In addition, the in vitro antibacterial and antifungal activities were tested against some human pathogen

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Publication Date
Thu Oct 31 2019
Journal Name
Al-kindy College Medical Journal
Stethoscope as potential occupational hazards for intra hospital carries of pathogenic microorganisms
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Background: The stethoscope is a tool that doctors use daily in the examination of patients and  it  can take part in the transmission of health care-associated infections. In a single day it may come in direct contact with multiple patients and the intra hospital environment  may be contaminated by various type of bacteria and possibly transmit to others.

Objective:- The study was to know the attitude and knowledge about   the stethoscope hygiene behavior among physicians  and to determine the types of  bacterial agents that can contaminate stethoscopes.

Type of the study: The study was a cross-sectional study

Metho

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Publication Date
Tue Dec 28 2021
Journal Name
The Iraqi Journal Of Veterinary Medicine
Evaluating Expression of the STAG1 Gene as a Potential Breast Cancer Biomarker
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STAG proteins, which are part of the cohesin complex and encoded by the STAG genes, are known as Irr1/Scc3 in yeast and as SA/STAG/stromalin in mammals. There are more variants as there are alternate splice sites, maybe three open reading frames (ORFs) code for three main proteins, including: SA1 (STAG1), SA2 (STAG2) and SA3 (STAG3). The cohesin protein complex has various essential roles in eukaryotic cell biology. This study compared the expression of the STAG1 gene in four different breast cancer cell lines, including: MCF-7, T-47D, MDA-MB-468, and MDA-MB-231 and normal breast tissue. RNA was extracted from these cell lines and mRNA was converted to cDNA, and then expression of the STAG1 gene was quantified by three sets of specific prim

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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)
Formulation and Clinical Evaluation of Orphenadrine citrate as a Plain Tablet
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Orphenadrine is an anticholinergic ,antimuscarinic , centrally acting skeletal muscle relaxant .It presents in the form of citrate and HCl salts which are used in treatment of the symptoms of mild Parkinson's disease and also it is used as adjuvant with other drugs in the therapy .

      Many trials were made to formulate Orphenadrine citrate as a plain tablet using wet granulation or direct compression technique in order to get a satisfactory formula through studying the effect of various factors such as binders , diluents and disintegrants types .

    The best formula was obtained by using Poly Vinyl Pyrolidine (PVP) as a binder also the results indicated that starch and mannitol

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Publication Date
Mon Dec 25 2023
Journal Name
International Journal Of Drug Delivery Technology
Formulation, Characterization, Optimization, and In-vitro Evaluation of Rosuvastatin as Nanofiber
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Bioavailability is the objective for an optimum formulation. The target of the analysis is to maximize both the fluidity and disintegration profile of class II weakly compounds that are water-soluble. Anti-dyslipidemia drug rosuvastatin calcium (RC) (bioavailability 20%) through formulating as nanofibers (NFs) using electrospinning (ES) technology. Twenty formulas were prepared, and different polymers and polymer combinations with various concentrations were used such as polyethylene oxide (PEO) polyvinyl pyrrolidine (PVPK-30), and hydroxypropyl methylcellulose (HPMC). Three distinct groups of maximum parameters, including polymeric solution, electrospinning method, and ambient parameter, are capable of influencing the creation alon

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Publication Date
Tue Jan 01 2019
Journal Name
Biochem. Cell. Arch
ISOLATION, IDENTIFICATION AND EVALUATION OF LACTIC ACID BACTERIA AS ANTIBACTERIAL ACTIVITY
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Five species of Lactic acid bacteriawere isolated from raw milk, yoghurt, vegetables and pickles, Lactobacillus plantarum, Lactobacillus acidophilus, Lactobacillus brevis, Lactobacillus casei and Lactobacillus bulgaricus isolates were identified by 16S rRNA gene. Evaluate of antimicrobial activity against all the bacterial strains Staphylococcus aureus, Salmonella spp., Pseudomonas fluorescens, Escherichia coli, Bacillus cereus and Bacillus subtilis. It showed that bacteriocin of Lactic acid bacteriamore effective than supernatant of lactic acid bacteria, the results showed that isolatemost efficient isolate belonging to Lactobacillus brevis, the diameter of the inhibition of the bacteriocin of Lactobacillus brevis were 27.7, 26.3 and 25.1

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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)
Preparation and Evaluation of Chloramphenicol as Thermosensitive Ocular in- situ Gel
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The purpose of this study was to develop poloxamer-based in-situ gel of chloramphenicol aiming to increase bioavailability and prolong corneal contact time, controlling drug release, and enhancing ocular bioavailability. The in-situ gel was prepared using different concentrations of poloxamer 407 combined with hydroxypropyl methyl cellulose (HPMC) or carbapol 940 to achieve gelation temperature about physiological temperature and improve rheological behavior and gelling properties of poloxamer gel. The prepared formulations were evaluated for their appearance, pH, and sol-gel transition temperature. The formulations F2, F3, and F5 have a gelation temperature within the accepted range 35-370C an

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Publication Date
Sun Mar 26 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Evaluation of Nystatin Microparticles as a Sustained Release System
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Nystatin is the drug of choice for treatment of cutaneous fungal infections with main disadvantage that is the need for multiple applications to achieve complete eradication which may reduce patient compliance. Microparticles offer a solution for such issue as they are one of sustained release preparations that achieve slow release of drug over an extended period of time. The objectives of this study were to fabricate nystatin-loaded chitosan microparticles with the ultimate goal of prolonging drug release and to analyze the influence of polymer concentration on various properties of microparticles. Microparticles were prepared by chemical cross-linking method using glutaraldehyde as cross-linking agent. Five formulas, namely N1C1, N1C2,

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Publication Date
Sun Dec 22 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and In-Vitro Evaluation of Darifenacin Hydrobromide as Buccal Films
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         Darifenacin hydrobromide (DH) is the more recent uroselective M3 receptor antagonist for treating uncomplicated overactive bladder (OAB). This study was aimed to formulate DH as fast dissolving buccal films (FDBFs) using a solvent casting method to enhance patient’s compliance.

         Films were prepared by using polyvinyl alcohol (PVA) as a film forming polymer. Different types and concentrations of superdisintegrants (croscarmellose sodium, sodium starch glycolate, indion 414) were used to select the best formula by studying the physicochemical properties of the films, disintegration time (DT) and percent drug release.

 &nb

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Publication Date
Sun Jul 23 2023
Journal Name
University Of Samarra
Synthesis, spectral characterization and thermal ‎study of complexes of ions of some metallic ‎elements with new cyclic ligands
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The purpose of my thesis is to prepare four new ligands (L1-L4) that have been ‎used to prepare a series of metal complexes by reacting them with metal ions:‎ ‎ M=(Mn(II), Co(II), Ni(II), Cu(II), Zn(II), Cd(II), Hg(II) ‎ ‎ Where succinyl chloride was used as a raw material for the preparation of ‎bi-dented ligands (L1-L4) by reacting it with potassium thiocyanate as a first ‎step and then reacting with (2-aminobenzothiazole, Benzylamine, 4-‎aminoantipyrine, Sulfamethoxazole) respectively as a second step with the use ‎of dry acetone as a solvent, the chemical formula of the four ligands prepared in ‎succession:‎ N1,N4-bis(benzo[d]thiazol-2-ylcarbamothioyl)succinamide (L1)‎ N1,N4-bis(benzylcarbamothioyl)succinami

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