bluuebunny/crossref_metadata_2025_split huggingface dataset:
Synthesis and Biological Investigations of Some New Thiazolylbenzimidazoles and Benzimidazolylthiazolo[3,2‐a]pyridines
Authors: Rida S. M. , Habib N. S. , Badawey E. A. M. , Fahmy H. T. Y. , Ghozlan H. A. 
Published: October 2006

Abstract2‐[(4‐Oxo‐4,5‐dihydrothiazol‐2‐yl)methyl]‐1H‐benzimidazole (2) was prepared through the reaction of 2‐cyanomethyl‐1H‐benzimidazole (1) with thioglycolic acid. The syntheses of its arylidene 3 and diazo‐coupled compounds 5 and the cyclization of the aforementioned thiazolylbenzimidazole to benzimidazolylthiazolo[3,2‐a]pyridines 8 were also performed. The prepared compounds were screened for their in‐vitro antibacterial, antifungal, anti‐HIV, and anticancer activities: they show promising antifungal activity.
Platelet Aggregation Inhibiting and Anticoagulant Effects of Oligoamines, XXIX: Influence of the Antithrombotic Oligoamine RE 1492 on the Storage of Red Blood Cells, Morphology, their Potassium and ATP Content, Hemolysis and Viability
Authors: Rehse Klaus , Müller Susann 
Published: October 2006

AbstractThe influence of RE 1492 on the storage of red blood cells (RBCs) was investigated. RE 1492 (c ⩾ 50 μmol/L) induces the formation of cup cells and hence delays the appearance of echinocytes and crenated spheres in the blood. A concentration of 50 μmol/L RE 1492 drops hemolysis by 50 %. At this concentration after 6 h of storage the potassium efflux was enhanced significantly. The ATP concentration was decreased between 12 h and 24 h of storage. During the first 6 h these alterations have no effect on the in vivo viability of RBCs. After 12 h of storage a significant reduction in viability is observed. We suppose that the changes observed are due to the intercalation of RE 1492 in the phospholipid matrix of the RBC membrane, followed by an accelerated substrate turnover in the RBCs.
Preparation and In Vitro Pharmacology of 5‐HT4 Receptor Ligands. Partial Agonism and Antagonism of Metoclopramide Analogous Benzoic Esters
Authors: Elz Sigurd , Keller Andreas 
Published: October 2006

AbstractAlicyclic ester analogues of the gastroprokinetic benzamide metoclopramide (1) and its ester congener SDZ 205557 (2), a 5‐HT4 receptor antagonist, were prepared by O‐alkylation of 4‐amino‐5‐chloro‐2‐methoxybenzoate with N‐(2‐chloroethyl) substituted alicyclic amines. The bromo and iodo analogue of compound 13b (2‐(1‐piperidinyl)ethyl 4‐amino‐5‐chloro‐2‐methoxybenzoate) were obtained by halogenation of dechloro‐13b with N‐halogenated succinimides. The series was evaluated in functional in vitro assays with regard to affinity for serotoninergic 5‐HT4, 5‐HT3 and muscarinic M3 receptors. The affinities for 5‐HT4 and M3 receptors were below 6.0 (pKB or pA2). On 5‐HT4 receptors in guinea‐pig ileal longitudinal muscle and rat oesophagus, the majority of compounds revealed partial 5‐HT4 receptor agonism susceptible to blockade by SDZ 205557, a reference 5‐HT4 receptor antagonist (pKb = 7.25 − 7.73 (guinea‐pig ileum) and 7.09 — 7.43 (rat oesophagus)). The relative agonist potency was in the range of 5 – 303 % (5‐HT: 100 %). Compound 13b and its bromo analogue 17 were the most potent esters of the series. The enantiomers of 13g ((R)‐ and (S)‐2‐(2‐methyl‐1‐piperidinyl)ethyl 4‐amino‐5‐chloro‐2‐methoxybenzoate) interacted stereoselectively with 5‐HT4 receptors and displayed enantiomeric potency ratios (R)/(S) of 4.3 — 8.7. There was an excellent correlation between (a) antagonist affinity on guinea‐pig ileum and rat oesophagus, (b) relative agonist potency on guinea‐pig ileum and rat oesophagus, and (c) between antagonist affinity and relative agonist potency within each assay (r2 > 0.91). The new compounds may serve as academic tools in evaluating the functional role of 5‐HT4 receptors. The selective partial 5‐HT4 receptor agonists presented in this paper may be useful to restore physiological motility and secretion in the gut with reduced or absent propensity to elicit tachycardia and desensitization of the intestinal target receptor.
Synthesis of GABA‐Valproic Acid Derivatives and Evaluation of Their Anticonvulsant and Antioxidant Activity
Authors: Rekatas George V. , Tani Ekaterini , Demopoulos Vassilis J. , Kourounakis Panos N. 
Published: October 2006

