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Synthesis, Characterization, and Biological Evaluation of New Cyclic Quinazoline Derivatives as Potential Antibacterial and Antifungal Agents
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Heterocyclic compounds are crucial for medicinal chemistry and the development of therapeutic agents like broad-spectrum antibiotics. This study devised a facile procedure to synthesize novel antimicrobial bicyclic heterocycles from 2-mercapto-3-phenylquinazolin-4(3H)-one. Advanced analytical techniques including 1 H and 13C NMR, elemental analysis, and FT-IR spectroscopy characterized the intricate chemical structures of the products. In vitro assays tested the heterocycles against aerobic and anaerobic bacterial strains using fluconazole and ciprofloxacin as antifungal and antibacterial controls. Results demonstrated the formidable broad-spectrum antibacterial and antifungal activities of the synthesized compounds, with growth inhibition approaching that of the positive controls. These findings highlight the immense potential of these novel heterocyclic compounds as antimicrobial agents. Further research can optimize their drug-like properties for eventual clinical use in combating drug-resistant infections.

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Publication Date
Fri Jun 09 2017
Journal Name
Iraqi National Journal Of Chemistry
Synthesis and Characterization of some New Oxazepine Compounds Derived from D-Erythroascorbic Acid
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This search include the synthesis of some new 1,3-oxazepine derivatives have been prepared, starting from reaction of L-ascorbic acid with dry acetone in presence of dry hydrogen chloride afforded the acetal (I). Treatment of the latter with p-nitrobenzoyl chloride in pyridine yielded the ester (II) which was dissolved in (65%) acetic acid in absolute ethanol yielded the glycol (III). The reaction of the glycol (III) with sodium periodate in distilled water at room temperature produced the aldehyde (IV). The compound (V) [4-(1,3-dioxoisoindolin-2-yl)benzoic acid] was synthesized by reaction p-aminobenzoic acid and phthalic anhydride in presence of (gla. CH3COOH). Reaction of compound (V) with thionyl chloride produced [4-(1,3-dioxoisoindoli

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Publication Date
Fri Nov 01 2024
Journal Name
Current Medicinal Chemistry
Synthesis, In Silico Prediction, and In Vitro Evaluation of Anti-tumor Activities of Novel 4'-Hydroxybiphenyl-4-carboxylic Acid Derivatives as EGFR Allosteric Site Inhibitors
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Introduction:

Allosteric inhibition of EGFR tyrosine kinase (TK) is currently among the most attractive approaches for designing and developing anti-cancer drugs to avoid chemoresistance exhibited by clinically approved ATP-competitive inhibitors. The current work aimed to synthesize new biphenyl-containing derivatives that were predicted to act as EGFR TK allosteric site inhibitors based on molecular docking studies.

Methods:

A new series of 4'-hydroxybiphenyl-4-carboxylic acid derivatives, including hydrazine-1-carbothioamide (S3-S6) and 1,2,4-triazole (S7-S10) derivatives, were synthesized and characterized using IR, 1HNMR, 13CNMR

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Publication Date
Sat Jan 20 2024
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Modification, Characterization of New Thiazolidinone and Oxazolidinone Derived from Levofloxacin and Evaluation of Anti-Oxidant
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The research study included the synthesis of a new series of heterocyclic derivatives containing the antibiotic Levofloxacin. The first way provides for the reaction of  Levofloxacin with thionyl chloride in benzene as a solvent to give an acid chloride derivative. A new class of acid hydrazide synthesized from Levofloxacin was studied. Schiff bases were produced via the reaction of acid hydrazide with substituted aromatic ketones in methanol. The next stage involved the response of Schiff bases with thioglycolic acid and mono chloroacetic acid in DMF to produce derivatives of the antibiotic levofloxacin that have five heterocyclic members, including the derivatives thiazolidine-4-one and oxazolidine-5-one. The FTIR, 1HNMR, a

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Publication Date
Fri Jul 19 2024
Journal Name
Baghdad Science Journal
Synthesis, Characterization, and Thermal Studying of VO(II), Cu(II), Zn (II), Cd(II), and Au (III) Complexes with Azo Dye and Evaluation as Antioxidants
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حضرت معقدات كل من الفنادايل, الخارصين, النحاس والكادميوم بتكافؤهم الثنائي والذهب بتكافؤه الثلاثي بأستخدام صبغة ازوجديدة (6،4،2-ثلاثي هيدروكسي-3-((3-هيدروكسي فنيل) ثنائي زينيل ) فنيل ) ايثان-1-اون المحضرة من ملح الديازونيوم مع ٦,٤,٢- ثلاثي هيدروكسي اسيتوفينون بعد عزل (E)-1-(2,4,6-trihydroxy-3-((3-hydroxyphenyl)diazenyl)phenyl)ethan-1-one تم تشخيصها بواسطة الطرق الطيفية المتاحة  والتقنيات التشخيصية لكل من التحليل الدقيق للعناصرواطياف كل من ال

