Synthesis and investigation of the cholinesterase inhibitory and antioxidant capacities of some novel N'-(quinolin-4-ylmethylene)propanehydrazides against Alzheimer's disease.

One of the worst long-term health issues of the past few decades is Alzheimer's disease (AD). Unfortunately, there are currently insufficient choices for treating and caring for AD, which makes it a popular subject for drug development research. Studies on the development of drugs for AD have primarily concentrated on the use of multitarget directed ligands. Following this strategy, we designed new ChE inhibitors with additional antioxidant and metal chelator effects. In this research, eight novel N'-(quinolin-4-ylmethylene)propanehydrazide derivatives were synthesized and characterized. We then evaluated the inhibition potency of all the final compounds for cholinesterase enzymes. Among them, 4e (IC50 acetylcholinesterase [AChE] = 0.69 µM and butyrylcholinesterase [BChE]= 26.00 µM) and 4h (IC50's AChE= 7.04 µM and BChE= 16.06 µM) were found to be the most potent AChE and BChE inhibitors, respectively.

Synthesis and evaluation of multitarget new 2-aminothiazole derivatives as potential anti-Alzheimer's agents.

In this study, two diverse series of 2-aminothiazole-based multitarget compounds, one propenamide and the other propanamide derivatives, were designed and synthesized. Subsequently, their anticholinesterease and antioxidant (ORAC) activities were tested. Among them, compound 3e was the most potent acetylcholinesterase (AChE) inhibitor (AChE IC50 = 0.5 µM, butyrylcholinesterase [BChE] IC50 = 14.7 µM) and compound 9e was the most potent BChE inhibitor (AChE IC50 = 3.13 µM, BChE IC50 = 0.9 µM). Kinetic experiments showed that both compounds were mixed-type inhibitors. According to the anticholinesterease activity results, five compounds (3e, 4e, 5e, 9d, and 9e) were selected for further activity studies, all of which are dual cholinesterase inhibitors. Then, selected compounds were investigated in terms of their metal chelation activity. Moreover, their neuroprotective effects against H2 O2 -induced damage in the PC12 cell line were evaluated at 10 µM and the results showed that the neuroprotective effect of 3e was 53% compared with the reference ferulic acid (77%). 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) results of selected compounds revealed that the compounds were noncytotoxic. Additionally, 3e was more effective in reducing lipopolysaccharides-induced interleukin-1ß (IL-1ß), IL-6, tumor necrosis factor-α (TNF-α), and nitric oxide (NO) production in the human monocyte derived from patient with acute monocytic leukemia cell line compared with other selected compounds. Finally, a molecular docking study was also performed.

Meta-analytic relations between personality and cognitive ability.

Cognitive ability and personality are fundamental domains of human psychology. Despite a century of vast research, most ability-personality relations remain unestablished. Using contemporary hierarchical personality and cognitive abilities frameworks, we meta-analyze unexamined links between personality traits and cognitive abilities and offer large-scale evidence of their relations. This research quantitatively summarizes 60,690 relations between 79 personality and 97 cognitive ability constructs in 3,543 meta-analyses based on data from millions of individuals. Sets of novel relations are illuminated by distinguishing hierarchical personality and ability constructs (e.g., factors, aspects, facets). The links between personality traits and cognitive abilities are not limited to openness and its components. Some aspects and facets of neuroticism, extraversion, and conscientiousness are also considerably related to primary as well as specific abilities. Overall, the results provide an encyclopedic quantification of what is currently known about personality-ability relations, identify previously unrecognized trait pairings, and reveal knowledge gaps. The meta-analytic findings are visualized in an interactive webtool. The database of coded studies and relations is offered to the scientific community to further advance research, understanding, and applications.

New thiourea and benzamide derivatives of 2-aminothiazole as multi-target agents against Alzheimer's disease: Design, synthesis, and biological evaluation.

