Synthesis of five and six-membered N-phenylacetamido substituted heterocycles as formyl peptide receptor agonists

Formyl peptide receptors (FPRs) are G-protein-coupled receptors that play an important role in the regulation of inflammatory process and cellular dysfunction. In humans, three different isoforms are expressed (FPR1, FPR2 and FPR3). FPR2 appears to be directly involved in the resolution of inflammation (ROI), an active process carried out by specific pro-resolving mediators that modulate specific receptors. Previously, we identified 2-arylacetamido pyridazin-3(2H)-ones as FPR1- or FPR2-selective agonists, as well as a large number of mixed-agonists for the three isoforms. Here, we report a new series of 2-arylacetamido pyridazinones substituted at position 5 and their development as FPR agonists. We also synthesized a new series of 2-oxothiazolones bearing a 4-bromophenylacetamido fragment, which was fundamental for activity in the pyridazinone series. The compounds of most interest were 4a, a potent, mixed FPR agonist recognized by all three isotypes (FPR1 EC(50) = 19 nM, FPR2 EC(50) = 43 nM, FPR3 EC(50) = 40 nM), and 4b, which had potent activity and a preference for FPR2 (EC(50) = 13 nM). These novel compounds may represent valuable tools for studying FPR activation and signaling

L’invasion mondiale de Drosophila suzukii : être une espèce « cousine » d’un organisme-modèle aide-t-il réellement à établir un contrôle biologique ? Espoirs, désillusions et nouvelles perspectives

L’invasion récente et rapide de Drosophila suzukii en Europe et en Amérique du Nord a suscité de nombreuses études sur le terrain comme en laboratoire. Cette drosophile est en effet à la fois un ravageur important, du fait de son développement dans des fruits à maturité, et une « cousine » de l’espèce modèle Drosophila melanogaster dont la biologie et la génétique sont bien connues. Cet article s’appuie sur les données publiées par différentes équipes et sur des résultats préliminaires pour discuter de l’avancée des recherches et notamment des questions suivantes: en quoi nos connaissances sur D. melanogaster peuvent-elles ou non aider à comprendre et gérer l’invasion de D. suzukii ? Les résultats obtenus en condition de laboratoire avec cette espèce sont-ils représentatifs de sa biologie ? Comment mesurer l’impact écologique d’une espèce invasive si la niche qu’elle vient occuper est peu décrite localement en termes d’espèces présentes et de réseaux trophiques ? Cet article discute aussi des pistes et contraintes en termes de lutte biologique et de biocontrôleThe recent and rapid invasion of Europe and North-America by Drosophila suzukii has generated numerous laboratory and field studies since this fly species is an agricultural pest that causes economical losses by laying eggs and developing in ripening fruits, but also because of its relatedness with the model species Drosophila melanogaster whose biology and genetics are well described. This commentary is based on recent data published by different research groups as well as some of our own preliminary results. It discusses the state of research on D. suzukii and addresses the main following questions: can the wide knowledge on D. melanogaster help us to understand and manage the D. suzukii invasion and how? Are lab results on D. suzukii really informative on its biology? How can the ecological impact of an invasive species be evaluated if the ecological niche is poorly described in terms of biodiversity and trophic network? We also outline constraints for the biological control of this pest species and suggest new possible approaches for its long-term managemen

Final report of EURAMET.M.G-K3 regional comparison of absolute gravimeters

The regional key comparison of absolute gravimeters, EURAMET.M.G-K3 and the simultaneously organized additional comparison, was held in Germany at the Geodetic Observatory Wettzell of the German Federal Agency for Cartography and Geodesy in the spring of 2018.Here we present the list of the participants who actually performed measurements during the comparison, the data submitted by the operators as well as the results of the determination of the gravity as a function of height at the comparison sites. The measurement strategy is briefly discussed and the results of the data harmonization is documented. Finally, the results of the constrained least squares adjustment are presented including the degrees of equivalence of each gravimeter and the key comparison reference values.Main textTo reach the main text of this paper, click on Final Report. Note that this text is that which appears in Appendix B of the BIPM key comparison database kcdb.bipm.org/.The final report has been peer-reviewed and approved for publication by the CCM, according to the provisions of the CIPM Mutual Recognition Arrangement (CIPM MRA).Export citation and abstract BibTeX RIS

Regional comparison of absolute gravimeters SIM.M.G-K1 key comparison

Twelve absolute gravimeters were compared during the regional Key Comparison SIM.M.G-K1 of absolute gravimeters. The four gravimeters were from different NMIs and DIs. The comparison was linked to the CCM.G-K2 through EURAMET.M.G-K2 via the DI gravimeter FG5X-216. Overall, the results and uncertainties indicate an excellent agreement among the gravimeters, with a standard deviation of the gravimeters' DoEs better than 1.3 μGal. In the case of the official solution, all the gravimeters are in equivalence well within the declared uncertainties. == Main text To reach the main text of this paper, click on Final Report [http://www.bipm.org/utils/common/pdf/final_reports/M/G-K1/SIM.M.G-K1.pdf] . Note that this text is that which appears in Appendix B of the BIPM key comparison database kcdb.bipm.org/ [http://kcdb.bipm.org/] . The final report has been peer-reviewed and approved for publication by the CCM, according to the provisions of the CIPM Mutual Recognition Arrangement (CIPM MRA)

Foreign ownership, bank information environments, and the international mobility of corporate governance

This paper investigates how foreign ownership shapes bank information environments. Using a sample of listed banks from 60 countries over 1997–2012, we show that foreign ownership is significantly associated with greater (lower) informativeness (synchronicity) in bank stock prices. We also find that stock returns of foreign-owned banks reflect more information about future earnings. In addition, the positive association between price informativeness and foreign ownership is stronger for foreign-owned banks in countries with stronger governance, stronger banking supervision, and lower monitoring costs. Overall, our evidence suggests that foreign ownership reduces bank opacity by exporting governance, yielding important implications for regulators and governments

Regional comparison of absolute gravimeters, EURAMET.M.G-K2 key comparison

In the framework of the regional EURAMET.M.G-K2 comparison of absolute gravimeters, 17 gravimeters were compared in November 2015. Four gravimeters were from different NMIs and DIs, they were used to link the regional comparison to the CCM.G.K2 by means of linking converter. Combined least-squares adjustments with weighted constraint was used to determine KCRV. Several pilot solutions are presented and compared with the official solution to demonstrate influences of different approaches (e.g. definition of weights and the constraint) on results of the adjustment. In case of the official solution, all the gravimeters are in equivalence with declared uncertainties. == Main text To reach the main text of this paper, click on Final Report [http://www.bipm.org/utils/common/pdf/final_reports/M/G-K2/EURAMET.M.G-K2.pdf] . Note that this text is that which appears in Appendix B of the BIPM key comparison database kcdb.bipm.org/ [http://kcdb.bipm.org/] . The final report has been peer-reviewed and approved for publication by the CCM, according to the provisions of the CIPM Mutual Recognition Arrangement (CIPM MRA)