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Publication Date
Thu Jun 01 2023
Journal Name
Journal Of Population Therapeutics And Clinical Pharmacology
Synthesis, Characterization, Biological and Antioxidant estimation of Mixed Schiff Base Ligand and Heterocyclic Compound with Some Metal ions
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In this research, a group of complexes were prepared which were derived from Schiff base ligands, which is called (1E,1'E)-1,1'-(1,2-phenylene)bis(N-(2,4-dichlorophenyl) methanimine) (L) with ortho-phenanthroline (o-phen).The prepared complexes areM(II) [Co(II),Ni(II),Cu(II), Zn(II), Cd(II),and Hg(II)].A range of spectroscopic and technical techniques have been used to characterizethese materials, including:The FTIR, 1H-NMR, LC-Mass Spectrum, UV-Visbale, molar conductance, and magnaticmoment, atomic absorbtion, chlorid contents. Spectral results obtainedare showen that (ortho-phen) and (L) behave as neutral coordinating to the central metal ion by the donatingatoms(N2)of the both compounds. The geometry sha

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Publication Date
Thu Feb 01 2024
Journal Name
Baghdad Science Journal
Synthesis, Characterisation and Biological Activity of New Co, Ni, Zn and Cd Polymeric Complexes Derived from Dithiocarbamate Ligand
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Synthesis of a new class of Schiff-base ligand with a tetrazole moiety to form polymeric metal complexes with CoII, NiII, ZnII, and CdII ions has been demonstrated. The ligand was synthesised by a multi-steps by treating 5-amino-2-chlorobenzonitrile and cyclohexane -1,3-dione, the 5,5'-(((1E,3E)-cyclohexane-1,3-diylidene)bis(azanylylidene))bis(2-chlorobenzonitrile) was obtained. The precursor (M) was prepared  from the reaction 5,5'-(((1E,3E)-cyclohexane-1,3-diylidene)bis(azanylylidene))bis(2-chlorobenzonitrile) with NaN3 to obtained (1E,3E)-N1,N3-bis(4-chloro-3-(1H-tetrazol-5-yl)phenyl)cyclohexane-1,3-diimine (N). By reacting the precursor (M) with CS2

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Publication Date
Wed Aug 09 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Antimicrobial Evaluation of Some Bis-1, 3, 4-Butane-1-3, 4-Oxadiazole Derivatives
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A series of new Bis-1,4-Butane -1,3,4 – Oxadizole derivatives [III a-j] were synthesized from adipic acid dihydrazide and different aromatic acids in the presence of phosphours oxychloide. There compounds were characterized by their IR, microanalysis, and mass spectral data.    In vitro antimicrobial were synthesized. In vitro antimicrobial activity of these compounds against (Gram negative) and (Gram positive) were reported, some of these compounds prepared derivatives exhibited antimicrobial activity

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Publication Date
Thu Oct 20 2022
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Biological Evaluation and Antioxidant Studies of Nio, Pdo and Pt Nanoparticles Synthesized from a New Schiff Base Complexes
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This research included the preparation of Ni, Pd oxide and Pt metal nanoparticles derived from Schiff base (E)-2-(((2,5-dichlorophenyl)imino)methyl)-4-methyl phenol octahedral from Ni(II) complex and square planar from Pd(II) and Pt(II) complexes using pulsed laser ablation immersed in deionized water. The optical properties of the prepared NiO, PdO, and Pt nanoparticles were investigated using UV-Visible spectra and FTIR spectrophotometer. The shape and structure were analyzed by Transmission Electron Microscope (TEM) and the X-ray Diffraction Instrument XRDBy using the Scherrer equation, the results showed Ni, Pd, and Pt nanos with average particle sizes of 28.53nm, 20.47nm, and 22.30nm. The biological acti

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Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Synthesis and Evaluation of Antimicrobial activity of several new Maleimides to Benzothiazole moiety
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In this work, a series of new maleimides linked to substituted benzothiazole moiety were synthesized. Synthesis of these new cyclic imides were performed via three steps, the first one involved preparation of a series of 2-aminobenzothiazole substituted with different substituents via reaction of different primary aromatic amines with ammonium thiocyanate and bromine in glacial acetic acid. The prepared 2- amino benzothiozoles were introduced in the second step in reaction with maleic anhydride producing a series of N-(substituted benzothiazole-2-yl) maleamic acids.The resulted maleamic acids were dehydrated in the third step via treatment with acetic anhydride and anhydrous sodium acetate to afford a series of the desirable N-(substitu

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Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis of New Nucleoside Analogues From Benzimidazole and Evaluation of Their Antimicrobial Activity
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Our goal in this research, some new nucleoside analogues was synthesized. Starting from ?-D glucose which was converted to per acetylated ?-D gluco pyronoside then converted to active from(1-Bromo Sugar (2) as a sugar moiety.The base moiety 2-substituted benzimidazole was prepared from condensation of phenylene diamine with different aromatic aldehydes, which were subjected to amino alkylation via Mannich reaction forming new nucleobase derivatives. Condensation of nucleobase with bromo sugar through nucleophilic substitution of anomeric carbon with nitrogen forming new protected nucleoside analogues then hydrolyzed with sodium methoxide in methanol to obtain our target, the free nucleoside analogues. All prepared compound were identified b

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