AbstractThe synthesis and the anticonvulsant activity of a number of GABA and valproic acid derivatives are reported. The lipophilicity of these compounds and their inhibitory effect on lipid peroxidation were also investigated, in an effort to correlate the anticonvulsant activity with lipophilicity and inhibitory effect on lipid peroxidation. The synthesized compounds exhibited anticonvulsant effects which were stronger for the more lipophilic derivatives. One of the active anticonvulsants showed appreciable antioxidant properties. Finally, a good correlation was found between the experimentally derived (RM) and calculated (σ and log PSK) lipophilicity for this series of compounds.
Passive Kühlung und sommerliche Überhitzung – Sind Simulationen auf der Grundlage des Test Reference Year (TRY) ein geeignetes Bewertungskriterium?
Authors: Rozynski Matthias 
Published: October 2006

AbstractDie beobachteten Klimaänderungen führen zu einer Häufung warmer Sommer. Die sechs heißesten wurden in den letzten neun Jahren seit Beginn der Gebietsmittelzeitreihe – d. h. beginnend mit dem Jahr 1901 – gemessen, die Spitze bildet dabei der Rekordsommer 2003. Deshalb stellt sich die Frage, mit welchen Maßnahmen hohe Raumtemperaturen in Verwaltungsgebäuden, insbesondere im Sanierungsfall, wirksam verhindert werden können.
„Und setzet eure Worte nicht auf Schrauben”︁ Medizinische Semiotik vom Ende des 18. bis zum Beginn des 20. Jahrhunderts ‐ Gegenstand und Forschung
Authors: Eckart Wolfgang U. 
Published: October 2006

AbstractThere is no doubt that medical semiotics are having a revival at the moment. Different aspects of yesterday's and today's interest in semiotics and in the historical interpretation of signs of disease in the context of theory and history of medicine can be illuminated: their deciphering as the history of the sign in medicine by historic science, their overestimation by philosophy during the Age of Enlightenment, their reduction to a phenomenology of medicine and natural science during the first half of the 19th century and their transformation to medical diagnostics since the middle of the 19th century and recently even their functionalization as methodical instrument within the history of science. The following will show the change in meaning of medical semiotics. Modern development and especially the transition to medicine, based on natural science, will be emphasized.
Wie Huren und Betrüger — die Begegnung des jungen Descartes mit der Welt der Praktiker der Mathematik
Authors: Schneider Ivo 
Published: October 2006

AbstractDescartes describes in the Discours de la méthode his stay in Germany in winter 1619/20 as decisive for his intellectual development. In Germany he was especially interested in the mathematics of German reckoningmasters and mathematical practitioners. Frustrated from their form of representation, from their mathematical „style”︁, he began to create his own, which he considered a first step in the development of his method in order to secure true knowledge. Descartes could derive additional confirmation for his task by the mentalities of orthodox and heterodox protestantism. He learned that Johannes Faulhaber one of the leading German mathematicians had strong connections to the rosicrucian movement, a very popular form of heterodox protestantism. The convictions and aims of the supporters of the rosicrucian movement in part agreed with and in part contradicted seriously those of Descartes, whereas the arguments of the orthodox protestants in their fight against the rosicrucian movement interacted positively with the ideas of Descartes. The reaction of Descartes to his encounter with German protestantism offers an important element for the explanation of the strong positive and negative reactions to Cartesianism in protestant countries, especially in the Netherlands.
Lebens‐Geschichte ‐ Wissenschafts‐Geschichte. Vom Nutzen der Biographie für Geschichtswissenschaft und Wissenschaftsgeschichte
Authors: Szöllösi‐Janze Margit 
Published: October 2006

AbstractBiography as a genre of historiography had been dismissed for some years, criticized for being conservative, resistant to theoretical approaches, and hostile to methodological innovations. But the predominance of a historiography devoted to structures, functions, and statistics has, however, led to a renewed interest in the human factor in history. This paper argues that the pluralism of methods and theories which has emerged thereafter reopened the case for an innovative biography, thus facilitating the convergence of general history and the history of science.
Wissenschaft im Gehäuse: Vom Nutzen und Nachteil institutionengeschichtlicher Perspektiven
Authors: vom Bruch Rüdiger 
Published: October 2006

