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1.
Freddy A. Bernal Dr. Marcel Kaiser Prof. Dr. Bernhard Wünsch Prof. Dr. Thomas J. Schmidt 《ChemMedChem》2020,15(1):68-78
Protozoal infections are still a global health problem, threatening the lives of millions of people around the world, mainly in impoverished tropical and sub-tropical regions. Thus, in view of the lack of efficient therapies and increasing resistances against existing drugs, this study describes the antiprotozoal potential of synthetic cinnamate ester analogues and their structure-activity relationships. In general, Leishmania donovani and Trypanosoma brucei were quite susceptible to the compounds in a structure-dependent manner. Detailed analysis revealed a key role of the substitution pattern on the aromatic ring and a marked effect of the side chain on the activity against these two parasites. The high antileishmanial potency and remarkable selectivity of the nitro-aromatic derivatives suggested them as promising candidates for further studies. On the other hand, the high in vitro potency of catechol-type compounds against T. brucei could not be extrapolated to an in vivo mouse model. 相似文献
2.
F Douaud N Le Roch J Renault R Havouis M Vaultier JP Moulinoux N Seiler 《Canadian Metallurgical Quarterly》1997,12(8):621-633
Several dimethylsilane tetramines [homologs of spermine with an Si(CH3)2 group in the central carbon chain], a carbon analog of the dimethylsilane tetramines [containing C(CH3)2 instead of Si(CH3)2] and a dimethylsilane hexamine were studied with regard to their cytotoxic activity and their ability to interact with double-stranded DNA. All polyamine analogs exerted cytostatic effects to several cell lines at micromolar concentrations. Their ability to condense DNA was comparable to and their ability to displace ethidium bromide from binding to DNA was superior to that of spermine. Their cytostatic effect was not correlated with the depletion of cellular spermidine concentrations. It is suggested that the new polyamine analogs act mainly by displacing spermidine from binding sites which are essential for the promotion of cell growth. 相似文献
3.
Bernhard Steffen
Jens Knoop
《Theoretical computer science》1991,80(2):303-318Constant propagation, the replacement of program terms which represent a unique value at run time by their values, is a classical program optimization method. In spite of being treated for years, constant propagation still has been in the unsatisfactory phase of heuristics. We enhance the known constant propagation techniques to obtain an algorithm which is optimal for programs without loops. Fundamental is the introduction of a new decidable set of constants, the finite constants. This set has two different characterizations: a denotational one, which directly specifies our iterative algorithm and an operational one, which delivers the completeness or optimality of this algorithm for programs without loops. The algorithm is implemented in a commercial compiler project. 相似文献
4.
Zusammenfassung Komplexit?t, Anforderungsmanagement und Variantenvielfalt sind zentrale Herausforderungen bei der Entwicklung und Evolution
heutiger softwaregesteuerter Systeme. Diesen wird zunehmend durch den Einsatz modellbasierter Entwicklungsmethoden begegnet.
Dadurch wird das Modell zum zentralen Artefakt und die Erstellung und Nutzung von Modellen zu einer zentralen T?tigkeit in
der Softwareentwicklung. Mit der Bedeutung der Modelle steigen auch die Ansprüche an ihre Qualit?t. Dieser Beitrag untersucht
die Implikationen, die daraus entstehen, insbesondere werden sinnvolle Qualit?tsmerkmale für softwarebeschreibende Modelle
identifiziert und diskutiert. 相似文献
5.
Colzato Lorenza S.; Raffone Antonino; Hommel Bernhard 《Canadian Metallurgical Quarterly》2006,32(3):705
Four experiments were conducted to investigate the relationship between the binding of visual features (as measured by their aftereffects on subsequent binding) and the learning of feature-conjunction probabilities. Both binding and learning effects were obtained, but they did not interact. Interestingly, (shape-color) binding effects disappeared with increasing practice, presumably because of the fact that only 1 of the features involved was relevant to the task. However, this instability was only observed for arbitrary, not highly overlearned combinations of simple geometric features and not for real objects (colored pictures of a banana and strawberry), where binding effects were strong and resistant to practice. These findings suggest that learning has no direct impact on the strength or resistance of bindings or on speed with which features are bound; however, learning does affect the amount of attention particular feature dimensions attract, which again can influence which features are considered in binding. (PsycINFO Database Record (c) 2011 APA, all rights reserved) 相似文献
6.
