bluuebunny/crossref_metadata_2025 huggingface dataset:
Binding of Clozapine Metabolites and Analogues to the Histamine H3 Receptor in Rat Brain Cortex
Authors: Alves‐Rodrigues Alexandra , Leurs Rob , Willems Edwin , Timmerman Henk
Published: October 2006

Following up the finding that the non‐imidazole drug clozapine shows a considerable histamine H3 receptor antagonistic activity[1,2], a series of analogues and metabolites (clozapine‐N‐oxide, and N‐desmethylclozapine) were tested for their affinity towards the H3 receptor using the radiolabelled H3 antagonist [125I]‐iodophenpropit.

Qualitative structure affinity relationships are derived for the tested compounds. In the clozapine molecule four structurally different moieties may be considered. In comparison with the affinity for the H3 receptor shown by clozapine, the following main conclusions can be drawn: The 4‐piperazinyl region does not allow substituents longer than a CH3 or electronegative atoms such as an O (as in clozapine‐N‐oxide); the lack of the CH3 group (as in N‐desmethylclozapine) also reduces the affinity for H3 receptors. Substitutions at the 5‐diazepine position do not drastically alter the affinity for the H3 receptor, although a basic nitrogen is favoured over CH2, O, or S. The 8 position in ring I is an important modulatory site for H3 affinity; electronegative substituents such as chloro and fluoro in this aromatic ring increase the affinity. When these substituents are, however, present at position X2 in the ring, they disable binding to the H3 receptor.

The two major clozapine metabolites (clozapine‐N‐oxide, and N‐desmethylclozapine) will not be responsible for a possible contribution of the H3 receptor antagonism to the clinical profile of clozapine.
In Vitro Anti‐Mycobacterium avium Activity of N‐(2‐Hydroxyethyl)‐1,2‐benzisothiazol‐3(2H)‐one and ‐thione Carbamic Esters
Authors: Pagani Giuseppe , Borgna Pietro , Piersimoni Claudio , Nista Domenico , Terreni Marco , Pregnolato Massimo
Published: October 2006

A series of N‐(2‐hydroxyethyl)‐1,2‐benzisothiazol‐3(2H)‐one and ‐thione carbamic esters have been synthesised and tested against Mycobacterium avium strains. The MIC values determined by the radiometric broth dilution method were between 2 and 8 μg/mL for the benzisothiazolthione derivatives and between 16 and 32 μg/mL or higher for the corresponding benzisothiazolone derivatives.
Synthesis and Antimicrobial Properties of New 4‐(Alkylidene/arylidene)‐amino‐5‐(2‐furanyl)‐2,4‐dihydro‐3H‐1,2,4‐triazole‐3‐thiones and 6‐Aryl‐3‐(2‐furanyl)‐7H‐1,2,4‐triazolo[3,4‐b][1,3,4]thiadiazines
Authors: Ergenç Nedime , Ulusoy Nuray , Çapan Gültaze , Sanis Gülten Ötük , Kiraz Muammer
Published: October 2006

A series of 4‐(alkylidene/arylidene)amino‐5‐(2‐furanyl)‐2,4‐dihydro‐3H‐1,2,4‐triazole‐3‐thiones (2) and 6‐aryl‐3‐(2‐furanyl)‐7H‐1,2,4‐triazolo[3,4‐b][1,3,4] thiadiazines (3) were synthesized. The configuration of 2g was assigned on the basis of 1H‐NMR data. Of the new derivatives tested, only 2b, 2g, and 4f were found to be active against Staphylococcus aureus and/or Staphylococcus epidermidis (MIC 125–1.95 μg/ml), whereas all exhibited varying degrees of antifungal activity (MIC 25–0.8 μg/ml).
Synthesis and Antibacterial Activity of 1‐β‐Methylcarbapenem Having a 1,3‐Diazabicyclo[3.3.0]octan‐4‐one Moiety
Authors: Nam Ki Hong , Oh Chang‐Hyun , Cho Jin Koo , Kim Hyo Jung , Lee Ki‐Soo , Cho Jung‐Hyuck
Published: October 2006

The synthesis of new series of 1‐β‐methylcarbapenems having a 1,3‐diazabicyclo[3.3.0]octan‐4‐one moiety is described. Their in vitro antibacterial activities against both Gram‐positive and Gram negative bacteria are reported and the effect of the substituent on the bicyclic ring was investigated and was in agreement with findings from our previous studies.
Three Lupane Derivatives from Leptospermum scoparium
Authors: Mayer Ralf
Published: October 2006

The ether extract of the aerial parts of Leptospermum scoparium cultivars yielded a lactone with a 20,29,30‐ trinorlupane skeleton (1). Furthermore, 2α‐hydroxyursolic acid (2), platanic acid (3) and 3β,30‐dihydroxy‐lup‐20(29)‐en‐28‐oic acid (4) were isolated.
Antimalarial Activity of 1,4‐Epidioxy‐bisabola‐2,12‐diene Derivatives
Authors: Rücker Gerhard , Breitmaier Eberhard , Manns Detlef , Maier Walter , Marek Anne , Heinzmann Berta , Heiden Klemens , Seggewies Stephan
Published: October 2006

1,4‐Epidioxy‐bisabola‐2,12‐diene (3) and aromatic hydroperoxides (4, 5) were prepared by photoxidation of γ‐curcumene (1). Reduction and esterification of 6 and 7 afforded compounds 9 to 10. All compounds were tested in vitro for antimalarial activity. The activity could not be increased significantly, compared with 3. The most active compounds, 3 and 9, did not show in vivo antimalarial activity in mice.
Pyridazines 82[1]. Synthesis of Pyridazino[3,4‐b][1,5]benzodiazepin‐5‐ones and their Biological Evaluation as Non‐nucleoside HIV Reverse Transcriptase Inhibitors
Authors: Heinisch Gottfried , Huber Elisabeth , Matuszczak Barbara , Maurer Astrid , Prillinger Ulrike
Published: October 2006

