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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
Fri Jul 01 2016
Journal Name
Tetrahedron
Novel bent-core mesogenic of 4-amino-triazole derivatives: synthesis, characterization and liquid crystalline study
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Publication Date
Sat May 30 2020
Journal Name
Neuroquantology
Synthesis and Study NiO Charactrization of Extract from Green Tea Plant Prepared by Chemical Method
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Publication Date
Thu Jan 23 2014
Journal Name
مجلة إبن الھيثم للعلوم الصرفة و التطبيقية
Synthesis of Tetra Dentate N2O2 and their Complexes With Cu[II), Zn[II), Cd[II) and Hg[II) Ions
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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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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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Publication Date
Mon Mar 13 2017
Journal Name
Journal Of Baghdad College Of Dentistry
Effect of Different Fluoride Agents on the Load Deflection Characteristics of Heat Activated Nickel Titanium Arch Wires (An in Vitro Study)
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ABSTRACT Background:Hydrogen absorption and related degradation in the mechanical properties of Ni-Ti based orthodontic wires has been demonstrated following exposure to fluoride prophylactic agents. This study was designed to investigate the effects of three fluoride containing agents on the load deflection characteristics of heat activated nickel titanium arch wires during unloading phase. Material and method: Eighty specimens of heat activated nickel titanium arch wires were obtained from Ortho Technology Company, half of which had a 0.016 inch round and 0.019x0.025 rectangular. Ten specimens from both wire size were immersed in one of the tested fluoride prophylactic agents (neutral sodium fluoride gel, stannous fluoride gel or phos-flu

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Publication Date
Mon Mar 13 2017
Journal Name
Journal Of Baghdad College Of Dentistry
The Effects of Enamel Protective Agents on Shear Bond Strength After Rebonding of Stainless Steel Orthodontic Bracket (An in Vitro Study)
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ABSTRACT Background: Bracket rebonding is a common problem in orthodontics which may result in many drawbacks. The aims of this study were to evaluate the effects of application of two enamel protective agents “Icon” and “ProSeal” on shear bond strength before and after rebonding of stainless steel orthodontic brackets using conventional orthodontic adhesive and to assess the site of bond failure. Materials and methods: Fifty sound extracted human upper first premolar teeth were selected and randomly divided into two equal groups; the first time bonding and the rebonding groups (n=30). Each group was subdivided into control, Icon and ProSeal subgroups. The enamel protective agents were applied after etching (precondi

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Publication Date
Fri Dec 01 2023
Journal Name
Baghdad Science Journal
Ni2+, Pt4+, Pd2+, and Mn2+ Metal ions Complexes with Azo Derived from Quinolin-2-ol and 3-amino-N-(5-methylisoxazol-3-yl) Benzenesulfonamide: Synthesis, Characterization, Thermal Study ,and Antioxidant Activity
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Diazotization reaction between quinolin-2-ol and (2-chloro-1-(4-(N-(5-methylisoxazol-3-yl)sulfamoyl)phenyl)-2l4-diazyn-1-ium was carried out resulting in ligand-HL, this in turn reacted with the next metal ions (Ni2+, Pt4+, Pd2+, and Mn2+)  forming stable complexes with unique geometries such as (tetrahedral for both Ni2+ and Mn2+, octahedral for Pt4+ and square planer for Pd2+ ). The creation of such complexes was detected by employing spectroscopic means involving ultraviolet-visible which proved the obtained geometries, fourier transfer proved the formation of azo group and the coordination with metal ion through it. Pyrolysis (TGA &

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Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Preparation, characterization and study of biological activity and laser effect on the new Cu(II) complexes containing mixed benziloxime and furfuraldehydeazine ligands
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Abstract: New copper(II) complexes with mixed ligand benziloxime (BOxH) and furfural-dehydeazine (FA) using classical (with and without solvent) and microwave heating methods have been prepared. The resulting complexes have been characterized using physico-chemical techniques. The study suggested that the ligands formed neutral complexes had general formulas [Cu(FA)(BOXH)(Ac)2] and [Cu(FA)(BOX)(OH)] in neutral (or acidic) and basic medium, respectively. Accordingly, hexa-coordinated mono-nuclear complexes have been investigated by this study and having distorted octahedral geometry. The effect of laser have been studied on solid ligands and solid complexes, no effect have been observed on most compounds through the results of melting poin

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Publication Date
Sat Aug 03 2013
Journal Name
European Journal Of Scientific Research
Serum Levels of Anti Intrinsic Factor Antibodies and α1- Antitrypsin in Alcohol-Dependent Males
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Excess alcohol consumption is associated with numerous metabolic changes and homeostasis disturbances of many macro- and micro-elements in the body. It has been associated with multiple pathologies at all levels. In the digestive apparatus, alcohol has generally been related to its toxic effects upon the liver. Alpha-1 antitrypsin (α-1 AT or AAT) plays an important role in controlling inflammation, coagulation and repair mechanisms in the body and most α-1 AT in the body is produced by the liver; from the other hand, Intrinsic factor (IF), which is a glycoprotein produced by the parietal cells of the stomach is necessary for the absorption of vitamin B12 in the small intestine. This study was designed to assess serum levels of α-1 AT and

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