AbstractResearch is realized in social and cultural context, it is established in institutions, as far as different forms and conditions of practice are concerned. In this article some German examples demonstrate how flexible and varied the institutions of research can be during the course of history of science. The first part deals with historically grown, yet chronologically overlapping institutions of research: beginning with the lonely scholar, going on to hierarchally organized big science and ending up with virtual institutions. In the second part, at the intersection of political‐social administration and styles of scientific thought terms like German Realpolitik, science in context, and science policy are discussed within the modernization process.
Raum und Disziplin. Klinische Wissenschaft im Krankenhaus
Authors: Hess Volker 
Published: October 2006

AbstractThe historical shift in the function of the hospital from an asylum for the care of the indigent sick to a medical‐therapeutic institution is intimately associated with the exploitation of the hospital as a clinical facility. Thus, over the course of the 19th century the space of the hospital and its disciplinary structure was permeated and reorganized by clinical practices.Drawing on the example of the Charite hospital in Berlin, it can be shown how the historical shift in the hospital's outward social function went hand in hand with the creation of a differentiated internal clinical space. In this compartmentalized clinical space the discipline of the hospital was replaced with methods of clinical examination, techniques of observation, and procedures of documentation, all of which helped to transform the hospital into a knowledge‐space.
Aspekte zur Sammlungs‐ und Einrichtungsgeschichte des Berliner Pergamonmuseums
Authors: Matthes Olaf 
Published: October 2006

AbstractThis article focuses on the development of the Pergamon‐Museum of Berlin and its various collections. The predecessor of the current museum building gave only place for the Great Altar of Pergamon and some other architectural pieces of the hellenistic period. After its abolishment in 1908 the new erected building (which opened only in 1930) contained before World War II three museum departments (Deutsches Museum, Pergamon‐Museum, and the Vorderasiatisches Museum). ‐ There were some long‐lasting frictions between the directors Wilhelm von Bode, Theodor Wiegand, and the architect Ludwig Hoffmann about the question whether roman provincial architecture is worth to be exhibited in a museum or not ‐ here exemplified on the Market Gate of Miletus. Wilhelm II, the Kaiser, was strongly involved not only in this but was generally interested in all museum matters. It was always he who made the last decision, and the museum directors tried very often to persuade him of their ideas.
Hypercross‐Linked Fiber and its Adsorption of Cyclohexane Vapor
Authors: Yanli Z. , Li D. G. , Jiang D. G. 
Published: October 2006

AbstractA novel hypercross‐linked fiber which has an excellent adsorption capacity for cyclohexane vapor was prepared by cross‐linking PP‐ST‐DVB fibers with p‐xylylenedichloride according to the Friedel‐Crafts reaction. The effects of several important factors on the Friedel‐Crafts reaction, including reaction temperature, reaction time, catalyst type, and material ratio were investigated in detail and the optimal synthesis conditions of hypercross‐linked fiber were obtained. The adsorption equilibrium for cyclohexane vapor on hypercross‐linked fiber was measured by a static volumetric technique. The equilibrium measurements were performed at 298, 323 and 348 K and pressures of up to 6.04 kPa. The results can be well fitted by the Freundlich model. The isosteric heat curve was derived from the equilibrium data, and indicates that the hypercross‐linked fiber has an energetically heterogeneous surface.
Donor/Conductor/Acceptor Triads Spatially Organized on the Micrometer‐Length Scale: An Alternative Approach to Photovoltaic Cells
Authors: Llabrés i Xamena Francesc X. , Teruel Laura , Alvaro Mercedes , Garcia Hermenegildo 
Published: October 2006

