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Anti-cancer and Antioxidant Activities of Some New Synthesized Mannich Bases Containing an Imidazo (2, 1-B) Thiazole Moiety
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       Synthesis and preliminary biological evaluation of imidazo (2, 1-b) Thiazole derivatives is reported. Under Mannich conditions, a series of new imidazo (2, 1-b) Thiazole derivatives were synthesized. Starting from the reaction of 2- amino thiazole with 4- bromo phenyl bromide to produce 5-(4-bromo phenyl) imidazo (2, 1-b) thiazoles, following by introduce the substituted aminomethyl at position 6-by reacting with different aromatic amines under Mannich conditions to afford 6-secondary amine-5-(4-bromo phenyl) imidazo (2,1-b) thiazole in high yields.

FT-IR, 1H NMR, and 13C NMR techniques were used to characterize the synthesized derivatives. In addition, all compounds were tested for their antioxidant activity, and three of them were examined for cytotoxic activity against kidney cancer using an MTT assay. The product (A9) has shown an excellent anti-cancer activity with 69.69 value.

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Publication Date
Mon Oct 10 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]imidazole1,3(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 hydroxyl for t

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Publication Date
Sun Sep 25 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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Publication Date
Thu Aug 20 2020
Journal Name
Al-mustansiriyah Journal Of Science
The Importance of 2-AminoThiazole Schiff Bases as Antimicrobial and Anticancer Agents
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The pharmacophore 2-aminothiazole has an interesting role in pharmaceutical chemistry as this led to the synthesis of many types of compounds with diverse biological activity. Schiff base derivatives at the same time contribute to drug evolution importantly. In this review, the Schiff base derivatives of 2-aminothiazole formed and some of their metal complexes are being focused on, and the antimicrobial and anticancer activity of them is being illustrated.

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Publication Date
Sat Jan 20 2024
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Modification, Characterization of New Thiazolidinone and Oxazolidinone Derived from Levofloxacin and Evaluation of Anti-Oxidant
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The research study included the synthesis of a new series of heterocyclic derivatives containing the antibiotic Levofloxacin. The first way provides for the reaction of  Levofloxacin with thionyl chloride in benzene as a solvent to give an acid chloride derivative. A new class of acid hydrazide synthesized from Levofloxacin was studied. Schiff bases were produced via the reaction of acid hydrazide with substituted aromatic ketones in methanol. The next stage involved the response of Schiff bases with thioglycolic acid and mono chloroacetic acid in DMF to produce derivatives of the antibiotic levofloxacin that have five heterocyclic members, including the derivatives thiazolidine-4-one and oxazolidine-5-one. The FTIR, 1HNMR, a

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Publication Date
Thu Sep 26 2019
Journal Name
International Journal Of Pharmaceutical Research
Synthesis and identification of novel 2-thioxoimidazolidin- 4-one derivatives containing azo and ester groups
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The compounds 3-[4̄-(4˭-methoxybenzoyloxy) benzylideneamino]-2-thioxo-imidazolidine-4-one(3)aand 4-(1-(5-oxo- 2-thioxoimidazolidin-1-ylimino)ethyl)phenyl acetate(3)b were prepared from the reaction of aromatic aldehyde or ketone(1)a,bwith thiosemicarbazide to give aryl thiosemicarbazones(2)a,b ,followed by cyclization with ethylchloroacetate in the presence of fused sodium acetate. Treatment the compounds(3)a,bwith 4- hydroxybenzenediazoniumchloride yielded the correspondings4-((4-((4-hydroxyphenyl)diazenyl)-5-oxo-2- thioxoimidazolidin-1-ylimino)methyl)phenyl 4-methoxybenzoate(4)aand4-(1-(4-((4-hydroxyphenyl)diazenyl)-5-oxo-2- thioxoimidazolidin-1-ylimino)ethyl)phenyl acetate(4)b.The new 2-thioxo-imidazolidin-4-one with esters (5-7)a,b sy

