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Synthesis of some Novel Nitrogenous Heterocyclic Compounds with Expected Biological Activity as Antimicrobial and Cytotoxic Agents
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This study includes synthesis of some nitrogenous heterocyclic compounds linked to amino acid esters or heterocyclic amines that may have a potential  activity as antimicrobial and/or cytotoxic.  Quinolines are an important group of organic compounds that possess useful biological activity as antibacterial, antifungal and antitumor .8-Hydroxyquinoline (8-HQ) and numerous of its derivatives exhibit potent activities against fungi and bacteria which make them good candidates for the treatment of many parasitic and microbial infection diseases.

These pharmacological properties of quinolones  aroused our  interest in synthesizing several new compounds featuring heterocyclic rings of the quinoline derivatives linked to amino acid ester or heterocyclic amine with the aim of obtaining a pharmacologically active compounds.O-alkylation has been done on( 8-hydroxyquinoline ) to get (O-alkylated ester) derivatives which are deesterfied to get acetic acid derivatives, then coupled with amino acid that have protected carboxyl group (amino acid esters) or heterocyclic amine by using conventional solution  method for peptide synthesis as a coupling method.

The proposed analogues were successfully synthesized and the processing of the reactions confirmed by TLC ,the synthesized  analogues with the proposed structures as they were characterized and proved by  melting point, infrared spectroscopy (IR) and elemental microanalysis.

The tested analogues showed cytotoxic activity on the HEp-2 cell line (tumor of larynx) with inhibitory concentration percent of (IC %) range (32.43 % - 49.55%) and showed that the tested compounds had variable antimicrobial activities against selected bacteria and yeast when compared with selected standard drugs.

Keywords: Quinolones, 8-hydroxyquinoline , N-heterocycles biological activity.

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Publication Date
Sun Dec 01 2024
Journal Name
Russian Journal Of General Chemistry
Synthesis, Characterization, and Biological Evaluation for New Derivatives Based on 2Сhloro-N-[4-(5-phenyl-1,3,4-oxadiazol-2-yl)phenyl]acetamide
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Publication Date
Mon Jul 01 2024
Journal Name
Iranian Journal Of Catalysis (ijc)
Preparation, characterization, and antioxidant activity of novel metal (Mn (II), Ni (II), Pd (II), Pt (IV)) complexes: Application of Pd complex in Suzuki-Miyaura cross-coupling reaction
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Publication Date
Sun Dec 25 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Quantitative Determination and Cytotoxic Effect of Oleanolic Acid from Olea europaea Leaves Extract Cultivated in Iraq
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Since its first description as a cytotoxic agent, Olea europaea leaves extract gained significant popularity against human breast cancer, ethyl acetate extract of Olea europaea leaves obtained by acid hydrolysis method was evaluated in vitro as cytotoxic agent against new human breast cancer (AMJ13) cell line, using the MTT assay. One main pentacyclic triterpenoid; oleanolic acid, was isolated from leaves of Olea europaea by well-known two different methods, but not used for this compound before, the acidic hydrolysis method and basic acidic method. The presence of oleanolic acid was proved in both methods with qualitative and quantitative d

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Publication Date
Thu Aug 01 2024
Journal Name
Journal Of Taibah University Medical Sciences
Cytotoxic properties of Pelargonium graveolens leaf extract and its green-synthesized gold nanoparticles (in vitro study)
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Publication Date
Fri Dec 15 2017
Journal Name
Journal Of Baghdad College Of Dentistry
The Effect of Addition of Zirconium Nano Particles on Antifungal Activity and Some Properties of Soft Denture Lining Material
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Background Microorganisms and fungal growth especially Candida albicans, on soft denture lining material are the most common problem which can lead to chronic mucosal inflammation. The aim of this study was to evaluate the effect of zirconium nanoparticles into acrylic-based heat cured soft denture lining material against Candida albicans, and the amount of zirconium ion release of soft liner/ZrNPs composite. Furthermore, evaluate shear bond strength after ZrNPs addition to soft liner. Materials and methods: Zirconium nanoparticles were added into acrylic-based soft denture liner in various percentages (1%, and 1.5% by weight). Two hundred and fifty specimens were arranged and isolated into four groups as per the test to be done The antifu

