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.
Orphenadrine is an anticholinergic ,antimuscarinic , centrally acting skeletal muscle relaxant .It presents in the form of citrate and HCl salts which are used in treatment of the symptoms of mild Parkinson's disease and also it is used as adjuvant with other drugs in the therapy .
Many trials were made to formulate Orphenadrine citrate as a plain tablet using wet granulation or direct compression technique in order to get a satisfactory formula through studying the effect of various factors such as binders , diluents and disintegrants types .
The best formula was obtained by using Poly Vinyl Pyrolidine (PVP) as a binder also the results indicated that starch and mannitol
... Show MoreNystatin is the drug of choice for treatment of cutaneous fungal infections with main disadvantage that is the need for multiple applications to achieve complete eradication which may reduce patient compliance. Microparticles offer a solution for such issue as they are one of sustained release preparations that achieve slow release of drug over an extended period of time. The objectives of this study were to fabricate nystatin-loaded chitosan microparticles with the ultimate goal of prolonging drug release and to analyze the influence of polymer concentration on various properties of microparticles. Microparticles were prepared by chemical cross-linking method using glutaraldehyde as cross-linking agent. Five formulas, namely N1C1, N1C2,
... Show MoreThis paper designed a fault tolerance for soft real time distributed system (FTRTDS). This system is designed to be independently on specific mechanisms and facilities of the underlying real time distributed system. It is designed to be distributed on all the computers in the distributed system and controlled by a central unit.
Besides gathering information about a target program spontaneously, it provides information about the target operating system and the target hardware in order to diagnose the fault before occurring, so it can handle the situation before it comes on. And it provides a distributed system with the reactive capability of reconfiguring and reinitializing after the occurrence of a failure.
In this paper the variable structure control theory is utilized to derive a discontinuous controller to the magnetic levitation system. The magnetic levitation system model is considered uncertain, which subjected to the uncertainty in system parameters, also it is open-loop unstable and strongly nonlinear. The proposed variable structure control to magnetic levitation system is proved, and the area of attraction is determined. Additionally, the chattering, which induced due to the discontinuity in control law, is attenuated by using a non-smooth approximate. With this approximation the resulted controller is a continuous variable structure controller with a determined steady state error according to the selected control
... Show MoreAmino glycoside derivation including, Neomycin, Streptomycin, Kanamycin and Gentamycin with special reagents, which are benzoylchloride; benzene sulfonyl chloride and phthalic anhydride were made to enhance Uv-detectability for HPLC analysis. But there are many problems facing pre column derivation and in order to solve this, the conductivity of antibiotic derivatives were used to calculate the dissociation constant and the hydrolysis rate which determined concern type reaction. In addition the characteristics those controlling the hydrolysis of antibiotic-derivatives were investigated.
In this paper, variable gain nonlinear PD and PI fuzzy logic controllers are designed and the effect of the variable gain characteristic of these controllers is analyzed to show its contribution in enhancing the performance of the closed loop system over a conventional linear PID controller. Simulation results and time domain performance characteristics show how these fuzzy controllers outperform the conventional PID controller when used to control a nonlinear plant and a plant that has time delay.