Diels-alder cycloaddition in the synthesis of 1-azafagomine, analogs, and derivatives as glycosidase inhibitors

This comprehensive review deals with the synthesis of 1-azafagomine, analogs, and derivatives having the Diels-Alder cycloaddition as the key step. Most of the compounds referred are racemic or have been resolved by lipase transesterification. There are two asymmetric cycloadditions leading to 1-azafagomine or to an analog. In one case both enantiomers of 1-azafagomine were prepared together with a pair of derivatives. The study comprises glycosidase inhibition studies of the target compounds to a set of glycosidic enzymes, and evidenced molecular features that enhance or diminish their activity as glycosidase inhibitors

Topical Application of Imiquimod as a Treatment for Chromoblastomycosis

Peer reviewedPublisher PD

Early magnetic resonance imaging control after temporomandibular joint arthrocentesis

Temporomandibular joint (TMJ) lysis and lavage arthrocentesis with viscosupplementation are an effective treatment for acute disc displacement (DD) without reduction. Clinical success seems to be related to multiple factors despite the lack of understanding of its mechanisms. The authors present a case report of 17-year-old women with acute open mouth limitation (12 mm), right TMJ pain-8/10 visual analog scale, right deviation when opening her mouth. The clinical and magnetic resonance imaging (MRI) diagnosis was acute DD without reduction of right TMJ. Right TMJ arthrocentesis was purposed to the patient with lysis, lavage, and viscosupplementation of the upper joint space. After 5 days, a new MRI was performed to confirm upper joint space distension and disc position. Clinical improvement was obtained 5 days and 1 month after arthrocentesis. Upper joint space increased 6 mm and the disc remained displaced. We report the first early TMJ MRI image postoperative, with measurable upper joint space.info:eu-repo/semantics/publishedVersio

Diastereo-selectivity in diels–alder cycloadditions of erythrose benzylidene-acetal 1,3-Butadienes with maleimides

Maleimides were combined with D-erythrose benzylidene-acetal 1,3-butadienes 1 and 2 to study the facial selectivity of the Diels-Alder cycloadditions. The selectivity was found to be from moderate to good. The reaction diastereotopicity can be reversed with the temperature. Simultaneous coordination of diene 1, having a free hydroxyl group, and maleimide 3 to a chiral bimetallic Lewis acid catalyst (LACASA-DA reaction) occurs with complete diastereo-control to give a single adduct, using an extra chiral inductor either R- or S-BINOL.Thanks are due to FCT for project funding PTDC/QUI/67407/2006 and FCT and FEDER for funding the NMR spectrometer Bruker Avance III 400 as part of the National NMR Network. V. C. M. D. also thanks for PhD grant (SFRH/BD/61290/2009)

Nintendo® WII? For the Elderly, Yes! Contributions to a Better Inclusion and Quality of Life for the Elderly

Os videojogos estão direcionados a um público mais jovem, no entanto, com a realização deste estudo pretendemos demonstrar que os mesmos podem ser potencializados também com os idosos. O principal objetivo foi o de investigar se a Nintendo® Wii, possui caraterísticas que permitam promover e melhorar a inclusão e qualidade vida dos idosos. Em termos metodológicos, optou-se por se um estudo exploratório, porque os constrangimentos de confinamento associados à pandemia não permitiram a participação de um grupo maior, no qual foi aplicado o método de observação participante. A recolha de dados foi realizada no Centro de Atividades de um município do distrito de Castelo Branco, com a participação de três utentes. Após as atividades realizadas verifica-se que os videojogos contribuem para a inclusão e qualidade de vida dos idosos, pelo facto de se sentir um ambiente colaborativo entre os participantes, pelo ambiente descontraído e de entreajuda e pelos sorrisos e gargalhadas que se ouviram. O facto de dominarem um recurso tecnológico também foi enfatizado porque lhes conferiu um sentimento de inclusão num mundo tecnológico ao qual, na maioria dos casos, se sentem à margem. Em suma, a utilização da Nintendo® Wii permitiu verificar que pode promover e contribuir para uma vida mais saudável e inclusiva dos idosos.Video games are aimed at a younger audience, however, with this study we intend to demonstrate that they can also be leveraged with the elderly. The main objective was to investigate whether the Nintendo® Wii has characteristics that allow promoting and improving the inclusion and quality of life of the elderly. In methodological terms, an exploratory study was chosen, because the confinement constraints associated with the pandemic did not allow the participation of a larger group, in which the participant observation method was applied. Data collection was carried out at the Activities Center of a municipality in the district of Castelo Branco, with the participation of three users. After the activities carried out, it appears that video games contribute to the inclusion and quality of life of the elderly, due to the fact that a collaborative environment is felt among the participants, the relaxed and mutual environment and the smiles and laughter that were heard. The fact that they mastered a technological resource was also emphasized because it gave them a feeling of inclusion in a technological world to which, in most cases, they feel on the sidelines. In short, the use of the Nintendo® Wii made it possible to verify that it can promote and contribute to a healthier and more inclusive life for the elderly.info:eu-repo/semantics/publishedVersio

