A convenient and efficient approach for the construction of aryl trifluoromethyl selenoethers from aryl iodides under mild conditions is reported. Electrochemical activation of stable and inexpensive NiBr2bipy (bipy – bipyridine) complex instead of labile Ni(COD)2 (COD – cyclooctadiene) catalyst. [NMe4][SeCF3] is employed as shelf-stable source of SeCF3 fragment. The reaction tolerates a wide range of substrates, including modification of drug-like molecules. Cyclic voltammetry studies allow insight into the reaction mechanism. 相似文献
In this work, the Stöber process was applied to produce uniform silica nanoparticles (SNPs) in the meso-scale size range. The novel aspect of this work was to control the produced silica particle size by only varying the volume of the solvent ethanol used, whilst fixing the other reaction conditions. Using this one-step Stöber-based solvent varying (SV) method, seven batches of SNPs with target diameters ranging from 70 to 400 nm were repeatedly reproduced, and the size distribution in terms of the polydispersity index (PDI) was well maintained (within 0.1). An exponential equation was used to fit the relationship between the particle diameter and ethanol volume. This equation allows the prediction of the amount of ethanol required in order to produce particles of any target diameter within this size range. In addition, it was found that the reaction was completed in approximately 2 h for all batches regardless of the volume of ethanol. Structurally coloured artificial opal photonic crystals (PCs) were fabricated from the prepared SNPs by self-assembly under gravity sedimentation.
A new kind of catanionic assembly was developed that associates a sugar-based surfactant with a non-steroidal anti-inflammatory drug (NSAID). Three different assemblies using indomethacin, ibuprofen and ketoprofen as NSAIDs were easily obtained in water by an acid-base reaction. These assemblies formed new amphiphilic entities because of electrostatic and hydrophobic effects in water and led to the spontaneous formation of vesicles. These catanionic vesicles were then tested as potential NSAID delivery systems for dermatological application. The anti-inflammatory activity was evaluated in vivo, and this study clearly showed an improved therapeutic effect for NSAIDs that were formulated as catanionic vesicles. These vesicles ensured a slower diffusion of the NSAID through the skin. This release probably increased the time of retention of the NSAID in the targeted strata of the skin. Thus, the present study suggests that this catanionic bioactive formulation could be a promising dermal delivery system for NSAIDs in the course of skin inflammation treatment. 相似文献
The hydrogen bond complexes between phenols and N-heteroaromatic bases 2,4,6-tri(2-pyridyl)-1,3,5-triazine, 2,2′,2′-terpyridine, quinoxaline, pyrido[2,3-b]pyrazine, pyzazino [2,3f]quinoxaline and 5-nitrozphenanthroline are investigated by infrared spectroscopy in 1,2-dichloroethane. The stability constants of the complexes involving N-heteroaromatic bases characterized by tow vicinal nitrogen atoms having lone pairs pointing to each other are higher than predicted from their basicity. Possible differences between protonation and hydrogen bond formation are discussed. Nheteroaromatic bases such as tri(2-pyridyl)-1,3,5-triazine or phenanthrolines cannot be considered as proton sponges but their behaviour is intermediate between that of the classical heteroaromatic bases and the proton sponges. 相似文献
When fiber optics' quadratic dispersion is compensated, the cubic dispersion determines the transmission quality in an optical link. Although the third-order dispersion coefficient is small in standard fiber optics at the third window, it is not in the linearly chirped grating used to the second-order dispersion equalization. The influence of the grating parameters on its third-order dispersion value is systematically studied and an efficient and low-cost device is proposed thatis numerically proven to cancel the global third-order dispersion that arises from the optical link. 相似文献
The lactam 16 , the hydroximolactams 8 , 20 , 23 , and 27 , and the imidazole 32 were prepared following known methods. They were tested together with the known tetrazole 35 and the hydroximolactams 2 and 36 as inhibitors of the cellobiohydrolases Cel7A and Cel6A from Trichoderma reesei. Cel7A is only weakly inhibited by these compounds. Comparing their inhibitory activity evidences the importance of occupying subsites +1 and +2. The results strongly suggest that the shape of none of the variants of the lactone-type inhibitor motif embodied by these inhibitors is complementary to the subsite −1, i. e., analogous to the transition state. Cel6A is rather strongly inhibited by the cellobiose analogues 20 , 23 , and 32 , and by the cellotriose analogue 27 . Their relative inhibitory activities evidence that binding at subsite −2 depends upon the shape of the moiety occupying subsite −1. There is only a small difference between the inhibition by the hydroximolactams 20 and 23 , which may be (partially) protonated by the catalytic acid of either anti- or syn-protonating glycosidases, and the imidazole 32 , which can only be protonated by anti-protonating glycosidases. The results strongly suggest that shape requirements must be met by glycosidase inhibitors before they can be used to characterize the proton trajectory of glycosidases. 相似文献
Pests and diseases are responsible for most of the losses related to agricultural crops, either in the field or in storage. Moreover, due to indiscriminate use of synthetic pesticides over the years, several issues have come along, such as pest resistance and contamination of important planet sources, such as water, air and soil. Therefore, in order to improve efficiency of crop production and reduce food crisis in a sustainable manner, while preserving consumer’s health, plant-derived pesticides may be a green alternative to synthetic ones. They are cheap, biodegradable, ecofriendly and act by several mechanisms of action in a more specific way, suggesting that they are less of a hazard to humans and the environment. Natural plant products with bioactivity toward insects include several classes of molecules, for example: terpenes, flavonoids, alkaloids, polyphenols, cyanogenic glucosides, quinones, amides, aldehydes, thiophenes, amino acids, saccharides and polyketides (which is not an exhaustive list of insecticidal substances). In general, those compounds have important ecological activities in nature, such as: antifeedant, attractant, nematicide, fungicide, repellent, insecticide, insect growth regulator and allelopathic agents, acting as a promising source for novel pest control agents or biopesticides. However, several factors appear to limit their commercialization. In this critical review, a compilation of plant-derived metabolites, along with their corresponding toxicology and mechanisms of action, will be approached, as well as the different strategies developed in order to meet the required commercial standards through more efficient methods. 相似文献
Time for SOme MOre : For the first time SOMO (singly occupied molecular orbital) activation has been exploited to allow a new approach to the α‐chlorination of aldehydes. This transformation can be readily implemented as part of a linchpin catalysis approach to the enantioselective production of terminal epoxides.