N-Substituted Nipecotic Acids as (S)-SNAP-5114 Analogues with Modified Lipophilic Domains

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.     

西藏南部地区人工爆炸地震探测的地壳结构

众所周如,西藏地区是研究地球深部结构和构造的窗口,是研究大陆板块学说的重要场所,也是寻找热源和其它矿产资源的有利地区.因此,世界各国地学科学家都希望在本地区进行科学研究工作,或与我国科学工作者协作共同探索这一重要地区.中国和法国的地质、地球物理科学家经商讨共同组成“中法喜马拉雅山地质研究队”,对西藏中部广大地区进行地质、地球物理的科学研究工作.深部地震探测是地球物理研究中的重要内容.中法双方共同决定,在中国西藏南部的日喀则地区至北边的那曲地区作地震探测工作.为了探测地壳上地幔的结构,1981年在西藏的南部佩枯错至普莫雍错500公里的喜马拉雅山北麓——雅鲁藏布江地区进行了人工爆炸地震探测工作.本文是中法地质研究队合作的深部地震探测资料的解释结果.     

Inhibiting and deactivating effects of water on the selective catalytic reduction of nitric oxide with ammonia over MnOx/Al2O3

The effect of water on the selective catalytic reduction (SCR) of nitric oxide with ammonia over alumina supported with 2–15 wt.-% manganese oxide was investigated in the temperature range 385–600 K, with the emphasis on the low side of this temperature window. Studies on the effect of 1–5 vol.-% water vapour on the SCR reaction rate and selectivity were combined with TPD experiments to reveal the influence of water on the adsorption of the single SCR reactants. It turned out that the activity decrease due to water addition can be divided into a reversible inhibition and an irreversible deactivation. Inhibition is caused by molecular adsorption of water. TPD studies showed that water can adsorb competitively with both ammonia and nitric oxide. Additional kinetic experiments revealed that adsorbed ammonia is present in excess on the catalyst surface, even in the presence of water. Reduced nitric oxide adsorption is responsible for the observed reversible decrease in the reaction rate; the fractional reaction order changes from 0.79 in the absence of water to 1.07 in its presence. Deactivation is probably due to the dissociative adsorption of water, resulting in the formation of additional surface hydroxyls. As the amount of surface hydroxyls formed is limited to a saturation level, the deactivating effect on the catalyst is limited too. The additional hydroxyls condense and desorb in the temperature range 525–775 K, resulting in a lower degree of deactivation at higher temperature. A high temperature treatment at 775 K results in a complete regeneration. The amount of surface hydroxyls formed per unit surface area decreases at increasing MnO_x-loading. The selectivity to the production of nitrogen is enhanced significantly by the presence of gas phase water.     

Syntactic mismatches in machine translation

This paper addresses one of the central problems arising at the transfer stage in machine translation: syntactic mismatches, that is, mismatches between a source-language sentence structure and its equivalent target-language sentence structure. The level at which we assume the transfer to be carried out is the Deep-Syntactic Structure (DSyntS) as proposed in the Meaning-Text Theory (MTT). DSyntS is abstract enough to avoid all types of divergences that result either from restricted lexical co-occurrence or from surface-syntactic discrepancies between languages. As for the remaining types of syntactic divergences, all of them occur not only interlinguistically, but also intralinguistically; this means that establishing correspondences between semantically equivalent expressions of the source and target languages that diverge with respect to their syntactic structure is nothing else than paraphrasing. This allows us to adapt the powerful intralinguistic paraphrasing mechanism developed in MTT for purposes of interlinguistic transfer.     

Application of differential quadrature to static analysis of structural components

The numerical technique of differential quadrature for the solution of linear and non-linear partial differential equations, first introduced by Bellman and his associates, is applied to the equations governing the deflection and buckling behaviour of one- and two-dimensional structural components. Separate transformations are used for higher-order derivatives, as suggested by Mingle, thus extending the method to treat fourth-order equations and to include multiple, boundary conditions in the respective co-ordinate directions. Results are obtained for various boundary and loading conditions and are compared with existing exact and numerical solutions by other methods. The application of differential quadrature to this class of problems is seen to lead to accurate results with relatively small computational effort.     

Editorial

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