Synthesis and reactions of two stereoisomeric 4.5.5.5 fenestranes with bridgehead substituents

The [4.5.5.5]fenestranes 2 and 3 with two different functionalities were prepared in seven steps with overall yields of 5% and 10%, respectively. For introduction of a bridgehead double bond the removal of the tertiary hydroxy group was investigated in the two stereoisomeric hydroxyketones 12 and 15. Whereas the dehydration readily occurred in 12, a ring opening reaction was observed for 15. (C) 2011 Elsevier Ltd. All rights reserved.

Factors associated with the incidence of type 2 diabetes mellitus in HIV-infected participants in the Swiss HIV Cohort Study

BACKGROUND: Human immunodeficiency virus (HIV)-infected persons may be at increased risk for developing type 2 diabetes mellitus because of viral coinfection and adverse effects of treatment. METHODS: We studied associations of new-onset diabetes mellitus with hepatitis B virus and hepatitis C virus coinfections and antiretroviral therapy in participants in the Swiss HIV Cohort Study, using Poisson regression. RESULTS: A total of 123 of 6513 persons experienced diabetes mellitus during 27,798 person-years of follow-up (PYFU), resulting in an incidence of 4.4 cases per 1000 PYFU (95% confidence interval [CI], 3.7-5.3 cases per 1000 PYFU). An increased incidence rate ratio (IRR) was found for male subjects (IRR, 2.5; 95% CI, 1.5-4.2), older age (IRR for subjects >60 years old, 4.3; 95% CI, 2.3-8.2), black (IRR, 2.1; 95% CI, 1.1-4.0) and Asian (IRR, 4.9; 95% CI, 2.2-10.9) ethnicity, Centers for Disease Control and Prevention disease stage C (IRR, 1.6; 95% CI, 1.04-2.4), and obesity (IRR, 4.7; 95% CI, 3.1-7.0), but results for hepatitis C virus infection or active hepatitis B virus infection were inconclusive. Strong associations were found for current treatment with nucleoside reverse-transcriptase inhibitors (IRR, 2.22; 95% CI, 1.11-4.45), nucleoside reverse-transcriptase inhibitors plus protease inhibitors (IRR, 2.48; 95% CI, 1.42-4.31), and nucleoside reverse-transcriptase inhibitors plus protease inhibitors and nonnucleoside reverse-transcriptase inhibitors (IRR, 3.25; 95% CI, 1.59-6.67) but were not found for treatment with nucleoside reverse-transcriptase inhibitors plus nonnucleoside reverse-transcriptase inhibitors (IRR, 1.47; 95% CI, 0.77-2.82). CONCLUSIONS: In addition to traditional risk factors, current treatment with protease inhibitor- and nucleoside reverse-transcriptase inhibitor-containing regimens was associated with the risk of developing type 2 diabetes mellitus. Our study did not find a significant association between viral hepatitis infection and risk of incident diabetes.

Differential response of porcine osteoblasts and chondrocytes in cell or tissue culture after 5-aminolevulinic acid-based photodynamic therapy

OBJECTIVE: Outcome in osteochondral allografting is limited by the immunological incompatibility of the grafted tissue. Based on a resistance of chondrocytes to photodynamic therapy in cell culture it is proposed that 5-aminolevulinic acid-based photodynamic therapy (5-ALA-PDT) might be used to inactivate bone while maintaining viability of chondrocytes and thus immunomodulate bone selectively. METHODS: Chondrocytes and osteoblasts from porcine humeral heads were either isolated (cell culture) or treated in situ (tissue culture). To quantify cytotoxic effects of 5-ALA-PDT (0-20J/cm(2), 100mW/cm(2)) an (3-(4,5-dimethylthiazol-2-yl)-2,5-di-phenyltetrazolium bromide) (MTT)-assay was used in cell culture and in situ hybridization in tissue culture to assess metabolic active cells (functional osteoblasts: colalpha(1)(I) mRNA, functional chondrocytes: colalpha(1)(II) mRNA). RESULTS: In cell culture, survival after 5-ALA-PDT was significantly higher for chondrocytes (5J/cm(2): 87+/-12% compared to untreated cells) than for osteoblasts (5J/cm(2): 12+/-11%). In tissue culture, the percentage of functional chondrocytes in cartilage showed a decrease after 5-ALA-PDT (direct fixation: 92+/-2%, 20J/cm(2): 35+/-15%; P<0.0001). A significant decrease in the percentage of bone surfaces covered by functional osteoblasts was observed in freshly harvested (31+/-3%) compared to untreated tissues maintained in culture (11+/-4%, P<0.0001), with no further decrease after 5-ALA-PDT. CONCLUSION: Chondrocytes were more resistant to 5-ALA-PDT than osteoblasts in cell culture, while in tissue culture a loss of functional chondrocytes was observed after 5-ALA-PDT. Since osteoblasts - but not chondrocytes - were sensitive to the tissue culture conditions, devitalized bone with functional cartilage might already be achieved by applying specific tissue culture conditions even without 5-ALA-PDT.

