Synthesis of 7-methyl-4,6,6a,7,10,10a-hexa-hydroindolo[4,3-fg]quinazoline derivatives

The synthesis of a series of compounds indolo[4,3-fg]quinazoline related to ergoline (indolo[4,3-fg]quinoline) is reported. The key step of the synthetic sequence is the ring cleavage of the ketone IV. The stereochemistry of the chiral centers is established by the chirality of dihydrolysergic acid I.     

Effects of mobile phone exposure on time frequency fine structure of transiently evoked otoacoustic emissions

Mobile phones have become very commonly used worldwide within a short period of time. To date there is only limited knowledge about interaction between electromagnetic fields (EMFs) emitted by mobile phones and the auditory function. Moreover, there is widespread concern that there may be potential for harm. The aim of this study was to assess potential subtle changes in cochlear function by measuring the temporal and spectral fine structure of transiently evoked otoacoustic emissions (TEOAE) in normal hearing subjects after exposure to EMFs emitted by Global System for Mobile Communication (GSM) mobile phones. TEOAEs were recorded in 27 healthy young adults before and after 10 min of real or sham exposure in a double-blind design. TEOAE data were analyzed both globally (broadband analysis) and using the Wavelet Transform (analysis of the time-frequency fine structure). The broadband analysis revealed no significant effect on TEOAEs related to exposure, confirming results of previous studies; in addition, no significant change was detected in the analysis of the elementary wavelet components, suggesting that the temporal and spectral fine structure of TEOAEs is not affected by 10 min exposure to low-intensity EMFs emitted by GSM mobile phones.     

Cyclodextrin complexation improves aqueous solubility of the antiepileptic drug,rufinamide: solution and solid state characterization of compound-cyclodextrin binary systems

Rufinamide (RUF) was characterized in terms of cyclodextrin (CD) complexation in order to improve its aqueous solubility. Binary systems of RUF with three CDs—β-cyclodextrin (β-CD), randomly methylated-β-cyclodextrin (RAMEB) and sulfobutylether-β-cyclodextrin (SBE-β-CD)—were characterized with a wide variety of analytical techniques. Liquid state characterization was carried out by complementary techniques such as nuclear magnetic resonance spectroscopy (NMR), capillary electrophoresis (CE), mass spectrometry (MS) and phase solubility studies. The latter revealed that the stability of the complexes decreased in the order of RAMEB?>?β-CD?>?SBE-β-CD. A_L-type diagrams were obtained in all cases, characteristic of 1:1 stoichiometry, with a maximum of over 15-fold increase in RUF solubility, when complexed with RAMEB. NMR Job plot and MS studies confirmed phase solubility results, regarding the binding stoichiometry. ¹H NMR and 2D ROESY investigations revealed the inclusion of the triazole moiety of RUF, confirmed by molecular modeling. Solid state complexation in 1:1 molar ratio was carried out by kneading method and investigated by differential scanning calorimetry (DSC) and infrared spectroscopy (IR). Comparative dissolution studies indicated an over two-fold improvement in dissolution efficacy of the kneaded products, when compared to the pure drug. Results of the present study might pave the way for a drug formulation with improved bioavailability.     

On the turbulent couette flow of an incompressible fluid with temperature-dependent viscosity

Summary Starting from energy and Navier-Stokes equations with temperature-dependent viscosity, we have obtained the Reynolds equations for the mean values of velocity, temperature and pressure. We have then applied these equations to the Couette flow; on the well-known hypothesis of mixing-length and Prandtl turbulent number, the above mentioned relations have been written in a more amenable form.Some general considerations concerning the reciprocal dependence between temperature and velocity gradients at wall have been deduced.Finally some solutions numerically obtained for several values of Reynolds number are given and discussed in some detail to point out the influence of the temperature-dependent viscosity.

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Sommario Introducendo nelle equazioni dell'energia e di Navier-Stokes le parti medie e fluttuanti della velocità, temperatura, pressione e viscosità, vengono ricavate le cosiddette equazioni di Reynolds, ossia le equazioni che descrivono i campi di velocità e temperatura medi. Dal confronto di quest'ultime, in cui la viscosità è considerata dipendente dalla temperatura, con quelle originarie di Reynolds si deduce la forma che nel caso in esame assumono gli sforzi apparenti.Successivamente le equazioni ottenute vengono applicate al moto a Couette e discusse, dopo aver introdotto in esse le ipotesi della lunghezza di miscelamento e del numero di Prandtl turbolento; da questa analisi vengono tratte alcune conclusioni di carattere generale riguardanti i legami tra il campo dinamico e quello termico. Infine vengono date alcune soluzioni ottenute per via numerica, le quali illustrano l'influenza che sulle distribuzioni di temperatura e velocità viene esercitata dalla dipendenza della viscosità dalla temperatura.

