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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
Tue Apr 15 2025
Journal Name
Bulletin Of The Chemical Society Of Ethiopia
Synthesis, characterization and evaluation of anticancer and antioxidant activity of new azo dye derivatives from tryptamine and complexes
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This new azo dye 3-((2-(1H-indol-3-yl) ethyl) diazenyl) quinoline-2-ol was subsequently used to prepare a series of complexes with the metal ions of Cr+3, Cu+2, VO+2, Mn+2and Mo+6. The compounds identified by 1H and 13C-NMR, FT-IR, UV-Vis, mass spectroscopy, as well as TGA, DSC, and C.H.N., conductivity, magnetic susceptibility, metal and chlorine content. The results showed that the ligand behaves in a bidantate, and that the complexes gave octahedral, excepting for VO+2 square pyramid was given, that all complexes are non-electrolytes. The effectiveness of mention the compounds in inhibiting free radicals was evaluated by the ability to act as an antioxidant was measured using DPPH as a free radical and gallic acid as a standard s

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Publication Date
Wed Jun 24 2020
Journal Name
Systematic Reviews In Pharmacy
Synthesis, Characterization and Spectroscopic Study of New Metal Complexes form Heterocyclic Compounds for Photostability Study
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In present project, new Schiff base of 4, 4'- (((1E, 1'E)-1,4-.phenylenebis- (methane-ylylidene))-bis-(azane-ylylidene)) bis-(5-(4-chlorophenyl) -4H -1,2,4-triazole-3-thione) (L3) has been synthesized by condensation of 4-amino-5-(4-chlorophenyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione with benzene-1,4-dicarboxaldehyde. The new asymmetrical Schiff base (L3) used as a ligand to synthesize a new complex with Co(II), Ni(II), Cu(II), Pd(II), and Pt(IV) metal ions by 1:2 (Metal: ligand) ratio. New ligand and their complexes have been exanimated and Confirmed by Fourier-transform infrared (FT-IR), Ultraviolet-visible (UV-visible), Proton nuclear magnetic resonance (1HNMR), carbon13 nuclear magnetic resonance (13CNMR), carbon-hydrogen nitrogen sulf

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Publication Date
Sun Jun 16 2013
Journal Name
International Journal For Sciences And Technology
Synthesis and Characterization of Some New Thiazine-4-Ones Containing 1, 3, 4-Thiadiazole Moiety
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Small ring heterocycles containing nitrogen and sulfur have been under investigation for a long time because of their important medicinal properties. Among the wide range of heterocycles explored to develop pharmaceutically important molecules, thiadiazoles had played an important role in medicinal chemistry. A survey of literature had shown that compounds having thiadiazole nucleus possess a broad range of biological activities such as anti-inflammatory (1), antibacterial (2), and antifungal activities (3). Thiazine-4-one and their derivatives are import classes of compounds in organic and medicinal chemistry. The thiazine-4-one ring system is a core structure in various synthetic pharmaceutical agents, displaying a broad spectrum of biolo

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Publication Date
Mon May 18 2009
Journal Name
Journal Of Global Pharma Technology
Synthesis, Thermal and Electrochemical Properties of Four New Bis Oxadiazole Copolymers Based on Azo Monomer
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Four new copolymers were synthesized from reaction of bis acid monomer 3-((4-carboxyphenyl) diazenyl)-5-chloro-2-hydroxybenzoic acid with five diacidhydrazide in presence of poly phosphoric acid. The resulted monomers and copolymers have been characterized by FT-IR, 1H-NMR, 13C-NMR spectroscopy as well as EIMs technique. The number averages of molecular weights of the copolymers are between 4822 and 9144, and their polydispersity indexes are between 1.02 and 2.15. All the copolymers show good thermal stability with the temperatures higher than 305.86 C when losing 10% weight under nitrogen. The cyclic voltammetry (CV) measurement and the electrochemical band gaps (Eg) of these copolymers are found below 2.00 ev.