Starting from 3,6‐dichloro‐N‐(2−chloro‐5‐nitrophenyl)‐pyrid‐azine‐4‐carboxamide (7) a series of 6,11‐dialkylated pyridazino‐[3,4‐b][1,5]benzodiazepin‐5‐ones with a 3−chloro‐8‐nitro, 8‐amino, 8‐acetylamino, or 8−chloro substitution pattern was prepared via N‐alkyl‐3‐alkylamino‐6−chloro‐N‐(2−chloro‐5‐nitro‐phenyl)‐pyridazine‐4‐carboxamides. The new compounds were screened as non‐nucleoside reverse transcriptase inhibitors. The influence of the substitution pattern in compounds 10–13 on inhibitory potency is discussed.
Synthesis and In Vitro Evaluation of 3‐(1‐Azolylmethyl)‐1H‐indoles and 3‐(1‐Azolyl‐1‐phenylmethyl)‐1H‐indoles as Inhibitors of P450 arom
Authors: Borgne Marc Le , Marchand Pascal , Duflos Muriel , Delevoye‐Seiller Bénédicte , Piessard‐Robert Sylvie , Baut Guillaume Le , Hartmann Rolf W. , Palzer M.
Published: October 2006

In the challenge to develop potent inhibitors of aromatase for reducing the levels of estrogens, we found that azolyl‐substituted indoles inhibit aromatase activity. 3‐(1‐Azolylmethyl)‐1H‐indoles 9–15 and 3‐(1‐azolyl‐1‐phenylmethyl)‐1H‐indoles 22–25 were prepared, and tested on their ability to inhibit P450 arom. Analysis of the inhibitory effect exerted by several derivatives (11, 12, 22, and 23) on microsomal aromatase in vitro activity indicates that azolyl‐substituted indoles containing an imidazole moiety are more potent inhibitors than triazole derivatives. In the first series, the introduction of the N‐benzyl moiety has been found to enhance the inhibitory profile of these 3‐(1‐azolylmethyl)‐1H‐indole derivatives. The corresponding 4‐fluoro derivative 12 displays the highest inhibitory activity (IC50 = 0.0718 μM) of all investigated compounds; thus, 12 is 258 times as potent as aminoglutethimide (AG). The presence of a chloro grouping in para position of the phenyl ring in compounds 22 and 24 exerts a positive effect only in the triazol‐1‐yl sub‐series: compound 25 is 4‐fold more potent than 24.
Conformational Flexibility of Serotonin1A Receptor Ligands from Crystallographic Data. Updated Model of the Receptor Pharmacophore
Authors: Chilmonczyk Zdzislaw , Szelejewska‐Wozniakowska Agnieszka , Cybulski Jacek , Cybulski Marcin , Koziol Anna E. , Gdaniec Maria
Published: October 2006

Preparation and affinity to 5‐HT1A and 5‐HT2A receptors of new buspirone analogues 7–17 are reported. The compounds possess high to low affinity to 5‐HT1A and moderate to low to 5‐HT2A receptors. The crystal structures have been determined for compounds 11, 12, 13, and 14. For low affinity ligand (15) of 5‐HT1A receptor conformational analysis was performed and compared with similar analyses performed for know high (buspirone 1) and very high (WY‐48, 723 2) affinity ligands of the receptor. Structure‐activity relationship is discussed for the affinity to 5‐HT1A receptor. A three‐point pharmacophore explaining interactions of buspirone‐like molecules with the receptor binding site is proposed.
Synthesis and Antitumor Activity of 9‐Anilino, Phenylhydrazino, and Sulphonamido Analogs of 2‐ or 4‐Methoxy‐6‐nitroacridines
Authors: El‐Subbagh H. I. , Abadi A. H. , Al‐Khamees H. A.
Published: October 2006

Synthesis of several new 9‐anilino, phenylhydrazino, and sulphonamido analogs of 2‐ or 4‐methoxy‐6‐nitroacridine derivatives is described. The prepared compounds were tested for their in vitro antitumor activity against 60 human tumor cell lines by the National Cancer Institute (NCI) and showed a potential anticancer activity. Compounds 9‐(phenylhydrazino)‐2‐methoxy‐6‐nitroacridine (8a) and 9‐(4‐chlorophenylhydrazino)‐4‐methoxy‐6‐nitroacridine (9b) exhibited a broad spectrum antitumor activity with full panel (MG‐MID) median growth inhibition (GI50), of 16.1 and 10.9 μM and total growth inhibition (TGI) of 66.7 and 37.9 μM, respectively. Meanwhile, compounds 15a and 15b showed moderate selectivity toward leukemia cell lines. As a trial to explore the mode of action of their antitumor activity, the 6‐nitroacridine analogs were evaluated for their inhibitory effect on major cell cycle control proteins cdc2 kinase and cdc25 phosphatase as possible molecular targets that may account for antimitotic potency. None of the tested compounds proved to exert their activity via this antimitotic mode of action.
Novel 1,5‐Benzodiazepines as CCK‐B Ligands. Effect of Aryl‐Carbamic Substituents at the C‐3 Position Together with Halogen Substitution on the Benzo‐Fused Ring
Authors: Tranquillini M. Elvira , Cassarà Paolo G. , Corsi Mauro , Curotto Giovanni , Donati Daniele , Finizia Gabriella , Pentassuglia Giorgio , Polinelli Stefano , Tarzia Giorgio , Ursini Antonella , van Amsterdam Franciscus T. M.
Published: October 2006