In this study, two series of compounds were designed and synthesized, bearing thiourea and benzamide derivatives at position 2 of 4-subtituted-2-aminothiazole, respectively. Then, the inhibition potency of all final compounds for cholinesterase enzymes were evaluated. Among the thiourea derivatives, 3c (IC50 = 0.33 µM) was identified as the most potent and selective butyrylcholinesterase inhibitor. Additionally, benzamide derivative 10e (AChE IC50 = 1.47 and BChE IC50 = 11.40 µM) was found as a dual cholinesterase inhibitor. The type of inhibition for both compounds was determined by kinetic studies and the results showed that the compounds were mixed type inhibitors. Moreover, all title compounds were investigated in terms of their antioxidant (DPHH, ORAC) and metal chelator activities. In addition, the neuroprotective effects of selected compounds (3c, 3e, 6c, 6e and 10e) against H2O2-induced damage in the PC12 cell line were tested. The experimental findings demonstrated that thiourea-derived 6e (40.4 %) and benzamide-derived 10e (37.8 %) have a neuroprotective effect of about half as ferulic acid at 10 µM. Subsequently, the cytotoxicity of selected compounds was examined by the MTT assay, and the compounds were found not to have cytotoxic effect on the PC12 cell line in 24 h. Additionally, compounds 6e and 10e were also found to be more effective in inhibiting the release of IL-1ß, IL-6, TNF-α and NO compared to other selected compounds in this study.

Using natural language processing and machine learning to replace human content coders.

Content analysis is a common and flexible technique to quantify and make sense of qualitative data in psychological research. However, the practical implementation of content analysis is extremely labor-intensive and subject to human coder errors. Applying natural language processing (NLP) techniques can help address these limitations. We explain and illustrate these techniques to psychological researchers. For this purpose, we first present a study exploring the creation of psychometrically meaningful predictions of human content codes. Using an existing database of human content codes, we build an NLP algorithm to validly predict those codes, at generally acceptable standards. We then conduct a Monte-Carlo simulation to model how four dataset characteristics (i.e., sample size, unlabeled proportion of cases, classification base rate, and human coder reliability) influence content classification performance. The simulation indicated that the influence of sample size and unlabeled proportion on model classification performance tended to be curvilinear. In addition, base rate and human coder reliability had a strong effect on classification performance. Finally, using these results, we offer practical recommendations to psychologists on the necessary dataset characteristics to achieve valid prediction of content codes to guide researchers on the use of NLP models to replace human coders in content analysis research. (PsycInfo Database Record (c) 2022 APA, all rights reserved).

Nonmetric Variants of Anatolian Crania: A Preliminary Study.

Analysis of nonmetric cranial variants has been essential for identifying the human population through osteologic analysis and genetic affinities. This study aimed to examine the nonmetric cranial variants to evaluate differences among sex and side correlations in Anatolian dry skulls. This study was carried out on 50 Anatolian adult dry human skulls (22 males, 28 females) with suitable features (nonfractured and/or with necessary features) out of a total of 97 dry skulls. After sex analysis, each skull was photographed from the norma frontalis, lateralis, inferior, and superior. Eleven nonmetrical cranial variants were investigated. The cranial variants and side incidences were analyzed to determine their sex differences and interside correlations. After the classification, traits were marked as "present" or "absent" on the charts. Some variants in female crania were seen more frequently than in males. Most of the variants such as the supraorbital notch, infraorbital and zygomaticofacial foramen, showed high correlations between the right and left sides. Overall, there were no statistically significant sex or side differences found in the Anatolian crania.

Determining the musculoskeletal problems of academicians who transitioned to distance education during the COVID-19 pandemic.

BACKGROUND: Musculoskeletal disorders are a significant public health issue that negatively affects individuals and society both socially and economically, and increases the cost of care and cure. OBJECTIVE: This study aimed to determine the musculoskeletal problems and risk factors of academicians who transitioned to provide distance education during the COVID-19 pandemic. METHODS: The population of this descriptive cross-sectional study included academicians who worked in two public universities in Turkey. Ethical committee approval and institutional permissions were obtained between 1 and 28 February 2021. Data were collected using a personal information form, the Work Environment Evaluation Questionnaire, and the Musculoskeletal Pain Intensity Assessment Questionnaire. The data were analyzed using the number, percentage, independent group t-test, ANOVA test, and linear regression analysis (forward method). The analysis was interpreted at the 95% confidence level and 0.05 error margin. RESULTS: Of the academicians, 78% were women, 54.6% were married, 80.6% did not regularly exercise, and 73.5% had more workload during the distance education period. Academicians mostly experienced discomfort about their eyes, necks, and waists, and an increase at a significant level was detected in their musculoskeletal system problems during the distance education period. Increasing workload, duration of mobile phone use, active time, having an ergonomic chair, and gender predicted the musculoskeletal system pain intensity by 20%. CONCLUSION: Musculoskeletal system problems are a significant public health issue. Academicians should be informed and consulted for the protection of musculoskeletal system health during the distance education period.

