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Design, Synthesis and Preliminary Pharmacological Evaluation of New Non-Steroidal Anti-Inflammatory Agents Having a 4-(Methylsulfonyl) Aniline Pharmacophore
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A series of 4-(methylsulfonyl)aniline derivatives were synthesized in order to obtain new compounds as a potential anti-inflammatory agents with expected selectivity against COX-2 enzyme. In vivo acute anti-inflammatory activity of the final compounds 11–14 was evaluated in rat using an egg-white induced edema model of inflammation in a dose equivalent to 3 mg/Kg of diclofenac sodium. All tested compounds produced significant reduction of paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the activity of compounds 11 and 14 was significantly higher than that of diclofenac sodium (at 3 mg/Kg) in the 120–300 minute time interval, while compound 12 expressed a comparable effect to that of diclofenac sodium in the 60–240 minute time interval time, and compound 13 showed a comparable effect to that of diclofenac sodium at all experimental times. The result of this study indicates that the incorporation of the 4-(methylsulfonyl)aniline pharamacophore into naproxen, indomethacine, diclofenac and mefanamic acid maintained their anti-inflammatory activity and may increase selectivity towards the COX-2 enzyme which will be confirmed in the future by assessing COX-2: COX-1 inhibitory ratios using a whole blood assay.

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Publication Date
Wed Sep 27 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Evaluation of Anti-inflammatory Effects of Cinnamic Acid Against Dextran Sodium Sulfate Induced Ulcerative Colitis in Male Mice
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Inflammatory bowel disease (IBD) is a common chronic inflammatory disease of the gastrointestinal tract, including ulcerative colitis and Crohn's disease. ulcerative colitis (UC)  disease is characterized by chronic, persistent, recurrent, and nonspecific intestinal ulcers and mucosal inflammation. This study investigated the protective effects of cinnamic acid on dextran sodium sulfate (DSS) induced ulcerative colitis in mice. Forty adult male mice were collected and randomly divided into five groups, group Ӏ received a suspension of distill water and poloxamer, and group ӀӀ received 3% DSS in drinking water for 7 consecutive days. Two treatment groups received an oral suspension of cinnamic acid 50 and 25 mg/kg respectively an

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Publication Date
Wed Jul 01 2020
Journal Name
International Journal Of Pharmaceutical Research
Synthesis, Design, Docking and biological activity of new benzo hydrazide derivatives.
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Publication Date
Thu Apr 22 2021
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
The Anti-Inflammatory Effect of Vitamin K in Aging
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        Vitamin K is a fundamental enzymatic co-factor implicated in the carboxylation of several vitamin K dependent proteins involved in the pathogenesis of certain age – related diseases. Inflammation is realized as an important factor in such diseases. Vitamin K is recognized to play an anti-inflammatory behavior that is distinct of its action as an enzymatic co- factor by suppressing many signaling pathways mainly the nuclear factor κB (NF-κB) signal transduction pathway. As well as to play a role as an antioxidant versus the generation of reactive oxidative species (ROS). The purpose of this review is to focus on the protective function of vitamin K as an anti-inflammatory agent

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Publication Date
Fri Jan 01 2021
Journal Name
Materials Today: Proceedings
In silico analysis of quercetin as potential anti-cancer agents
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Publication Date
Sat Jan 20 2024
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis of New Bismaleimide Homopolymer and Copolymers Derived from 4, 4ˉ-Bis[4-(N-maleimidyl) Phenyl Schiff Base] Tolidine
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Polyimides are widely used in high-temperature plastics, adhesives, dielectrics, photoresists, nonlinear optical materials, separation membrane materials, and Langmuir-Blodgett (LB) films. They are commonly regarded as the most heat-resistant polymers. This work involved the synthesis of a new bismaleimide homopolymer and copolymer by performing many steps. The synthesis of compound (1) (bis [4-(amino phenyl) Schiff base] tolidine) via condensation of o-tolidine with two moles of 4-aminoacetophenone. Secondly, compound (1) was combined with maleic anhydride to form compound (2) (4, 4ˉ-bis[4-(N-maleamic acid) phenyl Schiff base] toluidine). Thirdly, a dehydration reaction was carried out affording compound (3) (4,4ˉ-bis [4-(N-maleimidyl

