Search results for "ECL"

Discovery of 5-benzyl-3-phenyl-4,5-dihydroisoxazoles and 5-benzyl-3-phenyl-1,4,2-dioxazoles as potent firefly luciferase inhibitors.

2013

Luciferase reporter assays are commonly used in high-throughput screening methods. Here, we report new firefly luciferase (FLuc) inhibitors based on 5-benzyl-3-phenyl-4,5-dihydroisoxazoles and 5-benzyl-3-phenyl-1,4,2-dioxazoles, which showed up as "false positives" in a luciferase reporter gene-based assay for nuclear receptor antagonists. The inhibition was shown to be noncompetitive for both natural enzyme substrates (d-luciferin and ATP) and selective to FLuc and proven to arise from a direct interaction between the enzyme and the inhibitor. Of the 63 evaluated compounds, 28 showed significantly better inhibition potency than the well-known inhibitor resveratrol (IC(50) = 59 nM), with fi…

Solution versus Fluorous versus Solid-Phase Synthesis of 2,5-Disubstituted 1,3-Azoles. Preliminary Antibacterial Activity Studies

2009

A small library of compounds with an oxa(thia)zole scaffold and structural diversity in both positions 2 and 5 has been synthesized. Double acylation of a protected glycine affords intermediate α-amido-β-ketoesters, which in turn can be dehydrated to afford 1,3-oxazoles or reacted with Lawesson’s reagent to furnish 1,3-thiazoles. This procedure was designed with its adaptation to fluorous techniques in mind. Thus, when a protected glycine with a fluorous tag in the ester moiety is used as a starting material, the synthesis can be easily completed without column chromatography purification of intermediate compounds with good to excellent yields, thus affording a suitable entry to the prepara…

Cold recycling of reclaimed asphalt pavements

2018

Pavement engineers have in front of them multiple challenges linked to addressing issues related to social development and society’s expanding needs. One of the most substantial of these issues is perhaps how to effectively rehabilitate and/ or maintain the existing road network while preserving and sustaining limited natural resources. The re-usage of existing pavement materials to reconstruct/ rehabilitate our future pavements is the solution that is now more and more selected by the different road administrations around the world. However, upon closer inspection, one can find many areas and details, not negligible issues, that are simply extensions of HMA technology (i.e. mix design proc…

Women’s empowerment and child mortality: the case of Bangladesh

2018

A study of the B and Be star population in the field of the LMC open cluster NGC 2004 with VLT-FLAMES

2005

Observations of hot stars belonging to the young cluster LMC-NGC2004 and its surrounding region have been obtained with the VLT-GIRAFFE facilities in MEDUSA mode. 25 Be stars were discovered; the proportion of Be stars compared to B-type stars is found to be of the same order in the LMC and in the Galaxy fields. 23 hot stars were discovered as spectroscopic binaries (SB1 and SB2), 5 of these are found to be eclipsing systems from the MACHO database, with periods of a few days. About 75% of the spectra in our sample are polluted by hydrogen (Halpha and Hgamma), [SII] and [NII] nebular lines. These lines are typical of HII regions. They could be associated with patchy nebulosities with a bi-m…

Crida publica del motu-propri y constitucio de sa Santedat en fauor dels naturals del Regne de Valencia pera que los estrangers no puguen obtenir los…

1588

Escut pontifici en la port. - Caplletra Sign.: A8 Reclams

Alegacion juridica por el Licenciado Francisco de Castro, Presbitero, en la causa beneficial que sigue contra Mariana Inglès, y Vicente Marcilla, Cl…

1745

Caplletra ornada al començament del text Grav. xil. enmarcat a la port. de "S. Antonio de Padua" Sign.: [A]2, B-D2 Port. orlada Text amb postil·les marginals Reclams

Addiccion al memorial que se escriviò por el rector, clero y benef.dos. de la iglesia parroquial de San Bartholomè en esta ciudad en el pleito que …

1744

Caplletra ornada Text a 1 col. - Postil·les. - Reclams Sign.: A-C2

Allegacion en derecho, y hecho. Por el Dotor Luis Miguel, y Blasco clerigo, y el Dotor Bruno Ganga Presbytero, en la causa Beneficial. Contra Don Mig…

1699

Sig.: []2, A-M2 Port. amb orla tip. i grav. xil. - Errates tip. en pag.

Sentència. 1700, 03, 01

1700

Sig.: A4 Port. amb orla tip. i grav. xil.