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Design and Synthesis of New Non-Steroidal Anti-inflammatory Agents with Expected Selectivity toward Cyclooxygenase-2 Inhibition
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This study includes design and synthesis of new non-steroidal anti-inflammatory agents (NSAIDs) with expected cyclooxygenase-2 (COX-2) selective inhibition to achieve better activity and low gastric side effects. Two series of compounds have been designed and synthesized as potential NSAIDs,these  are:     Salicylamide derivatives (compounds 3,4,5 ) and Diflunisal derivatives (compounds 10&11). In vivo acute anti-inflammatory effect of one of the synthesized agents (compound 3)  was evaluated in the rat using egg-white induced paw edema model of inflammation. Preliminary pharmacological study revealed that compound 3 exhibited less anti-inflammatory effect  compared to that of aspirin after 120 and 210 minutes, which encourage the continuation of the search to demonstrate or identify the preliminary pharmacological activity for the  synthesized compounds and to identify their selectivity toward COX-2 isoenzymes.

Keywords:nonsteriodal anti-inflammatory drugs(NSAID),aspirin derivatives ,diflunisal, Cyclooxygenase -1(cox-1),cyclooxygenase-2(cox-2)

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Publication Date
Sun Mar 06 2016
Journal Name
Baghdad Science Journal
Isolation and Purification of a Cyclooxygenase-2 from the Blood of a Patient Suffering from Rheumatoid Arthritis and Studying the Effect of Natural Products of the Soapwort on the Activity of Purified Enzyme
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In this paper to isolate and study the properties of the cyclooxygenase-2 (EC: 1.14.99.1) enzyme in the blood of a patient suffering from rheumatoid arthritis and study the effect of natural products of the Soapwort on the activity of purified enzyme. The study involves taking 30 ml of blood from an adult woman 40 years old, who suffers from rheumatoid arthritis disease for 13 years. Serum is separated and subjected to a series of purification processes including: precipitation by ammonium sulfate, filtration by centrifugation radiator, dialysis in presence of ammonium bicarbonate, separation using the technology of ion exchange, lipholization and then estimating approximate molecular weight of the enzyme using gel filtration techni

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Publication Date
Thu Sep 10 2026
Journal Name
Iraqi Journal Of Science
Synthesis, Characterization and Quantum Mechanical Study of Some New 2-benzylidenehydrazinecarbothioamide Derivatives as Corrosion Inhibitors for Carbon/mild Steel in Acidic Medium.
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In this work, some of new 2-benzylidenehydrazinecarbothioamide derivatives have been prepared by condensation of thiosemicarbazide and different substituted aromatic benzaldehydes in presence of glacial acetic acid to give compounds (1-6), these compounds have characterized by its physical properties and spectroscopic methods. This work also included theoretical study to prove the ability of these compounds as corrosion inhibitors; The program package of Gaussian 09W with its graphical user interface GaussView 5.0 had used for this purpose; the methods of Density Functional Theory (DFT) with basis set of 6-311G (d,p) / hybrid function of B3LYP and semiempirical method of PM3 have been used, the study included theoretical simulation

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Publication Date
Sun Dec 06 2015
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Antibacterial of 2,3-Dihydrobenzo Thiazole-2-Carboxylic Acid Complexes with Some Selected Metal Ions
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A new ligand 2,3-dihydrobenzo [d] thiazole-2-carboxylic acid (L) has been prepared from the reaction of ortho amino phenyl thiol with dichloroacetic acid in mole ratio (1:1). It has been characterized by elemental analysis (C.H.N.), IR, UV- Vis.spectraand 1H, 13C-NMR. A new series complexes of the bivalent ions (Co, Ni, Cu, Pd, Cd, Hg and Pb) and the trivalent (Cr) have been prepared and characterized too. The structural has been established by elemental analysis (C.H.N.), IR, UV-Vis. spectra, molar conductivity, atomic absorption and magnetic susceptibility measurements. The synthesized complexes were prepared in (1:2) ratio correspond to (Co(II), Ni(II), Cu(II), Pd(II), Cd(II), Hg(II) and Pb(II) complexes while in case Cr(III) complex is

