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Synthesis and Characterization of Some Oxazolidine and Thiazolidine Derivatives and Study of their Antioxidants Activity
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 In this work, the preparation of some new oxazolidine and thiazolidine derivatives has been conducted. This was done over two steps; the first step included the synthesis of Schiff bases A1-A5 in 72-88% yields by the condensation of isonicotinic acid hydrazide and aldehydes. The second step includes the cyclization of derivatives A1-A5 with glycolic acid and thioglycolic acid to obtain the desired products, oxazolidine derivatives B1-B5 (44-60% yields) and thiazolidine derivatives C1-C5 (41-61% yields), respectively. The structure of the prepared compounds was characterized using FT-IR, 1H NMR, and 13C NMR spectroscopy. Some of the produced compounds were tested for antioxidant properties.  

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Publication Date
Wed Feb 08 2023
Journal Name
Iraqi Journal Of Science
Synthesis, Identification and Evaluation Biological Activity for Some New Triazole, Triazoline and Tetrazoline Derivatives From 2-Mercapto-3-phenyl-4(3H)Quinazolinone
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This research, involved synthesis of some new 1,2,3-triazoline and 1,2,3,4-tetrazole derivatives from antharanilic acid as starting material .The first step includes formation of 2-Mercapto-3-phenyl-4(3H)Quinazolinone (0) through reacted of anthranilic acid with phenylisothiocyanate in ethanol, then compound (0) reaction with chloro acetyl chloride in dimethyl foramamide (DMF) to prepare intermediate S-(α-chloroaceto-2-yl)-3-phenylquinazolin-4(3H)-one (1); compound (1) reacted with sodium azide to yield S-(α-azidoaceto-2-yl)-3-phenylquinazolin-4(3H)-one (2), while Schiff bases (3-10) were prepared from condensation of substituted primary aromatic amines with different aromatic aldehydes in absolute ethanol as a solvent. Compound (2) re

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Publication Date
Sat Dec 01 2012
Journal Name
Asian Journal Of Chemistry
Microwave assisted synthesis of new heterocyclic compounds: 1, 2, 3-triazoles and tetrazoles and study of their biological activity
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The work includes synthesis of 1,2,3-triazoles via click conditions and using the microwave irradiation starting from two synthesized azides: 2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyl azide (5) and perfluorobutylethyl azide (10) and different terminal alkynes. It also includes microwave enhanced synthesis of tetrazoles via the reaction of two synthesized azides i.e., perfluorobutylethyl azide (10) and 1,5-diazidopentane (13) with benzoyl cyanide. Most of the prepared compounds have been characterized by: TLC, FT-IR, 1H NMR, 13C NMR, LC-MS and microelemental analysis

Publication Date
Fri Nov 24 2023
Journal Name
Iraqi Journal Of Science
Synthesis, Characterization and Evaluation Antimicrobial Activity of Some New substituted 2-Mercapto-3-Phenyl-4(3H)-Quinazolinone
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This work includes synthesis of new heterocyclic derivatives of 2-mercpto-3-phenyl-4(3H)-quinazolinone bearing 1, 2, 4-triazole and acetylenic amines moieties by using two ways. The first way includes reaction of 2-mercpto-3-phenyl-4(3H)-quinazolinone (1) with ethyl-2-bromopropanoate in methanol as solvent to gives ester derivative (2). Then, compound (2) was converted to (hydrazide, simecarbazid, phenylsimecarbazide and thiosimecarbazide) derivatives through its reactions with (hydrazine hydrate, simecarbazid, phenylsimecarbazide and thiosimecarbazide) respectively to give compounds (3-6). Finally, the cyclization of compounds (4-6) in alkaline media (4N-NaOH) gave the corresponding substituted triazole derivatives (7-9) respectively. W

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Publication Date
Sun Jun 01 2008
Journal Name
Baghdad Science Journal
A New Derivatives of Benzodiazepine, Imidazole, Isatin, Maleimide, Pyrimidine and 1,2,4-Triazole: Synthesis and Characterization
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The synthesis of new benzodiazepine, imidazole, isatin, maleimide, pyrimidine and 1,2,4-triazole derived from 2-amino-4-hydroxy-1,3,5-triazine, via its cyclocondensation reaction with different organic reagents, is described. FT-IR, 1H-NMR and as well as 13C-NMR spectra disclosed the structures of the precursors and heterocyclic derivatives formed.

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Publication Date
Sun Jun 20 2021
Journal Name
Ijddt
Synthesis, antioxidant activity and molecular docking study of 1, 2, 4-Triazole and their corresponding fused rings containing 2-Methylphenol
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Newly 4-amino-1,2,4-triazole-3-thione ring 2 was formed at position six of 2-methylphenol from the reaction of 6-(5-thio1,3,4-oxadiazol-2-yl)-2-methylphenol 1 with hydrazine hydrochloride in the presence of anhydrase sodium acetate. Seven newly fused heterocyclic compounds were synthesized from compound 2. First fused heterocyclic was 6-(6-(3,5-di-tertbutyl-4-hydroxyphenyl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-3-yl)-2-methylphenol 3 synthesized from reaction compound 2 with 3,5-di-tert-butyl-4-hydroxybenzoic acid in POCl3. Reaction compound 2 with bromophencylbromide afford 6-(6-(4-bromophenyl)-5H-[1,2,4]triazolo[3,4-b][1,3,4]-thiadiazin-3-yl)-2-methylphenol 4. 6-(6-thio-1,7a-dihydro-[1,2,4] triazolo[3,4-b][1,3,4]-thiadiazol-3-yl)-2

