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Synthesis and Preliminary Biological study of New Chalcone Derivatives Containing Isoxazoline Moiety
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                          In this research work, synthesis, antimicrobial and antioxidant bioactivity of a chain of compounds having unsaturated ketones bond and isoxazoline moiety have been described. New chalcone derivatives containing isoxazoline moiety have been synthesized. Generally, Chalcones are unsaturated ketones bearing (-CO-CH=CH-) as reactive ketoethylenic group that give the bright yellow colored compounds due to this chromophore group.  Firstly, chalcones (IIa-d) have been prepared by cyclocondensation (Claisen-Schmidt condensation) of triphenyl aminobenzaldehyde with different substituted acetophenone in ethyl alcohol to produce a series of chalcones compounds with bright yellow colored as a starting material,. The next step involving the novel chalcones (IIa-d) reacted with hydroxylamine hydrochloride afforded a new isoxazoline compounds (IIIa-d) in basic medium. The prepared compounds were fully characterized by melting points, FTIR, 1H-NMR spectroscopy, 13 C-NMR for some compounds and CHNS techniques. The reactions have been monitored by TLC (Thin Layer Chromatography) technique. The synthesised compound IId showed significant bioactivity against the gram-negative bacteria species. Also, the antioxidant activity of the some new synthesized compounds was evaluated and determined against the DPPH radical (1.1-diphenyl-2-picrylhydrazyl) and compared to that of a standard natural antioxidant, Ascorbic acid, compound IIb showed higher antioxidant activity by using the free radical DPPH. The outcomes of   investigation enhanced the activity of new derivatives as antimicrobial reagent.   

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Publication Date
Mon Jun 04 2018
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and antimicrobial evaluation with DFT study for new thiazole derivatives
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Two compounds,[2-amino-4-(4-nitro phenyl) 1,3-thiazole],(4) and [2-amino-4-(4-bromo phenyl) 1,3-thiazole],(5), were synthesized by refluxing thiourea (1) with each of  para-ntiro and para-bomophanacyl bromides(2) and (3) respectively, in absolute methanol. Then, by reaction of [5] with 3,5-dinitrobenzoyl chloride in dimethylformamide (DMF) yielded  (6) .On the other hand, reaction of (4) with chloroacetyl chloride in dry benzene afforded (7), which is  upon treatment with thiourea in absolute methanol, af

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Publication Date
Mon Mar 20 2023
Journal Name
Liquid Crystals
Synthesis and study the mesomorphic behaviour of some new 1,3,4-thiadiazoline derivatives
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Investigation of mesomorphic properties of new 1,3,4-thiadiazolines (which are synthesised via many steps in Scheme 1) was carried out in this study. These compounds are designed to have a heterocyclic unit, a carboxylate linkage group and a polar ether chain at the end of the molecule adjacent to the benzene ring, which enhance the dipolar interactions forces (varied from one to eight carbons) to investigate the association properties of their phases. The structure of the target compounds and the intermediates were confirmed by 1H NMR, 13C NMR, mass and FTIR spectral techniques. Polarised microscopic studies revealed that all the compounds in the series exhibited enantiotropic liquid crystalline properties. This was further confirmed using

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Publication Date
Thu Jun 01 2017
Journal Name
Journal Of Al-nahrain University Science
Synthesis and Biological Activity Study of New Some Schiff Bases Derived From D-Erythroascorbic Acid
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Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
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 pr

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Publication Date
Wed Nov 20 2024
Journal Name
Future Medicinal Chemistry
New 4-amino-3-chloro benzoate ester derivatives as EGFR inhibitors: synthesis, in silico and biological analyses
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Publication Date
Wed Apr 30 2025
Journal Name
Academic Science Journal
Synthesis, Characterization and Study of Biological Activity of Some New Schiff Bases
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            In the present study, ( Schiff's bases 6a - 6e) and  (new amids derivatives 6f - 6j) have been synthesized . The glutaroyl chloride(2) has been prepared by the reacting of glutaric acid and thionyl chloride in presence of (DMF) . The new compound bis(4-formylphenyl) glutarate (3) has been Synthesized from reaction of one mole of glutaroyl chloride and two moles of 4-hydroxybenzaldehyde . Compound 4,4'-(glutaroylbis(oxy))dibenzoic acid (4) was Synthesized from one mole of glutaroyl chloride and two moles of 4-hydroxybenzoic acid, while compound bis(4-(chlorocarbonyl)phenyl) glutarate (5) was prepared from 4,4'-(glutaroylbis(oxy))dibenzoic acid and Thionyl chloride . Then Schiff's bases 6a - 6e that prepared