The synthesis and biological evaluation as potential CCK‐B receptor ligands of a number of 1‐isopentyl‐3‐aryloxycarbamoyl‐5‐aryl‐1,5‐benzodiazepines substituted with halogen atoms on the benzo‐fused ring is here briefly discussed.
Raumakustische Gestaltung offener Bürolandschaften
Authors: Fuchs Helmut V. , Renz Jochen
Published: October 2006

Die Verdichtung der Arbeitsplätze in Großraumbüros stößt an ergonomische Grenzen, weil der Lärm auf unvermeidbar hohe Pegel anschwillt. Nach herkömmlicher Vorstellung wird versucht, mit Akustikdecken und ‐stellwänden die durch die starke Kommunikation im Raum erzeugten Geräusche bei den hohen Frequenzen zu bedämpfen. Dies widerspricht aber nicht nur den aktuellen Trends zur thermischen Aktivierung und optischen Transparenz aller Begrenzungsflächen. Es löst vor allem, wie an zahlreichen Beispielen gezeigt werden kann, das Problem nicht an seinen Wurzeln, d.h. bei den Schallquellen selbst. Nur wenn man durch einen gleichmäßig niedrigen Nachhall bis zu den tiefsten Frequenzen herunter für beste Sprachverständlichkeit sorgt, kann man akustische Behaglichkeit herstellen und den für konzentriertes geistiges Arbeiten unerläßlichen Lärmschutz erreichen. Mit neuartigen, stets breitbandig wirksamen, kompakten Akustik‐Modulen und transparenten Schall‐Schirmen lassen sich jetzt völlig offene Bürolandschaften optisch attraktiv und akustisch optimal gestalten. Nach der Auflösung eines alten raumakustischen Dilemmas können so endlich brach liegende Büro‐Immobilien z. B. für Großraum‐(Gruppen‐ und Team‐)Büros mit nur 6 bis 12 m2 pro Mitarbeiter sehr flexibel und kostengünstig revitalisiert und nachhaltig in ihrem Wert gesteigert werden – reizvolle neue Aspekte für Projektentwickler und Investoren in einem noch wachsenden Markt.
Strom, Wärme und Kühlung mit intelligenten Fertigteilen aus Beton
Authors: Riffel Siegfried
Published: October 2006

Ausgehend von den heutigen ökologischen und ökonomischen Anforderungen an Gebäude werden künftig die regenerativen Energien wie Photovoltaik und Solarthermie einen hohen Stellenwert einnehmen und auch die Bautechnik und Architektur vom Städtebau bis hin zum Detail verändern. Der vorliegende Beitrag stellt die innovative Lösung für ein massives Dach‐ und Wandsystem aus Betonfertigteilen mit integrierten Solarkollektoren und PV‐Modulen vor.
Pest, Stadt, Wissenschaft — Wechselwirkungen in oberitalienischen Städten vom 14. bis 17. Jahrhundert
Authors: Bergdolt Klaus
Published: October 2006

After the Black Death of 1348 the Plague was not only the cause of personal disasters and individual despair, but was also of political and social significance. Each outbreak of the epidemic implied a crisis for the community with crucial consequences for trade, jurisdiction, administration, executive powers and for food supply. The faith in authority by the leading university medics was tragic, as they subscribed to the hippocratic‐galenical humoral pathology and to the miasmatic theory. On the other hand, municipal authorities, from the 14th century onwards responded to the epidemic in a pragmatic manner, isolating the sick, carrying out checks, imposing trade embargos and special epidemic laws. From the 15th century onwards people were also put under quarantine. The medics' role, their relationship with the government and their tendency to play down the diagnosis will be discussed at length, together with the questionable tradition of the Regimina pestis.
Camille Flammarion und der Zweite Hauptsatz der Thermodynamik
Authors: Kleinert Andreas
Published: October 2006

In Camille Flammarion's book La fin du monde, published in 1894, we find the picture shown in fig. 2: Some poorly dressed people, including a mother with her child, are shivering with cold in an extremely hostile environment of ice and snow. In two wide‐spread German history of science textbooks, this picture is given as an illustration of the pessimistic conclusions that some nineteenth century physicists (among them Hermann von Helmholtz) had drawn from the Second Law of Thermodynamics. They believed that in a remote future, the entropy of the universe would grow to a maximum, and all available energy would be transformed into heat. This apocalyptic vision was often called “heat death”, but as the average temperature would then be very low, the expression “cold death” was used as well.

By analysing Flammarion's text, it is shown that he was not a supporter of this vision of the end of the world. According to Flammarion, mankind would die of cold as a consequence of the lack of water vapour in the atmosphere, and this would occur about twenty million years before the exhaustion of the sun as a source of energy. The use of this picture as an illustration of the heat death (or cold death) theory derived from thermodynamics is a misinterpretation that reminds of the erroneous assumptions that were expressed with regard to another picture by Flammarion (fig. 1). This illustration stemming from L'Atmosphére: Météorologie populaire (Paris 1888) was for many years (and sometimes is still) falsely considered as a medieval German woodcut.
Natur‐Wissenschaft und Gotteserkenntnis: Das jüdische Modell
Authors: Niewöhner Friedrich
Published: October 2006

The thesis proposed here is that in Judaism creation is seen as a unique act of God at a specific point in time. In medieval philosophy the act of creation is interpreted as natural science, which concerns itself only with products of divine creation. This is contrasted with theology, which is concerned not with creation but with God. Francis Bacon takes this model from Moses Maimonides for his work Nova Atlantis. Natural science replaces theological studies for Bacon.
Überbewertung der eigenen Nation Der Anteil der eigenen Landsleute an naturwissenschaftshistorischen Lexika
Authors: Graf‐Stuhlhofer Franz
Published: October 2006