Correlations between transverse carpal ligament thickness measured on ultrasound and severity of carpal tunnel syndrome on electromyography and disease duration.

This study aimed to evaluate the relationship between transverse carpal ligament thickness on ultrasonography and disease severity according to electromyography findings. Fifty-eight patients with carpal tunnel syndrome, aged 30-75 years, with severe (Group 1) or moderate (Group 2) electromyography findings, who underwent surgery for carpal tunnel syndrome complaints in the previous 2 years were enrolled. Patient characteristics and clinical information were recorded. The patients completed the Boston carpal tunnel syndrome questionnaire and visual analog scale (VAS) pain score. Ultrasonography and electromyography records were examined. Electromyography showed that the median nerve area was similar in the two groups. Mean age, transverse carpal ligament thickness and symptom duration were greater in group 1, but not significantly. Mean VAS and Boston scores were significantly higher in group 1. Symptom duration did not affect median nerve area. Nerve area did not correlate significantly with VAS or Boston scores, transverse carpal ligament thickness or mean age, although averages were higher in patients with long symptom duration. Disease severity and symptom duration did not affect the ultrasonography findings. Disease severity in carpal tunnel syndrome could not be determined by measuring transverse carpal ligament thickness and median nerve area on ultrasonography without electromyography.

Agreeableness and Its Consequences: A Quantitative Review of Meta-Analytic Findings.

Agreeableness impacts people and real-world outcomes. In the most comprehensive quantitative review to date, we summarize results from 142 meta-analyses reporting effects for 275 variables, which represent N > 1.9 million participants from k > 3,900 studies. Arranging variables by their content and type, we use an organizational framework of 16 conceptual categories that presents a detailed account of Agreeableness' external relations. Overall, the trait has effects in a desirable direction for 93% of variables (grand mean ρ¯M=.16). We also review lower order trait evidence for 42 variables from 20 meta-analyses. Using these empirical findings, in tandem with existing theory, we synthesize eight general themes that describe Agreeableness' characteristic functioning across variables: self-transcendence, contentment, relational investment, teamworking, work investment, lower results emphasis, social norm orientation, and social integration. We conclude by discussing potential boundary conditions of findings, contributions and limitations of our review, and future research directions.

Design, synthesis and biological evaluation of new benzoxazolone/benzothiazolone derivatives as multi-target agents against Alzheimer's disease.

In this study, four series of compounds with benzoxazolone and benzothiazolone cores were designed, synthesized and evaluated as multifunctional agents against Alzheimer's disease (AD). Additionally, in order to shed light on the effect of the carbonyl groups of benzoxazolone/benzothiazolone, benzoxazole/benzothiazole-containing analogues were also synthesized and evaluated. Inhibition potency of all final compounds towards cholinesterase enzymes and their antioxidant activity were tested. Subsequently, the anti-inflammatory activity, cytotoxicity, apoptosis, and Aß aggregation inhibition tests were also performed for selected compounds. The results indicated that compounds 11c, a pentanamide derivative with benzothiazolone core, and 14b, a keton derivative with benzothiazolone core, were considered as promising multi-functional agents for further investigation against AD. The reversibility, kinetic and molecular docking studies were also performed for the compounds with the highest AChE 14b (eeAChE IC50 = 0.34 µM, huAChE IC50 = 0.46 µM) and BChE 11c (eqBChE IC50 = 2.98 µM, huBChE IC50 = 2.56 µM) inhibitory activities.

WristPrint: Characterizing User Re-identification Risks from Wrist-worn Accelerometry Data.