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Publication Date
Thu Nov 22 2018
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Thermal Electo Conductivity of Some New Triazole Derivatives Bearing Azo or Azomethain Group
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Newly acid hydrazide was synthesized from ethyl 2-(2,3-dimethoxyphenoxy) acetate (2), which is cyclized to the corresponding  4-amino-1,2,4-triazole (3). Five newly azo derivatives (4a-e) were synthesized from this 1,2,4-triazole by converting the amine group to diazonium salt then reacted with various substituent phenol,as well three newly imine derivatives (5a-c) were synthesized from reacting the amine group of compound (3) with three aryl aldehyde. The thermal electro conductivity of these compounds was tested at 30, 50, 75 and 100 áµ’C. compound 4a showed interesting electro conductivity at 75áµ’C as well 5a at 75áµ’C while 5b showed significant conductivity at 100 áµ’C

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Publication Date
Wed Dec 06 2023
Journal Name
Indonesian Journal Of Chemistry
Synthesis, Characterization and Biological Activity of New Oleander Complexes against Bacteria Found in Polluted Water
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Natural polymers are often non-toxic, biodegradable, biocompatible, and safe. A novel ligand was synthesized as a natural polymer using chitosan and oleander plant extract [(2R,3S,4R,5S)-5-(acetoxyamino)-4-hydroxy-3,6-dimethoxytetrahydro-2H-pyran-2-yl) methyl (16R)-3-(((2S,4S,5R)-4-methoxy-2,5-dimethyltetrahydro-2H-pyran-2-yl)oxy-10,13,16-trimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl) hexadecahydro-14H-cyclopenta [a] phenanthren-14-yl) phthalate] (Chitosan-Ph-Oleander). This ligand and its complexes with several metals (Cr+3, Mn+2, Fe+3, Ni+2, Cu+2, Zn+2) were characterized using FTIR, UV-visible and 1H-NMR spectroscopy, as well as by molar conductivity, magnetic moment, and TGA analysis. The biological activity for the prepared polymer

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Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis and Characterization of Some New Nucleoside Analogues from Substituted Benzimidazole via 1,3-Dipolar cycloaddition
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This paper includes the synthesis of some new nucleoside analogues starting with 2-substituted benzimidazole derivative (7-9), that synthesized by condensation of O-phenylenediamine with p-chloro benzaldehyde and two substituted benzoic acid , which on nucleophilic substitution with propargyl bromide gave a new N-substituted compounds (10-12). D-Fructose and D-galactose were chosen as a sugar moiety which were protected, brominated and azotated to give azido sugars (5) and (6), then they were subjected to 1,3-dipolar cycloaddition reaction with N-substuted compounds afforded bloked nucleoside analoges (13-16), which after hydrolysis gave our target the free nucleoside analogues (17-20). All prepared compounds were identified by FT-IR

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Publication Date
Sun Sep 04 2016
Journal Name
Baghdad Science Journal
Synthesis of Some New Nucleoside Analogues Containing Seven Membered Ring and Studying Their Biological Activity
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In this work, a series of new Nucleoside analogues (D-galactopyranose linked to oxepanebenzimidazole moiety) was synthesized via multisteps synthesis. The first step involved preparation of two benzimidazoles 2-styrylbenzimidazole and 2-(phenyl ethynyl) benzimidazole via reaction of phenylenediamine with cinnamic acid or ?-phenyl propiolic acid. Electrophilic addition of the prepared benzimidazoles by three anhydrides in the second step afforded (4-6) and (14-16) which in turn were treated with 1,2,3,4-di-O-isopropylidene galactopyranose in the third step to afford a series of the desirable protected nucleoside analogues (7-9) ,(17-19)which after hydrolysis in methanolic sodium methoxidein the fourth step afforded the free nucleoside analog

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Publication Date
Sun Jun 01 2014
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Antimicrobial Screening of New Schiff Bases Linked to Phthalimidyl Phenyl Sulfonate Moiety
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A series of Schiff bases linked to phthalimidyl phenyl sulfonate moiety have been synthesized via multistep synthesis. The first step involved reaction of phthalic anhydride with aniline producing N-phenyl phthalamic acid which was subsequently dehydrated to the corresponding N-phenyl phthalimide via treatment with acetic anhydride and anhydrous sodium acetate. The synthesized imide was treated with chlorosulfonic acid in the third step producing 4-(N-phthalimidyl) phenyl sulfonyl chloride which was introduced in reaction with 4-hydroxy acetophenone in the fourth step producing 4-[4-(N-phthalimidyl) phenyl sulfonate] acetophenone and this in turn was introduced successfully in condensation reaction with various aromatic primary amines affor

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Publication Date
Sun Dec 04 2016
Journal Name
Baghdad Science Journal
Synthesis and Characterization of some New 1,3,4-Oxadiazole derivatives based on 4-amino benzoic acid
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Various of 2,5- disubstituted 1,3,4-oxadiazole (Schiff base, ?- lactam and azo) were synthesized from 2,5-di (4,4?-amino-1,3,4-oxadiazole which usequently synth-esized from mixture of 4- amino benzoic acid and hydrazine arch of polyphosphorus acid. The synthesized compounds were cherecterized by using some spectral data (UV, FT-IR , and 1H-NMR)

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