Do editors of books on the history of science prefer scientists of their own country in their selection? Restricting ourselves to German, British and French scientists, a comparison of books in these languages shows that each editor takes more than half of the selected scientists from his respective nation and the remainder from the other two nations. The dictionaries of Fritz Krafft (‚Große Naturwissenschaftler’︁, 21986) and Ilse Jahn et al.: (‚Geschichte der Biologie. […] Kurzbiographien’︁, 1982) dedicate about 60% of their articles to German scientists, Trevor Illtyd Williams (‚A Biographical Dictionary of Scientists’︁, 1969) about 50% to British scientists and Maurice Daumas (‚Histoire de la Science’︁, 1957; according to the register) about 50% to French scientists.
Wissenschaftsgeschichte und Ur‐ und Frühgeschichte
Authors: Wiegert Mathias
Published: October 2006

During the past few years a history of special subjects and a history of science, being critical and historical as well as taking into account scientific theory and methodology, has established itself under the influence of philosophy in many domains of the sciences. Such a scientific history is now also required in the branch of the science of history. It demands the ability of re‐evaluating historical sources and studies as well as the knowledge of the political aspect of a future scientific history.

As a matter of fact a future scientific chronicle of prehistory has to examine not only the subject of historical research itself, but also its aim, method and the whole sociopolitical background. This is more important than a positivist study of individual and specific historical aspects, a thorough compilation of different approaches in historical research, scientists and institutions. It is also better than making an arbitrary selection of single biographies in order to have a political legitimation of the present state of research. Moreover, the danger of such a selection is the degradation of persons in history and the falsification of historical facts. Apart from a determination of the subject with regard to scientific and political aspects the search of historical clues as well as the re‐evaluation of historical and archeological sources could both lead to a revision of prehistory.
Zum ‚Zitieren’︁ in der mittelalterlichen Architektur
Authors: Glimme Hans‐Peter
Published: October 2006

About ‘citation’ in medieval architecture. ‐ The knowledge of art‐historical terms deriving from linguistics, especially concerning the term ‘citation’, is methodologically interesting. In the first instance, it is necessary to take a look at the meaning of the term regarding the history of architecture. The next step turns to the development of the linguistic model of the Indo‐European language and its influence on art‐historical vocabulary. The aspect of language starts with a remark on Gotthold Ephraim Lessing's Laokoon or About the borderline between painting and literature (‘Laokoon oder Über die Grenzen der Malerei und Poesie’). The paper carries on with the usage of the term ‘citation’ in architecture by discussing some leading scholars of architectural history. The appendix of the paper includes some good examples of architectural citation in textual sources of the middle ages.
Krieg und Technik im Zeitalter des Hellenismus
Authors: Schneider Helmuth
Published: October 2006

In the 4th century BC the Greek warfare underwent major changes because of the development of siege‐craft and the innovation of the catapult. Technicians who worked on catapults and other devices used in sieges gained in influence on warfare and military decisions. Technology became a major aspect in the waging of war, and mechanics tried to increase the efficiency of newly developed arms such as the catapult. Objections to the developments in military technology cannot be found in Greek literature.
Bazillen, Krankheit und Krieg Bakteriologie und politische Sprache im deutschen Kaiserreich
Authors: Gradmann Christoph
Published: October 2006

The text analyses metaphors of bacteriology which were extensively used in Germany during the era of William II. These display – in a vivid exchange with the scientific concepts of the age – a specific popular understanding of disease based on bacteriology. Disease is essentially seen as a war of physicians against microbes. While popularizing science bacteriological metaphors became part of the political language of their age. At the same time the prestige of bacteriology was in turn employed to lend credibility to pictures of assumed enemies – by portraying them as infectious diseases. Although the political language of bacteriology differed from the social darwinism of the age in important structural and semantic aspects, it nevertheless influenced the political language of its time, for example by becoming a blueprint of antisemitic rhetorics.
Faktor Mensch im Krieg Der Eintritt der Psychologie und Psychotechnik in den Krieg
Authors: Gundlach Horst
Published: October 2006

In the First World War representatives of the university discipline of psychology took the opportunity to apply their expertise in the armed forces. The initial undertakings in the German Empire and in the USA show some similarities and marked disparities. A comparison of events and circumstances in these principal belligerent states is linked with a sketch of their importance for the further development of psychology as an academic specialty and an emerging profession.
Vom Nationalsozialismus vertriebene Wissenschaftler auf dem Markt. Die Arbeitsvermittlung des englischen Academic Assistance Council (SPSL) am Beispiel von Türkeiemigranten
Authors: Erichsen Regine
Published: October 2006

After 1933 many scientists and university teachers were obliged to relinquish their posts in the universities of Germany because of national‐socialist laws. Organizations‐in‐aid like the Academic Assistance Council in Great Britain tried to ‘defend science and learning’ raising funds and finding new openings for the expelled academics. But as immigration laws were tight and jobs were scarce in the host countries the AAC and the other organizations had to select the most qualified from among the applicants for support. – The questions the article tries to answer are: What kind of criteria were applied in this selection? Who were the experts? How were the placements made? How did the applicants react to the decisions? Taking for example the AAC, it examines measures to assist a group of scientists who, having tried to settle down in England, finally emigrated to Turkey.
Seuchenkonzepte und frühneuzeitliche Gesellschaft: Deutungen von „Pestilenzen”︁ und städtischer Alltag
Authors: Kinzelbach Annemarie
Published: October 2006

