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41.
Potential mGAT4 inhibitors derived from the lead substance (S)-SNAP-5114 have been synthesized and characterized for their inhibitory potency. Variations from the parent compound included the substitution of one of its aromatic 4-methoxy and 4-methoxyphenyl groups, respectively, with a more polar moiety, including a carboxylic acid, alcohol, nitrile, carboxamide, sulfonamide, aldehyde or ketone function, or amino acid partial structures. Furthermore, it was investigated how the substitution of more than one of the aromatic 4-methoxy groups affects the potency and selectivity of the resulting compounds. Among the synthesized test substances (S)-1-{2-[(4-formylphenyl)bis(4-methoxyphenyl)-methoxy]ethyl}piperidine-3-carboxylic acid, that features a carbaldehyde function in place of one of the aromatic 4-methoxy moieties of (S)-SNAP-5114, was found to have a pIC50 value of 5.89±0.07, hence constituting a slightly more potent mGAT4 inhibitor than the parent substance while showing comparable subtype selectivity. 相似文献
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A conceptualization of intended learning outcomes supporting self‐regulated learners in indicating learning paths 下载免费PDF全文
P. Tangworakitthaworn L. Gilbert G.B. Wills 《Journal of Computer Assisted Learning》2015,31(5):393-404
Intended learning outcomes (ILOs) indicate what learners will be able to achieve after they are taught. Traditionally, ILOs are expressed as plain text or unstructured documents. What if all ILOs of a specific course of study can be conceptualized through a structured diagrammatic technique? It was hypothesized that learners can benefit from this conceptualization in learning, especially in self‐regulated learning. The aim of this study was to investigate whether the ILOs represented in unstructured or structured formats can facilitate learners to identify learning paths. The results revealed that the mean ratings of all learning paths were statistically significantly higher with structured ILOs. 相似文献
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Machine Learning - We propose a data-driven approach to quantify the uncertainty of models constructed by kernel methods. Our approach minimizes the needed distributional assumptions, hence,... 相似文献
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Manjin Kim Qinfen Gu Tanveer Hussain Yahia Ali Trevor B. Abbott Kazuhiro Nogita 《International Journal of Hydrogen Energy》2021,46(53):27096-27106
With superior properties of Mg such as high hydrogen storage capacity (7.6 wt% H/MgH2), low price, and low density, Mg has been widely studied as a promising candidate for solid-state hydrogen storage systems. However, a harsh activation procedure, slow hydrogenation/dehydrogenation process, and a high temperature for dehydrogenation prevent the use of Mg-based metal hydrides for practical applications. For these reasons, Mg-based alloys for hydrogen storage systems are generally alloyed with other elements to improve hydrogen sorption properties. In this article, we have added Na to cast Mg–La alloys and achieved a significant improvement in hydrogen absorption kinetics during the first activation cycle. The role of Na in Mg–La has been discussed based on the findings from microstructural observations, crystallography, and first principles calculations based on density functional theory. From our results in this study, we have found that the Na doped surface of Mg–La alloy systems have a lower adsorption energy for H2 compared to Na-free surfaces which facilitates adsorption and dissociation of hydrogen molecules leading to improvement of absorption kinetic. The effect of Na on the microstructure of these alloys, such as eutectic refinement and a density of twins is not highly correlated with absorption kinetics. 相似文献