A series of 4-(methylsulfonyl)aniline derivatives were synthesized in order to obtain new compounds as a potential anti-inflammatory agents with expected selectivity against COX-2 enzyme. In vivo acute anti-inflammatory activity of the final compounds 11–14 was evaluated in rat using an egg-white induced edema model of inflammation in a dose equivalent to 3 mg/Kg of diclofenac sodium. All tested compounds produced significant reduction of paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the activity of compounds 11 and 14 was significantly higher than that of diclofenac sodium (at 3 mg/Kg) in the 120–300 minute time interval, while compound 12 expressed a comparable effect to that of diclofenac sodium in the 60–240 minute time interval time, and compound 13 showed a comparable effect to that of diclofenac sodium at all experimental times. The result of this study indicates that the incorporation of the 4-(methylsulfonyl)aniline pharamacophore into naproxen, indomethacine, diclofenac and mefanamic acid maintained their anti-inflammatory activity and may increase selectivity towards the COX-2 enzyme which will be confirmed in the future by assessing COX-2: COX-1 inhibitory ratios using a whole blood assay.
Reducing of ethyl 4-((2-hydroxy-3-methoxybenzylidene)amino)benzoate (1) afford ethyl 4-((2-hydroxy-3-methoxybenzyl) amino)benzoate (2). Reaction of this compound with Vilsmeier reagent affords novel 2-chloro-[1,3] benzoxazine ring (3). The corresponding acid hydrazide of compound 3 was synthesized from reaction of compound (3) with hydrazine hydrate. Newly series of hydrazones(5a–i) were synthesized from reaction of acid hydrazide with various aryl aldehydes. Antibacterial activity of the hydrazones wassecerned utilizing gram-negative and gram-positive bacteria. Compound (5b) and (5c) exhibited significant antibacterial ability against both gram-negative and gram-positive bacteria, while the compounds(5a) showed mild antibacterial activit
... Show MorePower switches require snubbing networks for driving single – phase industrial heaters. Designing these networks, for controlling the maximum allowable rate of rise of anode current (di/dt) and excessive anode – cathode voltage rise (dv/dt) of power switching devices as thyristors and Triacs, is usually achieved using conventional methods like Time Constant Method (TCM), resonance Method (RM), and Runge-Kutta Method (RKM). In this paper an alternative design methodology using Fuzzy Logic Method (FLM) is proposed for designing the snubber network to control the voltage and current changes. Results of FLM, with fewer rules requirements, show the close similarity with those of conventional design methods in such a network of a Triac drivin
... Show Morerunning the requirement color important place in object of life activity both public and private, Fallon makes represents energy expressive and aesthetic in designing furniture street, especially (positions waiting buses passenger transport)which took looms large in attention receiver designer also, through civilized development and urban and change the city. Requirement, The positions of waiting progress jobs service and that would interact to produces Photos aesthetic Furniture for space street and understand receiver, affect the operation his life and the development of his environment and his psyche and culture of because they entity variable and sophisticated, impose on us to find foundations a design and conditions of chromatic esp
... Show MoreIn this work the effect of choosing tri-circular tube section had been addressed to minimize the end effector’s error, a comparison had been made between the tri-tube section and the traditional square cross section for a robot arm, the study shows that for the same weight of square section and tri-tube section the error may be reduced by about 33%.
A program had been built up by the use of MathCAD software to calculate the minimum weight of a square section robot arm that could with stand a given pay load and gives a minimum deflection. The second part of the program makes an optimization process for the dimension of the cross section and gives the dimensions of the tri-circular tube cross section that have the same weight of
... Show MoreThis work represents the preparation of the starting material, 3-chloro-2-oxo-1,4-dithiacyclohexane (S) using a new method. This material was reacted with, 4-phenylthiosemicarbazide to give (H3NS3) as a tetradentate ligand H3L. New complex of rhenium (V) with this ligand of the formula [ReO(L)] was prepared. New complexes of the general formula [M(HL)] of this ligand when reacted with some metal ions where: M = Ni(II), Cu(II), Cd(II), Zn(II), Hg(II) have been reported. The ligand and the complexes were characterized by infrared, ultraviolet–visible, mass, 1H nuclear magnetic resonance and atomic absorption spectroscopic techniques and by (HPLC), elemental analysis, and electrical conductivity. The proposed structure for H3L with Re (V) i
... Show MoreThe reaction of 2-amino benzoic acid with 1,2-dichloroethane under reflux in methanol and KOH as a base to gave the precursor [H4L]. The precursor under reflux and drops of CH3COOH which reacted with (2mole) from salicycaldehyde in methanol to gave a new type N2O4 ligand [H2L], this ligand was reacted with (MCl2) Where [M= Co (II), Ni(II), Cu(II) and Zn(II)] in (1:1) ratio at reflux in methanol using KOH as a base, to give complexes of the general formula [M(L)]. All compounds have been characterized by spectroscopic methods [1H NMR ( just to the ligand), FTIR, uv-vis, atomic absorption], melting point, conductivity, chloride content, as well as magnetic susceptibility measurements. From the above data, the proposed molecular structu
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