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Synthesis, Antimicrobial evaluation and Docking study of new Schiff bases of benzo[d]oxazol-5-amine derivatives.
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Objective: Benzoxazole derivatives have antifungal, anticancer, antibacterial, and anticonvulsant function. Encouraged by this comment, we agreed to synthesize new Benzoxazole compounds connected to the bases of Schiff's. Methods: 2,4-diaminophenol (1) was prepared by the reaction of 2,4-dinitrophenol and sodium dithionate. Compound (1) reacted with either acetic acid to afford compound (2) or with formic acid to afford compound (3). The Schiff bases were preparation from the reaction condensing reaction of compound (2) or (3) and aromatic aldehydes or ketone; [p-nitrobenzaldehyde, p-hydroxybenzaldehyde, p-chlorobenzaldehyde, p-bromoacetophenone and terephthaldehyde]. Results: FTIR and 1H-NMR spectroscopy characterized all of the preparation compounds. The synthesized derivatives against (Gram positive bacteria GPB) (Bacillus subtilis) and two (Gram-negative bacteria GNB) (Klebsiella pneumoniae and Escherichia coli) and (one fungal species Candida albicans), have been evaluated to their antibacterial activity in vitro. all results showed which most of them have good antibacterial activity, while their antifungal activity revealed that compounds displayed slight antifungal activity. The synthesized Benzoxazole derivatives were docked using, glucosamine 6-phosphate synthase as a ligand. Conclusion: The antimicrobial activity indicates that compounds (4), (7) and (8) have more potent antibacterial activity than the compounds (5) and (6). Molecular docking study revealed that compounds (7) and (8), with bulky phenyl groups are essential to block the active centers of (GluN-6-Ps) amino acids synthase in the bacteria.

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Publication Date
Thu Dec 16 2021
Journal Name
Journal Of Advance Research In Chemical Sciences
Study of Schiff Bases Complexes of Trimethoprim: A Review
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Trimethoprim derivative Schiff bases are versatile ligands synthesized with carbonyl groups from the condensation of primary amines (amino acids). Because of their broad range of biological activity, these compounds are very important in the medical and pharmaceutical fields. Biological activities such as antibacterial, antifungal and antitumor activity are often seen. Transition metal complexes derived from biological activity Schiff base ligands have been commonly used.

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Publication Date
Thu Sep 16 2021
Journal Name
Journal Of Advance Research In Chemical Sciences
Study of Schiff Bases Complexes of Trimethoprim: A Review
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Trimethoprim derivative Schiff bases are versatile ligands synthesized with carbonyl groups from the condensation of primary amines (amino acids). Because of their broad range of biological activity, these compounds are very important in the medical and pharmaceutical fields. Biological activities such as antibacterial, antifungal and antitumor activity are often seen. Transition metal complexes derived from biological activity Schiff base ligands have been commonly used

Publication Date
Tue Nov 01 2022
Journal Name
Chemical Methodologies
Synthesis and Characterization of New Substituted Coumarin Derivatives and Study Their Biological Activity
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New substituted coumarins derivatives were synthesized by using nitration reaction to produce different nitro coumarin isomers which were separated from these isomers by using different solvent, and the reduction of nitro compounds was done to give corresponding amino coumarins. Temperature and reaction time of reaction were very important factors in determining the most productive nitro isotopes. A low temperature for three hours was sufficient to give a high product of a compound 6-nitro coumarin while increasing the temperature for a period of twenty-four hours that gave a high product of 8-nitro-coumarin. The synthesized compounds were confirmed by FT-IR,1 H-NMR, and13 C-NMR spectroscopy and all final compounds were tested for their ant

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Publication Date
Fri Mar 28 2014
Journal Name
Advances In Life Science And Technology
Synthesis and Characterization of Novel Schiff Bases, N-Acyl and Diazetines Derived from 3-((5-hydrazinyl-4-phenyl-4H-1,2,4- triazol-3-yl)methyl)-1H-indole
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This work involves synthesis of some new heterocyclic compounds including 1, 3-diazetine. The new Schiff bases [VI] ad derived from 3-((5-hydrazinyl-4-phenyl-4H-1, 2, 4-triazol-3-yl) methyl)-1H-indole [V] which was synthesized by refluxing 5-((1H-indol-3-yl) methyl)-4-phenyl-4H-1, 2, 4-triazole-3-thiol [IV] with hydrazine hydrate in absolute ethanol and this amino compound [V] condensation with different aromatic aldehydes in absolute ethanol to yielded a new Schiff bases [VI] ad. N-acyl compounds [VII] ad were synthesized by addition reaction of acetyl chloride to imine group of Schiff bases in dry benzene. The new diazetine derivatives [VIII] ad synthesized by the reaction of N-acyl compounds [VII] ad with sodium azide in dimethylformamid