The synthesis of an homochiral aziridine as a useful synton to iminosugars and amino acid compounds

Fundação para a Ciência e a Tecnologia (FCT) - PTDC/QUI/67407/200

Nutritional, rheological, sensory characteristics and environmental impact of a yogurt-like dairy drink for children enriched with lupin flour

Studies have demonstrated that the addition of pulses to foods can make them more nutritious. We hypothesize that lupin flour adds nutritional benefits to yogurts. This study aimed to characterize a lupin-enriched yogurt in nutritional, rheological, and sensorial terms by a trained panel, and assess its environmental impact using the life cycle assessment (LCA) approach. For comparison, natural yogurt and a commercial formula were used as controls. The developed yogurt is “high in protein” (7g/100g), “source of fiber” (1.9g/100g), and “source of omega 3” (53 mg/100g). The lupin yogurt was the stiffest with the highest viscosity than controls according to rheological parameters. There were no significant sensory differences between the lupin-enriched yogurt and the controls, although some undesirable sensory characteristics such as bitterness, granularity, and after-taste were observed. The environmental impact per 100 g serving was similar to natural yogurt and slightly worse regarding commercial yogurt but better when expressed per Nutritional Density Unit (NDU). Using lupin flour to enrich yogurts for children can be an alternative to producing more nutritious products.N/

Targeting of prolamins by RNAi in bread wheat: Effectiveness of seven silencing-fragment combinations for obtaining lines devoid of coeliac disease epitopes from highly immunogenic gliadins

Gluten proteins are responsible for the viscoelastic properties of wheat flour but also for triggering pathologies in susceptible individuals, of which coeliac disease (CD) and noncoeliac gluten sensitivity may affect up to 8% of the population. The only effective treatment for affected persons is a strict gluten-free diet. Here, we report the effectiveness of seven plasmid combinations, encompassing RNAi fragments from a-, c-, x-gliadins, and LMW glutenin subunits, for silencing the expression of different prolamin fractions. Silencing patterns of transgenic lines were analysed by gel electrophoresis, RP-HPLC and mass spectrometry (LC-MS/ MS), whereas gluten immunogenicity was assayed by an anti-gliadin 33-mer monoclonal antibody (moAb). Plasmid combinations 1 and 2 downregulated only c- and a-gliadins, respectively. Four plasmid combinations were highly effective in the silencing of x-gliadins and c-gliadins, and three of these also silenced a-gliadins. HMW glutenins were upregulated in all but one plasmid combination, while LMW glutenins were downregulated in three plasmid combinations. Total protein and starch contents were unaffected regardless of the plasmid combination used. Six plasmid combinations provided strong reduction in the gluten content as measured by moAb and for two combinations, this reduction was higher than 90% in comparison with the wild type. CD epitope analysis in peptides identified in LC-MS/MS showed that lines from three plasmid combinations were totally devoid of CD epitopes from the highly immunogenic a- and x-gliadins. Our findings raise the prospect of breeding wheat species with low levels of harmful gluten, and of achieving the important goal of developing nontoxic wheat cultivars

Genetic variability and natural selection at the ligand domain of the Duffy binding protein in Brazilian Plasmodium vivax populations.

Background. Plasmodium vivax malaria is a major public health challenge in Latin America, Asia and Oceania, with 130-435 million clinical cases per year worldwide. Invasion of host blood cells by P. vivax mainly depends on a type I membrane protein called Duffy binding protein (PvDBP). The erythrocyte-binding motif of PvDBP is a 170 amino-acid stretch located in its cysteine-rich region II (PvDBPII), which is the most variable segment of the protein. Methods. To test whether diversifying natural selection has shaped the nucleotide diversity of PvDBPII in Brazilian populations, this region was sequenced in 122 isolates from six different geographic areas. A Bayesian method was applied to test for the action of natural selection under a population genetic model that incorporates recombination. The analysis was integrated with a structural model of PvDBPII, and T- and B-cell epitopes were localized on the 3-D structure. Results. The results suggest that: (i) recombination plays an important role in determining the haplotype structure of PvDBPII, and (ii) PvDBPII appears to contain neutrally evolving codons as well as codons evolving under natural selection. Diversifying selection preferentially acts on sites identified as epitopes, particularly on amino acid residues 417, 419, and 424, which show strong linkage disequilibrium. Conclusions. This study shows that some polymorphisms of PvDBPII are present near the erythrocyte-binding domain and might serve to elude antibodies that inhibit cell invasion. Therefore, these polymorphisms should be taken into account when designing vaccines aimed at eliciting antibodies to inhibit erythrocyte invasion