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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
Tue Jul 01 2025
Journal Name
Mastering The Minds Of Machines
The Impact of Transfer Learning and Pre-trained Models on Model Performance
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Publication Date
Thu Sep 01 2011
Journal Name
Journal Of Economics And Administrative Sciences
Interactive Effects of Status Judgments and Individualism -Collectivism Orientation on Organizational Identification
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يهدف البحث الحالي الى استكشاف علاقات التفاعل والتاثير بين الاحتكام للمكانة والتوجه للفردية– الجماعية والدمج التنظيمي مستنداً على مزج اختلاف القيم الشخصية مع افكار نظرية الهوية الاجتماعية لبلورة نموذج البحث. وفي ضوء هذا تم صياغة عدد من الفرضيات التي توضح علاقات التفاعل ما بين ابعاد الاحتكام للمكانة والتوجه للفردية– الجماعية للتنبؤ بوجود الدمج التنظيمي. جمعت البيانات باستخدام استمارة الاستبيان ووزع

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Publication Date
Wed Feb 01 2017
Journal Name
Journal Of Economics And Administrative Sciences
Performance Evaluation Strategy and its Impact on the Achievement of Organizational Effectiveness
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Abstract

The research aims to determine the impact of the strategy performance evaluation and of the Standards (leadership, people, knowledge, processes, financial) in the achievement of organizational effectiveness in accordance with the dimensions (planning and setting goals, Exploitation of the Environment, achieve the goals, the ability to adapt, information management and communications) and the relationship between them, the problem of the research in the growing interest in the process of performance evaluation for organizations, the erroneous belief that the performance evaluation activity is useful, and the fact that performance evaluation process is one of the main tasks of the work of the Office of the Inspecto

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Publication Date
Sun Jul 01 2018
Journal Name
Journal Of Construction Engineering And Management
Measuring and Evaluating Safety Maturity of Construction Contractors: Multicriteria Decision-Making Approach
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Publication Date
Fri Jun 16 2017
Journal Name
Computers
Enhancing BER Performance Limit of BCH and RS Codes Using Multipath Diversity
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Publication Date
Sun Jan 01 2017
Journal Name
Journal Of Epidemiology And Global Health
Incidence and prevalence rates of diabetes mellitus in Saudi Arabia: An overview
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Publication Date
Wed Jan 01 2020
Journal Name
Advanced Composites Letters
Enhanced thermal and electrical properties of epoxy/carbon fiber–silicon carbide composites
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The silicon carbide/carbon fiber (SiC/CF) hybrid fillers were introduced to improve the electrical and thermal conductivities of the epoxy resin composites. Results of Fourier transform infrared spectroscopy revealed that the peaks at 3532 and 2850 cm−1 relate to carboxylic acid O–H stretching and aldehyde C–H stretching appearing deeper with an increased volume fraction of SiC. Scanning electron microscopic image shows a better interface bonding between the fiber and the matrix when the volume fraction of SiC particles are increased. As frequency increases from 102 Hz to 106 Hz, dielectric constants decrease slightly. Dissipation factor (tan δ) values keep low a

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Publication Date
Wed Aug 01 2018
Journal Name
Iranian Journal Of Science And Technology, Transactions A: Science
Structural, Optical and Sensing Behavior of Neodymium-Doped Vanadium Pentoxide Thin Films
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Publication Date
Wed Jan 01 2025
Journal Name
Opennano
Development and characterization of bilastine nanosuspension for enhanced dissolution in orodispersible films
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Abstract Bilastine, a second-generation antihistamine, is commonly prescribed for managing allergic rhinoconjunctivitis and urticaria due to its prolonged action. However, its therapeutic potential is constrained by poor water solubility and low oral bioavailability. This study aimed to enhance bilastine dissolution and patient compliance by formulating a nanosuspension-based orodispersible film (ODF). An anti-solvent precipitation method was employed to produce nanosuspension using different hydrophilic stabilizers (Soluplus®, Poloxamer 188, and PEG 6000). The influence of formulation parameters, such as the stabilizer ratio, the anti-solvent ratio, stirring speed, and the stabilizer type, on particle size and polydispersity index (PDI)

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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 Evaluation of Sustained Release Sumatriptan Mucoadhesive Intranasal in-Situ Gel
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Sumatriptan(ST) is a selective agonist at serotonin 5-HTI receptors, as well as 5-HT1B/1D subtypes. It is effective for acute migraine attacks, but has a short half  life (about 2 hours) and low oral bioavailability (15%). The purpose of this study was to develop and optimize nasal mucoadhesive in-situ gel(IG) of ST to enhance nasal residence time for migraine management. Cold method was used to prepare different formulas of  ST nasal IG, using thermosensitive polymers (poloxamer 407  alone or with poloxamer 188) with a mucoadhesive polymer hyaluronic acid (HA) which were examined for gelation temperature and gelation time, pH, drug content, gel strength, spreadability, muc

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