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1.
Objective: To study the effect of halo substitution on disubstituted aryl semicarbazones on the anticonvulsant potential and model the activity based on quantum mechanics. Methods: A series of twenty-six compounds of N^4-(4-bromo-3-methylphenyl) semicarbazones were synthesized and evaluated for the anticonvulsant activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) seizure threshold tests. Some potential compounds were also tested in the subcutaneous strychnine (scSTY) and subcutaneous picrotoxin (scPIC) seizure threshold tests. The synthesized compounds were tested for behavioral impairment and CNS (central nervous system) depression in mice. Quantum mechanical modelling was carried out on these compounds to gain understanding on the structural features essential for activity. Results: Some compounds possessed broad spectrum anticonvulsant activity as indicated by their effect in pentylenetetrazole, strychnine, picrotoxin and maximal electroshock seizures models in resemblance to other aryl semicarbazone derivatives reported earlier. The higher the difference in HOMO (highest occupied molecular orbital) and LUMO (lowest unoccupied molecular orbital) energy levels was, the greater was the activity profile. Conclusion: The pharmacophoric requirements for compounds to exhibit anticonvulsant activity that includes one aryl unit in proximity to a hydrogen donor-acceptor domain and an electron donor have been justified with the molecular orbital surface analysis of the synthesized compounds.  相似文献   
2.
This paper attempts to compare some of the available models for journal acquisition and indicates their utility in library acquisitions.  相似文献   
3.
The purpose of this study was to use generalizability theory with both univariate and multivariate approaches to examine reliability of total body center of mass (CM) values calculated from cinematographical data. Twenty-eight college-aged male volunteers were filmed by a LOCAM camera at 100 fps while performing the basic locomotion skill of walking. Film analysis was conducted on each subject using six frames of film depicting a one-stride walking cycle consisting of right heel strike, right foot flat, left toe-off, left heel strike, left foot flat, and right toe-off. Nineteen segmental endpoints and a reference point were digitized by three experienced plotters. The digitizing sequence was replicated three times by each plotter. A FORTRAN program calculated nine CM values (three plotters by three repetitions) for each subject filmed in each of the six positions of the stride. The x- and y-coordinates of the CM values were the dependent variables analyzed by fully crossed 3-way univariate and multivariate ANOVAs (subjects by plotters by repetitions). All measurement facets were considered to be random. Results indicate that there was very little repetition error but considerable interplotter error for most frames. Phi-coefficients for x- and y-coordinates, separately, fluctuated across frames. The univariate values for the x-coordinates were similar but slightly less than the multivariate values. The Phi-coefficients for Y, however, were considerably lower than the multivariate values. The multivariate Phi-coefficients for generalizing over three plotters and three repetitions ranged from .82 to .90.(ABSTRACT TRUNCATED AT 250 WORDS)  相似文献   
4.
Diabetes and tuberculosis are world’s most deadly epidemics. People suffering from diabetes are susceptible to tuberculosis. Molecular link between the two is largely unknown. It is known that Vitamin A receptor (RXR) heterodimerizes with Vitamin D receptor (VDR) and Peroxisome proliferator-activator receptor-γ (PPARγ) to regulate Tryptophan-aspartate containing coat protein (TACO) expression and fatty acid metabolism respectively, so it would be interesting to check the expression of these genes in diabetes mellitus (DM) patients which might explain the susceptibility of diabetics to tuberculosis. In this study, we checked the expression of RXR, VDR, TACO and Interferon-γ (IFNγ) genes in type-2 DM patients for understanding the link between the two diseases. We observed down regulation of RXR gene and corresponding up regulation of TACO gene expression. We have not observed significant change in expression of VDR and IFNγ genes in type-2 DM patients. Repression of RXR gene could hamper VDR-RXR heterodimer formation and thus would up regulate TACO gene expression which may predispose the type-2 DM patients to tuberculosis. Also, decrease in RXR-PPARγ heterodimer could be involved in DM.  相似文献   
5.
While the debate rages on the role of social media technologies in the initial days of the Egyptian revolution of 2011, a more relevant research question today is the role of social media within an increasingly contested and turbulent political sphere. This article identifies three key modes by which social media is being exploited to impact political power, and uncovers the salience of each of these through 2 years of multisited ethnographies and interviews. First, I argue that political actors across the political spectrum, from liberals to Muslim Brotherhood (Ikhwan), are using technologies to build wider ranging, heterogeneous, and diverse networks of supporters, expanding their base from a more historically homogeneous core support group. Second, I argue that actors are working to build bridges between older and newer media platforms, recognizing that each platform is increasingly being shaped by the other. Finally, I describe some of the ways that technology is being used by activists to subvert their competition, promoting campaigns of misinformation and hacking at the expense of others.  相似文献   
6.
Clonorchis sinensis or the Chinese liver fluke is one of the most prevalent parasites affecting a major population in the oriental countries. The parasite lacks lipid generating mechanisms but is exposed to fatty acid rich bile in the liver. A secretory phospholipase A2, an enzyme that breaks down complex lipids, is important for the growth of the parasite. The enzyme is also implicated in the pathogenesis leading up to the hepatic fibrosis and its complications including cancer. The five isoforms of this particular enzyme from the parasite therefore qualify as potential drug targets. In this study, a detailed structural and ligand binding analysis of the isoforms has been done by modeling. The overall three dimensional structures of the isoforms are well conserved with three helices and a β-wing stabilized by four disulfide bonds. There are characteristic differences at the calcium binding loop, hydrophobic channel and the C-terminal domain that can potentially be exploited for drug binding. But the most significant feature pertains to the catalytic site where the isoforms exhibit three variations of either a histidine-aspartate-tyrosine or histidine-glutamate-tyrosine or histidine-aspartate-phenylalanine. Molecular docking studies show that isoform specific residues and their conformations in the substrate binding hydrophobic channel make unique interactions with certain inhibitor molecules resulting in a perfect tight fit. The proposed ligand molecules have a predicted affinity in micro-molar to nano-molar range. Interestingly, few of the ligand binding interaction patterns is in accordance to the phylogenetic studies to thereby establish the usefulness of evolutionary mechanisms in aiding ligand design. The molecular diversity of the parasitic PLA2 described in this study provides a platform for personalized medicine in the therapeutics of clonorchiasis.

