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1.
Synthesis of 2‐Unsubstituted 1,3‐Selenazoles by Cyclization of Selenoformamide with α‐Bromocarbonyl Compounds 下载免费PDF全文
Harald Below Wolf‐Diethard Pfeiffer Karlheinz Geisler Ashot S. Saghyan Christine Fischer Peter Langer 《Journal of heterocyclic chemistry》2015,52(2):592-596
2‐Unsubstituted 1,3‐selenazoles were prepared by cyclization of selenoformamide with α‐bromoacetophenones. Parent 1,3‐selenazole was prepared by cyclization of selenoformamide with α‐bromoacetaldehyde. 相似文献
2.
Fragment‐Based De Novo Design Reveals a Small‐Molecule Inhibitor of Helicobacter Pylori HtrA 下载免费PDF全文
Thomas P. Schmidt Dr. Manja Böhm Katharina Stutz Daniel Reker Dr. Bernhard Pfeiffer Prof. Dr. Karl‐Heinz Altmann Prof. Dr. Steffen Backert Prof. Dr. Silja Wessler Prof. Dr. Gisbert Schneider 《Angewandte Chemie (International ed. in English)》2015,54(35):10244-10248
Sustained identification of innovative chemical entities is key for the success of chemical biology and drug discovery. We report the fragment‐based, computer‐assisted de novo design of a small molecule inhibiting Helicobacter pylori HtrA protease. Molecular binding of the designed compound to HtrA was confirmed through biophysical methods, supporting its functional activity in vitro. Hit expansion led to the identification of the currently best‐in‐class HtrA inhibitor. The results obtained reinforce the validity of ligand‐based de novo design and binding‐kinetics‐guided optimization for the efficient discovery of pioneering lead structures and prototyping drug‐like chemical probes with tailored bioactivity. 相似文献
3.
H. H. Pfeiffer 《Rheologica Acta》1961,1(4-6):668-669
Ohne ZusammenfassungI thank Mr.Scott Blair for his answer reserving the term dilatancy for cases of real dilatation. Now it's only to wish that this terminology is used according to his Report on the principles of rheological nomenclature (Amsterdam 1949). 相似文献
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Anil Arya Clemens Löffler Brian Mittendorf Thomas Pfeiffer 《European Journal of Operational Research》2015
The prevalence of intermediaries (middlemen) in supply chains is often seen as a dying remnant of less efficient times. Despite predictions that supply chains will rapidly “cut out the middleman” as technological advances have eased logistics, middlemen have continued to thrive. In this paper, we demonstrate a transaction role of middlemen that may help clarify their staying power. In a model with self-interested decision-making by both a manufacturer and a retailer, wherein incentive misalignment creates investment and production inefficiencies, we show that the integrated (first-best) outcome can be achieved with simple cost-based contracts if and only if a middleman is present. We further show that the approach of utilizing a middleman to fully coordinate the supply chain is robust in that it can be applied to a variety of circumstances discussed in the literature, including multilateral investment/effort choices, multiple product providers, and logistical investments made by the middleman. 相似文献
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S. Krishna Prasad R. Shashidhar B. R. Ratna B. K. Sadashiva G. Heppke S. Pfeiffer 《Liquid crystals》2013,40(1):111-116
Abstract We present here precise measurements of the layer spacing for two compounds, viz. 4-n-heptyloxyphenyl-4′-(4″-cyanobenzoyloxy)benzoate and 4-n-undecyloxyphenyl-4′-(4″-cyanobenzyloxy)benzoate. Contrary to earlier reports our data do not show any jump in the layer spacing at the expected Ad-A2 transition temperature, showing thereby that for both compounds A2 evolves continuously from the Ad phase. 相似文献
9.
Nano titanium dioxide (nTiO2), generally considered to be toxicologically inert, is manufactured in large quantities and extensively applied in consumer products. The small size and large surface area endow them with an active group or intrinsic toxicity. Advances in instrumentation are making Raman spectroscopy the tool of choice for an increasing number of (bio) chemical applications. One of the great advantages of this technique is its ability to provide information on the concentration, structure and interaction of biochemical molecules in their microenvironments within intact cells and tissues, non-destructively. Zebrafish (Danio rerio), one of the most important vertebrate model organisms used in developmental biology, are increasingly used in biomedical research, particularly as a model of human disease. In the present work, an attempt is made to study the effect of titanium dioxide, both nano and bulk, on the microenvironment of the liver tissues of Zebrafish using FT-Raman spectroscopy. The results of the present study suggest that TiO2 exposure demonstrate a marked influence on the microenvironments of the liver tissues of Zebrafish. A shift to a higher wavenumber and an increase in the intensity of the band at ∼1087 cm−1 in the TiO2 exposed tissues suggest that some of the conformational changes resulting from the alkali recovery process takes place due to TiO2 exposure. The decreased intensity ratio (I3220/I3400) observed in the titanium-exposed tissues suggests a decreased water domain size, which could be interpreted in terms of weaker hydrogen-bonded molecular species of water in the TiO2 exposed tissues. The observed shift of COO− bands to higher frequencies shows the disruption of salt bridges as a result of a change in the oppositely charged partners and due to the enhanced random coil conformation. The variation in the intensity ratio of the tyrosyl doublet (I858/I825) indicates variation in the hydrogen bonding of the phenolic hydroxyl group due to TiO2 exposure. The results further suggest that the microenvironments are greatly altered due to titanium nano exposure when compared to titanium bulk. In conclusion, the results indicate that FT-Raman spectroscopy might be a useful tool for rapid assessment of nano particle biological interactions. 相似文献
10.
Cyclization of 4‐Phenylthiosemicarbazide with Phenacylbromide Revisited. Formation of 1,3,4‐Thiadiazines and of Isomeric 1,3‐Thiazoles 下载免费PDF全文
Wolf‐Diethard Pfeiffer Dieter Junghans Ashot S. Saghyan Peter Langer 《Journal of heterocyclic chemistry》2014,51(4):1063-1067
The cyclization of 4‐phenylthiosemicarbazide with phenacylbromide, carried out in refluxing ethanol, afforded 1,3,4‐thiadiazine 1 as the major product. In contrast to a previous report, 2‐phenylimino‐4‐phenyl‐2,3‐dihydro‐1,3‐thiazol‐3‐amine ( 2 ) and not 2‐hydrazono‐3,4‐diphenyl‐2,3‐dihydro‐1,3‐thiazole ( 8 ) was formed as a side‐product. This product is the main product when the reaction is carried out in concentrated hydrochloric acid. Our findings were independently confirmed by independent syntheses of the isomeric products and by a thorough study of their reactivity. It is important to note that the product distribution of the cyclization of thiosemicarbazides with haloketones strongly depends on the substitution pattern and on the reaction conditions. 相似文献