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排序方式: 共有7164条查询结果,搜索用时 31 毫秒
1.
2.
Steffen Vojacek Lukas Schulig Nathalie Wössner Norman Geist Prof. Dr. Walter Langel Prof. Dr. Manfred Jung Prof. Dr. Dennis Schade Prof. Dr. Andreas Link 《ChemMedChem》2019,14(8):853-864
Indoles are privileged structures in medicinal and bioorganic chemistry that are particularly well suited to serve as platforms for diversity. Among many other therapeutic areas, the indole scaffold has been used to design aromatic compounds useful to interfere with enzymes engaged in the regulation of substrate acylation status, such as sirtuins. However, the planarity of the indole ring is not necessarily optimal for all target enzymes, especially when functionalization with aromatic side chains is required. Replacement of flat scaffolds by nonplanar molecular cores dominated by sp3 hybridization is a common strategy to avoid the disadvantages associated with poor solubility and high promiscuity, while covering less-well-explored areas of chemical space. Thus, we synthesized fragment-like tetrahydroindoles suitable for fragment-based drug discovery as well as a well-characterized small library intended as multipurpose screening compounds. For proof of principle, these compounds were screened against sirtuins 1–3, enzymes known to be addressable by indoles. We found that 2,6,6-trimethyl-4-oxo-4,5,6,7-tetrahydro-1H-indole-3-carboxamides are potent and selective SIRT2 inhibitors. Compound 16 t displayed an IC50 value of 0.98 μm and could serve as exquisite starting point for hit-to-lead profiling. 相似文献
3.
Matthias Siemon Olaf Riese Burkhard Forell Dominic Krnung Walter Klein‐Heßling 《火与材料》2019,43(5):497-513
In the context of industrial buildings and power plants, electrical installations and cable trays represent a main fuel load and a potential initial fire source due to possible short circuits or comparable malfunction. Furthermore, a fire can spread from one tray to additional trays mounted above and/or horizontally on one tray. Because of the high significance of cable fires, several research projects have been carried out, investigating the fire behaviour of cables from small‐scale tests, eg, the cone calorimeter, up to large‐scale tests, analysing complete cable tray constructions. The goal of the work presented in this paper is the extension of the knowledge regarding the influence of geometrical parameters like the packing density and tray distance on the burning behaviour and fire spread of cable tray installations. The results are considered, together with test results from the literature, to quantify the main physical parameters describing the burning behaviour. In a next step, the general applicability of these parameters as input data for the parametrization of the source term of numerical simulations is shown. The test results show that the burning behaviour and the fire spreading highly depend on the cable arrangement of the cables on the cable tray, in combination with other boundary conditions. By applying the results as input for a fire simulation, the mass loss rate is considered appropriately. 相似文献
4.
Walter K. Sakamoto Darcy H. F. Kanda Francisco de Assis Andrade D. K. Das-Gupta 《Journal of Materials Science》2003,38(7):1465-1470
Vegetable-based polyurethane (PU) was prepared in the thin film form by spin coating. This polymer is synthesised from castor oil, which can be extracted from the seeds of a native plant in Brazil called mamona. This polymer is biocompatible and is being used as material for artificial bone. The PU was characterised by dielectric spectroscopy in a wide range of frequency (10–5 Hz to 105 Hz) and by thermally stimulated discharge current (TSDC) measurements. The glass transition temperature (T
g = 39°C) was determined and using the initial rise method the activation energy was found to be 1.58 eV. 相似文献
5.
Mantooth B.A. Weiss P.S. 《Proceedings of the IEEE. Institute of Electrical and Electronics Engineers》2003,91(11):1785-1802
One of the ultimate miniaturizations in nanotechnology is molecular electronics, where devices will consist of individual molecules. There are many complications associated with the use of molecules in electronic devices, such as the electronic perturbations in the molecule associated with being bonded to an electrode, how electrons traverse the metal-molecule junction, and the difficulty of macroscopically addressing single to very few molecules. Whether fabricating a test structure or a usable device, the use of self-assembly is fundamental to the fabrication of molecular electronic devices. We will discuss how to fabricate self-assembled monolayers into test assemblies and how to use intermolecular interactions to direct molecules into desired positions to create nanostructures and to connect functional molecules to the outside world. These assemblies serve as test structures for measurements on single or bundled molecules. The development of several experimental techniques, including various scanning probes, mercury drop junctions, break junctions, nanopores, crossed wires, and other techniques using nanoparticles have enabled the ability to test these structures and make reproducible measurements on single molecules. Many of these methods have been developed to test molecules with potential for integration into devices such as oligo (phenylene-ethynylene) molecules and other /spl pi/-conjugated molecules, in ensemble or single-molecule measurements. 相似文献
6.