Synthesis and in vitro characterization of radioiodinatable benzodiazepines selective for type 1 and type 2 cholecystokinin receptors

Radiolabeled antagonists of specific peptide receptors identify a higher number of receptor binding sites than agonists and may thus be preferable for in vivo tumor targeting. In this study, two novel radioiodinated 1,4-benzodiazepines, (S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea (9) and (R)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea (7), were developed. They were characterized in vitro as high affinity selective antagonists at cholecystokinin types 1 and 2 (CCK(1) and CCK(2)) receptors using receptor binding, calcium mobilization, and internalization studies. Their binding to human tumor tissues was assessed with in vitro receptor autoradiography and compared with an established peptidic CCK agonist radioligand. The (125)I-labeled CCK(1) receptor-selective compound 9 often revealed a substantially higher amount of CCK(1) receptor binding sites in tumors than the agonist (125)I-CCK. Conversely, the radioiodinated CCK(2) receptor-selective compound 7 showed generally weaker tumor binding than (125)I-CCK. In conclusion, compound 9 is an excellent radioiodinated nonpeptidic antagonist ligand for direct and selective labeling of CCK(1) receptors in vitro. Moreover, it represents a suitable candidate to test antagonist binding to CCK(1) receptor-expressing tumors in vivo.

Simple and efficient synthesis of substituted 2-pyrrolidinones, 2-pyrrolones and pyrrolidines from enaminones of Baylis-Hillman derivatives of 3-isoxazolecarbaldehydes

The enaminones, generated from derivatives of appropriately substituted Baylis-Hillman adducts of 3-isoxazolecarbaldehydes undergo intramolecular ring-closure reactions to afford substituted 2-pyrrolidinones, 1,5-dihydro-2-pyrrolones and N-substituted pyrrolidines in good yields.

Nucleic-Acid Analogs with Restricted Conformational Flexibility in the Sugar-Phosphate Backbone (‘Bicyclo-DNA’). Part 5. Synthesis, Characterization, and Pairing Properties of Oligo-αlpha-D-(bicyclodeoxynucleotides) of the Bases Adenine and Thymine (αlpha-Bicyclo-DNA)

10.1002/hlca.19950780816.abs A conformational analysis of the (3′S,5′R)-2′-deoxy-3′,5′-ethano-α-D-ribonucleosides (a-D-bicyclodeoxynucleosides) based on the X-ray analysis of N4-benzoyl-α-D-(bicyclodeoxycytidine) 6 and on 1H-NMR analysis of the α-D-bicyclodeoxynucleoside derivatives 1-7 reveals a rigid sugar structure with the furanose units in the l′-exo/2′-endo conformation and the secondary OH groups on the carbocyclic ring in the pseudoequatorial orientation. Oligonucleotides consisting of α-D-bicyclothymidine and α-D-bicyclodeoxyadenosine were successfully synthesized from the corresponding nucleosides by phosphoramidite methodology on a DNA synthesizer. An evaluation of their pairing properties with complementary natural RNA and DNA by means of UV/melting curves and CD spectroscopy show the following characteristics: i) α-bcd(A10) and α-bcd(T10) (α = short form of α-D)efficiently form complexes with complementary natural DNA and RNA. The stability of these hybrids is comparable or slightly lower as those with natural β-d(A10) or β-d(T10)( β = short form ofβ-D). ii) The strand orientation in α-bicyclo-DNA/β-DNA duplexes is parallel as was deduced from UV/melting curves of decamers with nonsymmetric base sequences. iii) CD Spectroscopy shows significant structural differences between α-bicyclo-DNA/β-DNA duplexes compared to α-DNA/β-DNA duplexes. Furthermore, α-bicyclo-DNA is ca. 100-fold more resistant to the enzyme snake-venom phosphodiesterase with respect to β-DNA and about equally resistant as α-DNA.

