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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 Mar 15 2022
Journal Name
Journal Of Baghdad College Of Dentistry
In vitro cytotoxic effect of annona squamosa pulp ex-tract as a mouthwash for children on human normal cell line
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Background: Fruits and their by-products are the primary sources of bioactive chemicals in plants. Because of its phytochemical richness, Annona squamosa fruits have gained the alertness of people willing in health-promoting diets. The purpose of this in vitro study was to evaluate the cytocompatibility effect of ethanolic crude extract of Annona squamosa pulp against a human normal cell line as a mouthwash for children. Material and method: The ethanolic extract of Annona squamosa pulp was extracted using the ultrasonic method and then lyophilized to make it powder. The MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide) test was performed to investigate the cytotoxic activity of the pulp extract on a human normal cell l

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Publication Date
Fri May 18 2018
Journal Name
Thesis
The Arabian killifish (Aphanius dispar) as a novel model for mycophysiological studies.
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Abstract Candida albicans is a commensal fungal pathogen that grows in yeast and hyphal forms in the human gut. C. albicans causes mucosal and cutaneous diseases that can result in significant mortality following systematic infections and it also exhibits drug resistance. Zebrafish have been an excellent model to investigate C. albicans infections because of their transparency and the availability of many transgenic lines. However, there is a limitation in using zebrafish as a model because the fish embryos cannot survive at 37°C therefore it is not suitable for studying Candida infections at physiological relevant human body temperature. In this thesis, the normal embryonic development of Arabian killifish (A. dispar) is investigated, rev

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Publication Date
Thu Feb 01 2024
Journal Name
Russian Journal Of Bioorganic Chemistry
Synthesis, Characterization of Formazan Derivatives from Isoniazid and Study Their Antioxidant Activity and Molecular Docking
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Objective: Synthesis, Characterization of formazan derivatives and studies the antioxidant activity of prepared compounds and molecular docking. Methods: In this study, formazan compounds (III–XIV) were produced by combining Schiff base compounds (I), (II) with diazonium salts resulting from reactions of different aromatic amines with sodium nitrate in the presence of Con.HCl at 0–5°C. When isonicotinic acid hydrazide reacts with (N,N-dimethylbenzaldehyde, 4-hydroxy-3-methoxybenzaldehyde) in the presence glacial acetic acid as a solvent Schiff base compounds are created. Results: The prepared compounds were identified by FT-IR, 1H NMR, 13C NMR, then the antioxidant activity of the derivatives and molecular docking were studied. D

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Publication Date
Thu Dec 01 2022
Journal Name
Baghdad Science Journal
Synthesis, Characterization of Chitosan para- hydroxyl Benzaldehyde Schiff Base Linked Maleic Anhydride and the Evaluation of Its Antimicrobial Activities
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Current research included preparation, characterization of some new chitosan- hydroxy benzaldehyde-Schiff bases with maleic anhydride. The present study aimed to the synthesis and characterization of novel chitosan Schiff base compounds using para- hydroxy benzaldeh and maleic anhydride. The  derivative of the  schiff-chitosan base, which is associated with different drugs, has been replaced with   different  amino  and  hydroxy  drugs.  The derivative is characterized by different analytical techniques. The results of FT-IR studies clearly indicate construction of the chief amine group in chitosan and the emergence of new bands that correspond to the association of maleic anhydride with the chitosan base. TGA, 1

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Publication Date
Sun Sep 03 2017
Journal Name
Baghdad Science Journal
Preparation and Characterization of Cu (II), Mn(II) and Zn(II)complexes with new sulfamethoxazole Compounds
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Acetophenone sulfamethoxazole and 3-Nitrobenzophenone sulfamethoxazole were prepared from the reaction of sulfamethoxazole with two ketones. The prepared ligands were identified by (C.H.N) analysis and UV-VIS, FT-IR spectroscopic techniques. Metal complexes of the two ligands were prepared in an aqueous alcohol with Zn (II), Mn (II) and Cu (II) ions with a molar ratio1:1. The proposed general formula for the resulting complexes was [ML.CL2.H2O]H2O .The complexes were characterized by (C.H.N) technique , spectroscopic methods ,conductivity, atomic absorption ,magnetic susceptibility measurements and melting point. According to the results obtained, the suggested geometry is to be octahedral for all the complexes.

