Preparation of 1-(4-hydroxy-iminomethylpyridinium)-3-pyridiniumpropane dibromide is described. This compound represents a new acetylcholinesterase (AChE) reactivator, which has no substituents on the second pyridinium ring as found in other commonly used AChE reactivators. The reactivation ability of this reactivator was tested on tabun- and cyclosarin-inhibited AChE. According to the results obtained, the new compound (without substitution and with decreased molecule size) showed increased reactivation potency in case of cyclosarin inhibited AChE. A potent oxime for treatment of tabun and cyclosarin-caused intoxications was thus obtained via slight modification of the reactivator structure (compared to trimedoxime and K027). 相似文献
Dioleoylphosphatidylcholine unilamellar vesicles made by extrusion technique (LUVETs) were studied as the delivery system for lipophilic water-insoluble potential photosensitizers for photodynamic therapy (PDT). Two azaphthalocyanines (AzaPcs) with hydrophobic substituents only and two also possessing two charged amino groups were introduced into the study. All compounds are insoluble in water and form aggregates in PBS with tetrahydrofuran as cosolvent. The size of these aggregates depends on the concentration of AzaPc in solution. AzaPcs with tert-butyl substituents were found to be incorporated into the lipid bilayer of vesicles in the monomeric form even at high concentrations. The stability of LUVETs with incorporated AzaPc was excellent for at least 4 weeks. Therefore, they are suitable for use as a delivery system for these water-insoluble photosensitizers. Very low amount of AzaPc with n-octyl substituents incorporated into LUVETs due to its stronger self-aggregation. Values of binding constants determined for all AzaPcs showed inverse order than expected from their lipophilicities. However, the binding constants followed the order of the strength of aggregation forces. Aggregation of AzaPcs in water medium plays a very important role in the interaction of AzaPcs with LUVETs. 相似文献
The efficient and straightforward NHC-rhodium-catalyzed thiol-silane and thiol-germanane coupling reactions, leading to new classes of functionalized SQ-based materials, are presented for the first time. The proposed strategies use commercially available reagents and show a broad functional groups tolerance, which opens a possibility of effective synthetic procedures of biologically active compounds. 相似文献
A novel, 100% water-soluble chalcone based chemosensing receptor {1-[3-(2-Hydroxy-phenyl)-3-oxo-propenyl]-naphthalen-2-yloxy}-acetic acid, L was synthesized and characterized. The receptor L is designed based on the chelation enhanced fluorescence (CHEF) mechanism. The chemosensing properties of L were evaluated by UV–vis and fluorescence spectrometric methods. It exhibits highly selective recognition ability towards aluminum ions in water over other metal ions. The binding stoichiometry of L? Al3+ complex is 2:1 by means of Job’s plot and the detection limit is 5.66?×?10??8 M. 相似文献
Three tetracationic porphyrins differing in the position of charged nitrogen atoms on the peripheral substituents — 5,10,15,20-tetrakis(N-methylpyridinium-4-yl)porphyrin (TMPyP4), 5,10,15,20-tetrakis(N-methylpyridinium-2-yl)porphyrin (TMPyP2), 5,10,15,20-tetrakis(4-trimethylammoniophenyl) porphyrin (TMAPP), and hydrophobic 5,10,15,20-tetraphenylporphyrin (TPP), were immobilized by adsorption
and encapsulation in poly(hydroxymethylsiloxane) (PHOMS). The so prepared porphyrin-PHOMS composites were characterized by
porosimetry, scanning electron microscopy, fluorescence and diffuse reflectance UV-VIS spectroscopy. It was found that porphyrins
are immobilized in the PHOMS matrix in the free base monomer form Their irradiation produced singlet oxygen O2(1Δg) with the lifetime of 10–30 μs. 相似文献
The interaction between bis(hexadecyldimethylammonium)hexane dibromide (16-6-16), bis(tetradecyldimethylammonium)hexane dibromide (14-6-14), their conventional counterparts cetyltrimethylammonium bromide (CTAB) and tetradecyltrimethylammonium bromide (TTAB) with polyvinylpyrrolidone (PVP) was investigated using the conductivity technique. The results show that gemini surfactants interact strongly with PVP as compared to conventional surfactants. The results also reveal that the surfactants with shorter hydrocarbon chain interact weakly as those of longer hydrocarbon chain. The interactions of 16-6-16 and 14-6-14 and their conventional counterparts with PVP were also studied using dynamic light scattering (DLS) measurements. We have also highlighted the effect of surfactant–polymer interactions on the dispersion force in the solution. Critical aggregation concentration (cac) and critical micelle concentration (cmc) were obtained using the conductivity data. The degrees of micelle ionization and free energies associated with aggregation, micellization, and transfer have also been evaluated and discussed. 相似文献
Click to view : Glycopolymers can be used to display glycans on microarrays in native‐like architectures. The structurally uniform alkyne‐terminated mucin mimetic glycopolymers (see picture; TR=fluorophore) were printed on azide‐functionalized chips by microcontact printing in the presence of a copper catalyst. The surface‐bound glycopolymers bind lectins in a ligand‐specific manner.
In this work, the usefulness of the inverse Laplace transformation (ILT) in the characterization of diffusion processes in the brain has been investigated. The method has been implemented on both phantom and in vivo cat brain data acquired at high resolution at 9.4 T. The results were compared with monoexponential and biexponential analyses of the same data. It is shown that in the case of diffusion restricted by white matter axonal tracts, the resulting diffusograms are in good agreement with the biexponential model. In gray matter, however, the non-monoexponential decay does not lead to a bimodal distribution in the ILT, even though the data can be fitted to a biexponential. This finding suggests the possibility of a distribution of diffusion coefficients rather than a discrete biexponential behavior. It is shown that this distribution is sensitive, for example, to experimental parameters such as the diffusion time. Thus, the ILT offers the possibility of implementing a unique tool for the analysis of heterogeneous diffusion, that is, the analysis of the diffusion coefficient distribution, which has the yet unexplored potential of being a valuable parameter in the characterization of tissue structure. 相似文献
In this study, steady-state turbulent forced flow and heat transfer in a horizontal smooth rectangular duct both experimentally and numerically investigated. The study was carried out in the transition to turbulence region where Reynolds numbers range from 2,323 to 9,899. Flow is hydrodynamically and thermally developing (simultaneously developing flow) under uniform bottom surface temperature condition. A commercial CFD program Ansys Fluent 12.1 with different turbulent models was used to carry out the numerical study. Based on the present experimental data and three-dimensional numerical solutions, new engineering correlations were presented for the heat transfer and friction coefficients in the form of $ {\text{Nu}} = {\text{C}}_{2} {\text{Re}}^{{{\text{n}}_{ 1} }} $ and $ {\text{f}} = {\text{C}}_{3} {\text{Re}}^{{{\text{n}}_{3} }} $, respectively. The results have shown that as the Reynolds number increases heat transfer coefficient increases but Darcy friction factor decreases. It is seen that there is a good agreement between the present experimental and numerical results. Examination of heat and mass transfer in rectangular cross-sectioned duct for different duct aspect ratio (α) was also carried out in this study. Average Nusselt number and average Darcy friction factor were expressed with graphics and correlations for different duct aspect ratios. 相似文献