86,533 research outputs found

    1H- and 13C-NMR spectra of thiocolchicine and derivatives: A complete analysis

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    Complete and unambiguous assignments of the 1H- and 13C-nmr spectra of thiocolchicine [1], 3-demethylthiocolchicine [2], and the thiocolchicosides [3] and [4] were made through extensive nmr studies, inclusive of homonuclear COSY and COSYLR, BIRDREV, APT, HETCOR, nOe difference, INEPT, and JMODXH experiments

    Glycosides. Part 1. New synthesis of 1.2-trans O-aryl glycosides, via tributyltin phenoxides

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    A new method of glycosidation of phenols has been studied. The reaction of tributyltin phenoxides 2 with 1,2,3,4,6-penta-O-acetyl-D-hexopyranosides 3. 7 and 9, in the presence of tin tetrachloride is described. Glycosides 4, 8 and 10 have been isolated in good yields with high 1,2-trans selectivity. The tributyltin phenoxides 2 have been isolated in quantitative yields, starting from phenols 1 and Bu3SnOMe. This simple method starts from the stable peracetylated sugar, an intermediate of easy access

    FINKELSTEIN REACTION WITH AQUEOUS HYDROGEN HALIDES EFFICIENTLY CATALYZED BY LIPOPHILIC QUARTERNARY ONIUM SALTS

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    The rate of halogen metathesis between halogenoalkanes RX 1-4 (X = F, Cl, Br, I) and aqueous concentrated hydrogen halides HY (Y = Cl, Br, I) is strongly accelerated under phase-transfer catalysis conditions, without solvent. The amount and nature of the nucleophilic species in the organic phase were determined

    Isothiazoles. Part IV. Cycloaddition reactions of diaryl-oxazolones and munchnones to 3-diethylamino-4-(4-methoxyphenyl)-isothiazole 1,1-dioxide: A new synthesis of triarylpyrroles

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    3-Diethylamino-4-(4-methoxyphenyl)-isothiazole 1,1-dioxide (3) readily reacts with oxazolones 2 and munchnones 7 affording with satisfactory yield 3-diethylamino-4,6-diaryl-3a,4-dihydro-3a-(4-methoxyphenyl)-6aH-pyrrol o[3,4-d]isothiazole 1,1-dioxides 4 and 3-diethylamino-4,6-diaryl-5-alkyl-3a-(4-methoxyphenyl)-pyrrolo[3,4-d]i sothiazole 1,1-dioxides 8, respectively. The behaviour of the cycloadducts towards elevated temperatures and/or basic conditions was investigated. Under these conditions the primary products lost SO2 and diethylcyanamide affording 1-alkyl-2,3,5-triarylpyrroles 9 and 1H-2,3,5-triarylpyrroles 10. These latter were found to be better obtained through thermal decompression of N-protected cycloadducts 8 and subsequent deprotecting the final pyrroles

    Farmers’ participation in territorial planning: a methodological approach for the case study of Huerta de Valencia

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    Participation in planning has become progressively important in territory management. As regards Territorial Planning, farmers are among the main stakeholders. In fact multifunctionality of agriculture admits a new role to primary sector. In particular the management of open areas is particularly strategic in peri-urban areas, where competition for resources is highest than in other areas, especially for the land. In this context, the involvement of farmers as privileged stakeholders to land management is even more important. This paper proposes a methodological approach for the evaluation of peri-urban land use plans by farmers, by means of direct surveys on a sample of Spanish farmers. In particular, it has been considered the "Territorial Action Plan of Valencia’s Huerta” (TAPVH)

    α-Pyrones. Part V. Structure effects on the intramolecular cyclization of functionalized 6-pyronylacetamides: synthesis of new 2,5,7-trioxo-pyrano[3,2-c]pyridines

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    Reaction of arylisocyanates 2 with methyl 2-oxo-2H-pyran-6-acetate 1 and with ylide 4 gave two classes of pyronylacetamides 3 and 5, respectively. Phosphoranes 5 were reduced to the corresponding acetamides 6 with zinc and acetic acid. Compounds 6 were alkylated under solid-liquid PTC conditions using anhydrous potassium carbonate as a base to give the Cα-alkyl derivatives 7 in good yields. Intramolecular cyclization with different bases and solvents of acetamides 3,5-7 to give the new 2,5,7-trioxo-pyrano[3,2-c]pyridines has been studied

    Susceptibility to entomopathogens and modulation of basal immunity in two insect models at different temperatures.