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Publication Date
Thu May 25 2023
Journal Name
Results In Chemistry
Synthesis and characterization of (E)-4-(((4-(5-mercapto-1, 3, 4-oxadiazol-2-yl) phenyl) amino) methyl)-2-methoxyphenol as a novel corrosion inhibitor for mild-steel in acidic medium
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Metal corrosion is a destructive process for many industrial operations, including oil well acidizing and acid pickling. Therefore, numerous efforts made by many researchers to control the steel corrosion. In the present work, A (E)-4-(((4-(5-mercapto-1,3,4-oxadiazol-2-yl) phenyl) amino) methyl)-2-methoxyphenol (MOPM) has been synthesized and characterized as a new corrosion inhibitor for mild steel in 0.1 M hydrochloric acid. FTIR and 1 HNMR were used in the diagnosis of MOPM, while electrochemical polarization technique was employed to test the performance of inhibitor at various temperatures and inhibitor concentrations. Electrochemical studies showed that MOPM acts as a mixed-type inhibitor with a maximum inhibition efficiency of

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Publication Date
Sun Jan 01 2023
Journal Name
Results In Chemistry
Synthesis and characterization of (E)-4-(((4-(5-mercapto-1, 3, 4-oxadiazol-2-yl) phenyl) amino) methyl)-2-methoxyphenol as a novel corrosion inhibitor for mild-steel in acidic medium
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Publication Date
Sat Dec 01 2018
Journal Name
Engineering And Technology Journal
Comparison between the Biological Activity of Agaricus bisporus Fruiting Bodies and Albizzia lebbeck Leaves Extract against Different Pathogenic Microoganisms
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Publication Date
Mon Jul 20 2020
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Antibacterial Activity of PEG Polycyclic Acetal Metal Complex/ PVA Polymer Blend Film
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     Polyacetal was synthesized from the reaction of Polyethylene glycol with4- dimethylaminobenzaldehyde.Polymer metal complex was synthesized by the reaction with Ag+; polymer blend with polyvinyl alcohol was synthesized solution casting technique. All synthesized compounds were characterized by FT-IR in addition to the antimicrobial activity. The FT-IR spectra indicate the formation of the polyacetal. The DSC resultsindicatethe thermal stability regarding the synthesized polymer blends. The synthesized polyacetal, its metal complex and PA blend against four types of bacteria (gram+ve) Staphylococcus aureas, Bacillus subtilis and (gram –ve)Klebsiella pneumoniae, Escherichia Coli w

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Publication Date
Thu Jun 18 2020
Journal Name
Biochem. Cell. Arch.
NEW DERIVATIVE OF CHITOSAN BASED ON EPICHLOROHYDRNE, SYNTHESIS, CHARACTERIZATION, ANTIBACTERIAL ACTIVITY AND SWELLING STUDY
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A novel series of chitosan derivatives were synthesized via reaction of chitosan with carbonyl compounds and grafted it’s by with different amine compounds substituted hydrogen. The produced polymers were characterized by different analyses FTIR, 1HCNMR, XRD, DSC and TGA. Solubility in water as well as many solvent was investigated, antibacterial activity of chitosan and its derivatives against two types of bacteria E. coli and S. aureus was also investigated. The results showed that derivatives sort of have antibacterial activities against Esherichia coli (Gram negative) better than chitosan whilst compound IX has better antibacterial against Staphylococcus aureus (Gram positive). SEM analysis showed that increase of surface roughness wi

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