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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 adenocarcinoma and mouse hepatoblastoma cells with low cytotoxic effect against normal human breast cells. Their binding mode to the active site of several histone deacetylases has been studied by docking and the results gave a preliminary indication that they could be successful histone deacetylase inhibitors.

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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
Wed Nov 30 2022
Journal Name
Iraqi Journal Of Science
Synthesis and Characterization of Ni2O3 as a Phase of Nickel Oxide Nanomaterial
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    Ni2O3 nanomaterial, a phase of nickel oxide, is synthesized by a simple chemical process. The pure raw materials used in the present process were nickel chloride hexahydrate NiCl2.6H2O and potassium hydroxide KOH by utilizing temperature at 250 oC for 2 hour.  The structural, morphological and optical properties of the synthesized specimens of Ni2O3 were investigated employing diverse techniques such as XRD, AFM, SEM and UV-Vis, respectively. The XRD technique confirms the presence of Ni2O3 nanomaterial with crystal size of 57.083 nm which indexing to the (2θ) of 31.82; this results revealed the Ni2O3 was a phase of nickel oxide with Nano structure. The synthesized Ni2O3 will be useful in manufacturng electrodes materials f

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Publication Date
Sun Jun 01 2014
Journal Name
Baghdad Science Journal
Synthesis and Characterization of New heterocyclic Polyacrylamides from Derivatives 2-Aminobenzothiazole
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The present work involved preparation of new hetro cyclic polyacrylamides (1-9) using reaction of polyacryloyl chloride with 2-aminobenzothiazole which prepeard by thiocyanogen method in the presence of a suitable solvent and amount tri ethyl amine (Et3N) with heating. The structure confirmation of polymers were proved using FT-IR,1H-NMR,C13NMR and UV spectroscopy.Other physical properties including softening and melting points, and solubility of the polymers were also measured.

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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
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 Jun 25 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization and Antibacterial Activity Evaluation of New Indole-Based Derivatives
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A new series of N-acyl hydrazones (4a-g) derived from indole-3-propionic acid (IPA) were synthesized. These N-acyl hydrazones were prepared by the reaction of 3-(1H-indol-3-yl) propane hydrazide and aldehyde in the existence of glacial acetic acid as a catalyst. 1HNMR and FT-IR analyses were used to identify the synthesized compounds and they were in vitro evaluated as antibacterial agents against six different types of microorganisms by using well diffusion method. All the tested N-acyl hydrazones (4a-g) displayed moderate activity against the Gram-negative E.coli, comparable to that of Amoxicillin. Some of the tested N-acyl hydrazones also exhibited intermediate activity ag

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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
Sat Apr 01 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis of 3 - 3 - gem - di - C -Nitromethyl Nucleoside Analogues of Possible Biological Activity
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Synthesis of new nucleoside analogues of the type : 3¢ , 3¢ - gem – di – C – nitromethly , expected to have useful application in the chemotherapeutic treatment of AIDS , cancer and microbial infections. The synthesis involved the condensation of the appropriate sugar derivative ( i.e . 3¢ , 3¢ –  gem – di – C – nitromethly – 1–  ribofuranose ) with nitrogen bases , such as , uracil and theophllin following a multi step scheme starting from diacetone golucose (1) (scheme 1) .The prepared compound were identified by spectroscopic methods ; ir , mass , 1H and 13C nmr.

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