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.
Allopurinol derivative were prepared by reacting the (1-chloroacetyl)-2-Hydropyrazolo{3,4-d}pyrimidine-4-oneiwith 5- methoxy- 2-aminoibenzothiazoleiunder certain conditions to obtain new compound ( N- (2-aminoacetyl (5-methoxy) benzothiazole -2yl) (A4), Reaction of 5-(P-dimethyl amine benzene)-2-amino-1,3,4- oxadiazole in the presence of potassium carbonate anhydrous to yield new compound (N-(2- aminoacetyl-5-(P-dimethyl amine benzene )-1,3,4-oxadiazoles-2-yl)(A30) and Azo compound (N-(5-(Azo-2-hydroxy-5-amino benzene)-1,3-Diazol-2yl)Allopurinol(A46). The structure of prepared compounds were confirmed by (FT-IR)
... Show MoreSheet piles are necessary with hydraulic structures as seepage cut-off to reduce the seepage. In this research, the computational work methodology was followed by building a numerical model using Geo-Studio program to check the efficiency of using concrete sheet piles as a cut-off or reducer for seepage with time if the sheet piles facing the drawdown technique. Al-Kifil regulator was chosen as a case study, an accurate model was built with a help of observed reading of the measuring devices, which was satisfactory and helped in checking the sheet piles efficiency. Through the study, three scenarios were adopted (with and without) drawdown technique, it was found that at the short time there's no effect of the drawdown technique on
... Show MoreBackground: Antibiotic resistance is a problem leading to difficulty in treating microbial infections thatmay occur due to many causes. For the important pharmacist role as a reference for the information and theability to access to medications, they are vital members in lowering the development of antibiotic resistance,and also they support the proper use and control of antibioticsmisuse. Our goal is comparing the knowledge,attitude, practice of undergraduate and postgraduate pharmacy students and their perceptions about thecausing factors of antibiotic resistance in Iraq.Method: A cross sectional study was conducted involving the final year bachelor and postgraduate (masterand Philosophical doctor) students from different private
... Show MoreAn indoor spraying robot is built in this research to solve numerous challenges associated with manual spraying. The mechanical, hardware and essential technologies used are all detailed and designed. The proposed spraying robot's conceptual design is split into two parts: hardware and software. The mechanical design, manufacturing, electrical, and electronics systems are described in the hardware part, while the control of the robot is described in the software section. This robot's kinematic and dynamic models were developed using three links that move in the x, y, and z directions. The robot was then designed using SolidWorks software to compute each connection's deflection and maximum stresses. The characteristics of the stepper moto
... Show MoreVariable-Length Subnet Masks (VLSM), often referred to as "subnetting a subnet", is used to maximize addressing efficiency. The network administrator is able to use a long mask on networks with few hosts, and a short mask on subnets with many hosts. This addressing scheme allows growth and does not involve wasting addresses. VLSM gives a way of subnetting a network with
minimal loses of IP addresses for a specific range. Unfortunately, the network administrator has to perform several mathematical steps (or use charts) to get the required results from VLSM. In this paper, a simple graph simulator is proposed (using Visual Basic 6.0 Language) to perform all the required mathematical steps and to display the obtained required informatio
This research includes theoretical and evaluation design of a polarizer filter of high transmission in the near IR region of (900-1200nm) for different incidence angles to obtain a long wave and short wave pass filter using analytical calculations. Results refer to a new configuration design in fewer layers than used in previous studies in the long wave pass at incidence angles (45o,50o,55o). Adopted Hafnium dioxide (HfO2) and Magnesium fluoride (MgF2) as coating material at design wavelength (933nm), the study also included design short wave pass polarizer by using the same coating material.
Variable-Length Subnet Masks (VLSM), often referred to as "subnetting a subnet", is used to maximize addressing efficiency. The network administrator is able to use a long mask on networks with few hosts, and a short mask on subnets with many hosts. This addressing scheme allows growth and does not involve wasting addresses. VLSM gives a way of subnetting a network with minimal loses of IP addresses for a specific range. Unfortunately, the network administrator has to perform several mathematical steps (or use charts) to get the required results from VLSM. In this paper, a simple graph simulator is proposed (using Visual Basic 6.0 Language) to perform all the required mathematical steps and to display the obtained required information (the
... Show MoreCopper (I) complex containing folic acid ligand was prepared and characterized on the basis of metal analyses, UV-VIS, FTIR spectroscopies and magnetic susceptibility. The density functional theory (DFT) as molecular modeling calculations was used to determine the donor atoms of folic acid ligand which appear clearly at oxygen atoms binding to hydrogen. Detection of donation sights is supported by theoretical parameters such as geometry, mulliken population, mulliken charge and HOMO-LUMO gap obtained by DFT calculations.
Sulfamethoxazole (SMX) is the most significant antibiotic in the sulfonamide family. It was chosen as the representative of this category because of its widespread use. Starting with sulfamethoxazole, a new series of 2-Azetidinone (M1-M6) was synthesized, the structure of these new derivatives was confirmed using spectral methods, starting with the synthesis of Schiff’s bases by reflux of different aromatic benzaldehydes, separately, with Sulfamethoxazole in ethanol with few drops of acetic acid. The final compounds were obtained by ketene-imine synthesis of β-lactam using chloroacetyl chloride. The designed chemicals’ synthesis has been completed successfully. Physical parameters (melting points and Rf values), Fourier transfo
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