AbstractWe have used porous anodised Al2O3 membranes as inert matrix for constructing and organizing spatially ternary donor/conductor/acceptor (DCA) systems exhibiting photovoltaic cell activity on the micrometric‐length scale. These DCA triads were built stepwise by first growing a conducting polymer inside the membrane pores, thus forming nanorods that completely fill the internal pore space of the membrane. Then, an electron donor and an electron acceptor were adsorbed one on each side of the membrane, so that they were separated by a distance equal to the membrane thickness (ca. 60 μm), but electronically connected through the conductive polymer. When this device was placed between two electrodes and irradiated with visible light, electrons jumped from the donor molecule, crossed the membrane from side to side through the conductive polymer (a journey of about 60 μm!) until they finally reach the acceptor molecule. In so doing, an electric voltage was generated between the two electrodes, capable of maintaining an electric current flow from the membrane to an external circuit. Our DCA device constitutes the proof of a novel concept of photovoltaic cells, since it is based on the spatial organization at the micrometric scale of complementary, but not covalently linked, electron‐donor and electron‐acceptor organic species. Thus, our cell is based in translating photoinduced electron transfer between donors and acceptors, which is known to occur at the molecular nanometric scale, to the micrometric range in a spatially organised system. In addition our cell does not need the use of liquid electrolytes in order to operate, which is one of the main drawbacks in dye‐sensitised solar cells.
Palladium‐Catalyzed Intramolecular C(sp3)H Functionalization: Catalyst Development and Synthetic Applications
Authors: Hitce Julien , Retailleau Pascal , Baudoin Olivier 
Published: October 2006

AbstractA novel catalytic system, based on a mixture of palladium acetate and tris(5‐fluoro‐2‐methylphenyl)phosphane (F‐TOTP), has been designed for the intramolecular CH functionalization of alkane segments. Among other analogues of tris(2‐methylphenyl)phosphane (P(o‐tol)3), F‐TOTP was shown to have the optimal metal‐bonding properties for this reaction. This catalytic system operated under milder reaction conditions that allowed the regioselective production of various olefins adjacent to a quaternary benzylic carbon atom, as well as novel bi‐ and tricyclic molecules. A general mechanism was proposed, with the preferential formation of a six‐membered palladium(II) palladacycle after oxidative addition and cyclopalladation. The regioselective CH functionalization of alkyl groups into olefins was illustrated in the synthesis of the antihypertensive drug verapamil (14) and an analogue (19). A particularly mild ruthenium‐catalyzed direct hydroamidation of the intermediate olefin in this synthesis is also reported.
Synthesis, Structures, and Properties of meso‐Phosphorylporphyrins: Self‐Organization through P–Oxo–Zinc Coordination
Authors: Matano Yoshihiro , Matsumoto Kazuaki , Terasaka Yukiko , Hotta Hiroki , Araki Yasuyuki , Ito Osamu , Shiro Motoo , Sasamori Takahiro , Tokitoh Norihiro , Imahori Hiroshi 
Published: October 2006

AbstractThe synthesis, structures, and optical and electrochemical properties of meso‐phosphorylporphyrins are described. The copper‐catalyzed carbon–phosphorus cross‐coupling reaction of a meso‐iodoporphyrin with di‐n‐butyl phosphite and diphenylphosphane oxide has proved to be an efficient and general method for the synthesis of meso‐phosphorylporphyrins. Zinc phosphorylporphyrins thus obtained readily undergo self‐organization through P–oxo–Zn coordination to form noncovalently linked, cofacial porphyrin dimers or linear oligomers, which have been characterized by spectroscopic methods and X‐ray crystallographic analyses. In toluene, CH2Cl2, and CHCl3, the zinc phosphorylporphyrins exist mostly as dimers or monomers, depending on their concentrations, the temperature, and the presence of additives. The self‐association constants for dimerization in toluene have been determined by UV/Vis absorption titration measurements. The meso‐diphenylphosphorylporphyrin dimer displays excitonic coupling of the Soret band with a splitting energy of 940 cm−1. Fluorescence lifetimes of the zinc phosphorylporphyrins have been found to be affected only slightly by the concentration of the solution, and by the addition of triphenylphosphane oxide, suggesting that the effect of dimerization on their photodynamics in the S1 state is negligible. On the other hand, the effect of dimerization is clearly reflected in their electrochemical oxidation processes, as the initially produced radical cations are efficiently delocalized over the two porphyrin rings. These findings demonstrate the potential utility of meso‐phosphorylporphyrins as new models for the special pair in photosynthesis and as new building blocks for porphyrin‐based supramolecular materials.
Semiclassical determination of exponentially small intermode transitions for 1 + 1 spacetime scattering systems
Authors: Joye Alain , Marx Magali 
Published: October 2006