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Publication Date
Thu Sep 26 2019
Journal Name
Journal Of Pharmaceutical Research International
Synthesis and identification of novel 2-thioxoimidazolidin-4-one derivatives containing azo and ester groups
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The compounds 3-[4̄-(4˭-methoxybenzoyloxy) benzylideneamino]-2-thioxo-imidazolidine-4-one(3)aand 4-(1-(5-oxo- 2-thioxoimidazolidin-1-ylimino)ethyl)phenyl acetate(3)b were prepared from the reaction of aromatic aldehyde or ketone(1)a,bwith thiosemicarbazide to give aryl thiosemicarbazones(2)a,b ,followed by cyclization with ethylchloroacetate in the presence of fused sodium acetate. Treatment the compounds(3)a,bwith 4- hydroxybenzenediazoniumchloride yielded the correspondings4-((4-((4-hydroxyphenyl)diazenyl)-5-oxo-2- thioxoimidazolidin-1-ylimino)methyl)phenyl 4-methoxybenzoate(4)aand4-(1-(4-((4-hydroxyphenyl)diazenyl)-5-oxo-2- thioxoimidazolidin-1-ylimino)ethyl)phenyl acetate(4)b.The new 2-thioxo-imidazolidin-4-one with esters (5-7)a,b sy

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Publication Date
Mon Dec 05 2022
Journal Name
Baghdad Science Journal
Heavy Metal Complexes of 1, 2, 3-Triazole derivative: Synthesis, Characterization, and Cytotoxicity Appraisal Against Breast Cancer Cell Lines (MDA-MB-231)
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     New chelating ligand derived from triazole and its complexes with metal ions Rhodium, Platinum and Gold were synthesized. Through a copper (I)-catalyzed click reaction, the ligand produced 1,3-dipolar cycloaddition between 2,6-bis((prop-2-yn-1-yloxy) methyl) pyridine and 1-azidododecane. All structures of these new compounds were rigorously characterized in the solid state using spectroscopic techniques like: 1HNMR, 13CNMR, Uv-Vis, FTIR, metal and elemental analyses, magnetic susceptibility and conductivity measurements at room temperature, it was found that the ligand acts as a penta and tetradentate chelate through N3O2, N2O2, and the geometry of the new complex

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Publication Date
Mon Dec 05 2022
Journal Name
Baghdad Science Journal
Heavy Metal Complexes of 1, 2, 3-Triazole derivative: Synthesis, Characterization, and Cytotoxicity Appraisal Against Breast Cancer Cell Lines (MDA-MB-231)
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     New chelating ligand derived from triazole and its complexes with metal ions Rhodium, Platinum and Gold were synthesized. Through a copper (I)-catalyzed click reaction, the ligand produced 1,3-dipolar cycloaddition between 2,6-bis((prop-2-yn-1-yloxy) methyl) pyridine and 1-azidododecane. All structures of these new compounds were rigorously characterized in the solid state using spectroscopic techniques like: 1HNMR, 13CNMR, Uv-Vis, FTIR, metal and elemental analyses, magnetic susceptibility and conductivity measurements at room temperature, it was found that the ligand acts as a penta and tetradentate chelate through N3O2, N2O2, and the geometry of the new complexes are identified as octahedral for (Rh & Pt) complexes a

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Publication Date
Sat Nov 04 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Preliminary Anti-Inflammatory and Anti-Microbial Evaluation of New 4,5-Dihydro-1H-Pyrazole Derivatives
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Abstract      Organic compounds with pyrazole cores have a variety of uses, notably in the pharmaceutical and agrochemical sectors. The interest in creating pyrazole compounds, examining their many features, and looking for potential uses is growing. Our work has concert with synthesis of  chalcones and pyrazolines, then finally pyrazoline-aniline derivatives and evaluation their anti-inflammatory, antibacterial and antifungal activities

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Publication Date
Sat May 27 2017
Journal Name
Journal Of Pharmaceutical Sciences And Research
Synthesis, Preliminary Antimicrobial Evaluation and Molecular Docking of new Schiff bases of Ceftizoxime
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Schiff bases of Ceftizoxime sodium were synthesized in an attempt to improve the antimicrobial spectrum of Ceftizoxime. Aminothiazole ring of Ceftizoxime is linked directly through an imino group to different aromatic aldehydes reacted by nucleophilic addition using trimethylamine (TEA), as a catalyst and refluxed in methanol. The antimicrobial activity was evaluated for such Schiff bases using disc diffusion method. Molecular docking was conducted on certain penicillin-binding proteins (PBPs) and carboxypeptidases using 1- click docking software. Schiff bases of Ceftizoxime were prepared with reasonable yields and their chemical structures were confirmed by spectral analysis (FTIR, 1H-NMR) and elemental microanalysis (CHNS). The antibacter

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