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    Abstract In this work, we analysed the efficacy of different commercial bio-insecticides (Steinernema feltiae, Steinernema carpocapsae, Heterorhabditis bacteriophora and Bacillus thuringiensis) by valuating the mortality induced on two insect models, Galleria mellonella (Lepidoptera) and Sarcophaga africa (Diptera) after exposure to different temperatures (10, 20 and 30 °C). Moreover, we investigated the effects of temperature on the basal humoral immunity of the two target insects; particularly, phenoloxidase (PO) and lysozyme activity. Our results show that G. mellonella is susceptible to all bio-insecticides at all the examined temperatures, except when infected at 10 °C with S. carpocapsae and at 30 °C with S. feltiae and B. thuringiensis. S. africa is more susceptible at 30 °C to all bioinsecticides; whereas, when infected at 10 and 20 °C, H. bacteriophora is the most efficient. Temperature modulates PO activity of both G. mellonella and S. africa, otherwise variations in lysozyme activity is observed only in G. mellonella. Except for a possible correlation between the increased lysozyme activity and the delayed Bt efficacy recorded on G. mellonella at 30 °C, a different resistance to bio-insecticides at different temperatures does not seem to be associated to variations of the host basal immunity, probably due to immunoevasive and immunodepressive strategies of these entomopathogens

    Variations on the Author

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    “Variations on the Author” discusses two of Eduardo Coutinho’s recent films (Um Dia na Vida, from 2010, and Últimas Conversas, posthumously released in 2015) and their contribution to the general question of documentary authorship. The director’s filmography is characterized by a consistent yet self-effacing form of authorial self-inscription: Coutinho often features as an interviewer that rather than express opinions propels discourses; an interviewer that is good at listening. This mode of self-inscription characterizes him as an author who is not expressive but who is nonetheless markedly present on the screen. In Um Dia na Vida, however, Coutinho is completely absent form the image, while Últimas Conversas, on the contrary, includes a confessional prologue that moves the director from the margins to the center of his films. This article examines the ways in which these works stand out in the filmography of a director who offers new insights into the notion of cinematic authorship

    Histone acetylation deficits in lymphoblastoid cell lines from patients with Rubinstein-Taybi syndrome.

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    ABSTRACT Background RubinsteineTaybi syndrome (RSTS) is a congenital neurodevelopmental disorder defined by postnatal growth deficiency, characteristic skeletal abnormalities and mental retardation and caused by mutations in the genes encoding for the transcriptional co-activators with intrinsic lysine acetyltransferase (KAT) activity CBP and p300. Previous studies have shown that neuronal histone acetylation is reduced in mouse models of RSTS. Methods The authors identified different mutations at the CREBBP locus and generated lymphoblastoid cell lines derived from nine patients with RSTS carrying distinct CREBBP mutations that illustrate different grades of the clinical severity in the spectrum of the syndrome. They next assessed whether histone acetylation levels were altered in these cell lines. Results The comparison of CREBBP-mutated RSTS cell lines with cell lines derived from patients with an unrelated mental retardation syndrome or healthy controls revealed significant deficits in histone acetylation, affecting primarily histone H2B and histone H2A. The most severe defects were observed in the lines carrying the whole deletion of the CREBBP gene and the truncating mutation, both leading to a haploinsufficiency state. Interestingly, this deficit was rescued by treatment with an inhibitor of histone deacetylases (HDACi). Conclusions The authors’ results extend to humans the seminal observations in RSTS mouse models and point to histone acetylation defects, mainly involving H2B and H2A, as relevant molecular markers of the disease

    [Newspaper Clipping: Author Claims Evidence of Second JFK Assassin #1]

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    Newspaper article titled "Author Claims Evidence of Second JFK Assassin." The article states that author Richard J. Whalen concluded "that there is circumstantial evidence to support the theory of a second assassin in the shooting of President John F. Kennedy.
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