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Design, Synthesis, and Docking Study of Acyl Thiourea Derivatives as Possible Histone Deacetylase Inhibitors with a Novel Zinc Binding Group
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Histone deacetylase inhibitors with zinc binding groups often exhibit drawbacks like non-selectivity or toxic effects. Thus, there are continuous efforts to modify the currently available inhibitors or to discover new derivatives to overcome these problems. One approach is to synthesize new compounds with novel zinc binding groups. The present study describes the utilization of acyl thiourea functionality, known to possess the ability to complex with metals, to be a novel zinc binding group incorporated into the designed histone deacetylase inhibitors. N-adipoyl monoanilide thiourea (4) and N-pimeloyl monoanilide thiourea (5) have been synthesized and characterized successfully. They showed inhibition of growth of human colon adenocarcinoma and mouse hepatoblastoma cells with low cytotoxic effect against normal human breast cells. Their binding mode to the active site of several histone deacetylases has been studied by docking and the results gave a preliminary indication that they could be successful histone deacetylase inhibitors.

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Publication Date
Sun Dec 02 2012
Journal Name
Baghdad Science Journal
Synthesis and Characterization of Derivatives Based on 4, - Dimercaptobiphenyl
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Starting from 4, - Dimercaptobiphenyl, a variety of phenolic Schiff bases (methylolic, etheric, epoxy) derivatives have been synthesized. All proposed structure were supported by FTIR, 1H-NMR, 13C-NMR Elemental analysis all analysis were performed in center of consultation in Jordan Universty.

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Publication Date
Sun Dec 04 2016
Journal Name
Baghdad Science Journal
Synthesis and Characterization of New 2-Quinolone Sulfonamide Derivatives
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A series of new 2-quinolone derivatives linked to benzene sulphonyl moieties were performed by many steps: the first step involved preparation of different coumarins (A1,A2) by condensation of different substituted phenols with ethyl acetoacetate. The compound A1 was treated with nitric acid to afford two isomers of nitrocoumarin derivatives (A3) and (A4). The prepared compounds (A2, A3) were treated with hydrazine hydrate to synthesize different 2-quinolone compounds (A5,A6) while the coumarin treated with different amines gave compounds (A7,A8). Then the synthesized 2-quinolone compounds (A5-A8) treated with benzene sulphonyl chloride to afford new sulfonamide derivatives (A9-A12). The synthesized compounds were characterized by FT-IR, 1H

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Publication Date
Sat Dec 24 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Antimicrobial Activity of Nitrogen-Containing Anthraquinone Derivatives
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New substituted anthraquinones with amino derivations fragments were synthesized through the substitution of bromine atom by different amines using the Ullmann coupling reaction. Obtained compounds based on anthraquinone used for experimental antimicrobial studies. The structure of the synthesized compounds was confirmed by LC-MS and 1H, 13C NMR spectroscopy. Studies on planktonic microorganisms have shown that the first synthesized anthraquinone derivatives have an inhibitory effect against bacteria and fungi. The triazene 1-(3-(benzoic acid(triaz-1-en-1-ol(-4-(1H-imidazol-1-yl(-9,10-dioxo-9,10-dihydroanthracene -2-sulfonic acid, have wide spectrum of activity, growth retardation zones against gram-positive micro

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Publication Date
Sat Jun 19 2021
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization and Antibacterial Evaluation of Some Coumarin Derivatives
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Coumarin derivatives have shown different biological activities, such as antifungal, antibacterial   antiinflammatory, and antioxidant activities, besides antibiotic resistance modulating effects, and anti-HIV, hepatoprotective, and antitumor effect. So, new coumarin derivatives (hydrazones and an amide) were synthesized through multisteps reactions. All the synthesized target compounds were characterized by FT-IR spectroscopy, 1HNMR analysis. The compounds then evaluated for their anti-bacterial activity by means of well-diffusion method against two gram-positive bacteria (Staphylococcus aureus, Streptococcus pneumoniae) and two gram-negative bacteria  (E.coli and Pseudomonas aeruginosa). The highest activity was demonstr

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Publication Date
Mon Jul 01 2019
Journal Name
J. Pharm. Sci. & Res.
Methods of Synthesis Phthalimide Derivatives and Biological Activity-Review
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Phthalimide formation of Phthalic anhydride with various amines using microwave or without a method with the difference of the catalyst used in a prepared Phthalimide, either structure general are C6H4CONRCO and used as starting materials in synthesis several compounds derivative phthalimides are an important compounds because spectrum wide biological activities including Antimicrobial activity, anticonvulsant activity, Anti-inflammatory activity,Analgesic activity, Anti- influenza activity and Thromboxane inhibitory activity

