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.
In this paper, an analytical solution describing the deflection of a cracked beam repaired with piezoelectric patch is introduced. The solution is derived using perturbation method. A novel analytical model to calculate the proper dimensions of piezoelectric patches used to repair cracked beams is also introduced. This model shows that the thickness of the piezoelectric patch depends mainly on the thickness of the cracked beam, the electro-mechanical properties of the patch material, the applied load and the crack location. Furthermore, the model shows that the length of the piezoelectric patches depends on the thickness of the patch as well as it depends on the length of the cracked beam and the crack depth. The additio
... Show MoreIn this paper, an analytical solution describing the deflection of a cracked beam repaired with piezoelectric patch is introduced. The solution is derived using perturbation method. A novel analytical model to calculate the proper dimensions of piezoelectric patches used to repair cracked beams is also introduced. This model shows that the thickness of the piezoelectric patch depends mainly on the thickness of the cracked beam, the electro-mechanical properties of the patch material, the applied load and the crack location. Furthermore, the model shows that the length of the piezoelectric patches depends on the thickness of the patch as well as it depends on the length of the cracked beam and the crack depth. The additional flexibil
... Show MoreZinc oxide thin films were deposited by chemical spray pyrolysis onto glass substrates which are held at a temperature of 673 K. Some structural, electrical, optical and gas sensing properties of films were studied. The resistance of ZnO thin film exhibits a change of magnitude as the ambient gas is cycled from air to oxygen and nitrogen dioxide
In this study, new derivatives of 3-C-spiro ring nucleoside analogues were synthesized. The structures of these derivatives were characterized by infrared spectroscopy,1 HNMR (some of them) and elemental analysis. The nucleoside derivatives were tested for inhibition of E-coli and were all found to be active.
the use of diffrent concectration of Na and Mg ions were shown to causes in increase in the bindings at oncentration
Prednisolone (SAID) was conjugated with ibuprofen (NSAID) through an amino acid (glycine) as a spacer arm to synthesize the following compound:
Prednisolone – glycine – ibuprofen.
The method employed consists of converting the carboxylic acid function of (R,S) – ibuprofen – glycine to the highly reactive acid chloride and subsequent reaction with the C21 hydroxyl group of prednisolone. This reactive intermediate was found to react as well with the C17 tertiary hydroxyl group of the steroid to form three compounds and eight diastereomers. These results were confirmed by T.L.C, and the desired compound was separated by column chromatograph
... Show MoreA novel series of mixed-ligand complexes of the type, [ML 1 (L 2 ) 3 ]Cl x [M = Cr(III), Fe(III), Co(II),Ni(II), Cu(II), Cd(II) and Hg(II), n = 2, 3], was synthesized using Schiffbase (HL 1 ) as main ligand, nicotinamide (L 2 ) as secondary ligand, and the corresponding metal ions in 1:3:1 molar ratio. The main ligand, HL 1 was prepared by the interaction of ampicillin drug and 4-chlorobenzophenone. The synthesized mixed ligand complexes were characterized by elemental analysis, UV-Vis, FT-IR, 1 H-NMR, 13 C-NMR and TG/DTG studies. In the mixed-ligand complexes, the Schiffbase ligand, HL 1 showed coordination to the central metal ion in tridentate manner via azomethine nitrogen, β-lactam ring oxygen and deprotonated carboxylic oxy- gen atom
... Show MoreHydrogels are hydrophilic biocompatible polymers that can be used as a drug delivery material in different medical branches, including vital pulp therapy. The aim of this study is to characterize the physical and biological properties of the newly developed formula as a candidate direct pulp-capping material. The hydrogel composite was prepared from natural and synthetic origins (polyvinyl alcohol (PVA), hyaluronic acid (HA), and sodium alginate (SA)) with the incorporation of bioactive Moringa. Different formulas of hydrogel containing different concentrations were evaluated for physicochemical (FTIR, XRD, SEM, degradation, and swelling), mechanical (viscosity, folding endurance, film thickness), and biological (antioxidant, antibacterial,
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