Reactions of CF3-enones with arenes under superelectrophilic activation: a pathway to trans-1,3-diaryl-1-CF3-indanes, new cannabinoid receptor ligands

4-Aryl-1,1,1-trifluorobut-3-en-2-ones ArCH[double bond, length as m-dash]CHCOCF3 (CF3-enones) react with arenes in excess of Brønsted superacids (TfOH, FSO3H) to give, stereoselectively, trans-1,3-diaryl-1-trifluoromethyl indanes in 35-85% yields. The reaction intermediates, the O-protonated ArCH[double bond, length as m-dash]CHC(OH(+))CF3 and the O,C-diprotonated ArHC(+)CH2C(OH(+))CF3 species, have been studied by means of (1)H, (13)C, (19)F NMR, and DFT calculations. Both types of the cations may participate in the reaction, depending on their electrophilicity and electron-donating properties of the arenes. The formation of CF3-indanes is a result of cascade reaction of protonated CF3-enones to form chemo-, regio- and stereoselectively three new C-C bonds. The obtained trans-1,3-diaryl-1-trifluoromethyl indanes were investigated as potential ligands for cannabinoid receptors CB1 and CB2 types. The most potent compound showed sub-micromolar affinity for both receptor subtypes with a 6-fold selectivity toward the CB2 receptor with no appreciable cytotoxicity toward SHSY5Y cells.

Landschaft mit Dame im Gras [Illustration]

Arthur Segal

Unemployment Insurance Generosity: A Trans-Atlantic Comparison

The goal of this paper is to establish if unemployment insurance policies are more generous in Europe than in the United States, and by how much. We take the examples of France and one particular American state, Ohio, and use the methodology of Pallage, Scruggs and Zimmermann (2008) to find a unique parameter value for each region that fully characterizes the generosity of the system. These two values can then be used in structural models that compare the regions, for example to explain the differences in unemployment rates.

Spirit of Mardis Gras in Hartford

This is a news video produced by Journalism student Jackie Marsiglia. This is to test streaming functionality in the UConn Digital Commons. The RealPlayer movies have been shortened.

Sieg der Reform und des Geistes. Abschiedspredigt über Jesaias 40,8 : "es dorret das Gras; es welket die Blume; doch unseres Gottes Wort besteht in Ewigkeit"

gehalten in der Hauptsynagoge zu Frankfurt a. M. am Trostsabbath 5622 (9. August 1862) von Leopold Stein

Das Pampas-Gras und die verwandten Schilfarten

Vom Professor Dr. Karl Koch

[Ein Gras, dessen Fruchtrispe sich verkehrt in die grundständige Blattrosette eingetaucht hat]

Louise von Panhuys

Julie Aimée Joseph Gras-Dorus, Hüftbild

Signatur des Originals: S 36/G00738

Julie Aimée Joseph Gras-Dorus als Marguerite de Valois, Rollenbild, Hüftbild, in: Giacomo Meyerbeer: Les Huguenots

Signatur des Originals: S 36/G00740

Gras, Ganzfigurbildnis, am Flügel

Signatur des Originals: S 36/G00964

Julie Aimée Joseph Gras-Dorus, Rollenbild, Kniestück

Signatur des Originals: S 36/G04008

Einzelheiten höherer Pflanzen : 23. Panicum turgidum: Blattquerschnitt, Gras - 24. Orthostemon sellowianus: Knospe im Längenschnitt - 25. Orthostemon sellowianus: Fruchtknotenquerschnitt - 26. Conium maculatum: Frucht, Schierling - 27. Conium maculatum: F

AR

{\it cis\/} -acting elements and {\it trans\/} -acting factors that control serum amyloid A gene expression during inflammation

To understand how the serum amyloid A (SAA) genes are regulated, the cis-acting elements and trans-acting factors involved in the regulation of mouse SAA3 and rat SAA1 genes expression during inflammation were analyzed.^ To identify DNA sequences involved in the liver-specific expression of the mouse SAA3 gene, the 5$\sp\prime$ flanking region of this gene was analyzed by transient transfection studies. Results suggest that C/EBP, a liver-enriched transcription factor, plays an important role for the enhanced expression of the mouse SAA3 gene in hepatocytes.^ Transfection studies of the regulation of the expression of rat SAA1 gene indicated that a 322 bp fragment ($-$304 to +18) of the gene contains sufficient information for cytokine-induced expression of the reporter gene in a liver cell-specific manner. Further functional analysis of the 5$\sp\prime$ flanking region of the rat SAA1 gene demonstrated that a 65 bp DNA fragment ($-$138/$-$73) can confer cytokine-inducibility onto a heterologous promoter both in liver and nonliver cells. DNase I footprint and gel retardation assays identified five putative cis-regulatory elements within the 5$\sp\prime$ flanking region of the gene: one inducible element, a NF$\kappa$B binding site and four constitutive elements. Two constitutive elements, footprint regions I and III, were identified as C/EBP binding sites with region III having over a 10-fold higher affinity for C/EBP binding than region I. Functional analysis of the cis-elements indicated that C/EBP(I) and C/EBP(III) confer liver cell-specific activation onto a heterologous promoter, while sequences corresponding to the NF$\kappa$B element and C/EBP(I) impart cytokine responsiveness onto the heterologous promoter. These results suggest that C/EBP(I) possesses two functions: liver-specific activation and cytokine responsiveness. The identification of two cytokine responsive elements (NF$\kappa$B and C/EBP(I)), and two liver-specific elements (C/EBP(I) and C/EBP(III)) implies that multiple cis-acting elements are involved in the regulation of the expression of the rat SAA1 gene. The tissue-specific and cytokine-induced expression of rat SAA1 gene is likely the result of the interactions of these cis-acting elements with their cognate trans-acting factors as well as the interplay between the different cis-acting elements and their binding factors. (Abstract shortened with permission of author.) ^