Structure−Activity Relationships of Cinnamate Ester Analogues as Potent Antiprotozoal Agents

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.     

Finite constants: characterizations of a new decidable set of constants

Constant 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.     

Modellqualität als Indikator für Softwarequalität: eine Taxonomie

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.     

What do we learn from binding features? Evidence for multilevel feature integration.

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)     

Continuous assay of proteases using a microtiter plate fluorescence reader

The present study was designed to determine if spinal calcium channels, calmodulin, and calcium/calmodulin-dependent protein kinase II were involved in the production of antinociception induced by cold water swimming stress (CWSS). The effects of intrathecal (i.t.) injection of nimodipine, omega-conotoxin GVIA, calmidazolium, or (S)-5-isoquinolinesulfonic acid, 4-[2-[(5-isoquinolinyl-sulfonyl)methylamino]-3-oxo-3-(4-phenyl-1-piperaz inyl)-propyl]phenyl ester (KN-62) on CWSS-induced antinociception were studied in ICR mice. The antinociception was assessed by the tail-flick test. CWSS produced inhibition of the tail-flick response. Various doses of nimodipine (10-40 ng), omega-conotoxin GVIA (5-40 ng), calmidazolium (10-40 ng), or KN-62 (5-40 ng) injected i.t. alone did not show any antinociceptive effect in the tail-flick test. I.t. pretreatment with omega-conotoxin GVIA, calmidazolium, or KN-62 dose dependently attenuated the CWSS-induced inhibition of the tail-flick response. However, i.t. pretreatment with nimodipine did not affect the inhibition of the tail-flick response induced by CWSS. Our results suggest that spinal N-type calcium channel, calmodulin and calcium/calmodulin-dependent protein kinase II may be involved in the production of antinociception induced by CWSS. On the other hand, CWSS-induced antinociception appears not to be mediated via the spinal L-type calcium channel.     

Zur Frage der Elastizität,der Beanspruchung und der Festigkeit warmbetriebener Rohrleitungen

Zusammenfassung Die Entwicklung der Dampfkraftanlagen zu immer h?heren Temperaturen, Drücken und Leistungen zwingt den Rohrleitungsbauer, sich noch eingehender als bisher mit den Fragen der Elastizit?t, der Beanspruchung und der Festigkeit der Rohrleitung zu besch?ftigen. Zu einigen der wesentlichen Fragen werden im folgenden rechnerische und experimentelle Beitr?ge mitgeteilt. VDI     

Symbolic control of visual attention: The role of working memory and attentional control settings.

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)     

Novel Readout Electronics for Thickness Shear-Mode Liquid Sensors Compensating for Spurious Conductivity and Capacitances

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     

Hydroformylierung einfach und mehrfach ungesättigter Fettstoffe mit heterogenisierten Cobaltcarbonyl- und R

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 160–180^oC. 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).