This study shows how the different concepts of epidemic diseases met with the everyday needs of the late medieval and early modern society. The analysis of practice and discourse in the context of „pestilences”︁ covers broad social strata from representatives of the authorities and medical doctors to artisans and the „poor”︁ in German Imperial Towns and their territories. Generally, those persons acted according to a variety of concepts. Their seemingly contradictory actions cannot be explained refering to their ignorance about infection, but have to be interpreted in the appropriate situational context. In this context it is possible to understand how the variety and parallelism of different concepts enabled groups as well as individuals to choose those notions of the spreading of diseases which promised the least interference with their plans and intentions.
Begründung der wissenschaftlichen Geographie durch Bernhard Varenius (1622‐1650)? Gedanken zu den Defiziten der Varenius‐Forschung aus Anlaß des Varenius‐Jahres 2000
Authors: Büttner Manfred
Published: October 2006

Beeing sofar a part of mathematics Geography was drafted by Bernard Varenius in 1650 as full‐geography (Büttner: Vollgeographie) which contents mathematical, physical and even human geography. Whereas the «Geographia Generalis» has been published in England for several times its influence in continental Europe seems to have been marginal. Therefore Varenius cannot be considered as founder of modern geography. The relation of general and special geography is discussed und a lot of mistakes and absurdities in Varenius' work is exposed.
Die Gesellschaft Naturforschender Freunde zu Berlin ‐ Bestand und Wandel einer gelehrten Gesellschaft Ein Überblick
Authors: Böhme Katrin
Published: October 2006

The article deals with the foundation and development of the society Gesellschaft Naturforschender Freunde zu Berlin in the 18th and 19th centuries, its position as a privat society for natural history in Berlin, and its relation to Freemasonry. The paper shows the change of meaning of these society, especially after the foundation of the Berlin university in 1810.
Thermodynamic Properties of (NH4)2Ca [B4O5(OH)4] 2×8H2O.
Authors: Han Wei‐He , Liu Zhi‐Hong , Zhang Wen‐Juan , Zuo Chuan‐Feng , Liang Sheng‐Jun
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Synthesis of 2‐Alkylidenepyrrolidines and Pyrroles by Condensation of 1,3‐Dicarbonyl Dianions with α‐Azidoketones and Subsequent Intramolecular Staudinger—Aza‐Wittig Reaction.
Authors: Freifeld Ilia , Shojaei Heydar , Langer Peter
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Copper‐Free and Copper‐Promoted Conjugate Addition Reactions of Bis(triorganosilyl) Zincs and Tris(triorganosilyl) Zincates.
Authors: Auer Gertrud , Weiner Barbara , Oestreich Martin
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
CrAsH (I): A Biarsenical Multi‐Use Affinity Probe with Low Non‐Specific Fluorescence.
Authors: Cao Haishi , Chen Baowei , Squier Thomas C. , Mayer M. Uljana
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Recent Advances in CuI/IIY: Experiments and Modeling.
Authors: Berthomieu Dorothee , Delahay Garard
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Experimental Approaches to the Preparation of Supported Metal Nanoparticles
Authors: Barkhuizen David , Mabaso Itai , Viljoen Elvera , Welker Cathrin , Claeys Michael , van Steen Eric , Fletcher Jack C. Q.
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
1,2,4‐Triazolo[1,5‐a][1,3,5]triazines (5‐Azapurines): Synthesis and Biological Activity
Authors: Dolzhenko Anton V. , Dolzhenko Anna V. , Chui Wai‐Keung
Published: October 2006

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Serum epidermal growth factor receptor/HER‐2 predicts poor survival in patients with metastatic breast cancer
Authors: Souder Christopher , Leitzel Kim , Ali Suhail M. , Demers Laurence , Evans Dean B. , Chaudri‐Ross Hilary A. , Hackl Wolfgang , Hamer Peter , Carney Walter , Lipton Allan
Published: October 2006

BACKGROUND.

Epidermal growth factor receptor (EGFR, HER‐1, and erbB1) is overexpressed in primary breast cancer and had been identified as a poor prognostic factor.

METHODS.

Pretreatment serum EGFR levels were quantified by using an enzyme‐linked immunoadsorbent assay in a Phase III first‐line trial of letrozole and tamoxifen and were correlated with patient outcomes.

RESULTS.

Serum EGFR levels in a control group of 117 healthy, postmenopausal women measured 64.1 ± 13.3 ng/mL (mean ± standard deviation). Using a cutoff EGFR level of 44.1 ng/mL from the control group (5% nonparametric method), 53 of 535 patients (10%) had decreased serum levels of EGFR. Patients with decreased serum EGFR had no significant difference in objective response rate (ORR), clinical benefit rate (CBR), time to progression (TTP), or time to treatment failure (TTF); however, they did have significantly reduced survival compared with patients who had normal serum EGFR levels (median survival, 23.3 months vs. 30.9 months; P = .007). A combined analysis of pretreatment serum EGFR and HER‐2 yielded no additional predictive information for ORR, CBR, TTP, or TTF compared to serum HER‐2 alone. However, in the current analysis, a subgroup of patients who had decreased serum EGFR and normal serum HER‐2 was identified (n = 39 of 535 patients; 7.3%) that had significantly reduced survival compared with patients who had normal serum levels of both EGFR and HER‐2 (median survival, 23.5 months vs. 37.1 months; P = .005). In multivariate analysis, a decreased serum EGFR level remained a significant independent prognostic factor for decreased survival (hazards ratio, 1.58; P = .007).

CONCLUSIONS.

In patients who had metastatic breast cancer, decreased serum EGFR/normal serum HER‐2 predicted shorter survival compared with patients who had normal levels of serum EGFR/HER‐2. This patient subgroup deserves further study to assess their response to and selection for anti‐EGFR‐directed therapies. Cancer 2006. © 2006 American Cancer Society.
A population‐based study of the impact of specific symptoms on quality of life in women with breast cancer 1 year after diagnosis
Authors: Arndt Volker , Stegmaier Christa , Ziegler Hartwig , Brenner Hermann
Published: October 2006

BACKGROUND.

