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1.
In the present work, novel 5-((1-benzyl-1,2,3-triazol-4-yl)methoxybenzylidene)-2-(arylamino)thiazol-4-one thiazolone incorporated triazole derivatives have been designed as tyrosinase inhibitors. The compounds were synthesized through click reaction in good yield. Moreover, the antityrosinas activity of the synthesized derivatives was evaluated. In the search for establishing a click copper-catalyzed azide/alkyne cycloaddition (CuAAC) reaction under strict conditions, in terms of a novel air-stable, a recyclable and efficient magnetic catalyst was planned for new triazole derivatives as a well-organized copper iodide supported on the functionalized Fe3O4@SiO2 core-shell (CuI/Fe3O4@SiO2(TMS-EDTA) nanoparticles). The engineered nanocatalyst synthesized for the first time and characterized by different methods, including FT-IR spectroscopy, XRD, FESEM, EDX, TEM, TGA, and BET analysis. The excellent catalytic performance in ethanol with high surface area (351.7 m2g−1) and short reaction time for diverse functional groups (120–200 min), no use of toxic solvents, reusability of the catalyst, and using eco-friendly conditions are the advantageous of this work. Moreover,the nanocatalyst can be used at least five times without any significant decrease in the yield of the reaction. The thiazolidine-triazole derivatives 9a , 9c , 9e , and 9 g showed promising tyrosinase inhibitory activity with IC50 values in the range of 5.90–9.81 μM. The compounds were found to be considerably more potent tyrosinase inhibitors than the reference inhibitor kojic acid (IC50 = 18.36 μM).  相似文献   
2.
Research on Chemical Intermediates - MCM-41-SO3H, ordered mesoporous silica material MCM-41 with covalently anchored sulfonic acid groups, was used as a solid acid catalyst for the convenient,...  相似文献   
3.
Copper complexes with chiral iminopyridine ligands were screened for their catalytic efficiency in carbene (cyclopropanation) and nitrene transfer reactions (aziridination, C? H amidation). Both pre‐formed and in situ formed complexes were considered. The results highlighted the poor catalytic efficiency of these complexes in cyclopropanation reactions employing methyl phenyldiazoacetate as the carbene source, whereas better results were obtained in nitrene transfer reactions, particularly in the amidation of C? H bonds, albeit the enantioselectivity of the reactions was negligible in nearly all cases. Finally, copper complexes were also found to promote an interesting oxidative functionalization of alkynes with PhI(OAc)2 at room temperature. Copyright © 2014 John Wiley & Sons, Ltd.  相似文献   
4.
Some new amidated fentanyl (=N‐[1‐(2‐phenylethyl)piperidin‐4‐yl]‐N‐phenylpropanamide) analogs with a 4‐(N‐phenylamido)piperidine scaffold and additional amide bonds have been designed and synthesized through Ugi four‐component reaction (Ugi‐4CR). Good‐to‐high yields, diversity‐oriented synthesis, and possible applications in drug discovery are advantages of this approach.  相似文献   
5.
The application of the recently introduced dispersive liquid–liquid microextraction (DLLME) for the separation and determination of an inorganic selenite [Se(IV)] derivative by means of a gas chromatography–electron-capture detection system has been studied. The selenium derivative was extracted with the DLLME technique using a mixture of ethanol (disperser solvent) and chlorobenzene (extraction solvent). The influences of the various analytical parameters on the derivatization reaction and microextraction procedure have been evaluated and optimized. Under the optimum conditions, an enrichment factor of 122 was obtained for only 5.00 mL of the water sample. The calibration graph was linear in the range of 0.015–10 μg L?1 with a detection limit of 0.005 μg L?1. The relative standard deviation for ten replicate measurements of 2 μg L?1 of selenium was 4.1%. The method was applied to the determination of selenium in environmental surface water samples with satisfactory recovery.  相似文献   
6.
A mild and efficient method for the copper-catalyzed arylation of phenylurea is described. The coupling reaction of phenylurea with different functionalized aryl iodides in the presence of air stable CuI, N,N′-dibenzylethylenediamine as a ligand, and KF/Al2O3 as a base gives symmetrical and unsymmetrical diarylureas in relatively high yields.  相似文献   
7.
The progress of the compaction process to produce from an assembly of particles a coherent mass can be achieved by the application of shear and normal stress. The achievement of a densified coherent mass necessitates, together with the yielding of material, the movement of particles over and between each other. In uniaxial compaction the angle of internal friction, δE, is a projection of the unique critical state line which divides a three dimensional relationship between volume change (V), shear stress (?) and normal stress (σ) into yield domains and surfaces. There is one region for failure and flow (the Hvorslev surface) and another region for failure and consolidation (the Roscoe surface). In this paper the concepts of the Roscoe and Hvorslev surfaces together with the Coulomb yield criterion have been applied to the uniaxial compaction, over a range of compactable stresses, of titanium dioxide (20–2000 kPa). The characteristics of applied and shear stress, angle of internal friction (δE), angle of shearing resistance (?) and surface area (SBET) were measured and correlated with the compaction stress (σc) and diametral strength (σf) of the compacts to investigate the phenomena of uniaxial compaction.  相似文献   
8.
Journal of Thermal Analysis and Calorimetry - This study was conducted with the aim of investigating the Newtonian nanofluid flow in a catheterized tapered artery through using a completely...  相似文献   
9.
An ultra-preconcentration technique composed of solid-phase extraction (SPE) and dispersive liquid–liquid microextraction (DLLME) coupled with gas chromatography–flame photometric detection (GC–FPD) was used for determination of thirteen organophosphorus pesticides (OPPs) including phorate, diazinon, disolfotane, methyl parathion, sumithion, chlorpyrifos, malathion, fenthion, profenphose, ethion, phosalone, azinphose-methyl and co-ral in aqueous samples. The analytes were collected from large volumes of aqueous solutions (100 mL) into 100 mg of a SPE C18 sorbent. The effective variables of SPE including type and volume of elution solvent, volume and flow rate of sample solution, and salt concentration were investigated and optimized. Acetone was selected as eluent in SPE and disperser solvent in DLLME and chlorobenzene was used as extraction solvent. Under the optimal conditions, the enrichment factors were between 15,160 and 21,000 and extraction recoveries were 75.8–105.0%. The linear range was 1–10,000 ng L?1 and limits of detection (LODs) were between 0.2 and 1.5 ng L?1. The relative standard deviations (RSDs) for 50 ng L?1 of OPPs in water with and without an internal standard, were in the range of 1.4–7.9% (n = 5) and 4.0–11.6%, respectively. The relative recoveries of OPPs from well and farm water sat spiking levels of 25 and 250 ng L?1 were 88–109%.  相似文献   
10.
<正>A new practical method for the synthesis of unsymmetrical ureas was achieved by reaction of phenylurea with primary and secondary amines under neutral and mild condition in very good yields.The reaction took place in refluxing dioxane and does not require any catalyst or additives.  相似文献   
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