Novel quinoxalinone-1,2,3-triazole derivatives as potential antifungal agents for plant anthrax disease:Design,synthesis,antifungal activity and SAR study

A series of quinoxalinone-1,2,3-triazole derivatives have been synthesized and tested for antifungal activity against phytopathogenic fungus through mycelial growth inhibition in vitro,spore germination inhibition in vitro and control effect in vivo.The results showed that the pharmacophore quinoxalinone and 1,2,3-triazole displayed promising antifungal activity.The EC50 value against C.gloeosporioides of 6a-1 was 1.17μg/mL and the compound 6c-1 showed the good bioactivity against C.fragariae Brooks and P.oryzae Cav.,displaying EC50 values of 5.56,4.62μg/mL,respectively.The inhibitory of spore germination by 6a-1 was performed with EC50 value of 1.91μg/mL.In addition,the in vivo bioassay indicated that 6a-1 possessed effective control against Pepper Anthrax Disease in protective treatment.For given activity data of target compounds,structure-activity relationship(SAR)study was operated,hoping for optimizing the target structure to find lead compound with higher activity.

Research on Children’s Game Activity Design Strategies Based on Embodied Cognition Theory

Edutainment,in the kindergarten education stage,emphasizes the game as the basic activity and combines the content of education with the form of the game,thus it also forms the educational method of gamification teaching.Through investigation and analysis,it is found that the current kindergarten game activity design has the problem of improper combination of educational content and game form.The current kindergarten game activity design has problems such as stereotypes,children’s lack of active learning opportunities in activities,teachers’insufficient theoretical understanding,inappropriate teacher guidance methods,and so on.Embodied cognition theory attaches importance to the important role of the body in the development of cognition,provides new guidance for classroom teaching,and opens up a new path for classroom teaching reform.Based on the perspective of embodied cognition theory,the concept of body and mind integration should be adhered to in kindergarten teaching with games as the basic activity,experiential teaching situation should be created,children’s subjective experience should be respected,and games and interactions should be designed to promote children’s physical and mental participation,thus laying a foundation for the realization of children’s individual freedom,autonomy,and all-round development.Therefore,this paper aims at the existing problems in the current kindergarten gamification teaching and discusses the design strategy of children’s game activities based on embodied cognition theory.

Differences in transportation and leisure physical activity by neighborhood design controlling for residential choice

Background:Cross-sectional studies provide useful insight about the associations between the built environment and physical activity(PA),particularly when reasons for neighborhood choice are considered.Our study analyzed the relationship between levels of weekly transportation and leisure PA among 3 neighborhood designs,statistically adjusting for sociodemographic characteristics and reasons for neighborhood choice.Methods:A stratified random sample of adults(age>20 years)living in Calgary(Canada)neighborhoods with different neighborhood designs(grid,warped-grid,and curvilinear)and socioeconomic status completed a self-administered questionnaire capturing PA,sociodemographic characteristics,and reasons for neighborhood choice(response rate=10.1%;n=1023).Generalized linear models estimated associations between neighborhood design and transportation and leisure PA outcomes(participation(any vs.none)and volume(metabolic equivalent:h/week)),adjusting for neighborhood socioeconomic status,sociodemographic characteristics(gender,age,ethnicity,education,household income,marital status,children,vehicle access,dog ownership,and injury),and reasons for neighborhood choice(e.g.,proximity and quality of recreational and utilitarian destinations,proximity to work,highway access,aesthetics,and sense of community).Results:Overall,854 participants had resided in their neighborhood for at least 12 months and provided complete data.Compared with those living in curvilinear neighborhoods,grid neighborhood participants had greater odds(p<0.05)of participating in any transportation walking(odds ratio(OR)=2.17),transportation and leisure cycling(OR=2.39 and OR=1.70),active transportation(OR=2.16),and high-intensity leisure PA(≥6 metabolic equivalent;OR=1.74),respectively.There were no neighborhood differences in the volume of any transportation or leisure PA undertaken.Adjustment for neighborhood selection had minimal impact on the statistical or practical importance of model estimates.Conclusion:Neighborhood design is associated with PA patterns in adults,independent of reasons for neighborhood choice and sociodemogranhic factors.