Electronic supplementary material

The online version of this article (doi:10.1007/s12291-013-0377-1) contains supplementary material, which is available to authorized users.  相似文献   
7.
Curriculum development is particularly challenging in computing-related disciplines as the computing industry changes more quickly than most. As information technology degrees have become relatively pervasive, some institutions that offer information systems degrees have recognized a need to develop specialist studies in information systems. This detailed case study shows the forces related to a successful implementation of new Health Informatics degrees. The case describes both an unsuccessful and then a successful attempt at essentially the same curriculum development. Although the case includes some local political factors, these represent typical considerations that a curriculum developer is likely to encounter.  相似文献   
8.
Thyroid function tests are very important for the diagnosis and monitoring of patients with thyroid dysfunction. The guidelines recommend serum thyroid stimulating hormone (TSH) as the single most reliable test to diagnose all common forms of hypothyroidism and hyperthyroidism. The aim of this study was to analyze the ordering pattern for thyroid function tests by physicians and the analysis of results based on the clinical history. The mean age of the patients was 32.5 ± 6.5 years. Majority of samples (87.7% of total) were received from the departments of Medicine and Gynae. Thyroid profiles (47.5%) were ordered more frequently as compared to TSH only (46%). There was no significant difference in the percentage of normal reports for both types of tests. 77.8% of TFT and 76.6% of TSH samples had results within the reference range. The percentage of abnormal results was 13.7% in the patients who were screened for thyroid disorders. There is a need to redefine the case definition for thyroid dysfunction and order the appropriate test in a rational and cost effective manner.  相似文献   
9.
ABSTRACT

Formal education was used by the apartheid government to prepare black South Africans for manual labour, thus there was little curricular focus on the development of higher-order cognitive skills. With the abolition of apartheid in 1994, the education system was re-valued and re-evaluated to provide wider access to quality education; the focus of education policies moved towards the development of self-regulation and higher-order cognitive skills for all learners. There is now a generation of learners who have experienced their schooling in the transformed education system, and it would be useful to understand, from their perspective, what they value in their development of learning within the higher education space. This study answers the question ‘Post-apartheid, what learning methods and resources do first-years perceive to be valuable to their learning when they enter university?’ Participants included 344 students taking a Biology course provided to medical science students at a South African university in 2018. Two questionnaires were administered towards the end of a six-week lecture period, responses were evaluated quantitatively and qualitatively. The first survey, comprised of Likert-style questions, was conducted to determine the students’ views on the mechanisms which they used to support their learning. The second questionnaire comprised open-ended questions and focused on the students’ perception of their learning experience in the course. The findings show that there was a significant (p?<?.001) percentage of first-years who thought that rote-learning would suffice for examination preparation at university, and preferred to engage with their peers and the textbook before they engaged with their lecturers when navigating challenging concepts. Schwartz's model of social values is used to show that more needs to be done for the development of higher-order thinking and self-regulation when students enter university, and to mitigate alienation between students and staff.  相似文献   
10.
Mortality and morbidity attributed to asthma remains to be the biggest nightmare worldwide. Hence, the study was aimed to compare the cardio metabolic risk factors as assessed by Body mass index (BMI), waist hip ratio (WHR), serum triacylglycerol and uric acid in well controlled and poorly controlled asthmatics and to correlate these parameters with the severity of asthma. A case control study was conducted on 90 subjects who were segregated into well controlled asthmatics (n = 30) and poorly controlled asthmatics (n = 30) who were diagnosed based on Global initiative for Asthma management guidelines and healthy volunteers (n = 30). Centrifuged fasting venous blood samples were used for biochemical analysis, pulmonary function test, BMI, and waist hip ratio (WHR) were measured. The statistical analysis was done using SPSS version 17. There was a significant increase in BMI, WHR, lipid profile, serum uric acid and decrease in forced expiratory volume (FEV1), forced vital capacity (FVC), and FEV1/FVC in poorly controlled asthmatics. There was a significant association between FEV1 and serum uric acid, BMI and Triacylgycerol in poorly controlled asthmatics. Poorly controlled asthmatics have greater risk of developing cardiometabolic problems. Serum uric acid can be used as one of the severity markers in asthma to assess cardio metabolic risk.  相似文献   
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