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Publication Date
Sun Dec 25 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Molecular Docking Study and Cytotoxicity Evaluation of some Quinazolinone Derivatives as Nonclassical Antifolates and Potential Cytotoxic Agents
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Abstract

A series of new 4(3H)-quinazolinone derivatives (S1-S4) were synthesized and characterized   by FTIR,1HNMR and 13CNMR .Their cytotoxic activity against a set of human cancer cell lines MCF-7 (breast) and A549 (lung) was evaluated using MTT assay. To detect their selectivity toward cancer cells, the compounds were also tested against epithelial cells derived from normal human fibroblast (NHF). Methotrexate (MTX) was used as a reference for comparison . All the tested compounds exhibited toxicity against the normal cells lower than cancer cells. All the tested compounds displayed higher cytotoxicity against lung cancer cell line (A549) than MTX with the most

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Publication Date
Wed Sep 28 2022
Journal Name
Research Journal Of Pharmacy And Technology
Synthesis, Characterization and Preliminary Antimicrobial Evaluation of New Schiff bases and Aminothiadiazole Derivatives of N- Substituted Phthalimide
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A new series of schiff base and aminothiadiazole derivatives of N- substituted phthalimide (I-VI) were synthesized. In this work, the intermediate 4-(1,3-dioxoisoindolin-2-yl)benzaldehyde compound (I), was formed by reaction of 4-amino benzaldehyde with phthalic anhydride in glacial acetic acid(GAA). A series of Schiff bases (IV-VI) was prepared by the reaction of benzidine with compound (I) in ethanol and presence of GAA as a catalyst to form compound (IV) which react with compound (I) and p-nitro benzyldehyde to give compound (V) and (VI) respectively. A new phthalimide thiosemi-carbazone derivative (ll) was prepared by reaction of compound (l) with thiosemi-carbazide HCl in the presence of equimolar amount of sodium acetate. Fina

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Publication Date
Mon Feb 08 2016
Journal Name
Iraqi Journal Of Science,
Synthesis, Identification and Evaluation Biological Activity for Some New Triazole, Triazoline and Tetrazoline Derivatives From 2-Mercapto-3- phenyl-4(3H)Quinazolinone
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This research, involved synthesis of some new 1,2,3-triazoline and 1,2,3,4- tetrazole derivatives from antharanilic acid as starting material .The first step includes formation of 2-Mercapto-3-phenyl-4(3H)Quinazolinone (0) through reacted of anthranilic acid with phenylisothiocyanate in ethanol, then compound (0) reaction with chloro acetyl chloride in dimethyl foramamide (DMF) to prepare intermediate S-(α-chloroaceto-2-yl)-3-phenylquinazolin-4(3H)-one (1); compound (1) reacted with sodium azide to yield S-(α-azidoaceto-2-yl)-3-phenylquinazolin-4(3H)-one (2), while Schiff bases (3-10) were prepared from condensation of substituted primary aromatic amines with different aromatic aldehydes in absolute ethanol as a solvent. Compound (2)

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Publication Date
Sat Jun 29 2024
Journal Name
Iraqi Journal Of Pharmaceutical Sciences( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Characterization of New 5-Fluoroisatin-Chalcone Conjugates with Expected Antimicrobial Activity
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Pathogenic microorganisms are becoming more and more resistant to antimicrobial agents. So the synthesis of new antimicrobial agents is very important. In this work, new 5-fluoroisatin-chalcone conjugates 5(a–g) were synthesized based on previous research that showed the modifications of the isatin moiety led to the synthesis of many derivatives that have antimicrobial activity. 4-aminoacetophenone reacts with 5-fluoroisatin to form Schiff base (3), which in turn reacts with two different groups of aromatic (carbocyclic and heterocyclic) aldehydes 4(a–g) separately to form the final compounds 5(a–g). Proton-nuclear magnetic resonance (¹H-NMR) and Fourier-transform infrared (FT-IR) spectroscopy were used to confirm the chemic

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Publication Date
Thu Mar 09 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
New Schiff Base Derived From Folic Acid and 3Aminoacetophenone and its Metal Complexes with Some Transition Metals and Evaluation of Their Biological Activity
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 The ligand [Potassium (E)-(4-(((2-((1-(3-aminophenyl) ethylidene) amino)-4-oxo-1,4dihydropteridin-6-yl) methyl) amino)benzoyl)-L-glutamate] was prepared from the condensation reaction of folic acid with (3-aminoacetophenone) through Schiff reaction to give a new Schiff base ligand [H2L]. The ligand [H2L] was characterized by elemental analysis CHN, atomic absorption (A.A), (FT-I.R.), (U.V.-Vis), TLC, E.S. mass (for spectroscopes), molar conductance, and melting point. The new Schiff base ligand [H2L], reacts with Mn(II), Co(II), Ni(II), Cu(II), Cr(III) and Cd(II) metal ions and (2-aminophenol), (metal : derivative ligand : 2-aminophenol) to give a series of  new mixed complexes in  the general formula:- K3[M2(HL)(HA)2], (

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