7 research outputs found
The impact of stereotype threat on endogenous poverty-elimination dynamics in generationally poor individuals
IntroductionThe study examines the impact of stereotype threat on generationally poor individuals and its effect on achievement motivation. It also explores the extent to which self-affirmation has an intervention effect on the negative impact of stereotype threat.Methods and resultsIn Study 1, statements that contained negative stereotypes were used to elicit stereotype threat in generationally poor individuals; the results show that stereotype threat reduced the performance of generationally poor individuals in a mental-rotation task. Study 2 used a questionnaire to measure the endogenous dynamics of generationally poor individuals attempting to escape poverty after experiencing stereotype threat; participants in the stereotype-threat group showed lower-level endogenous poverty-elimination dynamics than those in the control group. In Study 3, a self-affirmation intervention was administered to the stereotype-threat group after the stereotype threat was induced. Participants in the self-affirmation group were shown to have higher-level endogenous poverty-elimination dynamics than those in the control group.DiscussionThese findings confirm the negative effect of stereotype threat on endogenous poverty-elimination dynamics and verify the effectiveness of self-affirmation in mitigating the negative effects of stereotype threat
First-generation structure-activity relationship studies of 2,3,4,9-tetrahydro-1H-carbazol-1-amines as CpxA phosphatase inhibitors
Genetic activation of the bacterial two-component signal transduction system, CpxRA, abolishes the virulence of a number of pathogens in human and murine infection models. Recently, 2,3,4,9-tetrahydro-1H-carbazol-1-amines were shown to activate the CpxRA system by inhibiting the phosphatase activity of CpxA. Herein we report the initial structure-activity relationships of this scaffold by focusing on three approaches 1) A-ring substitution, 2) B-ring deconstruction to provide N-arylated amino acid derivatives, and 3) C-ring elimination to give 2-ethylamino substituted indoles. These studies demonstrate that the A-ring is amenable to functionalization and provides a promising avenue for continued optimization of this chemotype. Further investigations revealed that the C-ring is not necessary for activity, although it likely provides conformational constraint that is beneficial to potency, and that the (R) stereochemistry is required at the primary amine. Simplification of the scaffold through deconstruction of the B-ring led to inactive compounds, highlighting the importance of the indole core. A new lead compound 26 was identified, which manifests a ∼30-fold improvement in CpxA phosphatase inhibition over the initial hit. Comparison of amino and des-amino derivatives in bacterial strains differing in membrane permeability and efflux capabilities demonstrate that the amine is required not only for target engagement but also for permeation and accumulation in Escherichia coli
Palladium-Catalyzed Alkynylation of Morita–Baylis–Hillman Carbonates with (Triisopropylsilyl)acetylene on Water
Direct
alkynylation of Morita–Baylis–Hillman carbonates with
(triisopropylsilyl)acetylene catalyzed by a Pd(OAc)<sub>2</sub>–NHC
complex was developed “on water” to give the corresponding
1,4-enynes. The significant effects of water amount in the solvent
on further transformations of 1,4-enynes were investigated
Tunable Heck–Mizoroki Reaction of Dibromonaphthalene Diimide with Aryl Ethylenes: Design, Synthesis, and Characterization of Coplanar NDI-Based Conjugated Molecules
Rational
design of coplanar NDI-based conjugated molecules was
achieved by covalently connecting naphthalene diimide (NDI) units
with aryl (Ar) groups through vinylene (V) linkers via Heck–Mizoroki
reaction. Two series of products, diolefination products (Ar<i>V</i>NDI<i>V</i>Ar) and hydroxylated and mono-olefination
products (HONDI<i>V</i>Ar), can be obtained, respectively,
in moderate to excellent yields (45–90%) under controlled conditions,
in which catalyst and base play the key roles. Density functional
theory calculation discloses the outstanding planarity of the two
types of products. Large bathochromic shifts are observed in both
the absorbance and photoluminescence spectra of the HONDI<i>V</i>Ar (144 and 229 nm) and Ar<i>V</i>NDI<i>V</i>Ar (180 and 242 nm) π-systems. Bathochromic shifts can be adjusted
within the broad wavelength range by introducing 4′-substituents,
either electron-withdrawing group (NO<sub>2</sub>) or electron-donating
group (NMe<sub>2</sub>), in the phenyl group of aryl ethylenes. Ar<i>V</i>NDI<i>V</i>Ars show bigger bathochromic shifts
than HONDI<i>V</i>Ars
Consequences of Depsipeptide Substitution on the ClpP Activation Activity of Antibacterial Acyldepsipeptides
The acyldepsipeptide
(ADEP) antibiotics operate through a clinically
unexploited mechanism of action and thus have attracted attention
from several antibacterial development groups. The ADEP scaffold is
synthetically tractable, and deep-seated modifications have produced
extremely potent antibacterial leads against Gram-positive pathogens.
Although newly identified ADEP analogs demonstrate remarkable antibacterial
activity against bacterial isolates and in mouse models of bacterial
infections, stability issues pertaining to the depsipeptide core remain.
To date, no study has been reported on the natural ADEP scaffold that
evaluates the sole importance of the macrocyclic linkage on target
engagement, molecular conformation, and bioactivity. To address this
gap in ADEP structure–activity relationships, we synthesized
three ADEP analogs that only differ in the linkage motif (i.e., ester,
amide, and <i>N</i>-methyl amide) and provide a side-by-side
comparison of conformational behavior and biological activity. We
demonstrate that while replacement of the naturally occurring ester
linkage with a secondary amide maintains <i>in vitro</i> biochemical activity, this simple substitution results in a significant
drop in whole-cell activity. This study provides direct evidence that
ester to amide linkage substitution is unlikely to provide a reasonable
solution for ADEP instability
Pan-proteomics: Technologies, applications, and challenges
Pan-genomics: Applications, Challenges, and Future Prospects covers current approaches, challenges and future prospects of pan-genomics. The book discusses bioinformatics tools and their applications and focuses on bacterial comparative genomics in order to leverage the development of precise drugs and treatments for specific organisms. The book is divided into three sections: the first, an "overview of pan-genomics and common approaches, brings the main concepts and current approaches on pan-genomics research; the second, case studies in pan-genomics, thoroughly discusses twelve case, and the last, current approaches and future prospects in pan-multiomics, encompasses the developments on omics studies to be applied on bacteria related studies. This book is a valuable source for bioinformaticians, genomics researchers and several members of biomedical field interested in understanding further bacterial organisms and their relationship to human health.Fil: Marques Da Silva, Wanderson. Instituto Nacional de Tecnología Agropecuaria. Centro de Investigación En Ciencias Veterinarias y Agronómicas. Instituto de Agrobiotecnología y Biología Molecular. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Parque Centenario. Instituto de Agrobiotecnología y Biología Molecular; ArgentinaFil: Seyffert, Nubia. Universidade Federal da Bahia; Brasi