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Design and Synthesis of New Non-Steroidal Anti-inflammatory Agents with Expected Selectivity toward Cyclooxygenase-2 Inhibition

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 Apr 30 2023
Journal Name
Iraqi Journal Of Science
Synthesis and Characterization of Some New Metal Complexes of 2-phenyl-2-(p-tolylamino) and 2-phenyl-2-(phenylamino) Acetonitrile Compounds

The synthesis and characterization of new complexes of Cr(III), Fe(III), Co(II), Ni(II), Cu(II) and Zn(II) with bidentate [L1: 2-phenyl-2-(p-tolylamino) acetonitrile] and [L2: 2-phenyl-2-(phenylamino) acetonitrile] ligands has been described. The two ligands were prepared by the reaction of p-toluidine and aniline with benzaldehyde, respectively in the presence of potassium cyanide and acidic medium. The complexes were synthesized by treating an ethanolic solution of the ligand with metal salts in a mole ratio of [1:2] [M:L]. The complexes were characterized by using metal and elemental analyses, electronic spectra, 1H-NMR, 13C-NMR, Thermal Gravimetric Analysis TGA, molar conductivity and magnetic susceptibility. According to the obtaine

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Publication Date
Thu Feb 01 2024
Journal Name
Surface Engineering And Applied Electrochemistry
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Publication Date
Sun Jun 01 2014
Journal Name
Baghdad Science Journal
Synthesis and Characterization of New heterocyclic Polyacrylamides from Derivatives 2-Aminobenzothiazole

The present work involved preparation of new hetro cyclic polyacrylamides (1-9) using reaction of polyacryloyl chloride with 2-aminobenzothiazole which prepeard by thiocyanogen method in the presence of a suitable solvent and amount tri ethyl amine (Et3N) with heating. The structure confirmation of polymers were proved using FT-IR,1H-NMR,C13NMR and UV spectroscopy.Other physical properties including softening and melting points, and solubility of the polymers were also measured.

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Publication Date
Fri Jan 01 2021
Journal Name
Materials Today: Proceedings
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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

        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
Mon Feb 20 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis of Some New 2-thioxoimidazolidin-4-one Derivatives

This research includes the synthesis of new series of heterocyclic compounds. Reaction of 2-nitro benzylidene)thiosemicarbazide(1) with ethyl chloro acetate gave (2-nitro benzylidene amino)-2-thioxomidazolidine-4-one(2) ,treatment(2) with methyl iodide to give(3)which was reacted with hydrazine to give 2-hydrazinyl-1-[(2-nitrobenzylidene)amino]- 1H-imidazol-5(4H)-one, andreation of compound(2) with aromatic aldehydes to give 5arylidene -3-({2-nitro benzylidene}amino)2-thioxo-3,5-dihydro-4H-imidazole-4-one(5a,5b), which was reacted with ethyl aceto acetate to give 4-aryl-1-[2-nitrobenzylidene, amino -6oxo-2-thioxo octa hydro-1H-benzo[d]imidazole-5-carboxylate and followed synthesis of βlactamederivtives(9a,9b) by treatment derivatives(

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Publication Date
Sun Apr 30 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis, Spectroscopic and Biological Studies of a New Some Complexes with N-Pyridin-2-Ylmethyl-Benzene-1,2Diamine

 N-Pyridin-2-ylmethyl-benzene-1,2-diamine (L) was prepared from the reaction of ortho amino phenyl thiol with 2 – amino methyl pyridine in mole ratio (1:1) . It was characterized by elemental analysis (C.H.N) , FT-IR , Uv – Vis , 1H , 13C-N.M.R . The 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 was established by elemental analysis (C.H.N) , FT-IR , Uv – Vis spectra , conductivity measurements , atomic absorption and magnetic susceptibility . The complexes showed characteristic behavior of octahedral geometry around the metal ions and the (N,N,N) ligand coordinated in tridentat mode except with Pd complexes sho

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Publication Date
Sat Apr 15 2023
Journal Name
Iraqi Journal Of Science
Synthesis, Characterization and Stability Constant study of New Schiff Bases Derived from 2-Amino -2-deoxy Chitosamine and aldehydes with Some Metal Complexes

Two new Schiff bases (S1,S2) derived from 2-Amino-2-deoxy chitosamine and mnitrobenzaldehyde
(S1), and with salicylaldehyde (S2) were prepared and
characterized using FTIR, UV and mass spectrometry. New complexes of the
transition metal ions Co (II), Ni (II), Pd (II), Pt (II) with the two ligands were
synthesized and their structures were elucidated depending on atomic absorption,
FTIR, UV-visible spectra in addition to magnetic susceptibility and electrical
conductivity measurement. Metal to ligand [M: L] ratio was obtained for all
complexes in ethanol using molar ratio method, which gave comparable results with
those obtained for the solid complexes. Stability constant of the complexes were
determined using s

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Publication Date
Fri Jan 20 2023
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis, Spectroscopic, and Biological Activity Study for New Complexes of Some Metal Ions with Schiff Bases Derived From 2-Hydroxy Naphthaldehyde with 2-amine benzhydrazide

This study describes the preparation of tetradentate Schiff base derived from the condensation of 2-Hydroxy naphthaldehyde with 2-amine benzhydrazide and the synthesis of new complexes series with a good yield.The prepared ligand was characterized using a microanalysis technique, UV-visible, FT-IR, nuclear magnetic resonance 1H-NMR, mass spectrometry, thermal gravimetric analysis TGA, and the addition of conductivity measurement and magnetic moment of complexes. The invitro antimicrobial activity of the prepared compounds was tested against  Gram-negative Klebsiella pneumonia, Gram-positive Staphylococcus aureu, and Candida albicans by the agar well diffusion method. The spectroscopy and measurement studies showed that the li

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Publication Date
Sat Jul 01 2023
Journal Name
Journal Of Medicinal And Chemical Sciences
Synthesis, Characterization, and Biological Activity of New Metal Ion Complexes with Schiff Base (Z)-3((E)-2-Hydroxybenzylidene) Hydrazineylidene) Indolin-2-One

The study involved preparing a new compound by combining between 2-hydroxybenzaldehyde and (Z)-3-hydrazineylideneindolin-2-one resulting in Schiff bases and metal ions: Mn(II), Co(II), Ni(II), Cu(II), and Zn(II) forming stable minerals-based-Schiff complexes. The formation of resulting Schiff bases is detected spectrally using LC-Mss which gave corresponding results with theoretical results, 1H-NMR proves the founding of N=CH signal, FT-IR indicates the occurrence of imine band and UV-VIs mean is proved the ligand formation. On the other hand, minerals-based-Schiff was characterized using the same spectral means that relied with ligand (Schiff bases). Those means gave satisfactory results and proved the suggested distinguishable geometries.

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