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Publication Date
Wed Apr 12 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
From Amine , Synthesis and Characterization of New Some Transition and Non-Transition Elemnts Metal Dinuclear Complexes Derived Schiff Base ligand 1- Chloro – 2- ( 2- chroroethoxy) Ethan
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   This research of the thesis includes the preparation and identification of two new tetra dentate Schiff's base ligand .        (H4L1 ) and then binuclear complexes with a group of transition metal ions in addition to cadmium with the general formula. [M2(L1)Cl2(H2O)2] M+2=[Mn,Co,Ni,Cu and Cd]    The prepared complexes and ligands were identified by in pared(FT-IR) spectroscopy ,Ultra violet-visible(UV-visible) spectroscopy and H-NMR spectroscopy of the prepared ligand, also microanalysis (C.H.N) of some of the prepared compounds has been carried out and the melting points, the molar conductivity and magnetic susceptibility  

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Publication Date
Sun Jun 02 2013
Journal Name
Baghdad Science Journal
Synthesis of New Pyrazoline - Phenoxathiin Derivatives
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Phenoxathiin was prepared by the reaction of diphenyl ether with sulfur in the presence of anhydrous aluminum chloride. This work comprised the synthesis of new phenoxathiin derivatives containing heterocyclic moieties. These heterocyclic compounds were synthesized in three groups. The first group was made up of 2-(oxoalken-1-yl) phenoxathiin derivatives (3a-3j) obtained from the reaction of 2-acetylphenoxathiin with different aromatic aldehyde in the presence of sodium hydroxide. The other two groups involved compounds produced from the reaction of (3a-3j) with hydrazine hydrate in acetic acid to get 2-(1-acetyl pyrazolin-3-yl) phenoxathiin derivatives (4a-4j), and phenyl hydrazine in the presence of piperidine to afford 2-(1-phenyl pyrazo

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Publication Date
Tue Jun 01 2010
Journal Name
Al-mustansiriya Journal For Sciences And Education
Synthesis and Identification of metal complexes of 1-phenyl-3,(2-(5-phenyl amine-1,3,4-thiadiazole-2-yl) phenyl thiourea
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Complexes of 1-phenyl-3-(2(-5-(phenyl amino)-1,3,4-thiadiazole-2-yl)phenyl) thiourea have been prepared and characteizedby elemental analysis, Ff-[R, and u.v./ visible spectra moreover,determination of metal content M%o by flame atomic absorptionspectroscopy, molar conductance in DMSO solution and magneticmoments (peffl.The result showed that the ligand (L) was coordinated to Mn+2, Ni+2,Ct+2,2n+2,Cd+2, and Hg+2 ions through the nitrogen atoms and sulpheratoms.From the result obtained, rhe following general formula [MLCl2] hasbeen given for the prepared complexes with an octahedral geometryaround the metal ions for all complexes.where M= Mn+2, Ni+2, cu+2, zn+2, cd+2, and Hg+2 l= l-phenyl-3-(2-(5-(phenyl amino

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Publication Date
Thu Feb 01 2024
Journal Name
Doklady Chemistry
Synthesis, Characterization, and Biological Evaluation of New Cyclic Quinazoline Derivatives as Potential Antibacterial and Antifungal Agents
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Heterocyclic compounds are crucial for medicinal chemistry and the development of therapeutic agents like broad-spectrum antibiotics. This study devised a facile procedure to synthesize novel antimicrobial bicyclic heterocycles from 2-mercapto-3-phenylquinazolin-4(3H)-one. Advanced analytical techniques including 1 H and 13C NMR, elemental analysis, and FT-IR spectroscopy characterized the intricate chemical structures of the products. In vitro assays tested the heterocycles against aerobic and anaerobic bacterial strains using fluconazole and ciprofloxacin as antifungal and antibacterial controls. Results demonstrated the formidable broad-spectrum antibacterial and antifungal activities of the synthesized compounds, with growth inhibition

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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
Sun Mar 07 2010
Journal Name
Baghdad Science Journal
Synthesis of New Heterocyclic Derivatives from 4-(3, 5-Dimethyl-1-phenyl-1H-pyrazol-4-ylazo)- benzoic acid
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In this work pyrazolin derivatives were prepared from the diazonium chloride salt of 4-aminobenzoic acid. Azo compounds were prepared from the reaction of an ethanolic solution of sodium acetate and calculated amount of active methylene compound namely, acetyl acetone to obtain the corresponding hydrazono derivative (1). Cyclocondensation reaction of compounds (1) with hydrazine hydrate and phenyl hydrazine in boiling ethanol affording the corresponding pyrazoline-5-one derivatives of 4-aminobenzoic acid (2,3). Then compound (3) was reacted with thionyl chloride to give the corresponding acid chloride derivative(4), followed by conversion into the corresponding acid hydrazide derivative (5) carboxylic acid thiosemicarbazide (11), esters

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