Public release of wrist-worn motion sensor data is growing. They enable and accelerate research in developing new algorithms to passively track daily activities, resulting in improved health and wellness utilities of smartwatches and activity trackers. But, when combined with sensitive attribute inference attack and linkage attack via re-identification of the same user in multiple datasets, undisclosed sensitive attributes can be revealed to unintended organizations with potentially adverse consequences for unsuspecting data contributing users. To guide both users and data collecting researchers, we characterize the re-identification risks inherent in motion sensor data collected from wrist-worn devices in users' natural environment. For this purpose, we use an open-set formulation, train a deep learning architecture with a new loss function, and apply our model to a new data set consisting of 10 weeks of daily sensor wearing by 353 users. We find that re-identification risk increases with an increase in the activity intensity. On average, such risk is 96% for a user when sharing a full day of sensor data.

Meta-analytic criterion profile analysis.

Intraindividual patterns or configurations are intuitive explanations for phenomena, and popular in both lay and research contexts. Criterion profile analysis (CPA; Davison & Davenport, 2002) is a well-established, regression-based pattern matching procedure that identifies a pattern of predictors that optimally relate to a criterion of interest and quantifies the strength of that association. Existing CPA methods require individual-level data, limiting opportunities for reanalysis of published work, including research synthesis via meta-analysis and associated corrections for psychometric artifacts. In this article, we develop methods for meta-analytic criterion profile analysis (MACPA), including new methods for estimating cross-validity and fungibility of criterion patterns. We also review key methodological considerations for applying MACPA, including homogeneity of studies in meta-analyses, corrections for statistical artifacts, and second-order sampling error. Finally, we present example applications of MACPA to published meta-analyses from organizational, educational, personality, and clinical psychological literatures. R code implementing these methods is provided in the configural package, available at https://cran.r-project.org/package=configural and at https://doi.org/10.17605/osf.io/aqmpc. (PsycInfo Database Record (c) 2020 APA, all rights reserved).

Meta-analytic five-factor model personality intercorrelations: Eeny, meeny, miney, moe, how, which, why, and where to go.

Meta-analysis is frequently combined with multiple regression or path analysis to examine how the Big Five/Five-Factor Model (FFM) personality traits relate to work outcomes. A common approach in such studies is to construct a synthetic correlation matrix by combining new meta-analyses of FFM-criterion correlations with previously published meta-analytic FFM intercorrelations. Many meta-analytic FFM intercorrelation matrices exist in the literature, with 3 matrices being frequently used in industrial-organizational (I-O) psychology and related fields (i.e., Mount, Barrick, Scullen, & Rounds, 2005; Ones, 1993; van der Linden, te Nijenhuis, & Bakker, 2010). However, it is unknown how the choice of FFM matrix influences study conclusions, why we observe such differences in the matrices, and which matrix researchers and practitioners should use for their specific studies. We conducted 3 studies to answer these questions. In Study 1, we demonstrate that researchers' choice of FFM matrix can substantively alter conclusions from meta-analytic regressions or path analyses. In Study 2, we present a new meta-analysis of FFM intercorrelations using measures explicitly constructed around the FFM and based on employee samples. In Study 3, we systematically explore the sources of differences in FFM intercorrelations using second-order meta-analyses of 44 meta-analytic FFM matrices. We find that personality rating source (self vs. other) and inventory-specific substantive and methodological features are the primary moderators of meta-analytic FFM intercorrelations. Based on the findings from these studies, we provide a framework to guide future researchers in choosing a meta-analytic FFM matrix that is most appropriate for their specific studies, research questions, and contexts. (PsycInfo Database Record (c) 2020 APA, all rights reserved).

The prevalence of obesity and related factors among primary and secondary school students.

OBJECTIVES: Obesity was previously seen as a problem in high-income countries. It is also a problem in low and middle-income countries today. The sedentary lifestyle has made this situation more pronounced. Childhood obesity continues in adulthood. Adequate and balanced nutrition and mobile lifestyle have a great role in the prevention and treatment of obesity. The aim of this study was to determine the prevalence of obesity among primary and secondary school students and related factors. METHODS: The sample size was calculated as 1278 (213 × 6) for the gender distribution to be appropriate and for the primary and secondary school students to be included in the district center and villages. Considering 15% of the students' non-response rate, the number of students planned to be reached is 1500. Selection was made after the students were ranked by class, gender and place of residence. Of the 1500 students who were sampled, 1298 (86.53%) were evaluated. RESULTS: There was no difference in body mass index between gender and place of residence. The prevalence of being overweight or obesity among secondary school students (25.2%) was significantly higher than primary school students (20.5%). CONCLUSION: In the childhood age group; sedentary lifestyle, having breakfast and obesity in parents had a significant effect on obesity. It is considered important for children and family members to have proper nutrition and mobile life behaviors.

