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The DNA-encoded library (DEL) technology is a new method for discovering hit compounds for target proteins in the pharmaceutical industry. The N-acylsulfonamide functional group has been reported to exhibit various pharmacological activities, and based on this, the demand for a method that allows its introduction into the DEL platform has increased. In this report, a procedure for synthesizing N-acylsulfonamide functional groups applicable to DEL construction was developed in the presence of a copper reagent and water as a nucleophile from simple alkynes or sulfonyl azides, which are widely commercially available. Furthermore, we prove that a new alternative procedure can be used to construct a DNA-encoded library.
Assuntos
Azidas , Cobre , Alcinos , Catálise , DNA , Estrutura MolecularRESUMO
INTRODUCTION: Adolescent dropouts experience various psychosocial difficulties such as social stigma, depressive symptoms, and anxiety after they leave school. This study examined the longitudinal effects of social stigma on depressive symptoms, and the mediating effects of ego-resilience in the relationship between these two variables among South Korean adolescent dropouts aged 14 to 19. METHODS: This study utilized four waves of data from the Out of School Panel Survey (N = 278), assessed annually from 2013 to 2017, which were analyzed using latent growth curve modeling. RESULTS: Both social stigma and depressive symptoms showed positive linear growth over time, while ego-resilience showed negative linear growth. The increase in social stigma was associated with an increase in depressive symptoms and a decrease in ego-resilience. Initial levels of ego-resilience mediated the relationship between the initial levels of social stigma and depressive symptoms. Moreover, changes in ego-resilience mediated the relationship between changes in social stigma and depressive symptoms. CONCLUSIONS: These findings highlight the need for tailored interventions and strategies for preventing depressive symptoms and building ego-resilience to help dropouts overcome social stigma.
Assuntos
Depressão/psicologia , Resiliência Psicológica , Estigma Social , Evasão Escolar/psicologia , Adolescente , Adulto , Depressão/epidemiologia , Feminino , Humanos , Estudos Longitudinais , Masculino , República da Coreia/epidemiologia , Inquéritos e Questionários , Adulto JovemRESUMO
We aimed to evaluate the effectiveness and safety of dronedarone versus sotalol in real-world practice in Asian patients with atrial fibrillation (AF). Using the Korean nationwide claims database from August 2013 to December 2016, we identified patients with AF recently prescribed dronedarone or sotalol and analyzed the hospitalization risk and all-cause death until December 2017. Overall, 3119 and 1575 patients treated with dronedarone and sotalol, respectively, were included. After propensity score weighting, no significant differences were observed between the treatment groups. Dronedarone use was associated with a lower risk of all-cause hospitalization than sotalol use (hazard ratio [HR], 0.79; 95% confidence interval [CI], 0.70-0.88). The dronedarone group demonstrated a significantly lower risk of cardiovascular (CV) hospitalization than the sotalol group (HR 0.62, 95% CI 0.53-0.72); however, no significant difference was observed in non-CV hospitalization. No difference in the risk of all-cause death was observed between groups. The dronedarone group was significantly less likely to receive nonpharmacological treatment for AF than the sotalol group (HR 0.63, 95% CI 0.51-0.77). In a large-scale population of Asian patients with AF, dronedarone was associated with a lower risk of CV hospitalization and a lower need for nonpharmacological treatment for AF than sotalol.
Assuntos
Antiarrítmicos/uso terapêutico , Fibrilação Atrial/tratamento farmacológico , Dronedarona/uso terapêutico , Sotalol/uso terapêutico , Idoso , Povo Asiático , Flutter Atrial/tratamento farmacológico , Causas de Morte , Feminino , Hospitalização , Humanos , Masculino , Pessoa de Meia-Idade , Pacientes , Estudos RetrospectivosRESUMO
Together with high conductivity, high flexibility is an important property required for next generation organic electronic components. Both properties are difficult to achieve together especially when the components are crystalline because of the intrinsic high brittleness of organic molecular crystals. We report an organic radical crystal system that has both high flexibility and high conductivity. The crystal consists of 9,10-bis(phenylethynyl)anthracene radical cation (BPEA.+ ) units, and shows flexibility under pressure with high conductivity in ambient condition exhibiting average conductivity of 2.68â S cm-1 when normal linear shape, as well as 2.43â S cm-1 when bent. The structural analysis reveals that both a short π-π distance (3.290â Å) between BPEA.+ units that are aligned along the crystal length direction, and the presence of PF6 - counter ions induce flexibility and high electrical conductivity.
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BACKGROUND: This study examined the trajectory groups of maternal depressive symptoms of Korean employed women with young children and the association between trajectory group membership and personal, family, social and sociodemographic factors. METHOD: This study used Nagin's semi-parametric, group-based modeling to analyze 2008 (Wave 1) to 2012 data (Wave 5) from the Panel Study on Korean Children, a nationally representative sample of children. RESULTS: Four distinct trajectory groups were identified, namely, a non-depressive symptoms group, increasing subclinical depressive symptoms group, stable moderate depressive symptoms group and severe depressive symptoms group. Results showed that self-esteem, parental stress, child care cooperation of husband, marital satisfaction and social support affected the likelihood of membership in the four depressive symptoms groups. CONCLUSION: Prevention or intervention toward trajectory groups requires integrative approaches that target various factors across multiple contexts.
Assuntos
Transtorno Depressivo/psicologia , Mulheres Trabalhadoras/psicologia , Adulto , Criança , Pré-Escolar , Transtorno Depressivo/epidemiologia , Feminino , Humanos , Modelos Logísticos , Estudos Longitudinais , Mães , Escalas de Graduação Psiquiátrica , República da Coreia/epidemiologia , Fatores de Risco , Índice de Gravidade de Doença , Apoio Social , Adulto JovemRESUMO
A novel transglycosylation reaction from sucrose to L-ascorbic acid by a recombinant sucrose phosphorylase from Bifidobacterium longum was used to produce a stable L-ascorbic acid derivative. The major product was detected by HPLC, and confirmed to be 2-O-alpha-D-glucopyranosyl-L-ascorbic acid by LC-MS/MS analysis.
Assuntos
Ácido Ascórbico/análogos & derivados , Ácido Ascórbico/química , Bifidobacterium/enzimologia , Glucosiltransferases/química , Sacarose/química , Bifidobacterium/genética , Ativação Enzimática , Escherichia coli/efeitos dos fármacos , Escherichia coli/enzimologia , Glucosiltransferases/genética , Proteínas Recombinantes/químicaRESUMO
A DNA fragment, which complemented the growth of E. coli both on M9 medium containing raffinose and on LB medium containing ampicillin, IPTG and 5-bromo-4-chloro-3-indoxyl-alpha-D-galactoside, was isolated from the genomic library of Bifidobacterium longum SJ32, which had been digested with EcoRI. In the cloned DNA fragment, a gene encoding a sucrose phosphorylase (splP) and a partially cloned putative sucrose regulator gene (splR) were identified using the deletion analysis and sequence analysis. A 56 kDa protein was synthesized in E. coli and partially purified by DEAE-ion exchange chromatography. The partially purified enzyme did not react with melibiose, melezitoze and raffinose but did with sucrose. It had transglucosylation activity in addition to hydrolytic activity.