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Synthesis and aggregation behaviour of a new sultaine surfactant

The aggregation properties of a new sultaine surfactant have been studied in buffered aqueous solution at pH 7.4 under controlled condition of osmolarity. Spontaneously formed sultaine vesicles with a mean diameter of about 1 μm can be observed by optical microscopy. The phase behaviour of the surfactant has been investigated by differential scanning calorimetry (DSC) and Nile Red fluorescence. Two critical vesicular concentrations (CVC(1) and CVC(2)) have been fluorimetrically measured, by using pyrene and Nile Red as the fluorescent probes. The two populations of vesicles behave differently as a consequence of their size. The stability of extruded large unilamellar vesicles (LUV) formed slightly above the CVC(1) has been evaluated in the temperature range 25-75°C by following the rate of spontaneous release of entrapped 5(6)-carboxyfluorescein (CF). The stability of the same vesicles at 70°C has also been investigated under osmotic stress obtained by adding NaCl or sucrose to the bulk solution. At a sultaine concentration above the CVC(2) LUV tend to associate and form stable larger closely packed aggregates as suggested by Dynamic Laser Light Scattering and rheological measurements.     

In vitro anti-HMPV activity of meroditerpenoids from marine alga Stypopodium zonale (Dictyotales)

In this paper, we evaluated the antiviral activity against HMPV replication of crude extract of the marine algae Stypopodium zonale and of two meroditerpenoids obtained from it, atomaric acid and epitaondiol, and a methyl ester derivative of atomaric acid. Their selectivity indexes were 20.78, >56.81, 49.26 and 12.82, respectively. Compared to ribavirin, the substances showed a relatively low cytotoxicity on LLC-MK2 cells, with a significant antiviral activity, inhibiting at least 90% of viral replication in vitro, which demonstrates the potential of these marine natural products to combat infections caused by HMPV in vitro.     

On partial tilting modules and right bounded complexes

We construct rather short partial tilting complexes [(T)\dot]{\dot T} such that quite different indecomposable right bounded complexes [(C)\dot]{\dot C} have the property that any morphism from [(T)\dot]{\dot T} to a shift of [(C)\dot]{\dot C} is homotopic to zero. We also show that, for some [(T)\dot]{\dot T} , the strategy to obtain a bounded complex [(C)\dot]{\dot C} as a mutation of [(T)\dot]{\dot T} is not unique.     

Synthesis of polysiloxane xerogels with fluorine-containing groups in the surface layer and their sorption properties

Hydrolysis and polycondensation reactions of tetraethoxysilane (TEOS) with 3,3,3-trifluoropropyl-trimethoxysilane (TFMS) or 1H,1H,2H,2H-perfluorooctyltriethoxysilane (PFES) were used to synthesize xerogels functionalized with fluorine-containing groups. According to transmission electron microscopy, the skeletons of synthesized polysiloxane xerogels have globular structures and consist of agglomerates of particles with fluorinated groups on their surfaces. FTIR spectroscopy showed that primary xerogel particles possess spatial polysiloxane networks, with fluorinated groups along with silanol groups and water in the surface layer. According to thermal analyses, the water content was 3–8 wt.%, and it decreased with increasing length of the fluorinated chain. Thermal destruction of the surface layer starts above 300 °C. The sorbents that were obtained were predominantly mesoporous materials with well-developed porous structures (S_BET = 400–960 m² g⁻¹, V_s = 0.66–0.93 cm³ g⁻¹). The influence of the TEOS/functional silane ratio and the natures of the functional groups on the structural and adsorptive properties were shown. The samples synthesized are organophilic. The affinity for n-hexane increases with increasing length of the fluorine-containing chain (PFES) and the content of fluorinated groups in the surface layer. The hybrid organic–inorganic materials that were obtained can be used for adsorption of hydrocarbons, including oil, from water.     

Uniqueness and symmetry results for solutions of a mean field equation on 𝕊2 via a new bubbling phenomenon

Motivated by the study of gauge field vortices, we consider a mean field equation on the standard sphere 𝕊² involving a Dirac distribution supported at a point P ∈ 𝕊². Consistently with the physical applications, we show that solutions “concentrate” precisely around the point P for some limiting value of a given parameter. We use this fact to obtain symmetry (about the axis ) and uniqueness property for the solution. The presence of the Dirac measure makes such a task particularly delicate to handle from the analytical point of view. In fact, the bubbling phenomenon about the singularity allows the existence of solution sequences with a double‐peak profile near P. The new and more delicate part of this paper is to exclude this possibility by using the method of moving planes together with the Alexandrov‐Bol inequality. © 2011 Wiley Periodicals, Inc.