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.
Phthalimide formation of Phthalic anhydride with various amines using microwave or without a method with the difference of the catalyst used in a prepared Phthalimide, either structure general are C6H4CONRCO and used as starting materials in synthesis several compounds derivative phthalimides are an important compounds because spectrum wide biological activities including Antimicrobial activity, anticonvulsant activity, Anti-inflammatory activity,Analgesic activity, Anti- influenza activity and Thromboxane inhibitory activity
Starting from 4, - Dimercaptobiphenyl, a variety of phenolic Schiff bases (methylolic, etheric, epoxy) derivatives have been synthesized. All proposed structure were supported by FTIR, 1H-NMR, 13C-NMR Elemental analysis all analysis were performed in center of consultation in Jordan Universty.
Coumarin derivatives have shown different biological activities, such as antifungal, antibacterial antiinflammatory, and antioxidant activities, besides antibiotic resistance modulating effects, and anti-HIV, hepatoprotective, and antitumor effect. So, new coumarin derivatives (hydrazones and an amide) were synthesized through multisteps reactions. All the synthesized target compounds were characterized by FT-IR spectroscopy, 1HNMR analysis. The compounds then evaluated for their anti-bacterial activity by means of well-diffusion method against two gram-positive bacteria (Staphylococcus aureus, Streptococcus pneumoniae) and two gram-negative bacteria (E.coli and Pseudomonas aeruginosa). The highest activity was demonstr
... Show MoreNew substituted anthraquinones with amino derivations fragments were synthesized through the substitution of bromine atom by different amines using the Ullmann coupling reaction. Obtained compounds based on anthraquinone used for experimental antimicrobial studies. The structure of the synthesized compounds was confirmed by LC-MS and 1H, 13C NMR spectroscopy. Studies on planktonic microorganisms have shown that the first synthesized anthraquinone derivatives have an inhibitory effect against bacteria and fungi. The triazene 1-(3-(benzoic acid(triaz-1-en-1-ol(-4-(1H-imidazol-1-yl(-9,10-dioxo-9,10-dihydroanthracene -2-sulfonic acid, have wide spectrum of activity, growth retardation zones against gram-positive micro
... Show MoreNew series of 4,4'-((2-(Aryl)-1H-benzo[d]imidazole1,3(2H)-diyl)bis(methylene))Diphenol(3a-g) was successfully synthesized from cyclization of the reduction product of bis Schiff bases (2) with aryl aldehydes bearing phenolic hydroxyl in the presence of acetic acid. The structure of these compounds was identified from FT-IR, 1H NMR, 13C NMR and EIMs. The Antioxidant capability was screened by DPPH and FRAP assays. Both assays showed antioxidant capability more than BHT as well. Compounds 3b and 3c showed antioxidant capacity slightly less than ascorbic acid. The docking study for theses compound was carried out as III DNA polymerase inhibitor. The results of docking demonstrated that the increase in hinderances around phenolic hydroxyl for t
... Show MoreNew series of 4,4'-((2-(Aryl)-1H-benzo[d]imidazole-1,3(2H)-diyl)bis(methylene))Diphenol(3a-g) was successfully synthesized from cyclization of the reduction product of bis Schiff bases (2) with aryl aldehydes bearing phenolic hydroxyl in the presence of acetic acid. The structure of these compounds was identified from FT-IR, 1H NMR, 13C NMR and EIMs. The Antioxidant capability was screened by DPPH and FRAP assays. Both assays showed antioxidant capability more than BHT as well. Compounds 3b and 3c showed antioxidant capacity slightly less than ascorbic acid. The docking study for theses compound was carried out as III DNA polymerase inhibitor. The results of docking demonstrated that the increase in hinderances around phenolic hydr
... Show MoreThis research includes the synthesis of some new N-Aroyl-N \ -Aryl thiourea derivatives namely: N-benzoyl-N \ -(p-aminophenyl) thiourea (STU1), N-benzoyl-N \ -(thiazole) thiourea (STU2), N-acetyl-N ` -(dibenzyl) thiourea (STU3). The series substituted thiourea derivatives were prepared from reaction of acids with thionyl chloride then treating the resulted with potassium thiocyanate to affored the corresponding N-Aroyl isothiocyanates which direct reaction with primary and secondary aryl amines, The purity of the synthesized compounds were checked by measuring the melting point and Thin Layer Chromatography (TLC) and their structure, were identified by spectral methods [FTIR,1H-NMR and 13C-NMR].These compounds were investigated as a
... Show MoreNew hydrazide compounds (A2) and (A9) were prepared from their corresponding esters (A1, A8) .These esters were also prepared from their precursors 5-ethoxy carbonyl-(4methoxyphenyl)-6-methyl-1,2,3,4-tetrahydropyrimidine-2-thione (A1) via multicomponent reaction type and from hippuric acid respectively. The hydrazide compounds were then allowed to react with some aldehydes forming the corresponding hydrazones (A3-7) and (A1014). The synthesized compounds were characterized by IR, 1H-NMR, 13C-NMR, and Mass spectroscopies and well discussed. .
The [2-aminobenzothiazole]was reacted with [2,4,6 triyhydroxy-acetophenon monohydrate] to give a new ligand [2-N-2,4,6-trihydroxyacetophenonyliden benzothiazole] [H3L]. This ligand was reacted with metal ions ( CoII, NiII,CuII and ZnII) in methanol as solvent with ( 1:2 ) metal : ligand ratio to give a series of new complexes with general formula [ M(H2L)2],(where:M= CoII, NiII ,CuIIand, ZnII).All compounds were characterized by spectroscopic methods ( I.R , U.V – vis,HPLC) atomic absorption, along with chloride content and conductivity measurements. According to the data of these measurements we suggested a tetrahedral
The study aims at measuring the dimensions of binding and non-binding social responsibility and its relation to the organizational performance in telecommunication companies in the Republic of Yemen using analytical descriptive approach and questionnaire as a main tool for data collection and comprehensive inventory method.
It has been found that there is a positive effect and significant moral relation between social responsibility with its binding and non-binding dimensions and the organizational performance of telecommunication companies in the Republic of Yemen at a level of significance below (0.05). It has also been found that the correlation between the non-binding social responsibilit
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