A century of research on conscientiousness at work.

Evidence from more than 100 y of research indicates that conscientiousness (C) is the most potent noncognitive construct for occupational performance. However, questions remain about the magnitudes of its effect sizes across occupational variables, its defining characteristics and functions in occupational settings, and potential moderators of its performance relation. Drawing on 92 unique meta-analyses reporting effects for 175 distinct variables, which represent n > 1.1 million participants across k > 2,500 studies, we present the most comprehensive, quantitative review and synthesis of the occupational effects of C available in the literature. Results show C has effects in a desirable direction for 98% of variables and a grand mean of [Formula: see text] (SD = 0.13), indicative of a potent, pervasive influence across occupational variables. Using the top 33% of effect sizes [Formula: see text] we synthesize 10 characteristic themes of C's occupational functioning: 1) motivation for goal-directed performance, 2) preference for more predictable environments, 3) interpersonal responsibility for shared goals, 4) commitment, 5) perseverance, 6) self-regulatory restraint to avoid counterproductivity, and 7) proficient performance-especially for 8) conventional goals, 9) requiring persistence. Finally, we examine C's relation to performance across 8 occupations. Results indicate that occupational complexity moderates this relation. That is, 10) high occupational complexity versus low-to-moderate occupational complexity attenuates the performance effect of C. Altogether, results suggest that goal-directed performance is fundamental to C and that motivational engagement, behavioral restraint, and environmental predictability influence its optimal occupational expression. We conclude by discussing applied and policy implications of our findings.

Extraversion advantages at work: A quantitative review and synthesis of the meta-analytic evidence.

How and to what extent does extraversion relate to work relevant variables across the lifespan? In the most extensive quantitative review to date, we summarize results from 97 published meta-analyses reporting relations of extraversion to 165 distinct work relevant variables, as well as relations of extraversion's lower order traits to 58 variables. We first update all effects using a common set of statistical corrections and, when possible, combine independent estimates using second-order meta-analysis (Schmidt & Oh, 2013). We then organize effects within a framework of four career domains-education, job application, on the job, and career/lifespan-and five conceptual categories: motivations, values, and interests; attitudes and well-being; interpersonal; performance; and counterproductivity. Overall, extraversion shows effects in a desirable direction for 90% of variables (grand mean ρ̄ = .14), indicative of a small, persistent advantage at work. Findings also show areas with more substantial effects (ρ̄ ≥ .20), which we synthesize into four extraversion advantages. These motivational, emotional, interpersonal, and performance advantages offer a concise account of extraversion's relations and a new lens for understanding its effects at work. Our review of the lower order trait evidence reveals diverse relations (e.g., the positive emotions facet has consistently advantageous effects, the sociability facet confers few benefits, the sensation-seeking facet is largely disadvantageous), and extends knowledge about the functioning of extraversion and its advantages. We conclude by discussing potential boundary conditions of findings, contributions and limitations of our review, and new research directions for extraversion at work. (PsycINFO Database Record (c) 2019 APA, all rights reserved).

Phenolic and tannin compounds in subtropical shrubs (Bituminaria bituminosa, Chamaecytisus proliferus, and Adenocarpus foliosus) and the effects on in vitro digestibility.

The objective of this study was to contribute to the characterization of nutritional potentials, with special attention to the total phenol and condensed tannins content and the effects on in vitro digestibility of some browsing shrub legumes traditionally used for ruminant feeding. The varieties selected were Bituminaria bituminosa var. bituminosa (BBB), Bituminaria bituminosa var. albormaginata (BBA), Chamaecytisus proliferus var. palmensis (CPP), Chamaecytisus proliferus var. canariae (CPC), and Adenocarpus foliosus (AF). Chemical composition, in vitro digestibility, and net energy for lactation (NE) were analyzed and compared among varieties; the effects of total phenol (TP) and condensed tannins (CT) compounds on digestibility were estimated. Condensed tannins ranged from 1 to 5 g/kg DM of tannins, while total phenols ranged from 9 to 32 g/kg DM of tannins. In vitro organic matter digestibility (OMD) ranged from 0.52 to 0.71, and estimated net energy for lactation (NE) ranged from 4.2 to 5.8 MJ/kg DM, with significant differences among all the varieties. This Chamaecytisus varieties (CPC, CPP) have higher feeding values, following CPC > CPP > AF > BBB > BBA in order. Although there were condensed tannins and total phenols in all the shrubs analyzed, total phenol contents differed significantly between the shrubs. The effect of the content of the total phenols and of the tannins condensed in the OMD of the varieties of shrubs analyzed, shows that the higher amounts of total phenols in some of the varieties of shrubs analyzed, increased the in vitro digestibility (OMD) of the shrubs but high amounts of CT decreased OMD.

