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bijps-731
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 the end products (5a-j) while  the compounds (5k-o) required further reaction to deprotect aliphatic amine this achieved by treating the compounds with TFA to remove tert-Butoxycarbonyl group (6a-e).

The alpha glucosidase inhibitory activity of some synthesized compounds (5a, 5f, 6a) were tested by using  -glucosidase from Saccharomyces cerevisiae, p-nitrophenol glucopyranoside (pNPG)  used as substrate and acarbose used as standard.

All these test compounds shows   excellent inhibitory activity according to IC50 values which is ranging from (4.61-7.32).

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Publication Date
Thu Feb 01 2024
Journal Name
Indonesian Journal Of Chemistry
Synthesis, Characterization, and Evaluation of MCF-7 (Breast Cancer) for Schiff, Mannich Bases, and Their Complexes
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A new synthesis of Schiff (K) 6 and Mannich bases (Q) 7 had formed compound (Q) 7 by reacting compound (K) with N-methylaniline at the presence of formalin 35% to given Mannich base (Q). Additionally, new complexes were formed by reacting Schiff base (K) with metal salts CuCl2·2H2O, PdCl2·2H2O, and PtCl6·6H2O by 2:1 of M:L ratio. New ligands and their complexes were characterized, exanimated, and confirmed through several techniques, including FTIR, UV-visible, 1H-NMR, 13C-NMR spectroscopy, CHN analysis, FAA, TG, molar conductivity, and magnetic susceptibility. These compounds and their complexes were screened against breast cancer cells. It was determined that several of these compounds had a significant anti-breast cancer effec

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Publication Date
Wed Aug 13 2025
Journal Name
Molecular Crystals And Liquid Crystals
Synthesis, characterization and mesomorphic behavior of twin pyrazole ligands and their metal complexes containing dithiocarbamat units
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Publication Date
Thu Oct 31 2019
Journal Name
Asian Journal Of Pharmaceutical And Clinical Research
DESIGN, SYNTHESIS, DOCKING, ANTITUMOR SCREENING, AND ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION PREDICTION OF NEW HESPERDIN DERIVATIVE
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Objective: Hesperidin (HSP) is a pharmacologically active organic compound found in citrus fruits and peppermint. We synthesized a new HSP derivative by reacting it with 5-Amino-1,3,4-thiadiazole-2-thiol in acetic acid. Methods: This compound was characterized by Fourier-transform infrared, proton nuclear magnetic resonance, and electron impact mass spectra. A molecular docking study explores the predicted binding of the compound and its possible mode of action. Bioavailability, site of absorption, drug mimic, and topological polar surface was predicted using absorption, distribution, metabolism, and excretion (ADME) studies. Results: The docking study predicts that the new compound binds to the active sites of Aurora-B

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Publication Date
Wed Jul 07 2010
Journal Name
Al-mustansiriya J. Sci
Synthesis and Spectroscopic Studies of New Heterocyclic Azo Dye and Their Complexes with Selected Metal Ion
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Coupling reaction of 4-aminoantipyrene with 8-hydroxyqunoline gave the new bidentate azo ligand 5-(4-antipyrene azo)-8-hydroxyqunoline. Treatment of this ligand with the following metals ions (MnII, CoII, NiII, CuII and ZnII) in aqueous ethanol with a 1:2 M:L ratio yielded a series of neutral complexes of the general formula [M(L)2Cl2]. The prepared complexes were characterized using flame atomic absorption, FT.IR, UV-Vis spectroscopic as well as magnetic susceptibility and conductivity measurements. Chloride ion content were also evaluated by (Mohr Method). From above data, the proposed molecular structure for these complexes as octahedral geometry.

Publication Date
Fri Sep 25 2020
Journal Name
International Journal Of Drug Delivery Technology
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 antibacteri

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Publication Date
Thu Jul 02 2020
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Antibacterial and Molecular Docking Study of Novel 2-Chloro-8-Methoxy-3-Aryl-[1,3] Benzoxazine Derivatives Using Vilsmeier Reagen
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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 wassecerned 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 activit

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Publication Date
Sun Jan 20 2019
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis, Antibacterial and Antifungal Activities for Novel Derivatives of 2,2'-(((1-benzylbenzoimidazol-2-yl)methyl)azanediyl)bis(ethan-1-ol)
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The compound 2,2'-(((1H-benzo(d)imidazol-2-yl)methyl)azanediyl)bis(ethan-1-ol) was reacted with benzyl bromide to afford compound (1) which used as row material to prepare a series of compounds through condensation reaction, the starting compound were reacted with tosyl chloride to protect the OH group  to afford compound 2, then reacted benzyl bromide to produce compound (2), then the compound (2) treated with three compounds ( 2-mercaptobenzthiazole, 2-mercaptobenimidazol and 2-chloromethyl benzimidazole) to form compounds 3a,b, 4a,b and 5a,b respectively. In the another step the click reaction of compound 2,2'-(((1H-benzo(d)imidazol-2-yl)methyl)azanediyl)bis(ethan-1-ol) with Propargyl bromide produce compound  6  which reacted

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Publication Date
Tue Oct 22 2019
Journal Name
Scientia Pharmaceutica
Design, Synthesis, and Docking Study of Acyl Thiourea Derivatives as Possible Histone Deacetylase Inhibitors with a Novel Zinc Binding Group
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Histone deacetylase inhibitors with zinc binding groups often exhibit drawbacks like non-selectivity or toxic effects. Thus, there are continuous efforts to modify the currently available inhibitors or to discover new derivatives to overcome these problems. One approach is to synthesize new compounds with novel zinc binding groups. The present study describes the utilization of acyl thiourea functionality, known to possess the ability to complex with metals, to be a novel zinc binding group incorporated into the designed histone deacetylase inhibitors. N-adipoyl monoanilide thiourea (4) and N-pimeloyl monoanilide thiourea (5) have been synthesized and characterized successfully. They showed inhibition of growth of human colon adenoc

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Publication Date
Thu Mar 25 2021
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Structural Study, and Biological Activity Evaluation of VO(II), Mn(II), Co(II), Ni(II), Cu(II), Zn(II), Cd(II), and Hg(II) Complexes with New Schiff Base Ligand Derived from Pyrazine
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New Schiff base [3-(3-acetylthioureido)pyrazine-2-carboxylic acid][L] has been prepared through 2 stages, the chloro acetyl chloride has been reacting with the ammonium thiocyanate in the initial phase for producing precursor [A], after that [A] has been reacting with the 3-amino pyrazine-2-carboxilic acid to provide a novel bidentate ligand [L], such ligand [L] has been reacting with certain metal ions in the Mn(II), VO(II), Ni(II), Co(II), Zn(II), Cu(II), Hg(II), and Cd(II) for providing series of new metal complexes regarding general molecular formula [M(L)2XY], in which; VO(II); X=SO4,Y=0, Co(II), Mn(II), Cu(II), Ni(II), Cd(II), Zn(II), and Hg(II); Y=Cl, X=Cl. Also, all the compounds were characterized through spectroscopic techniques [

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Publication Date
Tue Jan 01 2008
Journal Name
Al-mustansiriyah
Synthesis, Characterization of Some Metal Complexes with 1, 1bis- (orthoaminophenylthio)-methane
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