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Synthesis, Antibacterial, and Molecular Docking Study of Novel 2-Chloro-8-Methoxy-3-Aryl-[1,3] Benzoxazine Derivatives using Vilsmeier Reagent
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Reducing of ethyl 4-((2-hydroxy-3-methoxybenzylidene)amino)benzoate (1) afford ethyl 4-((2-hydroxy-3-methoxybenzyl)amino)benzoate (2). Reaction of this compound with Vilsmeier reagent affords novel 2-chloro-[1,3] benzoxazine ring (3). The corresponding acid hydrazide of compound 3 was synthesized from reaction of compound (3) with hydrazine hydrate. Newly series of hydrazones (5a–i) were synthesized from reaction of acid hydrazide with various aryl aldehydes. Antibacterial activity of the hydrazones was secerned utilizing gram-negative and gram-positive bacteria. Compound (5b) and (5c) exhibited significant antibacterial ability against both gram-negative and gram-positive bacteria, while the compounds (5a) showed mild antibacterial activity. Compounds (5d–i) did not display notable activity. The molecular docking of synthesised compounds were tested inside the pocket of bacterial gyrase enzyme target site by using MOE 2015 software, which acts as Adenosine triphosphate (ATP)-binding domain bacterial gyrase enzyme pocket and novobiocin was used as reference.

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Publication Date
Sun Mar 04 2012
Journal Name
Baghdad Science Journal
Synthesis of New Mannich Bases from Indole Derivatives
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This work includes two steps of synthesis, the first one is the synthesis of indole which was prepared according to literature of the reaction of phenyl hydrazine with acetaldehyde in glacial acetic acid afforded phenyl hydrazone of acetaldehyde , this product was fused with zinc chloride to give the indole.Reaction of cyclohexanone with phenyl hydrazine using the same procedure for the preparing giving 1,2,3,4-Tetrahydrocarbazole.Second step involved synthesis of a series of (17) of mannich bases derivatives of indole and 1,2,3,4-Tetrahydrocarbazle. Mannich reaction involves the condensation of aldehyde usually formaldehyde with different secondary amine and with compound containing an activated hydrogen.The reaction illustrated by the fo

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Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis, Characterization of Derivatives Tetrazoles for Trimethoprim Drug
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The present work involved synthesis of serval new substituted tetrazole via Schiff bases for trimethoprim drug by two steps. The first step involved direct reaction of different ketones and aldehydes with trimethoprim producing the corresponding Schiff bases (1-10), whereas the second step, involved preparation new tetrazoles derivatives (11-20) through reaction of the ready Schiff bases (in the first step) with sodium azidein in dioxin. The prepared compounds were characterized by UV, FT-IR, and some of them by 13C-NMR, 1H-NMR spectroscopy and physical properties.

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Publication Date
Tue Dec 16 2014
Journal Name
Iraqi National Journal Of Chemistry
Synthesis of Novel Heterocyclic Compounds via Schiff bases
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In the present study a series of some four-,five-and seven-membered heterocyclic compounds have been synthesized by the reaetion of Schiff bases (1a,b) with chloroacetyl chloride, sodium azide, thioglycolic acid or various anhydrides to give azetidinone (2a,b), tetrazole (3a,b), thiazolidinone (4a,b) and 1,3-oxazepine derivatives (5-8a,b) respectively. Schiff bases (1a,b)were prepared from the reaction of p-toluidine with aromatic aldehydes. All synthesized compounds were characterized by physical properties and spectral data.

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Publication Date
Tue Jun 05 2018
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization and Alpha Glucosidase Inhibition activity of new Phthalimide Derivatives
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 Three of imide intermediate products  were synthesized by reacting of phthalic anhydride with glycine (2a), and tetrachloro phthalic anhydride with glycine , (S)-2-[(tert-Butoxycarbonyl)amino]-3-aminopropionic acid ( 2b,c)  respectively   in  dry toluene  with azeotropic removal of water using Dean- stark apparatus then carboxyl functional group activated by refluxing with  thionyl chloride, the resulted acid chloride (3a-c) were reacted with different amine (5-flourouracil, 4-chloroaniline, 4-bromoaniline, 2-amino thiazole, and pyrrolidine) (4a-e) , the   resulted products consider as

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Publication Date
Mon Mar 01 2021
Journal Name
Journal Of Physics: Conference Series
Synthesis and characterization of some new thiazolidinone derivatives containing indole ring
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Many new heterocyclic compounds including 4-thiazolidinones containing indole with triazole units were described. The new Schiff bases [VII] a, b and [VIII] a, b synthesized by condensation acid hydrazides [II],[VI] with different (aromatic) aldehydes in absolute ethanol. The refluxing equimolar amounts of the Schiff bases ([VII] a, b,[VIII] a, b) with thioglycolic acid in benzene led to get thiazolidin-4-ones derivatives ([IX] a, b and [X] ad). Finally, the new derivatives [XI] ac run out via the reacted compound [IX] a with different n-alkyl bromide (methyl bromide, ethyl bromide, and butyl bromide)

