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Synthesis, Characterization, and Preliminary Evaluation of Antimicrobial activity of Imines derived from Vanillic Acid Conjugated to Heterocyclic
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The purpose of this research is to prepare new vanillic acid derivatives with 1,2,4-triazole-3-thiol heterocyclic ring and evaluate their antimicrobial activity in a preliminary assessment. A multistep synthesis was established for the preparation of new vanillic acid-triazole conjugates. The intermediate of 4-(4-amino-5-mercapto-4H-1,2,4-triazol-3-yl)-2-methoxyphenol (4) reacts with different heterocyclic aldehydes (thiophene-2-carboxaldehyde, pyrrole-2-carboxaldehyde, thiophene-3-carboxaldehyde, and furfural ) in ethanol containing few drops of acetic acid yielded the corresponding 4-(4-(substituted amino)-5-mercapto-4H-1,2,4-1triazol-3-yl)-2-methoxy phenol derivatives (5-8). These compounds were characterized spectroscopically by FT-1IR and 1H-1NMR. These imine derivatives (5-8) were tested for their antimicrobial activity and compared with three different standard references (amoxicillin, ciprofloxacin, and fluconazole). Overall, compounds 6 and 8 exhibited varying degrees of inhibitory effects on the growth of the examined bacterial species and fungus. The most active one is compound 6 having pyrrole ring imine derivative showed potent activity against C. 1albicans and moderate activity against all tested bacteria compared to other derivatives but no activity toward P. 1aeruginosa and P. 1mirabilis.

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Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis and characterization Studies of Metal Complexes with Schiff base derived from 4-[5-(2-hydoxy-phenyl)-[1,3,4-oxadiazol-2-ylimino methyl]-1,5-dimethyl-2-phenyl-1,2-dihydro-pyrazol-3-one
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New metal complexes of the ligand 4-[5-(2-hydoxy-phenyl)-[1,3,4- oxadiazol -2-ylimino methyl]-1,5-dimethyl-2-phenyl-1,2-dihydro-pyrazol-3-one (L) with the metal ions Co(II), Ni(II), Cu(II) and Zn(II) were prepared in alcoholic medium. The Schiff base was synthesized through condensate of [4-antipyrincarboxaldehyde] with[2-amino-5-(2-hydroxy-phenyl-1,3,4- oxadiazol] in alcoholic medium . Two tetradentate Schiff base ligand were used for complexation upon two metal ions of Co2+, Ni2+, Cu2+ and Zn2+ as dineucler formula M2L2.4H2O. The metal complexes were characterized by FTIR Spectroscopy, electronic Spectroscopy, elemental analysis, magnetic susceptidbility measurements, and also the ligand was characterized by 1H-NMR spectra, and m

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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
Sat Jan 03 2026
Journal Name
Journal Of Molecular Structure
Synthesis, characterization, DFT calculations, molecular docking, ADMET analysis and biological activity of Schiff base metal complexes against colon cancer cells
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Publication Date
Tue May 01 2018
Journal Name
Journal Of Physics: Conference Series
Cytotoxic effects of new synthesis heterocyclic derivatives of Amoxicillin on some cancer cell lines
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A new Schiff base [I] was prepared by refluxing Amoxicillin trihydrate and 4-Hydroxy- 3,5-dimethoxybenzaldehyde in aqueous methanol solution using glacial acetic acid as a catalyst. The new 1,3-oxazepine derivative [II] was obtained by Diels- Alder reaction of Schiff base [I] with phthalic anhydride in dry benzene. The reaction of Schiff base [I] with thioglycolic acid in dry benzene led to the formation of thiazolidin-4-one derivative [III]. While the imidazolidin-4-one [IV] derivative was produced by reacting the mentioned Schiff base [I] with glycine and triethylamine in ethanol for 9 hrs. Tetrazole derivative [V] was synthesized by refluxing Schiff base [I] with sodium azide in dimethylformamid DMF. The structure of synthesized compound

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Publication Date
Wed Sep 02 2020
Journal Name
International Journal Of Drug Delivery Technology
Synthesis of Levofloxacin Derivatives with some Amines and their Complexes with Copper(II) Salts and Evaluation of their Biological Activity
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Levofloxacin belongs to the fluoroquinolone family; it is a potent broad-spectrum bactericidal agent. The pharmacophore required for significant antibacterial activity is the C-3 carboxylic acid group and the 4-pyridine ring with the C-4 carbonyl group, into which binding to the DNA bases occur. In this work, we tried to show that by masking the carboxyl group through amide formation using certain amines to form levofloxacin carboxamides, an interesting activity is kept. Levofloxacin carboxamides on the C-3 group were prepared, followed by the formation of their copper complexes. The target compounds were characterized by FT-IR, elemental analysis. The antimicrobial activity of the target compounds was evaluated and showed satisfactory resu

