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Synthesis, Characterization of Some New 1,2,4-Triazole derivatives as Antimicrobial and Study of their Molecular docking
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This study outlines the synthesis of substituted 1,2,4-triazole derivatives through the cyclization reaction of thiourea derivatives. The process begins with the reaction of different halides with KSCN to produce isothiocyanate derivatives. then followed by a reaction with isonicotinic acid hydrazide to yield thioureas (1-6), with a yield rate of (72-88%). Then, compounds (1-6) were treated with alkaline medium 4 N (NaOH) to produced 1,2,4-triazole derivatives (7-12) with a yield (51-69%).The structure of the prepared compounds was characterized using FTIR,1HNMR and 13CNMR spectroscopy. Some of the synthesized compounds were tested for antimicrobial activity when, compound 9 showed strong activity against gram positive bacteria (Staphylococcus aureus, Staphylococcus epidermidis) and moderate activity against gram negative bacteria (Escherichia coli, Klebsiella pneumoniae) compared with drug ciprofloxacin. Also, examined compounds showed strong inhibition against (candida albicans) except compound 10 showed weak activity. Furthermore, the molecular docking was studied by Gold suite to examining the reaction between target compounds and active binding section of GABA-AT protein was the PLP fitness values of the docking compounds on GABA-AT ranged (57.71-67.55).

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Publication Date
Mon May 30 2022
Journal Name
Egyptian Journal Of Chemistry
Design ,Synthesis, Insilco Study and Biological Evaluation of New Coumarin-Oxadiazole Derivatives as Potent Histone Deacetylase Inhibitors
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Publication Date
Mon Sep 11 2023
Journal Name
University Of Anbar‎
Synthesis, ‎Characterization and ‎Thermal Study ‎of new aza-‎macrocyclic ligands with ‎some transition metals
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12 membered Schiff base macrocyclic ligands, 6,7,14,15-tetra phenyl-1,2,3,4, 4a,8a, 9,10, 11,12, 12a,16a-dodecahydro dibenzo [b,h] [1,4,7,10] tetraazacyclododecine L1, and 14 membered Schiff base macrocyclic ligands, 6,8,15,17-tetramethyl-1,2,3,4, 4a,7,9a, 10,11,12,13,13a,16,18a-tetra decahydro dibenzo[b,i] [1, 4,8,11] cyclotetradecine tetraaza L2, 7,16-bis(2,4- dichloro benz ylidene)-6,8,15,17-tetra methyl-1,2,3,4, 4a,7,9a, 10, 11,12, 13, 13a,16,18a-tetra deca hydro dibenzo [b,i] [1,4,8,11] tetra azacyclo tetra decine L3 and 6,8,15, 17-tetramethyl-1,2,3, 4,4a,9a,10, 11,12,13,13a,18a-dodecahydro dibenzo [b,i] [1,4,8, 11] tetraazacyclo tetradecine (7,16-diylidene) bis(methanylyli dene) bis (N,N-dimethylaniline) L4 were synthesized by condens

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Publication Date
Fri Jun 25 2021
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization, Thermal and Biological Study of New Organic Compound with Some Metal Complexes
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A new set of metal complexes by the general formula [M(P)2(H2O)2]Cl2 has been prepared through the interaction of the new Ligand [N1, N4-bis(4-methoxyphenyl)succinamide] (P) derived from succinyl chloride with p-anisidine with the transition metal ions [Cu(II), Mn(II), Cd(II), Co(II) and Ni(II)]. Compounds diagnosed by TGA, 1 H, 13CNMR and Mass spectra (for (P)), Fourier-transform infrared and Electronic spectrum, Magnetic measurement, molar conduct, (%M, %C, %H, %N). These measurements indicate that (P) is associated with the metal ion in a bi-dentate fashion by nitrogen atoms (the amide group), and the octahedral composition of these complexes is suggested. Staphylococcus Aureus (+) and Escherichia Coli (–) were studied for the antibact

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Publication Date
Wed Mar 25 2020
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization and Antimicrobial Evaluation of New Azo Compounds Derived from Sulfonamides and Isatin Schiff Base
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The present study deals with the synthesis of four different azo-azomethine derivatives; this is done by two steps; the first step is diazotization of sulfonamides (sulfanilamide, sulfacetamide, sulfamethoxazole, and sulfadiazine) separately, followed by the second step; the coupling reaction of diazotized compounds with isatin bis-Schiff base named 3-((4-nitrobenzylidene) hydrazono)indolin-2-one. The later one (bis-Schiff base) was synthesized by the reaction of 3-hydrazono-indolin-2-one with p-nitrobenzaldehyde. The chemical structures of newly synthesized compounds were approved on the basis of their FTIR, 1H-NMR, and CHNS elemental analysis data results. The synthesized azo compounds were tested in vitro for their antimicrobial potentia

