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.
Two arylenedisuccinamic acids, namely 1,4-phenylene-disuccinamic acid and 4,4'biphenyl-disuccinamic acid were prepared from the reaction of two moles of succinic anhydride with one mole of 1,4-phenylenediamine dihydrochloride and beinzidine respectively.Dehydration of arylenedisuccinamic acid in the pressence of polyvinyl alcohol (PVA) and catalytic amount of concentrated.H2SO4,gives N,N'-arylenedisuccinimidesPVAcomposite polymers. Dehydration of arylenedisuccinamic acid (without PVA) in the pressence of catalytic amount of conc. H2SO4 gives N,N'-arylenedisuccinimides. Arylenedisuccinamic acid and arylenedisuccinimides characterized by CHN-analysis,FT.IR and 1H,C13-NMR.Spectral analysis
Albizia lebbeck biomass was used as an adsorbent material in the present study to remove methyl red dye from an aqueous solution. A central composite rotatable design model was used to predict the dye removal efficiency. The optimization was accomplished under a temperature and mixing control system (37?C) with different particle size of 300 and 600 ?m. Highest adsorption efficiencies were obtained at lower dye concentrations and lower weight of adsorbent. The adsorption time, more than 48 h, was found to have a negative effect on the removal efficiency due to secondary metabolites compounds. However, the adsorption time was found to have a positive effect at high dye concentrations and high adsorbent weight. The colour removal effi
... Show MoreA new Schiff base [I] was prepared by refluxing Amoxicillin trihydrate and 4-Hydroxy- 3,5-dimethoxybenzaldehyde in aqueous methanol solution using glacial acetic acid as a catalyst. The new 1,3-oxazepine derivative [II] was obtained by Diels- Alder reaction of Schiff base [I] with phthalic anhydride in dry benzene. The reaction of Schiff base [I] with thioglycolic acid in dry benzene led to the formation of thiazolidin-4-one derivative [III]. While the imidazolidin-4-one [IV] derivative was produced by reacting the mentioned Schiff base [I] with glycine and triethylamine in ethanol for 9 hrs. Tetrazole derivative [V] was synthesized by refluxing Schiff base [I] with sodium azide in dimethylformamid DMF. The structure of synthesized compound
... Show MoreA new Schiff base [I] was prepared by refluxing Amoxicillin trihydrate and 4-Hydroxy- 3,5-dimethoxybenzaldehyde in aqueous methanol solution using glacial acetic acid as a catalyst. The new 1,3-oxazepine derivative [II] was obtained by Diels- Alder reaction of Schiff base [I] with phthalic anhydride in dry benzene. The reaction of Schiff base [I] with thioglycolic acid in dry benzene led to the formation of thiazolidin-4-one derivative [III]. While the imidazolidin-4-one [IV] derivative was produced by reacting the mentioned Schiff base [I] with glycine and triethylamine in ethanol for 9 hrs. Tetrazole derivative [V] was synthesized by refluxing Schiff base [I] with sodium azide in dimethylformamid DMF. The structure of synthesized compound
... Show MoreSystemic lupus erythematosus (SLE) is the prototypic multisystem autoimmune disorder with a broad spectrum of clinical presentations encompassing almost all organs and tissues. Aimes of study determination of integrin- linked kinase 1(ILK-1) and anti-smith antibody(ASAB) levels in serum of Iraqi patients with systemic lupus erythematosus, in addition, that ILK-1 may be as a diagnostic marker of SLE disease, and study the effect of systemic lupus erythematosus on renal function in these patients. This study included 100 females’ patients with systemic lupus erythematosus attending to the Rheumatology Unit in Baghdad Teaching Hospital, Medical City, (Baghdad), in addition to 30 healthy females as controller group were chosen without any chr
... Show MoreDevelopment of improved methods for the synthesis of metal oxide nanoparticles are of high priority for the advancement of material science and technology. Herein, the biosynthesis of ZnO using hydrahelix of beta vulgaris and the seed of abrus precatorius as an aqueaus extracts adduced respectivily as stablizer and reductant reagent. The support are characterized by spectroscopic methods ( Ft-IR, Uv-vis ).The FTIR confirmed the presence of ZnO band. The Uv-visible showed absorption peak at corresponds to the ZnO nanostructures. X-ray diffraction, scaning electron microscopy (SEM), dispersive X-ray spectroscopy (EDX) techniques are taken to investigation the size, structure and composition of synthesised ZnO nanocrystals. The XRD pattern mat
... Show More4-amino-3-(4-(((4-hydroxy-3, 5dimethoxybenzyl) oxy) methyl) phenyl)-1, 2, 4-triazole-5-thione was synthesized by to method the first one from melt reaction of 4-(((4-hydroxy-3, 5-dimethoxybenzyl) oxy) methyl) benzoic acid with Thiocarbonyldihydrazide, the second method from convert the corresponded acid hydrazide to potassium 2-(4-(((4-hydroxy-3, 5-dimethoxybenzyl) oxy) methyl) benzoyl) hydrazinecarbodithioate salt then react with hydrazine hydrate. Newly Schiff base (7a-7f) were synthesized from reaction the 4-amino-1, 2, 4-triazol with substituted hydroxybenzaldehyde. The resulting compounds were characterized by IR, 1H-NMR, 13C-NMR, and HRMS data. 2, 2-Diphenyl-1-picrylhydrazide (DPPH) and ferric reducing antioxidant power (FRAP) assays
... Show Morecompound [1] was formed from the reaction of benzoin and benzaldehyde in the presence of ammonia, which was reacted with sodium hydride in DMF to obtain imidazole salt. This salt was reacted with adipoyl chloride to give compound [2]. Acid hydrazide derivative [3] was obtained from the reaction of compound [2] with hydrazine hydrate. After that Shiff bases [4-9] have been synthesized from the reaction of compound [3] with different aromatic aldehydes. These new formed compounds were diagnosed by 13C-NMR, 1H-NMR for some of them (in Ahl-Albate University in Jordan) and FT-IR spectroscopy (In Baghdad University). All of the prepared products have been studied their biological activities toward two kinds of bacteria. These products show
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