Whereas the role of specific symptoms, such as pain and fatigue, for quality of life (QOL) is unquestioned, their relative importance for long‐lasting impairments in QOL in cancer patients has rarely been assessed quantitatively. The authors, therefore, aimed to identify symptoms most predictive of limitations to function and overall QOL in women with breast cancer after completion of primary therapy.

METHODS.

The European Organisation for Research and Treatment of Cancer questionnaire QLQ‐C30 and the breast–cancer‐specific module QLQ‐BR23 were used to measure QOL in a population‐based sample from Saarland (Germany) of 314 women with breast cancer 1 year after diagnosis. Symptoms most predictive for limitations to function and overall QOL were identified with a multiple linear regression analysis.

RESULTS.

Fatigue emerged as the strongest predictor by far of QOL, explaining around 30% to 50% of variability within function scores and overall QOL. Other symptoms, including pain, nausea and/or vomiting, breast symptoms, systemic therapy side effects, and arm symptoms, explained on average <5% of variability of various QOL scales beyond fatigue and age. Sociodemographic and clinical factors had little impact on QOL.

CONCLUSIONS.

Although QOL is a multidimensional concept, the analysis suggested that fatigue is the symptom that had, by far, the largest impact on limiting function and on overall QOL in breast cancer patients after their completion of primary therapy. Specific interventions to reduce the burden of fatigue may represent a particularly worthwhile effort to improve QOL in women with breast cancer. Cancer 2006. © 2006 AmericanCancer Society.
Differential expression of unconventional myosins in apoptotic and regenerating chick hair cells confirms two regeneration mechanisms
Authors: Duncan Luke J. , Mangiardi Dominic A. , Matsui Jonathan I. , Anderson Julia K. , MClaughlin‐Williamson Kate , Cotanche Douglas A.
Published: October 2006

Hair cells of the inner ear are damaged by intense noise, aging, and aminoglycoside antibiotics. Gentamicin causes oxidative damage to hair cells, inducing apoptosis. In mammals, hair cell loss results in a permanent deficit in hearing and balance. In contrast, avians can regenerate lost hair cells to restore auditory and vestibular function. This study examined the changes of myosin VI and myosin VIIa, two unconventional myosins that are critical for normal hair cell formation and function, during hair cell death and regeneration. During the late stages of apoptosis, damaged hair cells are ejected from the sensory epithelium. There was a 4–5‐fold increase in the labeling intensity of both myosins and a redistribution of myosin VI into the stereocilia bundle, concurrent with ejection. Two separate mechanisms were observed during hair cell regeneration. Proliferating supporting cells began DNA synthesis 60 hours after gentamicin treatment and peaked at 72 hours postgentamicin treatment. Some of these mitotically produced cells began to differentiate into hair cells at 108 hours after gentamicin (36 hours after bromodeoxyuridine (BrdU) administration), as demonstrated by the colabeling of myosin VI and BrdU. Myosin VIIa was not expressed in the new hair cells until 120 hours after gentamicin. Moreover, a population of supporting cells expressed myosin VI at 78 hours after gentamicin treatment and myosin VIIa at 90 hours. These cells did not label for BrdU and differentiated far too early to be of mitotic origin, suggesting they arose by direct transdifferentiation of supporting cells into hair cells. J. Comp. Neurol. 499:691–701, 2006. © 2006 Wiley‐Liss, Inc.
Efferent projections of reuniens and rhomboid nuclei of the thalamus in the rat
Authors: Vertes Robert P. , Hoover Walter B. , Do Valle Angela Cristina , Sherman Alexandra , Rodriguez J.J.
Published: October 2006

The nucleus reuniens (RE) is the largest of the midline nuclei of the thalamus and exerts strong excitatory actions on the hippocampus and medial prefrontal cortex. Although RE projections to the hippocampus have been well documented, no study using modern tracers has examined the totality of RE projections. With the anterograde anatomical tracer Phaseolus vulgaris leuccoagglutinin, we examined the efferent projections of RE as well as those of the rhomboid nucleus (RH) located dorsal to RE. Control injections were made in the central medial nucleus (CEM) of the thalamus. We showed that the output of RE is almost entirely directed to the hippocampus and “limbic” cortical structures. Specifically, RE projects strongly to the medial frontal polar, anterior piriform, medial and ventral orbital, anterior cingulate, prelimbic, infralimbic, insular, perirhinal, and entorhinal cortices as well as to CA1, dorsal and ventral subiculum, and parasubiculum of the hippocampus. RH distributes more widely than RE, that is, to several RE targets but also significantly to regions of motor, somatosensory, posterior parietal, retrosplenial, temporal, and occipital cortices; to nucleus accumbens; and to the basolateral nucleus of amygdala. The ventral midline thalamus is positioned to exert significant control over fairly widespread regions of the cortex (limbic, sensory, motor), hippocampus, dorsal and ventral striatum, and basal nuclei of the amygdala, possibly to coordinate limbic and sensorimotor functions. We suggest that RE/RH may represent an important conduit in the exchange of information between subcortical‐cortical and cortical‐cortical limbic structures potentially involved in the selection of appropriate responses to specific and changing sets of environmental conditions. J. Comp. Neurol. 499:768–796, 2006. © 2006 Wiley‐Liss, Inc.
Efferent projections of rat rostroventrolateral medulla C1 catecholamine neurons: Implications for the central control of cardiovascular regulation
Authors: Card J. Patrick , Sved Judy C. , Craig Brian , Raizada Mohan , Vazquez Jorge , Sved Alan F.
Published: October 2006

