Design,Synthesis, and Characterization of Macrocyclic Inhibitors of the Proprotein Convertase Furin

The activation of viral glycoproteins by the host protease furin is an essential step in the replication of numerous pathogenic viruses. Thus, effective inhibitors of furin could serve as broad-spectrum antiviral drugs. A crystal structure of an inhibitory hexapeptide derivative in complex with furin served as template for the rational design of various types of new cyclic inhibitors. Most of the prepared derivatives are relatively potent furin inhibitors with inhibition constants in the low nanomolar or even sub-nanomolar range. For seven derivatives the crystal structures in complex with furin could be determined. In three complexes, electron density was found for the entire inhibitor. In the other cases the structures could be determined only for the P6/P5-P1 segments, which directly interact with furin. The cyclic derivatives together with two non-cyclic reference compounds were tested as inhibitors of the proteolytic activation and replication of respiratory syncytial virus in cells. Significant antiviral activity was found for both linear reference inhibitors, whereas a negligible efficacy was determined for the cyclic derivatives.     

SELECTION OF CLAYS FOR SAGGERS OF PREDETERMINED RESISTANCE TO THERMAL SHOCK AND PREDICTION OF SAGGER LIFE IN SERVICE*

A series of twelve sagger bodies having a wide range in properties was prepared from fourteen different clays and grog made, in most instances, from the same clays. Experimental saggers heated to different temperatures were tested for resistance to thermal shock and the values compared with predetermined values assigned to each of the bodies. A chart was prepared which shows the relation between modulus of rupture, modulus of elasticity, linear thermal expansion, and resistance of saggers to thermal shock.     

THE QUANTITATIVE DETERMINATION OF IRON EXISTING AS FERROSILICON IN ARTIFICIAL CORUNDUM

A procedure is given for determining quantitatively the iron existing as ferrosilicon in artificial corundum.     

Development of a knowledge-base for automatic monitoring of renal function of intensive care patients over time

Renal dysfunction is a major problem in the management of critically ill patients. Monitoring of renal parameters over time is a prerequisite for detection of any significant deterioration of kidney function. Thus, we developed a knowledge-base for the dynamic monitoring of renal function of critically ill patients. A database with renal parameters of 750 intensive care patients was analyzed for distribution of parameters within predefined intervals of the creatinine clearance. Additionally, a subgroup of 11 patients with (quite) normal renal function over 11 days was selected and the daily variability of renal parameters was analyzed. An interdisciplinary expert team selected a set of nine clinically relevant renal parameters and formulated, on the basis of the data analysis and the parameter set, eight definitions of renal function, which represent four levels of renal performance. These definitions were arranged into an hierarchical structure, considering only clinically relevant changes of renal function. A change from one functional state to another inside of 2 days indicates a relevant alteration of renal function. Monitoring of time courses can additionally be performed by statistical analysis of the daily variability of parameters and comparison with their 'normal' variability. Moreover, rules were established for the plausibility check of results and interpretations of single parameters and parameter sets formulated.     

Zur Bestimmung großer Diffusionslängen in Silizium-Wafern mit der SPV-Methode

Übersicht Für die Bestimmung der Diffusionslänge mit der Surface-Photo-Voltage (SPV)-Methode wurde ein Auswerteverfahren entwickelt, das den Einfluß der Probenstruktur und der effektiven Lichtabsorption auf das Ladungsträgerprofil berücksichtigt. Es wird gezeigt, daß sich mit diesem Verfahren bei hoher Meßgenauigkeit noch Diffusionslängen, die der Waferdicke entsprechen, mit einer Genauigkeit >25% auflösen lassen.

---

The determination of large duffusion lengths in silicon wafers using the SPV-method

Contents A new method for the determination of carrier diffusion length by proper evaluation of the Surface Photo Voltage (SPV)-technique is presented. To obtain better and more specific results, we take into account the carrier profile and the effective absorption of the specimen structure and use a sophisticated and very accurate measurement technique. Diffusion lengths up to the magnitude of the wafer thickness can be determined with an accuracy better than 25%.

---

---

Herrn Prof. Dr. phil. nat. W. Gerlach zum 60. Geburtstag gewidmet