Mus Hs 208 - Sinfonia a 2 violini, 2 oboe, 2 flauti, 2 corni in G, 2 corni in D, 2 fagotti, viola e bassi ; Stimmen zu der Sinfonia von Mozart N. 31, componirt 26. April 1779

del ... Wolfgango Amadeo Mozart

Fragm. germ. II 5 - Tristan

Vorbesitzer: Johann Franz Roth

Fragm. germ. IV 5 - Das Buch der Natur

Trägerband: Ms. Carm. 1; Vorbesitzer: Karmeliterkloster Frankfurt am Main

Na 1 Nachlass Max Horkheimer, 656 - Dokumente zur Geschichte des Instituts für Sozialforschung (p. IX 49a-IX 55.1-5)

Max Horkheimer: Über Wissenschaft und Technologie in Israel. Begrüßungsrede für Mr. Ben Sira, gehalten am 8.1.1949; 1. Notizen zur Rede, 10 Blatt; 2. David Ben Gurion, "Science and Technology in Israel", Sonderdruck, 2 Blatt; Über die Antisemitismus-Forschungen des Instituts für Sozialforschung. Protokoll einer Sitzung der Frankfurter Gesellschaft für Christlich-Jüdische Zusammenarbeit, 16.Mai 1949. Typoskript (Kopie), 2 Blatt; Max Horkheimer: Über Arbeit und Pläne des Instituts für Sozialforschung in Frankfurt. Vortrag, gehalten 1949 in Frankfurt (Clubabend). Manuskript, 3 Blatt; Zur Begründung eines Instituts für Sozialforschung, 1922; 1. Senckenbergische Naturforschende Gesellschaft, Frankfurt: 1 Brief mit Unterschrift (Kopie) an die Universität Frankfurt, Kuratorium, Frankfurt, 22.8.1922; 2. Felix Weil und Kurt Albert Gerlach: "Denkschrift über die Begründung eines Instituts für Sozialforschung" (1922). Typoskript (Kopie), 5 Blatt; Carl Grünberg: Festrede, gehalten zur Einweihung des Instituts für Sozialforschung an der Universität Frankfurt am Main, am 22.6.1924. a) Kopie (Auszug) aus dem Abdruck der Rede in Frankfurter Universitätsreden 1924, 3 Blatt b) Sonderdruck Frankfurter Universitätsreden 1924, 16 Seiten; Darstellungen des Instituts für Sozialforschung (1925-51); 1. Gesellschaft für Sozialforschung, Frankfurt: "Institut für Sozialforschung an der Universität Frankfurt am Main". Sonderdruck (Kopie), Frankfurt, 1925, 29 Seiten; 1a. Hermann Weil: "Bericht über das Heimatfest in Waibstadt am 3. und 4. September und die feierliche Übergabge meines Mausoleums in den Schutz der Stadt Waibstadt". Sonderdruck, 1927, 7 Seiten; 1b. Felix Weil, 1 Brief mit Unterschrift (Kopie) an den Minister für Wissenschaft, Kunst und Volksbildung Berlin. Frankfurt, 1.11.1929, Typoskript, 31 Blatt; 1c. Columbia University: "Report of the President of Columbia University for 1934" (darin S.7: Erwähnung des Instituts für Sozialforschung und der Zeitschrift für Sozialforschung), Sonderdruck, New York, 1934, 80 Seiten; 2. "International Institute of Social Research: A short Description of Its History and Aims", New York 1935, Sonderdruck, 15 Seiten; 3. Briefbogen des Instituts für Sozialforschung mit den Namen des Research Staff und des Advisory Committee, 1 Blatt; 4. "International Institute of Social Research. A Report On Its History, Aims and Activities 1933-1938". Sonderdruck, New York 1939, 36 Seiten; 5. "Research Bureau For Post-War Economics and Its Cooperating Institutions. Annual Repost", Sonderdruck, New York, Mai 1939, 17 Seiten; 5a. Los Angeles University of Applied Education: "General Catalogue 1947-48" (mit Erwähnungen des Instituts für Sozialforschung bzw. von Mitarbeitern), Druck, 56 Seiten; 6. Einladung zur Eröffnung des Instituts für Sozialforschung am 14. November 1951. Sonderdruck, Frankfurt 1951, 2 Blatt; Über das Institut für Sozialforschung 1924-31. Tabellarische Zusammenstellung, 1931, Typoskript mit eigenhändigen und handschriftlichen Ergänzungen, 5 Blatt; Max Horkheimer: "Die gegenwärtige Lage der Sozialphilosophie und die Aufgaben eines Instituts für Sozialforschung". Öffentliche Antrittsvorlesung bei Übernahme des Lehrstuhls für Sozialphilosophie und der Leitung des Instituts für Sozialforschung, 24.1.1931, Kopie (Auszug) aus dem Abdruck der Rede in Frankfurter Universitätsreden 1931, 4 Blatt; "History and Program of the Institute of Social Research". Veröffentlicht unter dem Titel "International Institute of Social Research. A Short Description of Its History and Aims", New York (1934 od. 1935), Typoskript, 6 Blatt.; "A Digest of the History, Program and Needs of the International Institute of Social Research". 1934, als Typoskript vervielfältigt, 4 Blatt; Julian Gumperz: "Notes for a talk", Über Ziele und Methoden der Arbeit des Instituts für Sozialforschung, 1934. Typoskript mit handschriftlicher Korrektur, 10 Blatt; "Report of the President of Columbia University for the year ending June 30, 1934".Auszug daraus, 1934, Typoskript, 1 Blatt; Über Geschichte und Tätigkeiten des Instituts für Sozialforschung. Verschiedene Berichte, ca. 1934-1937: 1. Über Geschichte, Tätigkeiten und Ziele des Instituts, nicht vor 1934, Typoskript, 5 Blatt; 2. Bericht an den Präsidenten der Columbia University, 14.3.1936, Typoskript, 2 Blatt; 3. "Dr. Horkheimer's Paper Delivered on the Occasion of an Institute Luncheon Given to the Faculty of Social Sciences of Columbia University on January 12th, 1937". Typoskript, 13 Blatt; 4. Bericht an den Präsidenten der Columbia University. 18.3.1937, Typoskript, 3 Blatt; 5. Über Programm, Mitglieder und Tätigkeiten des Instituts, 1937, a) Typoskript, 2 Blatt, b) Entwurf, Typoskript, 4 Blatt; 6. Publikationsliste 1937, Typoskript, 1 Blatt; Über "Autorität und Familie" und die "Zeitschrift für Sozialforschung". 1937, Typoskript, französisch, mit eigenhändigen Korrekturen, 4 Blatt; Max Horkheimer: Über das Institut für Sozialforschung 1938: 1. Typoskript, englische Fassung, mit handschriftlichen Korrekturen, 38 Blatt; 2. Typoskript, deutsche Fassung mit eigenhändigen Korrekturen, 37 Blatt (G.S. 12, S. 132-164); 3. Julian Gumperz: 1 Brief an Herbert Marcuse, New York, 30.8.1938; 4. Teilstück aus früherer Fassung (?), Typoskript, 1 Blatt, 5. Entwurf zu 2., a) Typoskript, 1 Blatt, b) Typoskript mit eigenhändigen Korrekturen und Ergänzungen, 2 Blatt;

Grain size analysis of sediment coring site CRP-2 from the Ross Sea, Antarctica

The purpose of this note is to present results of grain size analyses from 118 samples of the CRP-2/2A core using sieve and Sedigraph techniques. The samples were selected to represent the range of facies encountered, and tend to become more widely spaced with depth. Fifteen came from the upper 27 m of Quaternary and Pliocene sediments, 62 from the early Miocene-late Oligocene strata (27 to 307 mbsf), and 41 from the early Oligocene strata beneath (307 to 624 mbsf). The results are intended to provide reference data for lithological descriptions in the core logs (Cape Roberts Science Team, 1999), and to help with facies interpretation. The analytical technique used for determining size frequency of the sand fraction in our samples (sieving) is simple, physical and widely practised for over a century. Thus it provides a useful reference point for analyses produced by other faster and more sophisticated techniques, such as the Malvern laser particle size analysis system (Woolfe et al., 2000), and estimates derived from measurements taken with down-hole logging tools (Bücker, pers. com., 1999).