Adsorption of Malachite Green Using Activated Carbon from Mangosteen Peel: Optimization Using Box-Behnken Design

In this research,activated carbon from mangosteen peel has been synthesized using sulfuric acid as an activator.The adsorption performance of the activated carbon was optimized using malachite green dye as absorbate.Mala-chite green dye waste is a toxic and non-biodegradable material that damages the environment.Optimization of adsorption processes was carried out using Response Surface Methodology(RSM)with a Box-Behnken Design(BBD).The synthesized activated carbon was characterized using FTIR and SEM instruments.The FTIR spectra confirmed the presence of a sulfonate group(-SO_(3)H)in the activated carbon,indicating that the activation pro-cess using sulfuric acid was successful.SEM characterization shows that activated carbon has porous morphology.Optimization was carried out for three adsorption parameters,namely contact time(20,60,and 120 min),adsor-bent mass(0.005,0.025,and 0.05 g),and initial concentration of malachite green solution(5,50,and 100 mg·L^(-1)).The concentration of the malachite green solution was determined using a UV-Vis spectrophotometer at the max-imum wavelength of malachite green,618 nm.The optimum of malachite green adsorption using mangosteen peel activated carbon was obtained at a contact time of 80 min,an adsorbent mass of 0.032 g,and malachite green initial concentration of 25 mg·L^(-1),with a maximum removal percentage and maximum adsorption capacity of 93.66%and 19.345 mg·g^(-1),respectively.

Optimization of Extraction Process and Determination of Antioxidant Activity of Myrica ruba Leaf Pigment by Orthogonal Design

[Objectives] To determine the optimum conditions and antioxidant activity of Myrica ruba leaf pigment,and provide reference for further development and use of Myrica ruba leaves. [Methods]Pigment of Myrica ruba leaves was extracted by ethanol extraction method. Absorbance was measured at wavelength of 300 nm. Effects of ethanol volume fraction,solid-to-liquid ratio,temperature,and extraction time were studied. L_9( 3~3) orthogonal experiment was carried out to optimize the extraction process,and DPPH scavenging ability was measured.[Results]The optimum extraction process of Myrica ruba leaf pigment was as follows: the ethanol volume fraction was 50%; the solid-to-liquid ratio was 1: 60( w/v),extraction temperature 70℃; extraction time was 60 min; after the concentration of purified Myrica ruba leaf pigment reached 0. 4455 mg/mL,the DPPH scavenging ability was basically the same as the same concentration Vc.[Conclusions] The experiment indicates that the optimized extraction process has a high yield rate,and Myrica ruba leaf pigment has high anti-oxidant activity.

Design of New Thiadiazole Derivatives with Improved Antidiabetic Activity

Diabetes is a serious, long-term (or chronic) disease that occurs when a person’s blood sugar levels are high because their body cannot produce enough insulin, or does not produce enough insulin or that it cannot effectively use the insulin it produces. According to the literature, this disease has several causes, but certain types of diabetes such as type 2 diabetes are most closely linked to a metabolic disorder due to abdominal obesity. Thus, the number of individuals with type 2 diabetes is increasing. It is with this in mind that we work to improve human health. The aim of this study is to design new derivatives of 1,3,4-thiadiazole with improved antidiabetic activity by the mathematical model of multiple linear regression (MLR) established previously. The analysis of the effect on the substituents influencing the antidiabetic activity, fourteen (14) new molecules coded CDTH were generated and presenting values of the potential of inhibitory concentration higher than that of the base compound (pIC50 = 2.526). But thirteen (13) of these new compounds belong to the domain of applicability of the MLR model established previously. In addition, the thermodynamic quantities of formation formed at 298K have been calculated. Lipinski’s rule and pharmacokinetic properties proved that five (5) (TH4, TH9, TH10, TH13 and TH14) new molecules can be used as diabetes medicine.

A study on the Application of the Activity Theory to Leaming Activity Design of MOOC in English Grammar Teaching

MOOC has become the topic of the education reform in recent years. From activity theory point of view, meaningful learning is an active, conscious, constructive, and socially medicated practice that includes reciprocal intention-action-reflection activities. This paper aims to try to give a MOOC learning activity design model in grammar teaching which tries to offer a reference for the MOOC teaching in grammar lesson.