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Publication Date
Sat May 01 2021
Journal Name
Journal Of Physics: Conference Series
Evaluation of Ceruloplasmin ferroxidase activity and lipid profiles in patients with Valvular heart diseases
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Abstract<p>One of the major health problems causing defects or damage to one or more of the four heart valves [aortic, mitral, pulmonary, and tricuspid] is valvular heart disease [VHD]; it occurs due to congenital abnormalities or acquired pathology. It is a defect that results in weak heart valves and is therefore unable to function as precise pathways of the blood. The aim of the current study was to evaluate the ferroxidase activity of ceruloplasmin (Cp) and the lipid profile of valvular heart disease patients in sera. Ninety subjects were included in this study and 60 patients with HDV were divided into two subgroups according to the affected valve: 33 patients with aortic valve disease (AV) and 27 patients</p> ... Show More
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Publication Date
Sun Sep 03 2017
Journal Name
Baghdad Science Journal
Measurement and purification of Alanine aminotransferase (ALT) enzyme activity in patients with celiac disease
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Celiac disease (CD) is the most common genetically - based disease in correlation with food intolerance. The aim of this study is to measure the activity of ALT enzyme and purify enzyme from sera women with celiac disease. Alanine aminotransferase (ALT) activity has been assayed in (30) women serum samples with celiac disease, age range between (20-40) year and (30) serum of healthy women as control group, age range between (22-38) year. In the present study, the mean value of ALT activity was significantly higher in patients with celiac disease than healthy group (p<0.01). The ALT enzyme was partial purified from sera women with celiac disease by dialysis, gel filtration using Sephadex G- 50 and ion exchange chr

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Publication Date
Sat Mar 04 2017
Journal Name
Baghdad Science Journal
Measurement and purification of Alanine aminotransferase (ALT) enzyme activity in patients with celiac disease
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Celiac disease (CD) is the most common genetically - based disease in correlation with food intolerance. The aim of this study is to measure the activity of ALT enzyme and purify enzyme from sera women with celiac disease. Alanine aminotransferase (ALT) activity has been assayed in (30) women serum samples with celiac disease, age range between (20-40) year and (30) serum of healthy women as control group, age range between (22-38) year. In the present study, the mean value of ALT activity was significantly higher in patients with celiac disease than healthy group (p<0.01). The ALT enzyme was partial purified from sera women with celiac disease by dialysis, gel filtration using Sephadex G- 50 and ion exchange chromatography using DEAE- cell

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Publication Date
Thu Dec 31 2015
Journal Name
Al-khwarizmi Engineering Journal
Modeling of Mass Transfer Coefficient in Rotating Biological Contactor with Perforated Discs (RPBC)
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Abstract

 In order to make an improvement associated with rotating biological contactor (RBC), a new design of biofilm reactor called as Rotating perforated disc biological contactor (RPBC) was developed in which the rotating discs are perforated. The transfer of oxygen from air to wastewater was investigated. Mass-transfer coefficient (KLa)  in the liquid phase was determined by measuring  the rate transfer of oxygen.  A   laboratory scale of (RPBC) consisted of a semicircular trough was used with a working capacity of 40 liters capacity of liquid. Synthetic wastewater was used as a liquid phase, while air was used as a gas phase.

The effects of m

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Publication Date
Sat Apr 01 2017
Journal Name
Iraqi Journal Of Cancer And Medical Genetics
Mitotic activity of cultured human lymphocytes treated with gold nanoparticles
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Potential health and environmental effects of nanoparticles need to be thoroughly assessed before their widespread commercialization. The present investigation was planned with the aims to determine the effects of gold nanoparticles (GNPs) on blast (BI) and mitotic (MI) indices of cultured lymphocytes. The results revealed that BI (50.3±2.3, 30.2±1.9, 10.5±0.7 and 0.0%, respectively) and MI (70.1±2.9, 20.4±1.1, 5.3±0.1 and 0.0%, respectively) showed a gradual decreased percentage as the concentration of GNPs was increased from 0.085 to 0.66 µg/mL, and the difference was significant compared to control culture (81.6±2.5 and 90.2±3.7%, respectively). A maximum inhibition of BI and MI was occurred at the concentration 0.66 µg/mL. In

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