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Publication Date
Thu Oct 26 2023
Journal Name
Malaysian Journal Of Science
HEMICAL ELUCIDATION AND BIOLOGICAL SCREENING STUDY OF NEW LIGAND DERIVED FROM 5, 6-O-ISO PROPYLIDENE-L-ASCORBIC ACID AND ITS METAL (II) COMPLEXES
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الوصف A simple chemistry method approach was used to synthesise new ligand derivate from L-ascorbic acid and its complexes. All of them were water-soluble and are used quite extensively in the medical and pharmaceutical fields. This study synthesised the new ligand derivative from L-ascorbic acid-base using the following steps: A 5, 6-O-isopropylidene-L-ascorbic acid was prepared by reacting dry acetone with L-ascorbic acid followed by reacting it with trichloroacetic acid to yield [chloro (carboxylic) methylidene]-5, 6-O-isopropylidene-L-ascorbic acid in the second stage. In the third stage, the derivative was reacted with (methyl (6-methyl-2-pyridylmethyl) amine to create a new ligand (ONMILA). This novel ligand was identified using

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Publication Date
Wed Sep 05 2018
Journal Name
Journal Of Education And Scientific Studies
Ligand-Mixed New of Evaluation Bacterial and Characterization ,Synthesis Some with phenanthroline1,10- and Dithiocarbamate Containing Complexes ions M
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(phen) (L(M [formula general a with complexes ligand-mixed new of series A methods analyses different by characterised and synthesised been have ,ligand arysecond as phenanthroline1,10- = phen and ligand primary as dithiocarbamate-1-azolebenzoimid-H-1)sulfinyl)methyl)yl-”-2pyriden)trifluroethoxy2,2,2- “(-4-methyl3-(((2-Sodium = L,ZnIIandCdII,CuII,NiII,CoII= M where,Cl)]phen)(L(Pd [Cland]2)O2H( ligands to metal ,moments magnetic and ,elementalanalysis ,spectrum mass ,surementsmea conductivity ,analysis thermal ,spectroscopy Vis-UV ,IR-FT ,NMR-C,13 H1 such dithiocarbamate the with formed coordination anisobidentate that showed spectra IRFT The.)phen:dithiocarbamate:M) (1:1:1(be to found been has complexes all in ratio nitrogen th

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Publication Date
Tue May 28 2024
Journal Name
Plant Science Today
Isolation and identification of hyperin and naringenin from guava cultivated in Iraq and evaluation of cytotoxic activity of hyperin
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The guava plant, Psidium guajava L., serves as proof of the abundant donations of nature, providing a delicious guava fruit; this plant is rich in groups of medicinal and nutritional benefits. Guava belonging to the Myrtaceae family, many previous studies reported many phytochemical constituents in its leaves that have many pharmacological activities and medicinal properties; this study focuses on the isolation, structural elucidation and calculation concentration of flavonoids, assessment of the cytotoxic activityof hyperin from Psidium guajava leaves newly cultivated in Iraq. The isolation process involved the use of thin-layer chromatography (TLC) and preparative high-performance liquid chromatography (PHPLC) and structural eluci

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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
Wed Jul 01 2020
Journal Name
International Journal Of Pharmaceutical Research
Synthesis, characterization of new Schiff base compounds contains 5H-thiazolo[3,4-b][1,3,4] thiadiazole and study its biological activity
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A new derivatives of Schiff bases connected with 5H-thiazolo[3,4-b][1,3,4]thiadiazole ring 5a-c were prepared via many reactions starting by treating 1,4-phenylene diamine 1 with chloroacetylchloride to prepared compound 2, then reaction with p-hydroxybenzaldehyde to synthesize compound 3 then, this was reacted with thioglycolic acid and thiosemicarazide to giveN,N-(1.4-phenylene)bis(2-(4-(2-amino-5Hthiazolo[4,3-b][1,3,4]thiadiazol-5-yl)phenoxy)acetamide) 4. Compound 4 was treated with different aromatic aldehydes to give a new derivatives of Schiff bases containing 5H-thiazolo[3,4-b][1,3,4]thiadiazole ring 5a-c. The synthesized compounds were characterized using FTIR spectrophotometer and 1H NMR spectroscopy and the biological activity of

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