Peretó Rivas, Rubén (ed.). Tolerancia. Teoría y práctica en la Edad Media, Brepols Publishers, Porto- Turhnout, 2012, 295 pp. ISBN: 978-2-503-54553-0.

La obra que aquí presentamos, editada por el Dr. Rubén Peretó Rivas y publicada por la prestigiosa editorial belga Brepols, es el fruto de una buena parte de los trabajos presentados en el marco de las VII Jornadas Internacionales de Pensamiento Medieval y del Coloquio Anual de la Federación Internacional de Institutos de Estudios Medievales (FIDEM). Ambas reuniones científicas fueron realizadas del 15 al 18 de junio del año pasado en la Facultad de Filosofía y Letras de la Universidad Nacional de Cuyo, en Mendoza. En estos encuentros académicos participaron numerosos especialistas de Latinoamérica, Europa y Estados Unidos. Asimismo, fue la primera vez que el Coloquio Anual de la FIDEM se realiza fuera del continente europeo. El presente ejemplar lleva por nombre Tolerancia. Teoría y práctica en la Edad Media. Se trata de un título que plantea inicialmente una discusión. En efecto, no hay acuerdo entre los estudiosos acerca de sí, efectivamente, podemos hablar de tolerancia en el Medioevo. Este nuevo volumen que llega a la comunidad académica muestra a ojos vista las prolíficas, originales y vigorosas tesis de diversas fuentes medievales en torno a la noción y a la práctica de la tolerancia. Asimismo, a nuestro juicio, el ejemplar de marras deja entrever el rigor y claridad con que cada investigador ha sabido abordar su estudio, y también el esmero y la cuidadosa edición e introducción de su editor, el Dr. Rubén Peretó Rivas. No nos queda más que invitar al lector al encuentro del presente estudio que, según creemos -y sin que el mismo posea una intención explícita -pone en tela de juicio diversos preconceptos históricos que suelen tenerse sobre la Edad Media y evidencia, además, que la teoría y la práctica de la tolerancia se ven enriquecida a través de los aportes de tantos y variados pensadores que atravesaron el período medieval.

Francisco García Bazán, Plotino y la Mística de las tres hipóstasis, Elhilodeariadna, Buenos Aires, 2011, pp. 533. ISBN 978-987-23546-2-6.

Fil: Verstraete, Miguel. Universidad Nacional de Cuyo. Facultad de Filosofía y Letras

Age determination, planktic foraminifera and stable istopes of sediment core MSM05/5_712-2

A sediment core from the West Spitsbergen continental margin was studied to reconstruct climate and paleoceanographic variability during the last ~9 ka in the eastern Fram Strait. Our multiproxy evidence suggests that the establishment of the modern oceanographic configuration in the eastern Fram Strait occurred stepwise, in response to the postglacial sea-level rise and the related onset of modern sea-ice production on the shallow Siberian shelves. The late Early and Mid Holocene interval (9 to 5 ka) was generally characterized by relatively unstable conditions. High abundance of the subpolar planktic foraminifer species Turborotalita quinqueloba implies strong intensity of Atlantic Water (AW) inflow with high productivity and/or high AW temperatures, resulting in a strong heat flux to the Arctic. A series of short-lived cooling events (8.2, 6.9. and 6.1 ka) occurred superimposed on the warm late Early and Mid Holocene conditions. Our proxy data imply that simultaneous to the complete postglacial flooding of Arctic shallow shelves and the initiation of modern sea-ice production, strong advance of polar waters initiated modern oceanographic conditions in the eastern Fram Strait at ~5.2 ka. The Late Holocene was marked by the dominance of the polar planktic foraminifer species Neogloboquadrina pachyderma, a significant expansion of sea ice/icebergs, and strong stratification of the water column. Although planktic foraminiferal assemblages as well as sea surface and subsurface temperatures suggest a return of slightly strengthened advection of subsurface Atlantic Water after 3 ka, a relatively stable cold-water layer prevailed at the sea surface and the study site was probably located within the seasonally fluctuating marginal ice zone during the Neoglacial period.