A replication‐defective lentivirus vector that expresses enhanced green fluorescent protein (EGFP) under the control of a synthetic dopamine‐β‐hydroxylase (DβH) promoter was used to define efferent projections of C1 catecholamine neurons in rat rostral ventrolateral medulla (RVLM). EGFP expression was restricted to C1 neurons and filled their somatodendritic compartments and efferent axons 7–28 days after vector injection. This included the descending projections to thoracic spinal cord and a network in brainstem, midbrain, and diencephalon. In caudal brainstem, restricted terminal fields were present in the dorsal motor vagal complex, A1, raphe pallidus and obscurus, and marginal layer of ventrolateral medulla. Innervation of raphe nuclei was most dense at the level of RVLM, but rostral levels of pallidus were devoid of innervation. A sparse commissural projection to contralateral RVLM was observed, and pericellular arbors were present in the dorsal reticular formation among the projection pathway of catecholamine axons. Rostral brainstem contained a dense innervation of locus coeruleus and the nucleus subcoeruleus. A restricted innervation of the ventrolateral column of the periaqueductal gray distinguished the midbrain. Forebrain labeling was restricted to the diencephalon, where distinctive terminal fields were observed in the paraventricular thalamic nucleus; the lateral hypothalamic area; and the paraventricular, dorsomedial, supraoptic, and median preoptic nuclei of hypothalamus. Projection fibers also coursed through the tuberal hypothalamus into the median eminence. Collectively, these data demonstrate that RVLM C1 neurons modulate the activity of other central cell groups known to participate in the regulation of cardiovascular and autonomic function. J. Comp. Neurol. 499:840–859, 2006. © 2006 Wiley‐Liss, Inc.
Metric‐based upscaling
Authors: Owhadi Houman , Zhang Lei
Published: October 2006

We consider divergence form elliptic operators in dimension n ge; 2 with L∞ coefficients. Although solutions of these operators are only Hölder‐continuous, we show that they are differentiable (C1, α) with respect to harmonic coordinates. It follows that numerical homogenization can be extended to situations where the medium has no ergodicity at small scales and is characterized by a continuum of scales. This new numerical homogenization method is based on the transfer of a new metric in addition to traditional averaged (homogenized) quantities from subgrid scales into computational scales. Error bounds can be given and this method can also be used as a compression tool for differential operators. © 2006 Wiley Periodicals, Inc.
Stability properties of steady water waves with vorticity
Authors: Constantin Adrian , Strauss Walter A.
Published: October 2006

We present two stability analyses for exact periodic traveling water waves with vorticity. The first approach leads in particular to linear stability properties of water waves for which the vorticity decreases with depth. The second approach leads to a formal stability property for long water waves that have small vorticity and amplitude although we do not use a small‐amplitude or long‐wave approximation. © 2006 Wiley Periodicals, Inc.
Deposition of Ni and Pd Sulfide Thin Films via Aerosol‐Assisted CVD
Authors: O'Brien P. , Waters J.
Published: October 2006

Thin films of nickel sulfide (NiS1.03, NiS2,α‐Ni7S6, or mixtures thereof) and palladium sulfide (PdS, Pd16S7, Pd4S, or mixtures thereof) have been prepared by aerosol‐assisted (AA)CVD using dithiocarbamate precursors of the type M(S2CNRR')2(M = Ni, Pd; RR' = Et2, MeEt, MenBu, or MenHex). The solid‐state structure of Ni(S2CNMenBu)2, was determined by X‐ray single‐crystal diffraction and is characteristic of known nickel dithiocarbamates. Films were grown on glass substrates at temperatures of 400–525 °C and characterized by X‐ray diffraction (XRD), energy dispersive analysis of X‐rays (EDAX), and scanning electron microscopy (SEM).
A Novel Potentiometric Membrane Sensor Based on Aryl Palladium Complex for Selective Determination of Thiocyanate in the Saliva and Urine of Cigarette Smokers
Authors: Hassan Saad S. M. , Mohmoud Wagiha H. , Elgazwy Abdel‐Sattar S. Hamad , Badawy Nahla M.
Published: October 2006

A highly selective potentiometric sensor for thiocyanate ion based on the use of a newly synthesized organo‐palladium ion exchanger complex dispersed in a plasticized poly(vinyl chloride) membrane is described. The sensor displays a Nernstian response (−57.8±0.2 mV decade−1) over a wide linear concentration range of thiocyanate (1.0×10−6–1.0×10−1 mol L−1 ), low detection limit (6.3×10−7 mol L−1), fast response (20 s), stable potential readings (±0.4 mV), good reproducibility (±0.9%), long term stability (8 weeks), high precision (±0.7%) and applicability over a wide pH range (4–10). Negligible interferences are caused by F−, Cl−, I−, Br−, NO3−, NO2−, CN−, SO42−, S2O32−, PO43−, citrate, acetate and oxalate ions. Under hydrodynamic mode of operation (FIA), the calibration slope is −51.1±0.1 mV decade−1, the linear response range is 1.0×10−5–1.0×10−1 mol L−1 SCN− and the sample throughput is 40–45 per hour. The sensor is satisfactory used for manual and flow injection potentiometric determination of SCN− in the saliva and urine of cigarette smokers and non smokers. The data agree fairly well with results obtained by the standard spectrophotometric technique. Direct potentiometry and potentiometric titration of SCN− with Ag+ are also monitored with the sensor.
A Study on Stripping Voltammetric Determination of Osmium(IV) at a Carbon Paste Electrode Modified In Situ with Cationic Surfactants
Authors: Galík Michal , Cholota Michal , Švancara Ivan , Bobrowski Andrzej , Vytřas Karel
Published: October 2006

