High yielding synthesis of N-ethyl dehydroamino acids

Recently we reported the use of a sequence of alkylation and dehydration methodologies to obtain N-ethyl-α, β-dehydroamino acid derivatives. The application of this N-alkylation procedure to several methyl esters of β, β-dibromo and β--bromo, β-substituted dehydroamino acids protected with standard amine protecting groups was subsequently reported. The corresponding N-ethyl, β-bromo dehydroamino acid derivatives were obtained in fair to high yields and some were used as substrates in Suzuki cross coupling reactions to give N-ethyl, β, β-disubstituted dehydroalanine derivatives. Herein, we further explore N-ethylation of β-halo dehydroamino acid derivatives using triethyloxonium tetrafluoroborate as alkylating agent but substituting N,N-diisopropylethylamine for potassium tert-butoxide as auxiliary base. In these conditions, for all β-halo dehydroamino acid derivatives, reactions were complete and the N-ethylated derivative could be isolated in high yield. This method was also applied for N-ethylation of non-halogenated dehydroamino acids. Again, with all compounds the reactions were complete and the N-ethyl dehydroamino acid derivatives could be isolated in high yields. Some of these N-ethyl dehydroamino acid methyl ester derivatives were converted in high yields to their corresponding acids and coupled to an amino acid methyl ester to give N-ethyl dehydrodipeptide derivatives in good yields. Thus, this method constitutes a general procedure for high yielding synthesis of N-ethylated dehydroamino acids, which can be further applied in peptide synthesis.Foundation for Science and Technology (FCT)-Portugal and Fundo Europeu de Desenvolvimento Regional (FEDER) for financial support to Chemistry Centre of University of Minho. The NMR spectrometer Bruker Avance II+ 400 is part of the National NMR Network and was purchased in the framework of the National Program for Scientific Re-equipment; contract REDE/1517/RMN/2005, with funds from POCI 2010, FEDER and FCT

A novel single-phase shunt active power filter based on a current-source converter with reduced Dc-Link

Nowadays, the majority of electronic equipment behave as nonlinear loads, introducing Power Quality (PQ) problems into the Power Grid (PG), namely, current harmonics and low power factor. These PQ problems contribute to the reduction of the efficiency of the transmission and distribution PG, as well as induce the malfunctioning of sensitive loads connected to the PG. Therefore, the development of equipment able to mitigate these PQ problems is extremely important. In this context, this paper presents a novel single-phase Shunt Active Power Filter (SAPF) based on a current-source converter, where the key differencing factor, when compared with the conventional approach, is the reduced dc-link. As the proposed topology requires a reduced dc-link, it represents a relevant advantage, since a typical current-source converter needs an inductor with a high inductance in dc-link, which results in higher losses, costs and component sizing. The proposed SAPF with reduced dc-link is introduced in detail along the paper and a comprehensive comparison with the conventional SAPF is established based on computer simulations. Besides, an experimental validation was carried-out with a developed laboratory prototype, validating the main advantages of the proposed SAPF with reduced dc-link.This work has been supported by FCT – Fundação para a Ciência e Tecnologia with-in the Project Scope: UID/CEC/00319/2019. This work has been supported by the FCT Project QUALITY4POWER PTDC/EEI-EEE/28813/2017, and by the FCT Project newERA4GRIDs PTDC/EEI-EEE/30283/2017

Incidence rates and trends of lip, oral and oro-pharyngeal cancers in Portugal

Objectives: To analyse the trends and patterns of lip, oral and oro‐pharyngeal cancer incidence in Portugal between 1998 and 2007. Patients and Methods: Data on lip, oral and oro‐pharyngeal cancers was collected from the databases maintained at the three main Regional Cancer Registries of Portugal (1998–2007). The data were analysed by gender, age and by site. Incidence rates were age standardized by the direct method, and joinpoint regression was used to estimate trends in incidence. Results: During this 10‐year period, a total of 9623 cases of lip, oral and oropharynx cancers were reported, 7565 (78.6%) in males and 2058 (21.4%) in females. There was an increase in the age‐standardized incidence of oral cancers by 1.96% per year for both sexes grouped together and an increase of 4.34% per year for the female group. Oro‐pharyngeal cancer showed an increase incidence trend of 3.49% per year for both sexes grouped together and an increase of 3.49% per year for male group among the sites analysed. Lip cancer showed a decrease in its incidence rate. Conclusion: In view of rising trends, it is necessary to implement policies on oral cancer control by initiating campaigns on oral cancer awareness and screening and to harness political measures on tobacco and alcohol control for the Portuguese population

Pharmacokinetic and pharmacodynamic modelling after subcutaneous, intravenous and buccal administration of a high-concentration formulation of buprenorphine in conscious cats

The aim of this study was to describe the joint pharmacokinetic-pharmacodynamic model and evaluate thermal antinociception of a high-concentration formulation of buprenorphine (Simbadol™) in cats

Tendances actuelles de l'expérimentation en matière de sélection bovine

International audienc

Mineralocorticoid receptor antagonists eplerenone and spironolactone modify adrenal cortex morphology and physiology

Mineralocorticoid receptor antagonists (MRAs) are a class of anti-hypertensive drugs that act by blocking aldosterone action. The aim of this study was to evaluate whether the MRAs spironolactone and eplerenone influence adrenal cortical physiology and morphology. Spontaneous hypertensive rats (SHR, n = 18) and normotensive rats (WKY, n = 18) were randomly exposed to a daily dose of spironolactone (n = 6), eplerenone (n = 6), or no drug (n = 6) over 28 days. After that, aldosterone, corticosterone, and 11-deoxycorticosterone plasma concentrations were quantified. Adrenal glands were subjected to morphological analysis to assess lipid droplets content, capsular width, cell proliferation, and steroidogenic proteins expression. The adrenal cortex in untreated SHR showed higher lipid droplet content as than in WKY. In SHR, MRA treatment was associated with higher circulating aldosterone levels and Ki-67 expression in aldosterone-secreting cells. In WKY, the only difference observed after MRA spironolactone treatment was a narrower capsule. There was no difference in abundance of steroidogenic enzyme between groups. In conclusion, MRAs modify adrenal gland function and morphology in SHR. The effects observed within the adrenal glomerulosa with aldosterone-secreting cell proliferation and higher circulating aldosterone levels suggests that MRA treatment provokes activation of the renin angiotensin system. The prognostic value of hyperaldosteronism secondary to MRAs blockade requires further investigation.Funding: This research was funded by the Associação dos Amigos do Serviço de Endocrinologia do Hospital de São João (2020–2021). Unit for Multidisciplinary Research in Biomedicine (UMIB) is funded by the Foundation for Science and Technology (FCT)-Portugal (UIDB/00215/2020 and UIDP/00215/2020—approval date: 2019)

The Kinematic Algebra From the Self-Dual Sector

We identify a diffeomorphism Lie algebra in the self-dual sector of Yang-Mills theory, and show that it determines the kinematic numerators of tree-level MHV amplitudes in the full theory. These amplitudes can be computed off-shell from Feynman diagrams with only cubic vertices, which are dressed with the structure constants of both the Yang-Mills colour algebra and the diffeomorphism algebra. Therefore, the latter algebra is the dual of the colour algebra, in the sense suggested by the work of Bern, Carrasco and Johansson. We further study perturbative gravity, both in the self-dual and in the MHV sectors, finding that the kinematic numerators of the theory are the BCJ squares of the Yang-Mills numerators.Comment: 29 pages, 5 figures. v2: references added, published versio