Publication Date
Sun Jun 09 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization and Preliminary Anti-inflammatory Evaluation of New Etodolac Derivatives
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Three new hydrazone derivatives of Etodolac were synthesized and evaluated for their anti-inflammatory activity by using egg white induced paw edema method. All the synthesized target compounds were characterized by CHN- microanalysis, FT-IR spectroscopy, and 1HNMR analysis. The synthesis of the target (P1-P3) compounds was accomplished following multistep reaction procedures. The synthesized target compounds were found to be active in reducing paw edema thickness and their anti-inflammatory effect was comparable to that of the standard (Etodolac).

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Publication Date
Mon Mar 01 2021
Journal Name
Journal Of Physics: Conference Series
Synthesis and characterization of some new thiazolidinone derivatives containing indole ring
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Abstract<p>Many new heterocyclic compounds including 4-thiazolidinones containing indole with triazole units were described. The new Schiff bases [VII]<sub>a, b</sub> and [VIII]<sub>a,b</sub> synthesized by condensation acid hydrazides [II],[VI] with different (aromatic) aldehydes in absolute ethanol. The refluxing equimolar amounts of the Schiff bases ([VII]<sub>a,b</sub>, [VIII]<sub>a,b</sub>) with thioglycolic acid in benzene led to get thiazolidin-4-ones derivatives ([IX]<sub>a,b</sub> and [X]<sub>a-d</sub>). Finally, the new derivatives [XI]<sub>a-c</sub> run out via the reacted compound [IX]<sub>a</sub> with di</p> ... Show More
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Publication Date
Thu Dec 29 2016
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Characterization of New Symmetrical Pyromellitdiimide Derivatives and Their Amic Acids
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               The new symmetry pyromellitdiimide [VII]a-c,n  were synthesized by two-step reactions from the corresponding pyromellitic dianhydride . A new symmetrical amic acid [VI]a-c,n was synthesized by the reaction of pyromellitic dianhydride with different heterocyclic amines in dry acetone . The second reaction step includes  intramolecular cyclization of amic acid in the presence of  sodium acetate -acetic anhydride system at 850C. Structures  of  the synthesized compounds have been ascertained by their melting points , C.H.N analysis , UV-Vis, FTIR and 1HNMR spectroscopy.

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Publication Date
Mon Feb 01 2021
Journal Name
Iop Conference Series: Materials Science And Engineering
Azo Coupling Reaction for indirect Spectrophotometric Determination of Furosemide using Resorcinol as a Reagent
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Abstract<p>A simple and accurate method to determinate furosemide (FUR) based on converting the secondary amine to primary amine with acidic hydrolysis then azotization by nitrous acid and coupled with resorcinol as a coupling agent in aqueous medium at pH 13. The optical characteristic like beers law limit found to be (0.25-2.5) μg.ml<sup>−1</sup>, detection and quantification limits (0.0196) (0.0654) μg.ml<sup>−1</sup>respectivly and Sandel sensitivity was 0.006738 μg.cm<sup>−2</sup>. The least-square method was used to evaluate the regression equation and the correlation coefficient. The resulted azo dye has a maximum absorbance at 430 nm with light oran</p> ... Show More
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Publication Date
Tue Jan 01 2013
Journal Name
Chemical And Process Engineering Research
Synthesis and Characterization of Complexes of Schiff Base [1, 2-Diphenyl -2- 2-{[1-(3-Amino-Phenyl)-Ethylidene]-Hydrazono Methyl}-Phenol] with Mn(II), Fe(II), Co(II), Cu(II), Zn(II), Cd(II), Ni(II), and Hg(II) Ions
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The new tridentate Schiff base ligand (HL)namely 2-{[1-(3-amino-phenyl)-ethylidene]-hydrazono methyl}- phenol containing (N N O)as donors atoms was prepared in two steps:Step (1): By the reaction of 3- aminoacetophenone with hydrazine monohydrate under reflux in methanol and drops of glacial acetic acid gave the intermediate compound 3-(1- hydrazono ethyl)-phenol amine.Step (2): By the reaction of 3-(1-hydrazono ethyl)-phenol amine with salicyaldehyde under reflux in methanol, gave the ligand (HL).The prepared ligand was characterized by I.R, U.V-Vis,1H- 13C NMR spectra and melting point and reacted with some metal ions under reflux in methanol with (1:1) ratio gave complexes of the general formula: [MClL]. Where: M= Mn(II), Fe(II), Co(II),

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