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Synthesis and Preliminary Pharmacological Study of Sulfonamide Conjugates with Ibuprofen and Indomethacin as New Anti-Inflammatory Agents
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          4-aminobenzenesulfonamide conjugates of ibuprofen (compound 10) and indomethacin (compound 11) have been designed and synthesized by the reaction of sulfanilamide (compound 7) with 2-(4-isobutylphenyl) propanoic acid (ibuprofen) and 2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)acetic acid (indomethacin) for the evaluation as potential anti-inflammatory agents with expected selectivity against COX-2 enzyme. In vivo acute anti-inflammatory activity of the synthesized final compounds (10 and 11) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (10mg/Kg) of ibuprofen and (2mg/kg) of indomethacin. The tested compounds produced significant reduction of the rat paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, compound (10) exhibited comparable anti-inflammatory activity to diclofenac (3mg/Kg) (reference group) while compound (11) exhibited less anti-inflammatory activity than diclofenac. The result of this study indicate that the incorporation of the 4-aminobenzenesulfonamide pharmacophore into ibuprofen and indomethacin maintained their anti-inflammatory activity & may increase their selectivity toward COX-2 enzyme which can be confirmed in future by assessing COX-2:COX-1 inhibitory ratio.

Key words: Cyclooxygenase; Anti-inflammatory activity; Ibuprofen; indomethacin; NSAIDs.

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Publication Date
Sat Jun 01 2024
Journal Name
Russian Journal Of Bioorganic Chemistry
Synthesis and Study the Biological Activity of Some New Pyrazole Compounds Containing 1,3,4-Oxadiazole Unite Through Vilsmeier–Haack Reaction
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Publication Date
Fri Dec 01 2023
Journal Name
Iraqi Journal Of Physics
Eco-Friendly Synthesis of Ag-ZnO Nanocomposite Using Aloe-vera, Hibiscus Sabdariffa Plants and Their Antibacterial and Anti-fungi Activities
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The current study used extracts from the aloe vera (AV) plant and the hibiscus sabdariffa flower to make Ag-ZnO nanoparticles (NPs) and Ag-ZnO nanocomposites (NCs). Ag/ZnO NCs were compared to Ag NPs and ZnO NPs. They exhibited unique properties against bacteria and fungi that aren't present in either of the individual parts. The Ag-ZnO NCs from AV showed the best performance against E. coli, with an inhibition zone of up to 27 mm, compared to the other samples. The maximum absorbance peaks were observed at 431 nm and 410 nm for Ag NPs, at 374 nm and 377 nm for ZnO NPs and at 384 nm and 391 nm for Ag-ZnO NCs using AV leaf extract and hibiscus sabdariffa flower extract, respectively. Using field emission-scanning electron microscopes (FE-

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Publication Date
Fri Dec 31 2021
Journal Name
Iraqi Journal Of Market Research And Consumer Protection
SYNTHESIS AND CHARACTERIZATION OF NEW β-LACTAM DERIVATVE FROM SULFADIAZINE DRUG BY MANY STEPS: SYNTHESIS AND CHARACTERIZATION OF NEW β-LACTAM DERIVATVE FROM SULFADIAZINE DRUG BY MANY STEPS
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This research involved synthesis of new β-Lactam derivative from Azo compound[4-amino-N-(pyrimidine-2-yl)-3-(pyrimidine-2-yldiazenyl) benzene sulfonamide] (S1) record previously by many steps. Starting conversion the free amino group in an azo comp. to chloro acetamide derivative(S2), then reacted it with urea to give the oxazole ring  derivative (S3) that which containing free amino group. The condensation reaction between the amino group and P-bromobenzaldehyde to produce Shiff base (B14). Finally staudinger's cyclo addition reaction go run between the Shiff base derivative (B14) and chloro acetyl chloride in the presence of tri ethyl amine (Et3N) as Base catalyst and dioxane a

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Publication Date
Sat Apr 23 2022
Journal Name
Research Journal Of Pharmacy And Technology
Synthesis, and Antimicrobial Evaluation of New hydrazone Derivatives of (2,4-dinitrophenyl) hydrazine
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In this work, novel compounds of hydrazones derived from (2,4-dinitrophenyl) hydrazine were synthesized. Benzamides derivatives and sulfonamides derivatives were prepared from p-amino benzaldehyde. Then these compounds were condensed with (2,4-dinitrophenyl) hydrazine through Imine bond formation to give hydrazones compounds. The compounds were characterized using FT-IR (IR Affinity-1) spectrometer, and 1HNMR analyses. The majority of the compounds have a moderate antimicrobial activity against “Gram-positive bacteria staphylococcus Aureus, and staphylococcus epidermidis, Gram-negative bacteria Escherichia coli, and Klebsiella pneumoniae, and fungi species Candida albicans” using concentrations of 250 µg\ml.