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Publication Date
Sat Oct 19 2024
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Studying Thermal Analysis for Complexes of Some Metal Ions and Determining Their Activity as Antioxidants
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وفقأ للدراسات السابقة تم تحضير ليكاند آزو جديد (ن-(3-اسيتايل-2-هيدروكسي-5-مثيل-فنيل)ن-(4-كاربوكسي-سايكلوهكسيل مثيل)-ملح الدايازونيوم) وبعد التحقق من الصيغة المقترحة وفق نتائج التحاليل وبعد استخدام الليكاند لتحضير سلسلة ن المعقدات باستخدام نسب مولية متساوية (1:1) من الليكاند وتفاعلها مع كل من املاح المنغنيز والكوبلت والنيكل والنحاس والخارصين وبعد التحقق وفق تقنيات التحاليل الطيفية والتشخيصية(الاشعة فوق البنف

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Publication Date
Mon Jan 01 2024
Journal Name
Baghdad Science Journal
Study of the Anticancer and Antimicrobial Biological Activity of a New Series of Thiohydantoin Derivatives
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        Recently, some prostate cancer patients have acquired resistance to the second -generation drugs (anzalutamide and apalutamide) prescribed for the treatment of this disease due to the emergence of the F876L mutation, which represents a challenge to modern medicine. In this study, a new series of 2-thiohydantoin derivatives were prepared through the reaction of different derivatives of maleimide (1c-4c) with isothiocyanate derivatives. The prepared compounds were diagnosed using FT-IR,1H-NMR ,13C-NMR, Mass spectra. The prepared series compounds has been studied against prostate cancer cells. The MTT assay was used to determine the activity of the prepared compounds against prostate cancer cells. The da

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Publication Date
Fri Jan 01 2016
Journal Name
Der Pharmacia Lettre
Synthesis, characterization and anticonvulsant evaluation of new derivatives derived from 5-methoxy-2-mercapto benzimidazole
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A new series of 5-methoxy-2-mercapto benzimidazole derivatives were synthesized by the reaction of 5-methoxy- 2-mercaptobenzimidazole with chloroacetic acid and affords 2-((5-methoxy-1H-benzo[d]imidazol-2-yl)thio) acetic acid (1),which on cyclization with acetic anhydride and pyridine gives 7- methoxybenzo[4,5]imidazo[2,1-b]thiazol- 3(2H)-one(2), which on condensation with different aryl aldehydes in the presence of anhydrous sodium acetate in glacial acetic acid, furnishes a arylidene thiazolidinone. The purity of the synthesized compounds was confirmed by melting point and TLC.The structures were established by different spectral analysis such as FTIR,1HNMR, and CHN analysis. The newly synthesized compounds (3a-d) were in vivo evaluated f

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Scopus
Publication Date
Thu Jan 15 2015
Journal Name
Journal Of Education For Pure Science
Synthesis and Characterization of New Conjugated Systems Derived from Piperazine-2,5-dione with antimicrobial screening
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Publication Date
Sun Jun 01 2014
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Antimicrobial Screening of New Schiff Bases Linked to Phthalimidyl Phenyl Sulfonate Moiety
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A series of Schiff bases linked to phthalimidyl phenyl sulfonate moiety have been synthesized via multistep synthesis. The first step involved reaction of phthalic anhydride with aniline producing N-phenyl phthalamic acid which was subsequently dehydrated to the corresponding N-phenyl phthalimide via treatment with acetic anhydride and anhydrous sodium acetate. The synthesized imide was treated with chlorosulfonic acid in the third step producing 4-(N-phthalimidyl) phenyl sulfonyl chloride which was introduced in reaction with 4-hydroxy acetophenone in the fourth step producing 4-[4-(N-phthalimidyl) phenyl sulfonate] acetophenone and this in turn was introduced successfully in condensation reaction with various aromatic primary amines affor

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Publication Date
Thu Aug 31 2023
Journal Name
Journal Of Wasit For Science And Medicine
Synthesis, Characterization and Antimicrobial Study of Polyacetal-Co complex/Nano Chitosan polymer blend
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Polycyclicacetal was prepared by the reaction of PEG with 4-nitrobenzaldehyde. Cobalt was used for producing a polymer metal complex and solution casting was used to produce a polymer blend including nano chitosan. All produced compounds have been characterized by FT-IR, DSC/ TGA, and SEM techniques as well as biological activity. The production of polyacetal is illustrated by the FT-IR analysis. The DSC/TGA results indicate the prepared polymer blends' thermal stability. Staphylococcus aureas, Klebsiella pneumoniae, Bacillus subtilis, and Escherichia coli were the four types of bacteria selected to study and evaluate the antibacterial activity of produced polyacetal, its metal complex, and polymer blend. Results indicates that ther

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