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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 Jan 01 2021
Journal Name
Biochem. Cell. Arch.
SYNTHESIS AND CHARACTERIZATION OF SOME NEW METALS COMPLEXES OF 2-(3-ACETYLTHIOUREIDO)-3-PHENYLPROPANOIC ACID (APA)
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ABSTRACT : A new ligand [ 2- (3-acetylthioureido)-3-phenylpropanoic acid (APA) is synthesized by reaction of acetyl isothiocyanate with phenylalanine (1:1). It is characterized by micro elemental analysis (C.H.N.S.), FT-IR, (UV-Vis) and 1H and 13CNMR spectra. Some metals ions complexes of this ligand were prepared and characterized by FT-IR, UV-Visible spectra, conductivity measurements, magnetic susceptibility and atomic absorption. From results obtained, the following formula [M(APA)2] where M2+ = Mn, Co, Ni, Cu, Zn, Cd and Hg, the proposed molecular structure for these complexes as tetrahedral geometry, except copper complex is has square planer geometry.

Publication Date
Thu Sep 26 2013
Journal Name
Chemistry: The Key To Our Sustainable Future
Synthesis and Characterization of Some New Metal Complexes of Condensation Reaction Products of 3-Amino-1,2,4-Triazole with Isatin, N-Acetylisatin and Bis (2,3-Dioxoindolin-1-yl)Mercury(II)
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Publication Date
Sun Oct 09 2022
Journal Name
Chemical Methodologies
Synthesis, Characterization and Thermal Analysis of Cr(III), Mn(II) and Zn(II)Complexes of a New Acidicazo Ligand
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The researchers wanted to make a novel azo imidazole as a follow-up to their previous work. We focused on the ligand 4-[(2-amino-4-phenylazo)- methyl]-cyclohexane carboxylic acid as a derivative of trans-4- (aminomethyl) cyclohexane carboxylic acid diazonium salt, synthesized a series of its chelate complexes with metal ions, and characterized these compounds using a variety techniques, including elemental analysis, FTIR, LC-Mass, NMR and UV-Vis spectral process as well TGA, conductivity and magnetic quantifications. Analytical data showed that the Cr(III), Mn(II) and Zn(II) complexes out to 1:1 metal-ligand ratio with octahedral geometry except Mn complex has tetrahedral geometry.

Publication Date
Wed Apr 12 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
Synthesis and Characterization New Schiff Bases, Pyrazole and Pyrazoline Compounds Derived From Acid Hydrazide Containing Isoxazoline Ring
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The work involves synthesis of new Schiff bases ([V] a, b and [VI] a, b), pyrazoles [VII] a, b and pyrazolines [VIII] a, b derivatives containing isoxazoline unit starting with chalcones. 4-bromoacetophenone was reacted with 4-hydroxybenzaldehyde or 4-hydroxyacetophenone was reacted with 4-bromobenzaldehyde in basic medium to give chalcone by Claisen-Schemidt reaction. The chalcons [I] a, b was reacted with hydroxylamine hydrochloride to form isoxazolines [II] a, b. which were reacted with ethyl chloro acetate in basic medium to get ester compounds [III] a, b. The condensation new ester [III] a, b with hydrazine hydrate80% yieldedacid hydrazide [IV] a, b. The later compound refluxing with 4-substituted benzaldehyde in dry benzene to give Sc

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Publication Date
Sat Apr 20 2024
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis, Characterization and Determination Antioxidant Activities for New Azo Dyederived from Sulfamethoxazole and Some Metal Ion Complexes
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Diazotization reaction between 1-(2,4,6-trihydroxy-phenyl)-ethanone and diazonium salts produced the ligand 4-(3-Acetyl-2,4,6-trihydroxy-phenylazo)-N-(5-methyl-isoxazol-3-yl)- benzenesulfonamide, which in turn reacted with the metal ions (Ni2+, Zn2+, Pd2+ and Pt4+) forming stable complexes with Octahedral geometry suggest of (Ni2+ and Pt4+), Zn2+ complex Tetrahedral and Pd2+ complex Square planer. The creation of such complexes was detected by employing spectroscopic means involving ultraviolet-visible, which proved the obtained geometries; FT-IR confirmed the formation of the azo group and the coordination with metal ions through it. Thermogravimetric analysis studies demonstrated the coordination of water residues (aqua or hydrate) with m

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Publication Date
Wed Mar 10 2021
Journal Name
Baghdad Science Journal
synthesis and study of some mixed ligand complexes of caffeine
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I've been in this research preparation and diagnostic complexes mixed Kandat of Alcavaúan Alpiculan ion Althaaossianat with some metal ions has been reactive in ethanol solvent and distilled water by (1:1) and water complexes and lotions to the accounts of the metal in the complex

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Publication Date
Thu Dec 30 2021
Journal Name
Al-kindy College Medical Journal
Inflammatory Odontogenic Cysts
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 Cystic conditions of the jaw cause bony destruction and may cause resorption or displacement of adjacent teeth. Odontogenic cysts have developmental or inflammatory origins. To describe in detail the inflammatory odontogenic cysts, a manual search was done in hard copy books of oral and maxillofacial pathology, and an electronic search was done in the google website, oral and maxillofacial pathology E-books, PubMed, Research Gate, Academia, and Google scholar using the keywords "odontogenic cysts," "classification of the odontogenic cysts," "radicular cyst," "periapical cyst," "lateral inflammatory cyst," "residual cyst," "paradental cyst," "collateral inflammatory cyst," "treatment of inflammatory odontogenic cysts," and matching

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Publication Date
Sat Apr 01 2023
Journal Name
Baghdad Science Journal
Development and Validation of a Simple and Sensitive Reverse-Phase High Performance Liquid Chromatographic Method for the Determination of Ibuprofen in Pharmaceutical Suspensions
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The aim of this work was to develop and validate a rapid and low cost method for estimation of ibuprofen in pharmaceutical suspensions using Reverse-Phase High Performance Liquid Chromatography. The proposed method was conducted and validated according to International Conference on Harmonization (ICH) requirements. The chromatographic parameters were as follows: column of octyldecylsilyl C18 with dimensions (150 × 4.6) mm, mobile phase composed of acetonitrile with phosphoric acid with a ratio of 50 to 50 each using isocratic mode, flow rate of 1.5 mL/min and injection volume of 5 μL. The detection was carried out using UV detector at 220 nm. The method was validated and showed short retention time for ibuprofen peak at 7.651 min, wit

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Publication Date
Mon Jan 01 2024
Journal Name
Vitae
Enzyme Inhibitory and Anti-cancer Properties of Moringa peregrina
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Background: Moringa peregrina is widely used in the traditional medicine of the Arabian Peninsula to treat various ailments, because it has many pharmacologically active components with several therapeutic effects. Objective: This study aimed to investigate the inhibitory effect of Moringa peregrina seed ethanolic extract (MPSE) against key enzymes involved in human pathologies, such as angiogenesis (thymidine phosphorylase), diabetes (α-glucosidase), and idiopathic intracranial hypertension (carbonic anhydrase). In addition, the anticancer properties were tested against the SH-SY5Y(human neuroblastoma). Results: MPSE extract significantly inhibited α-glucosidase, thymidine phosphorylase, and carbonic anhydrase with half-maximal i

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Publication Date
Wed Oct 05 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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