J. S. Kim D. G. Seiler R. A. Lancaster M. B. Reine 《Journal of Electronic Materials》1996,25(8):1215-1220
Variable-magnetic-field Hall measurements (0 to 1.5 T) are performed on very-narrow-gap bulk-grown Hg1−xCdxTe single crystals (0.165 ≤ x ≤ 0.2) at various temperatures (10 to 300K). The electron densities and mobilities are obtained
within the one-carrier (electrons) approximation of the reduced-con-ductivity-tensor scheme. The present data together with
the selected data set reported by other workers exhibit a pronounced peak when the electron mobility is plotted against the
alloy composition x-value which has been predicted to be due to the effective-mass minimum at the bandgap-crossing (Eg ≈ 0). The observed position (x ≈ 0.165), height (≈4 x 102 m2Vs), and width (≈0.01 in x) of the mobility-peak can be explained by a simple simulation involving only ionized-impurity scattering.
A lower bound of the effective mass is introduced as a fitting parameter to be consistent with the finiteness of the observed
electron mobility and is found to be of the order of 10−4 of the mass of a free electron. 相似文献
7.
8.
This study examined how 1 symbol is selected to control the allocation of attention when several symbols appear in the visual field. In Experiments 1-3, the critical target feature was color, and it was found that uninformative central arrows that matched the color of the target were selected and produced unintentional shifts of attention (i.e., involuntary, initiated slowly, producing long-lasting facilitatory effects). Experiment 4 tested whether such selection is the result of an attentional filter or of a competition bias due to a match of incoming information against integrated object representations stored in working memory. Here, the critical feature was shape and color was irrelevant, but matching color arrows were still selected. Thus, features of objects in working memory will bias the selection of symbols in the visual field, and such selected symbols are capable of producing unintentional shifts of attention. (PsycINFO Database Record (c) 2010 APA, all rights reserved) 相似文献
9.
Christian Riesch Bernhard Jakoby 《IEEE sensors journal》2007,7(3):464-469
In this paper, a readout circuit for a thickness shear-mode (TSM) resonator is presented which can be used for sensing applications in liquids such as viscosity sensing. The system features compensation of both spurious capacitances and conductances in parallel to the resonator. This allows measurements even in conductive liquids without the need for an elaborate sealing of the sensor. The influence of the spurious elements is determined by means of two orthogonal synchronous detectors and eliminated by active compensation using voltage-controlled amplifiers (VCAs). Furthermore, the circuit is robust against possible phase errors. The basic concept is discussed in detail, and a readout circuit is developed. A prototype is presented, and sample results are given, demonstrating the feasibility of the approach 相似文献
10.
Zhigao Xia Ullrich Klckner Bernhard Fell 《European Journal of Lipid Science and Technology》1996,98(9):313-321
Hydroformylation of mono and multiple unsaturated fatty substances with heterogenized cobaltcarbonyl and rhodiumcarbonyl catalysts. Heterogenized cobalt and rhodiumcarbonyl catalyst systems can be used for the hydroformylation of mono and polyunsatured fatty substances in a technically simple and satisfying manner to useful chemical intermediates. The used solid tert. phosphane complex ligands have a silicate matrix and therefore they are also suitable for the cobalt catalyzed hydroformylation which is best performed at temperatures of 160–180oC. The cobalt catalyzed reaction gives with polyunsaturated fatty substances almost only products with monofunctionalized fatty acid chains. Whereas, the rhodium catalyzed reaction gives with linolic acid compounds inhomogeneous mixtures of mono- and diformyl derivatives of these fatty substances. The heterogenized rhodium carbonyl catalyst systems therefore seem to be more suitable for the hydroformylation of monounsaturated compounds. This is also true for rhodiumcarbonylsupported aqueous phase-catalysts which give likewise mixtures of mono and diformyl derivatives in the hydroformylation of polyunsaturated fatty substances. In batch process after the complete conversion of the olefin and reduction of the CO/H2-pressure the loss of catalyst metal from the support is negligible and in most cases below the detection limit (<1 ppm). 相似文献