This article deals with the development of a method for the determination of osmium at a carbon paste electrode (CPE) modified with cationic surfactants of the quaternary ammonium salt type; namely, cetyltrimethylammonium bromide (CTAB) and 1‐(ethoxycarbonyl)‐pentadecyltrimethyl‐ammonium bromide (Septonex); both being added in situ and serving for preconcentration of osmium via its hexachloroosmate(IV) anion. The proper electrochemical detection was performed by cathodic scanning in the differential pulse voltammetric mode. Optimization studies concerning important experimental parameters also included a specially performed potentiometric titration, helping to define the actual stoichiometry for the ion‐pairing process, the main principle and driving force of the accumulation step. In a chloride/acetate buffer based supporting medium and with Septonex as the modifier of choice, the reduction signal for osmium was found to be proportional to the Os(IV) concentration in a range from 5×10−9 to 5×10−7 mol L−1 with a limit of detection close to 5×10−9 mol L−1 (with preconcentration for 60 s). The method capable to determine Os(IV) in the presence of both Pt(IV) and Ir(III) was tested on model solutions as well as with real sample of industrial waste water (spiked with the analyte); both yielding the recovery rates within 88–99%.
Seismic performance evaluation of non‐structural components: drywall partitions
Authors: Lee Tae‐Hyung , Kato Mikiko , Matsumiya Tomohiro , Suita Keiichiro , Nakashima Masayoshi
Published: October 2006

As the first part of non‐structural component test series, interior drywall partitions are selected for an experimental program. This test series will cover non‐structural components that are significant in the economic losses in buildings subjected to seismic loading, namely interior drywall partitions, exterior cladding and window glasses, and ceilings. Four full‐scale drywall partitions with light‐gage steel stud framing were tested to observe damage in cyclic loading conditions. Effects of a door and an intersecting wall on the behaviour of drywall partition are studied. Damage was concentrated to perimeter regions where gypsum boards made contacts with ceiling, floor, or columns. Dynamic loading did not amplify the damage on a drywall partition over the damage observed from the quasi‐static test. Damage–repair cost relationships show that the repair cost reaches almost the initial cost under 2% radian interstorey drift. Copyright © 2006 John Wiley & Sons, Ltd.
Practical causal hysteretic damping
Authors: Nakamura Naohiro
Published: October 2006

A number of experiments indicate that the internal damping corresponding to the energy dissipation of many materials is essentially frequency independent. Accordingly, an analysis model that can express such characteristics (called a hysteretic damping model) in the time domain is needed. Although a great number of investigations into this subject have been carried out, there are a few practical methods. In this paper, a simple hysteretic damping model which satisfies the causality condition is presented using an extension of the complex stiffness transfer method that the author has proposed. Compared with the energy proportional damping model and the Biot model, the applicability and the efficiency of this model to time history response analyses were confirmed well by example problems. Copyright © 2006 John Wiley & Sons, Ltd.
A symmetric time‐domain model for 3D dam–reservoir interaction including radiation damping
Authors: Birk C. , Ruge P.
Published: October 2006

In this paper a new strategy for the description of a 3D dam–reservoir system in the time‐domain is proposed. Here, the structure and a finite part of the reservoir of arbitrary geometry and foundation are treated using standard finite elements. In doing so, nonlinearities can be included. Radiation damping is taken into account accurately by means of an adjacent semi‐infinite fluid channel. The key step of the method is the novel treatment of this unbounded part of the system. Based on a semi‐discretization of the latter a frequency‐dependent modal stiffness coefficient relating the pressure at the fluid–fluid interface to the corresponding flux can be derived analytically. A rational approximation and algebraic splitting procedure enable the transformation of this spectral stiffness relationship into the time‐domain. A set of first‐order differential equations to represent the semi‐infinite fluid channel is obtained which can be coupled to the equations of motion of the bounded part of the system. The complete dam–reservoir system is finally described by a symmetric set of second‐order differential equations replacing the pressure by new state variables. Copyright © 2006 John Wiley & Sons, Ltd.
Coupling chemical weathering with soil production across soil‐mantled landscapes
Authors: Burke Benjamin C. , Heimsath Arjun M. , White Arthur F.
Published: October 2006

Soil‐covered upland landscapes constitute a critical part of the habitable world. Our understanding of how they evolve as a function of different climatic, tectonic and geological regimes is important across a wide range of disciplines and depends, in part, on understanding the links between chemical and physical weathering processes. Extensive previous work has shown that soil production rates decrease with increasing soil column thickness, but chemical weathering rates were not measured. Here we examine a granitic, soil‐mantled hillslope at Point Reyes, California, where soil production rates were determined using in situ produced cosmogenic nuclides (10Be and 26Al), and we quantify the extent as well as the rates of chemical weathering of the saprolite from beneath soil from across the landscape. We collected saprolite samples from the base of soil pits and analysed them for abrasion pH as well as for major and trace elements by X‐ray fluorescence spectroscopy, and for clay mineralogy by X‐ray diffraction spectroscopy. Our results show for the first time that chemical weathering rates decrease with increasing soil thickness and account for 13 to 51 per cent of total denudation. We also show that spatial variation in chemical weathering appears to be topographically controlled: weathering rate decreases with slope across the divergent ridge and increases with upslope contributing area in the convergent swale. Furthermore, to determine the best measure for the extent of saprolite weathering, we compared four different chemical weathering indices – the Vogt ratio, the chemical index of alteration (CIA), Parker's index, and the silicon–aluminium ratio – with saprolite pH. Measurements of the CIA were the most closely correlated with saprolite pH, showing that weathering intensity decreases linearly with an increase in saprolite pH from 4·7 to almost 7. Data presented here are among the first to couple directly rates of soil production and chemical weathering with how topography is likely to control weathering at a hillslope scale. Copyright © 2006 John Wiley & Sons, Ltd.