Direct and conceptual replications of the taxometric analysis of type a behavior.

We present direct and conceptual replications of the influential taxometric analysis of Type A Behavior (TAB; Strube, 1989), which reported evidence for the latent typology of the construct. Study 1, the direct replication (N = 2,373), duplicated sampling and methodological procedures of the original study, but results showed that the item indicators used in the original study lacked sufficient validity to unambiguously determine latent structure. Using improved factorial subscale indicators to further test the question, multiple taxometric procedures, in combination with parallel analyses of simulated data, failed to replicate the original typological finding. Study 2, the conceptual replication, tested the latent structure of the wider construct of TAB using the sample from the Caerphilly Prospective Study (N = 2,254), which contains responses to the three most widely used self-report measures of TAB: the Jenkins Activity Survey, Bortner scale, and Framingham scale. Factorial subscale indicators were derived from the measures and submitted to multiple taxometric procedures. Results of Study 2 converged with those of Study 1, providing clear evidence of latent dimensional structure. Overall, results suggest there is no evidence for the type in TAB. Findings imply that theoretical models of TAB, assessment practices, and data analytic procedures that assume a typology should be replaced by dimensional models, factorial subscale measures, and corresponding statistical approaches. Specific subscale measures that tap multiple Big Five trait domains, and show evidence of predictive utility, are also recommended. (PsycINFO Database Record (c) 2019 APA, all rights reserved).

Design, Synthesis and Investigation of New Diphenyl Substituted Pyridazinone Derivatives as Both Cholinesterase and Aß-Aggregation Inhibitors.

BACKGROUND: With respect to the increase in the average life expectancy, Alzheimer Disease (AD), the most common form of age-related dementia, has become a major threat to the population over the age of 65 during the past several decades. The majority of AD treatments are focused on cholinergic and amyloid hypotheses. OBJECTIVE: In this study, three series of diphenyl-2-(2-(4-substitutedpiperazin-1-yl)ethyl)pyridazin- 3(2H)-one derivatives were designed, synthesized and investigated for their ability to inhibit both cholinesterase enzymes and amyloid-ß aggregation. METHOD: The inhibitory activities of the synthesized compounds on AChE (from electric eel) and BChE (from equine serum) were determined by the modified Ellman's method. The reported thioflavin T-based fluorometric assay was performed to investigate the effect of the selected compounds on the aggregation of Aß1-42. The cytotoxic effect of the compounds (4g, 11g and 18g) was monitored in 3T3 cell lines to gain insight into therapeutic potential of the compounds by using MTT assay. The crystal structures of the AChE (1EVE) and BChE (1P0I) enzymes were retrieved from the RCSB Protein Data Bank and Molecular Operating Environment (MOE) software was used for molecular docking of the ligands. RESULTS: Among the tested compounds, 5,6-diphenyl derivative 18g was identified as the most potent and selective AChE inhibitor (IC50 = 1.75 µM, Selectivity Index for AChE > 22.857). 4,6- Diphenyl derivative 11g showed the highest and the most selectivity for BChE (IC50= 4.97 µM, SI for AChE < 0.124). Interestingly, 4,5-diphenyl derivative 4g presented dual cholinesterase inhibition (AChE IC50= 5.11 µM; BChE IC50= 14.16 µM, SI for AChE = 2.771). CONCLUSION: Based on biological activity results and low toxicity of the compounds, it can be said that diphenyl substituted pyridazinone core is a valuable scaffold. Especially, dual inhibitory potencies of 4,5-diphenylpyridazin-3(2H)-one core for the cholinesterase enzymes and Aß- aggregation makes this core a promising disease-modifying agent.