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Publication Date
Sun Dec 25 2016
Journal Name
University Of Baghdad / College Of Education For Pure Sciences / Ibn-al-‎haitham/ Chemistry Department
Synthesis and Spectroscopic Studies and ‎Biological Activity of New Ligands ‎Containing S,N,O Donor Atoms with their ‎Metal Complexes
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The 3-aminoacetophenone and 4-aminoantipyrine were used as ‎precursors to prepare new six ligands. The three new ligands (L1,L2 ‎and L3) were synthesis by reacting one mole of 3-aminoacetophenone ‎with one mole of (Acetyl chloride), (benzoyl chloride), (4-‎methoxybenzoyl chloride) and ammonium thiocyanat in acetone as a ‎solvent, they are:-‎ L1 (AAA) =[N-(3-acetylphenylcarbamothioyl)acetamide]‎ L2 (BAA) =[N-(3-acetylphenylcarbamothioyl)benzamide]‎ L3 (MAA) =[N-(3-acetylphenylcarbamothioyl)-4-methoxy benzamide]‎ Also three new derivatives of 4-aminoantipyrine were synthesis by ‎reacting one mole of 4-aminoantipyrine with one mole of (Acetyl ‎chloride), (benzoyl chloride), (4-methoxybenzoyl chloride) and ‎ammonium thio

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Publication Date
Sat Sep 23 2017
Journal Name
Oriental Journal Of Chemistry
Synthesis and Antioxidant Ability of some new 6-amino-7H- [1,2,4]triazolo[3,4-b][1,3,4]thiadiazin-3-yl) derivatives bearing 2,6-dimethoxy-4-(methoxymethyl)phenol moiety
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Compound 4-(((6-amino-7H-[1, 2, 4] triazolo [3, 4-b][1, 3, 4] thiadiazin-3-yl) methoxy) methyl)-2, 6-dimethoxyphenol (6) was synthesized by multi steps. The corresponding acetonitrile thioalkyl (7) was cyclized by refluxing with acetic acid to afford 4-(((6-amino-7H-[1, 2, 4] triazolo [3, 4-b][1, 3, 4] thiadiazin-3-yl) methoxy) methyl)-2, 6-dimethoxyphenol (8). Two new series of 4-(((6-(3-(4-aryl) thioureido)-7H-[1, 2, 4] triazolo [3, 4-b][1, 3, 4] thiadiazin-3-yl) methoxy) methyl)-2, 6-dimethoxyphenol (9a-c) and of 4-(((6-(substitutedbenzamido) 7H-[1, 2, 4] triazolo [3, 4-b][1, 3, 4] thiadiazin-3-yl) methoxy) methyl)-2, 6-dimethoxyphenol (10a-c) were synthesized as new derivatives for fused 1, 2, 4-trizaole-thiadiazine (8). The antioxidant

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Publication Date
Sat Sep 23 2017
Journal Name
Oriental Journal Of Chemistry
Synthesis and Antioxidant Ability of Some New 6-amino-7H- [1,2,4]triazolo[3,4-b][1,3,4]thiadiazin-3-yl) Derivatives Bearing 2,6-Dimethoxy-4-(methoxymethyl)Phenol Moiety
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Compound 4-(((6-amino-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazin-3-yl)methoxy)methyl)- 2,6-dimethoxyphenol (6) was synthesized by multi steps. The corresponding acetonitrile thioalkyl (7) was cyclized by refluxing with acetic acid to afford 4-(((6-amino-7H-[1,2,4]triazolo[3,4- b][1,3,4]thiadiazin-3-yl)methoxy)methyl)-2,6-dimethoxyphenol (8). Two new series of 4-(((6-(3- (4-aryl)thioureido)-7H-[1,2,4]triazolo[3,4-b][1,3,4] thiadiazin-3-yl)methoxy)methyl)-2,6- dimethoxyphenol (9a-c) and of 4-(((6-(substitutedbenzamido)7H-[1,2,4]triazolo[3,4- b][1,3,4]thiadiazin-3-yl)methoxy)methyl)-2,6-dimethoxyphenol (10a-c) were synthesized as new derivatives for fused 1,2,4-trizaole-thiadiazine(8). The antioxidants of newly compounds were evaluated by DPPH

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Publication Date
Mon Mar 15 2021
Journal Name
Egyptian Journal Of Chemistry
Antimicrobial Activity of New Synthesized Aza -Beta Lactam and Tetrazole Derivatives Bearing Imidazo[2,1-B]Benzothiazole Moiety
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