| 1. |
- Curran, S.J., et al.
(författare)
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On the absence of molecular absorption in high-redshift millimetre-band searches
- 2011
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Ingår i: Monthly Notices of the Royal Astronomical Society. - : Oxford University Press (OUP). - 0035-8711 .- 1365-2966. ; 416:3, s. 2143-2153
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Tidskriftsartikel (refereegranskat)abstract
- We have undertaken a search for millimetre-waveband absorption (through the CO and HCO(+) rotational transitions) in the host galaxies of reddened radio sources (z = 0.405-1.802). Despite the colour selection (optical-near-infrared colours of V - K greater than or similar to 5 in all but one source), no absorption was found in any of the eight quasars for which the background continuum flux was detected. On the basis of the previous (mostly intervening) H(2) and OH detections, the limits reached here and in some previous surveys should be deep enough to detect molecular absorption according to their V - K colours. However, our survey makes the assumption that the reddening is associated with dust close to the emission redshift of the quasar and that the narrow millimetre component of this emission is intercepted by the compact molecular cores. By using the known millimetre absorbers to define the colour depth and comparing this with the ultraviolet luminosities of the sources, we find that, even if these assumptions are valid, only 12 of the 40 objects (mainly from this work) are potentially detectable. This is assuming an excitation temperature of T(x) = 10 K at z = 0, with the number decreasing with increasing temperatures (to zero detectable at T(x) greater than or similar to 100 K).
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| 2. |
- Lazorova, Lucia, et al.
(författare)
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Structural Features Determining the Intestinal Epithelial Permeability and Efflux of Novel HIV-1 Protease Inhibitors
- 2011
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Ingår i: Journal of Pharmaceutical Sciences. - : Elsevier BV. - 0022-3549 .- 1520-6017. ; 100:9, s. 3763-3772
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Tidskriftsartikel (refereegranskat)abstract
- The primary aim of this study was to identify structural features that alter the intestinal epithelial permeability and efflux in a series of novel HIV-1 protease inhibitors (PIs). Eleven PIs were selected containing a tertiary alcohol in a transition-state mimicking scaffold, in which two substituents (R1 and R2) were varied systematically. Indinavir was selected as a reference compound. The apical-to-basolateral permeability was investigated in 2/4/A1 and Caco-2 monolayers. In addition, the basolateral-to-apical permeability was investigated in the Caco-2 monolayers and the efflux ratios were calculated. The absence of active drug transport processes in 2/4/A1 cells allowed identification and modeling of structural elements affecting the passive permeability. For instance, small aromatic R1 substituents and a small (bromo-) R2 substituent were associated with a high passive permeability. Efflux studies in Caco-2 cells indicated that amide-substituted neutral hydrophobic amino acids, such as valine and leucine, in the R1 position, reduced the apical-to-basolateral transport and enhanced the efflux. We conclude that our investigation revealed structural features that alter the intestinal epithelial permeability and efflux in the series of PIs and hope that these results can contribute to the synthesis of PIs with improved permeability and limited efflux properties.
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