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Publication Date
Tue Mar 28 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Antimicrobial Evaluation of New 6 and7 Substituted Derivatives of Coumarin
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A series of benzohydrazide derivatives attached to coumarin moiety at position 6 and 7 have been synthesized. The reaction of coumarin derivatives (coumarin I and II) with p-nitrophenyl hydrazine yield Schiff bases (compound1a and IIa).These Schiff bases were refluxed with benzoyl chloride to give benzohydrazide derivatives of coumarin substituted at its 6 or 7 nucleus position (Ia1 and IIa1).The reaction and the purity of the products were checked by thin layer chromatography (TLC). The structures of the final compounds  and  their intermediates were confirmed by their melting points, infra red spectroscopy, and elemental microanalysis(CHN).

Compounds (Ia1 and IIa1) were evaluated for&n

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Publication Date
Mon Mar 27 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis of New Cephalosporins of Expected Improved Activity and Resistance Against -Lactamases
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The development of new cephalosporins with improved activity against resistant microbes, such as, MRSA (methicillin resistant Staph. aureus), P. aeruginosa, is of high potential. Chemical synthesis of two new series of thiadiazole linked to cysteine (series 1) and cephalosporins containing thiadiazole linked to cysteine through disulfide bond (series 2) were achieved. The chemical structures of the synthesized compounds were confirmed using spectral (FT-IR, 1H-NMR) and elemental microanalysis. The incorporation of privileged chemical moieties, such as, thiadiazole, Schiff base, cysteine and sulfonamide, has been found to have great contribution to the antimicrobial activities. Compounds of series 1 (1

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Publication Date
Tue Jan 15 2008
Journal Name
Journal Of Kerbala University
Synthesis and Characterization of New Ligand type N2O2 and its complexes with (Co(II),Ni(II),Cu(II),Zn(II) and Cd(II) ions
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The [2-hydroxy-1, 2-diphynel-ethanone oxime] was reacted with 1, 2-dichloroethan to give the new ligand [H2L]. this ligand was reacted with some metal ions (Co (II), Ni (II), Cu (II), Zn (II) and Cd (II) in methanol as a solvent to give a series of new (1: 1) complexes of the general formula [M (HL)] Cl,(where: M= Co (II), Ni (II), Cu (II), Zn (II) and Cd (II)) are isolated All compounds have been characterized by spectroscopic methods [IR, UV-Vis] atomic absorption. Chloride content along with conductivity measurements. From the above data the proposed molecular structure for (Co, Cu, Ni, Zn and Cd) complexes adopting a tetrahedral structure

Publication Date
Wed May 07 2008
Journal Name
Journal Of Kerbala University
Synthesis and Characterization of New Ligand type N2O2 and its complexes with (Co(II),Ni(II),Cu(II),Zn(II) and Cd(II) ions
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The [2-hydroxy -1,2-diphynel-ethanone oxime] was reacted with 1,2- dichloroethan to give the new ligand [H2L].this ligand was reacted with some metal ions (Co(II),Ni(II),Cu(II),Zn(II) and Cd(II) in methanol as a solvent to give a series of new (1:1)complexes of the general formula [ M(HL)]Cl ,( where : M= Co(II),Ni(II),Cu(II),Zn(II) and Cd(II)) are isolated All compounds have been characterized by spectroscopic methods [ I.R , U.V -Vis ] atomic absorption . Chloride content along with conductivity measurements. From the above data the proposed molecular structure for (Co, Cu, Ni, Zn and Cd) complexes adopting a tetrahedral structure.

Publication Date
Sun Jul 02 2023
Journal Name
Nanomedicine Research Journal
Gold and Silver Nanoparticles with Modified Chitosan /PVA : Synthesis, Study The Toxicity and Anticancer Activity
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The new novel polymers nanocomposites based modified chitosan (CS) blending with polyvinyl alcohol (PVA) and coated gold or silver nanoparticles (AuNPs), AgNPs) were synthesized from many sequence reactions as presented in (Scheme1, 2 and 3). By utilizing 1H-NMR spectroscopy, FTIR, and Field Emission Scanning electron microscope , the synthesized compounds have been identified. Molecular docking is studied, where operations are used to predict the binding status of compounds with the enzyme and to calculate the free energy (ΔG) of the compounds prepared. Also, the antibacterial activity regarding the synthesized compounds against two resistant pathogenic bacteria (G+) S. aureus and E. coli (G-) was examined in vitro compare with standard a

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Publication Date
Thu Dec 01 2022
Journal Name
Baghdad Science Journal
Simultaneous Ratio Derivative Spectrophotometric Determination of Paracetamol, Caffeine and Ibuprofen in Their Ternary Form
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A new, accurate, precise and economic two spectrophotometric methods for determination of Paracetamol (Par), Ibuprofen (Ibu), and Caffeine (Caf) were suggested. Those methods were the first and second ratio derivative spectrum using a double devisor. Par, Ibu, and Caf showed many useful peaks for their quantified determination. The validity of all analysis modes for determination of the three compounds, peak to baseline, peak area and peak to peak were according to ICH. The linearity of two methods was between 5 µg/ml as a lower concentration and 50 µg/ml as the highest concentration for three compounds. Recovery percentage was around 100% and relative standard deviation was less than 2.6%. The methods were applied successfully in the

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