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.
Pathogenic microorganisms are becoming more and more resistant to antimicrobial agents. So the synthesis of new antimicrobial agents is very important. In this work, new 5-fluoroisatin-chalcone conjugates 5(a–g) were synthesized based on previous research that showed the modifications of the isatin moiety led to the synthesis of many derivatives that have antimicrobial activity. 4-aminoacetophenone reacts with 5-fluoroisatin to form Schiff base (3), which in turn reacts with two different groups of aromatic (carbocyclic and heterocyclic) aldehydes 4(a–g) separately to form the final compounds 5(a–g). Proton-nuclear magnetic resonance (¹H-NMR) and Fourier-transform infrared (FT-IR) spectroscopy were used to confirm the chemic
... Show MoreThis research focuses on the synthesis of carbon nanotube (CNT) and Poly(3-hexylthiophene) (P3HT) (pristine polymer) with Ag doped (CNT/ P3HT@Ag) nanocomposite thin films to be utilised in various practical applications. First, four samples of CNT solution and different ratios of the polymer (P3HT) [0.1, 0.3, 0.5, and 0.7 wt.%] are prepared to form thin layer of P3HT@CNT nanocomposites by dip-coating method of Ag. To investigate the absorption and conductivity properties for use in various practical applications, structure, morphology, optical, and photoluminescence properties of CNT/P3HT @Ag nanocomposite are systematically evaluated in this study. In this regard, the UV/Vis/NIR spectrophotometer in the wavelength range of 350 to 7
... Show More2-(2-amino-5-nitro-phenylazo) -phenol was ready by grouping the diazonium salt of 2-aminophenol with 4-nitroaniline.Thegeometry of azo ligand(HL)was resolved on the origin of (C.H.N) analysis, 1H and 13CNMR spectra, infrared spectra and UV–vis electronic absorption spectra. Dealing with the azo ligand produced with Nd+3,Cd+3,Dy+3 and Er+3at aqueous ethanol for a 1:2 metal: ligand rate, and in perfect ph. The formation for compounds have been described by utilizing flame atomic absorption,(C.H.N) Analyses, conductivity, infrared spectra and UV–vis spectral procedures. Nature in the produced compounds have been studied obey the ratio of mole and continuous variance manners, Beer's law yielded up a concentration rate (1×10-4 - 3×10-4M) .
... Show MoreOrtho amino hydrazobenzene (L) has been prepared from the reaction of ortho amino phenyl thiol with phenyl hyrazan in mole ratio(1:1). It has been characterized by elemental analysis (C, H, N), IR, UV–Vis. The complexes of the bivalent ions (Co, Ni, Cu, Zn, Pd, Cd, Hg and Pb) and the trivalent (Cr) have been prepared and characterized too. The structural have been established by elemental analysis(C,H,N), IR , UV – Vis spectra , conductivity measurements , atomic absorption and magnetic susceptibility . The complexes showed characteristic behaviour of octahedral geometry around the metal ion and the( N,N) ligand coordinated in bidentate modeexcept with pd showed square planer. ? ,kf , ?max for the complexes were estimated too . ? for Co
... Show MoreBackground: Immediate implant placement in the maxillary anterior region was challenging, especially with the jumping gap and limited primary implant stability. Objective: To assess the autogenous dentin graft biomaterial's ability to improve the esthetic outcomes of an immediately inserted implant. Methods: Twenty patients with non-restorable retained roots in the maxillary non-molar region surrounded by natural sound teeth were included in this study after a complete clinical and radiological examination, including patient health and clinical fitness for the immediate dental implant procedure. A single dental implant was inserted for each patient, and the resulting jump distance was filled with the mineralized dentin graft and co
... Show MoreDeveloping and researching antenna designs are analogous to excavating in an undiscovered mine. This paper proposes a multi-band antenna with a new hexagonal ring shape, theoretically designed, developed, and analyzed using a CST before being manufactured. The antenna has undergone six changes to provide the best performance. The results of the surface current distribution and the electric field distribution on the surface of the hexagonal patch were theoretically analyzed and studied. The sequential approach taken to determine the most effective design is logical, and prevents deviation from the work direction. After comparing the six theoretical results, the fifth model proved to be the best for making a prototype. Measured results rep
... Show MoreBored piles settlement behavior under vertical loaded is the main factor that affects the design requirements of single or group of piles in soft soils. The estimation of bored pile settlement is a complicated problem because it depends upon many factors which may include ground conditions, validation of bored pile design method through testing and validation of theoretical or numerical prediction of the settlement value. In this study, a prototype single and bored pile group model of arrangement (1*1, 1*2 and 2*2) for total length to diameter ratios (L/D) is 13.33 and clear spacing three times of diameter, subjected to vertical axial loads. The bored piles model used for the test was 2000
... Show MoreAdherence to cardiac medications makes a significant contribution to avoidance of morbidity and premature mortality in patients with cardiovascular disease. This quantitative study used cross‐sectional survey design to evaluate medication adherence and contributing factors among patients with cardiovascular disease, comparing patients who were admitted to a cardiac ward (
The new compounds synthesized by sequence reactions starting from a reaction of 4-hydroxybenzaldehyde with 1,5-dibromo pentane to produce dialdehyde)I( .Then compound )I( reacted with different aromatic amines to give schiff bases )IIIV(,thereafter added acetyl chloride to schiff bases to yield N-acyl derivatives)VVII(.While1,3-diazetine derivatives)VIII-X( were synthesized from the reaction of N-acyl derivatives with sodium azide.The reaction of thiourea with N-acyl compounds led to formation of thiourea derivatives (XI-XIII).Finally, the pyrimidine compounds )XIV-XVI( were synthesized by ring closure reaction of compounds(XIXIII) with diethyl malonate.The synthesized compounds were characterized by measurements of melting points,FTIR,1H-N
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