AbstractWe consider the semiclassical limit of systems of autonomous PDEs in 1 + 1 spacetime dimensions in a scattering regime. We assume the matrix‐valued coefficients are analytic in the space variable, and we further suppose that the corresponding dispersion relation admits real‐valued modes only with one‐dimensional polarization subspaces. Hence a BKW‐type analysis of the solutions is possible. We typically consider time‐dependent solutions to the PDE that are carried asymptotically in the past and as x → −∞ along one mode only and determine the piece of the solution that is carried for x → +∞ along some other mode in the future. Because of the assumed nondegeneracy of the modes, such transitions between modes are exponentially small in the semiclassical parameter; this is an expression of the Landau‐Zener mechanism. We completely elucidate the spacetime properties of the leading term of this exponentially small wave, when the semiclassical parameter is small, for large values of x and t, when some avoided crossing of finite width takes place between the involved modes. © 2006 Wiley Periodicals, Inc.
Bauaufsichtliche Einführung der DIN 1053‐100
Authors: Jäger Wolfram 
Published: October 2006

AbstractSeit August 2006 liegt die DIN 1053‐100 nach dem neuen Teilsicherheitskonzept in konsolidierter Fassung vor. Die Norm ist in die Musterliste der Technischen Baubestimmungen aufgenommen worden und kann nunmehr in den Bundesländern eingeführt werden. Die lange Phase von der Veröffentlichung bis zur Einführung ist begründet in einer gewissen Schlechterstellung der Nachweise für horizontale Einwirkungen, in den Verschärfungen durch die neuen Lastnormen sowie durch die Erdbebennorm und in einem Defizit in der “heißen” Bemessung (Feuerwiderstand). Ersteres wurde versucht abzudämpfen. Für den Nachweis der Feuerwiderstandsdauer konnten leider noch keine Gewinne, die sich bei vertikaler Belastung ergeben, nutzbar gemacht werden. Jedoch ist es gelungen, eine klare Lösung zu finden.Es ist nunmehr eine durchgängige Bemessung und Nachweisführung für Gebäude nach dem Teilsicherheitskonzept möglich. Der Beitrag gibt Hintergrundinformationen zu den Änderungen und Hinweise zur Anwendung der DIN 1053‐100.
Neuroblastoma tumors with favorable and unfavorable outcomes: Significant differences in mRNA expression of genes mapped at 1p36.2
Authors: Fransson Susanne , Martinsson Tommy , Ejeskär Katarina 
Published: October 2006

AbstractThe distal part of 1p is frequently deleted in aggressive neuroblastoma, and the region is believed to harbor one or more tumor suppressor genes relevant to tumor development. To analyze differences among neuroblastoma tumors, an expression profile was established for the genes mapped within a previously described shortest region of overlap of deletions at 1p36.2. The gene expression levels were quantified by TaqMan real‐time (RT)‐PCR for 30 transcripts using 55 primary neuroblastoma tumors. Here we report on a significant decrease in gene expression of the genes RERE, PIK3CD, LZIC, PGD, and PEX14 and an increase of SLC2A5 when comparing tumors of favorable biology to Stage 4 neuroblastomas. When comparing 1p‐deleted tumors of all stages to tumors with an intact 1p, a significant difference at gene‐by‐gene level in TNFRSF9, RERE, PIK3CD, CLSTN1, CTNNBIP1, and CASZ1 was detected. A complete loss of expression could not be seen for any single gene analyzed. Several of the genes with diminished expression in unfavorable or 1p‐deleted tumors have functions that could contribute to tumor development. It is also possible that a combination of lowly expressed genes at 1p, rather than one single classical tumor suppressor gene, causes the unfavorable outcome associated with 1p‐deletion in neuroblastoma. © 2006 Wiley‐Liss, Inc.
Overlay analysis of the oligonucleotide array gene expression profiles and copy number abnormalities as determined by array comparative genomic hybridization in medulloblastomas
Authors: Lo Ken C. , Rossi Michael R. , Burkhardt Tania , Pomeroy Scott L. , Cowell John K. 
Published: October 2006

AbstractCombined analysis of gene expression array data and array‐based comparative genomic hybridization data have been used in a series of 26 pediatric brain tumors to define up‐ and downregulated genes that coincide with losses, gains, and amplifications involving specific chromosome regions. Frequent losses were defined in chromosome arms 3q, 6q, 8p, 10q, 16q, 17p, and gains were identified in chromosome 7, and chromosome arms 9p and 17q. Amplification of a 2p region was seen in only one tumor, which corresponded to increased expression of the MYCN and DDX1 genes. To facilitate the analysis of the two data sets, we have developed a custom overlay tool that defines genes that are underexpressed in regions of deletions and overexpressed in regions of gain, across the genome and specifically within regions showing recurrent involvement in medulloblastomas. © 2006 Wiley‐Liss, Inc.