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Publication Date
Tue Jul 31 2012
Journal Name
Journal Of The College Of Education - University Of Tikrit
Synthesis, Spectroscopic and Biological Studies of some Metal Complexes with 1-phenyl-2(1-phenyl ethylidene) hydrozine.
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Publication Date
Thu Aug 15 2019
Journal Name
Journal Of Global Pharma Technology
Synthesis, Characterization and Study of the Biological Activity of New Metal Complexes of Ligand[2-(3-benzoylthioureido)-3-(-4- hydroxyphenyl) Propanoic Acid (BHP)
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In this paper, series of new complexes of Manganese(II), Cobalt(II), Nickel (II) Cupper(II) Zinc(II), Cadmium(II) and Mercury (II) are prepared from the new ligand [2-(3-benzoylthioureido)-3-(-4- hydroxyphenyl) propanoic acid (BHP) derived from tyrosine and benzoylisothiocyanate .Chemical structures are obtained from their 1 H, 13CNMR spectra (for BHP), elemental microanalyses, molar conductance, FTIR, UV–Vis, magnetic susceptibility in addition to TGA/DTG and DSC analysis, the suggested geometry for all complexes was tetrahedral. The biological activity of BHP and its complexes has been extensively studied against two bacterial species Staphylococcus aurous (G+) and Escherichia coli (G-) by agar-well diffusion technique, where Mn(II), Co

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Publication Date
Tue Mar 12 2024
Journal Name
Biomolecules
Limonene Exerts Anti-Inflammatory Effect on LPS-Induced Jejunal Injury in Mice by Inhibiting NF-κB/AP-1 Pathway
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The human gastrointestinal system is a complex ecosystem crucial for well-being. During sepsis-induced gut injury, the integrity of the intestinal barrier can be compromised. Lipopolysaccharide (LPS), an endotoxin from Gram-negative bacteria, disrupts the intestinal barrier, contributing to inflammation and various dysfunctions. The current study explores the protective effects of limonene, a natural compound with diverse biological properties, against LPS-induced jejunal injury in mice. Oral administration of limonene at dosages of 100 and 200 mg/kg was used in the LPS mouse model. The Murine Sepsis Score (MSS) was utilized to evaluate the severity of sepsis, while serum levels of urea and creatinine served as indicators of renal f

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Publication Date
Fri Jun 16 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Carvone exerts lung anti-inflammatory effect through hampering NF-KB pathway in lipopolysaccharide-induced acute lung injury in mice
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                Background: Acute lung injury (ALI) is among the most serious conditions characterized by an exacerbation of inflammatory response that can result from a persistent lung infection. Carvone is chiral monoterpenoid ketone present in the essential oils of dill, caraway, and spearmint. It shows antioxidant, anti-inflammatory, and antimicrobial effects among others. In this study, the lung anti-inflammatory and protective effects and potential mechanism of action of carvone were investigated in ALI induced by Lipopolysaccharide (LPS).

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Publication Date
Mon Oct 10 2022
Journal Name
Research Journal Of Chemistry And Environment
Synthesis, Antioxidant ability and Docking study for new 4,4'-((2-(Aryl)-1H-benzo[d]imidazole-1,3(2H)- diyl)bis(methylene))diphenol)
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New series of 4,4'-((2-(Aryl)-1H-benzo[d]imidazole1,3(2H)-diyl)bis(methylene))Diphenol(3a-g) was successfully synthesized from cyclization of the reduction product of bis Schiff bases (2) with aryl aldehydes bearing phenolic hydroxyl in the presence of acetic acid. The structure of these compounds was identified from FT-IR, 1H NMR, 13C NMR and EIMs. The Antioxidant capability was screened by DPPH and FRAP assays. Both assays showed antioxidant capability more than BHT as well. Compounds 3b and 3c showed antioxidant capacity slightly less than ascorbic acid. The docking study for theses compound was carried out as III DNA polymerase inhibitor. The results of docking demonstrated that the increase in hinderances around phenolic hydroxyl for t

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Publication Date
Sun Sep 25 2022
Journal Name
Research Journal Of Chemistry And Environment
Synthesis, Antioxidant ability and Docking study for new 4,4'-((2-(Aryl)-1H-benzo[d]imidazole-1,3(2H)-diyl)bis(methylene))diphenol)
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New series of 4,4'-((2-(Aryl)-1H-benzo[d]imidazole-1,3(2H)-diyl)bis(methylene))Diphenol(3a-g) was successfully synthesized from cyclization of the reduction product of bis Schiff bases (2) with aryl aldehydes bearing phenolic hydroxyl in the presence of acetic acid. The structure of these compounds was identified from FT-IR, 1H NMR, 13C NMR and EIMs. The Antioxidant capability was screened by DPPH and FRAP assays. Both assays showed antioxidant capability more than BHT as well. Compounds 3b and 3c showed antioxidant capacity slightly less than ascorbic acid. The docking study for theses compound was carried out as III DNA polymerase inhibitor. The results of docking demonstrated that the increase in hinderances around phenolic hydr

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Publication Date
Sun Dec 01 2024
Journal Name
Russian Journal Of General Chemistry
Synthesis, Characterization, and Biological Evaluation for New Derivatives Based on 2Сhloro-N-[4-(5-phenyl-1,3,4-oxadiazol-2-yl)phenyl]acetamide
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