MJ Weiss 《Canadian Metallurgical Quarterly》1997,11(6):1185-1198
Two advances in murine embryonic stem (ES) cell technology and their applications for the study of hematopoietic stem cells (HSCs) are discussed in this article. First, ES cells induced to differentiate in vitro form hematopoietic lineages in a fashion that recapitulates the ontogeny of blood formation in the embryo. This system offers a unique opportunity to isolate, examine, and manipulate the most primitive hematopoietic progenitors. Second, targeted gene ablation (knockout) studies in ES cells have identified several genes that are required for normal hematopoiesis and may function in the formation, maintenance, and differentiation of HSCs. Insights into murine hematopoiesis gained through the study of ES cells generally should be applicable to other vertebrates, including humans. 相似文献
7.
Larissa Canilha Walter Carvalho Marco Giulietti Maria Das Graças Almeida Felipe João Batista Almeida E Silva 《Journal of chemical technology and biotechnology (Oxford, Oxfordshire : 1986)》2008,83(5):715-721
BACKGROUND: Xylitol bioproduction from lignocellulosic residues comprises hydrolysis of the hemicellulose, detoxification of the hydrolysate, bioconversion of the xylose, and recovery of xylitol from the fermented hydrolysate. There are relatively few reports on xylitol recovery from fermented media. In the present study, ion‐exchange resins were used to clarify a fermented wheat straw hemicellulosic hydrolysate, which was then vacuum‐concentrated and submitted to cooling in the presence of ethanol for xylitol crystallization. RESULTS: Sequential adsorption into two anion‐exchange resins (A‐860S and A‐500PS) promoted considerable reductions in the content of soluble by‐products (up to 97.5%) and in medium coloration (99.5%). Vacuum concentration led to a dark‐colored viscous solution that inhibited xylitol crystallization. This inhibition could be overcome by mixing the concentrated medium with a commercial xylitol solution. Such a strategy led to xylitol crystals with up to 95.9% purity. The crystallization yield (43.5%) was close to that observed when using commercial xylitol solution (51.4%). CONCLUSION: The experimental data demonstrate the feasibility of using ion‐exchange resins followed by cooling in the presence of ethanol as a strategy to promote the fast recovery and purification of xylitol from hemicellulose‐derived fermentation media. Copyright © 2008 Society of Chemical Industry 相似文献
8.
I. Kasatkin F. Girgsdies T. Ressler R. A. Caruso J. H. Schattka J. Urban K. Weiss 《Journal of Materials Science》2004,39(6):2151-2157
The orientation relations m(100) || t(001), m[001] || t[110]; m(011) || t(100), m[100] || t[001]; m(100) || t(110), m[001] || t[001]; m(013) || t(116), m[001] || t[001] (indices for the primitive tetragonal cell) have been found between the tetragonal (t) and monoclinic (m) domains during the electron irradiation-induced m-t phase transition observed in-situ with HREM within isolated zirconia nanoparticles. Geometric models of the m-t interfaces are proposed. 相似文献
9.
George Weiss 《Mathematics of Control, Signals, and Systems (MCSS)》1991,4(2):193-203
We give an elementary proof of the well-known fact that shift-invariant operators onL
2[0, ∞) are represented by transfer functions which are bounded and analytic on the right open half-plane. We prove a generalization
to Banach space-valuedL
p
-functions, where 1≤p<∞. We show that the result no longer holds forp=∞.
This research was supported partially by the Weizmann Fellowship, and partially by the Air Force Office of Scientific Research
under Contract F49620-86-C-0111. 相似文献
10.
Hans-Dirk Walter 《Informatik-Spektrum》2008,31(4):333-343
Zusammenfassung ,,Rich Internet Applications“ (RIA) sind Webapplikationen, die mit einer wesentlich interaktiveren Benutzerschnittstelle ausgestattet
sind, als wir das bisher von den auf HTML basierten ,,poor ugly web applications“ (PUWA) gewohnt waren. 相似文献