Publication Date
Thu Oct 03 2024
Journal Name
Applied Organometallic Chemistry
Synthesis, Characterization, Molecular Docking, Cytotoxicity, and Antimicrobial Activity of Schiff Base Ligand and Its Metal Complexes
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ABSTRACT<p>A Schiff base ligand (L) was synthesized via condensation of <italic>N</italic>‐(1‐naphthyl)ethylenediamine dihydrochloride with phthalaldehyde. The ligand was characterized by FT‐IR, UV–Vis, <sup>1</sup>H NMR, mass spectrometry, and elemental analysis (C, H, N). Five metal complexes (Co(II), Ni(II), Cu(II), Zn(II), and Cd(II)) were prepared with the ligand in a 1:1 (M:L) ratio using an aqueous ethanol solution. The complexes were characterized by FT‐IR, UV–Vis, mass spectrometry, and elemental analysis (C, H, N). Additionally, <sup>1</sup>H NMR spectroscopy was employed for Cd(II) complex. Antimicrobial activity of the ligand and its metal complexes against </p> ... Show More
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Publication Date
Thu Apr 01 2021
Journal Name
Journal Of Molecular Structure
Mixed-ligand complexes of ampicillin derived Schiff base ligand and Nicotinamide: Synthesis, physico-chemical studies, DFT calculation, antibacterial study and molecular docking analysis
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A novel series of mixed-ligand complexes of the type, [ML1(L2)3]Clx [M= Cr(III), Fe(III), Co(II),Ni(II), Cu(II), Cd(II) and Hg(II), n = 2, 3], was synthesized using Schiff base (HL1) as main ligand, nicotinamide (L2) as secondary ligand, and the corresponding metal ions in 1:3:1 molar ratio. The main ligand, HL1 was prepared by the interaction of ampicillin drug and 4-chlorobenzophenone. The synthesized mixed ligand complexes were characterized by elemental analysis, UV-Vis, FT-IR,1H-NMR,13C-NMR and TG/DTG studies. In the mixed-ligand complexes, the Schiff base ligand, HL1 showed coordination to the central metal ion in tridentate manner via azomethine nitrogen, β-lactam ring oxygen and deprotonated carboxylic oxygen atoms, whereas the sec

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Publication Date
Sun Apr 02 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Conjugation of Steroidal and Non – Steroidal Anti- Inflammatory Drugs as Possible Mutual Prodrug
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Prednisolone (SAID) was conjugated with ibuprofen (NSAID) through an amino acid (glycine) as a spacer arm to synthesize the following compound:

Prednisolone – glycine – ibuprofen.

    The method employed consists of converting the carboxylic acid function of (R,S) – ibuprofen – glycine to the highly reactive acid chloride and subsequent reaction with the C21 hydroxyl group of prednisolone. This reactive intermediate was found to react as well with the C17 tertiary hydroxyl group of the steroid to form three compounds and eight diastereomers. These results were confirmed by T.L.C, and the desired compound was separated by column chromatograph

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Publication Date
Sat Jan 01 2011
Journal Name
Iraqi Journal Of Physics
Characteristics of Zinc Oxide Film Prepared by Chemical Spray Deposition as a Gas Sensor
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Zinc oxide thin films were deposited by chemical spray pyrolysis onto glass substrates which are held at a temperature of 673 K. Some structural, electrical, optical and gas sensing properties of films were studied. The resistance of ZnO thin film exhibits a change of magnitude as the ambient gas is cycled from air to oxygen and nitrogen dioxide

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Publication Date
Tue Jan 06 2009
Journal Name
مجلة ديالى للعلوم الانسانية
Synthesis and Characterization of Novel Bidentate Ligand type NO and Its Complexes with (CoII , NiII ,CuII and ZnII)
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The [2-aminobenzothiazole]was reacted with [2,4,6 triyhydroxy-acetophenon monohydrate] to give a new ligand [2-N-2,4,6-trihydroxyacetophenonyliden benzothiazole] [H3L]. This ligand was reacted with metal ions ( CoII, NiII,CuII and ZnII) in methanol as solvent with ( 1:2 ) metal : ligand ratio to give a series of new complexes with general formula [ M(H2L)2],(where:M= CoII, NiII ,CuIIand, ZnII).All compounds were characterized by spectroscopic methods ( I.R , U.V – vis,HPLC) atomic absorption, along with chloride content and conductivity measurements. According to the data of these measurements we suggested a tetrahedral