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Publication Date
Fri Dec 29 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Chemical Characterization and Pharmacological Evaluation of Phytophenols-Etodolac Mutual Prodrugs
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Etodolac is choice of drug for pain and inflammation but has major side effects of gastric ulcers that are due to free carboxylic group. Etodolac belongs to the chemical class of non-selective COX-inhibitor but preferentially COX-2 inhibitor. Here the ester linked mutual prodrugs of etodolac with phytophenols like vanillin, carvacrol, umbelliferone, guaiacol, sesamol and syringaldehyde were synthesized. All the prodrugs were characterized by IR-spectroscopy, 1H-NMR, 13C-NMR and mass spectrometry. Among the synthesized prodrugs, the Eto-van, Eto-umbe, Eto-sesa and Eto-syr showed improved analgesic and anti-inflammatory activity compared to etodolac. All the synthesized prodrugs showed less ulcerogenic side effects co

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Publication Date
Sat Jan 01 2022
Journal Name
P J M H S
Synthesis and Characterization of Some New Metals Complexes of ((4 Methoxy Benzoyl) Carbamothioyl) Glycine
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A new ligand ( 4- methoxy benzoyl ) carbamothioyl ) Glycine (MCG) is synthesized by reaction of (4- methoxy benzoyl isothiocyanate) with Glycine(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 byFT-IR,UV-Visible spectra, conductivity measurements, magnetic susceptibility and atomic absorption. From results obtained, the following formula [M(MCG)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
Wed Jan 01 2014
Journal Name
Iosr Journal Of Applied Chemistry (iosr-jac)
Synthesis and Characterization of new metals complexes of [N-(4- chlorobenzoylamino)-thioxomethyl]valine (cbv)
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A new ligand [N-(4-chlorobenzoyl amino) -thioxomethyl] valine (cbv) is synthesized by reaction of 4- chloro benzoyl iso thio cyanate with valine acid. The ligand is Characterized by elemental analysis ,FT-IR, and 13C 1H NMR spectra, some transition metals complex of this ligand were prepared and Characterized by FTIR , UV-Visible spectra , conductivity measurement's ,magnetic susceptibility , atomic absorption and determination of molar ratio (M:L), from results obtained , the following formula [M(cbv)2] where M+2 =Mn, Fe ,Co , Ni , Cu,Zn,Cd, and Hg and the proposed molecular structure for these complexes as tetrahedral geometry, except copper complex is have square planer geometry

Publication Date
Tue Aug 05 2014
Journal Name
International Journal Of Engineering Sciences & Research Technology
Synthesis and Characterization of Some New Metal Complexes 2-(4-nitrophenyl azo)-2,4- dimethylphenol.
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The Ligand 2-(4-nitrophenyl azo)-2,4-dimethylphenol derived from 4-nitroaniline and 2,4-dimethylphenol was synthesized. The prepared ligand was identified by FT-IR and UV-Vis spectroscopic techniques. Treatment of the ligand with the following metal ions ( CuII , ZnII ,CdII and HgII) in aqueous ethanol with a 1:2 M:L ratio. Characterization of these compounds has been done on the basis of FT-IR and UV-Vis, as well as magnetic susceptibility and conductivity measurements. On the basis of physicochemical data tetrahedral geometries were assigned for the complexes.

Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis and Characterization of New Mannich Bases Derived from 7-hydroxy-4-methyl Coumarin
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Coumarin is a natural substance isolated from different plants. It belonges to a group of benzobyrones which consists of a benzene ring joined to a pyrone nucleus. In the present research, a new series of coumarin derivatives were formed. Compound (1) (7-hydroxy-4-methyl Coumarin) was converted into 4-methylquinolin-2(H) derivative (2) by reaction with acetamide, and then reaction of (2) with thiosemicarbazide in ethanol leads to the synthesize of hydrazincarbothioamide derivative (3).The reaction of (3) with ethylchloroacetate in presence of sodium acetate leads to closure ring to get [(1-(5-oxo-2-thioxoimidazolidin-1-ylimino) ethyl)]quinolin-2(1H)-one (4). Mannich bases were prepared through the reaction of (4) with primary

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