A Study on the Design of Task Activity in the Post- task Stage of Middle School English Classroom

The task activity in the post-task stage is mainly to enable the students clearly aware of their own language learning process in the existing problems and effectively solve them through the ＂do-it-again＂ , language focus and other activities, and at the same time the focus of this lesson, difficulties are more clear and clear. It can be said that post-task activities play a vital role in highlighting priorities, breaking through difficulties, and achieving effective goals for teaching goals. The design of the activities in the post-task stage is to complete the task and language focus together, reflecting the distinctive characteristics of task-based teaching. The design of the activities in the post-task stage can be achieved through evaluation, language focus, and extra-curricular activities.

On Design Principles of Micro-lectures of theme-based English Vocabulary for High-grade Primary School Students——A Case Study of a Class of Fifth-grade students in ECNU Affiliated Primary School

For English education primary school,English vocabulary teaching should be attach importance to because in the traditional class of English vocabulary teaching,teachers just fill young minds with knowledge points of each word in a 35-minute class yet fail to lay emphasis of learners’meaningful learning and autonomic learning as well as their very limited attention spans.To support traditional English vocabulary teaching classes,the research proposes the theme-based English vocabulary micro-lectures designed on the basis of experiential learning theory and constructivist learning theory as well as the analyses of target users of high-level students in the primary school.After application of the micro-lectures into practice,the research assesses the effect of the micro-lectures on the learners and then makes suggestions for design principles of theme-based vocabulary micro-lectures about selection of contents and vocabulary themes,supplementary teaching activities and teacher interaction in the micro-lectures for high-level students in the primary school.Also,the designers should make multi-level English vocabulary micro-lectures according to learners’English proficiency and increase repetition rates of vocabularies in the micro-lectures.

Design and Application Research of Active Tag for Pig

The study aimed at introducing the design scheme of the active tag in 2.4 GHz frequency band for pig based on RFID technology. And through the actual circuit board test, the following results were come up： communication distance and signal strength gradually increased with the data transfer rate reducing in multiples; better communication effects were achieved in the data transfer rate of 60 kbps or 10 kbps; the active tags could be recognized accurately within 50 m, greatly improving the security of swine food safety traceability system.

The effects of a bike active video game on players' physical activity and motivation

Background: Players may not acquire adequate levels of moderate-to-vigorous physical activity(MVPA) when playing commercial video games.This study's goal was to evaluate the effects of an exercise bike video game played by using a mobile application-based exergame that was designed exclusively to promote participants' MVPA, with additional attention paid to this game's ability to promote greater situational interest.Methods: An experimental design was used with 163 students(aged 20.31 ± 1.30, 18–26 years, 61.3% male), all of whom were randomly allocated into an experimental group and a control group. Physical activity(PA) levels were assessed with Acti Graph GT3X+(Acti Graph Inc., Fort Walton Beach, FL, USA) accelerometers. The situational interest scale was used to evaluate students' situational interest in both groups.Multivariate analysis of variance was conducted to examine the differences between sedentary behavior, PA levels, and situational interest between groups. Regression analyses were also used, with the purpose being to evaluate the strength of the relationship between PA and situational interest.Results: Results revealed that the experimental group had higher degrees of sedentary behavior, light PA, total interest, instant enjoyment,exploration intention, attention demand, novelty, and challenge, whereas the control group received higher scores for MVPA(control 95.01% vs.experimental group 89.94%). Regression analysis indicated that instant enjoyment(β = 0.49, p < 0.01), exploration intention(β = 0.18, p < 0.05),and attention demand(β = 0.17, p < 0.05) were positive predictors for total interest, explaining 43% of its variance.Conclusion: A newly designed mobile application-based exergame played via an exercise bike may enhance situational interest and provide a decent level of PA for players.

Design approaches for active,semi-active and passive control systems based on analysis of characteristics of active control force

In this paper, the characteristics of forces in active control systems connected to adjacent levels of a building are analyzed. The following characteristics are observed： （1） active control can provide significantly superior supplemental damping to a building, but causes a small frequency shift; （2） the linear quadratic regulator （LQR）-based control force is composed of an elastic restoring force component and a damping force component, where the damping force is almost identical to the total control force, however, the elastic restoring force is very small; and （3） the active control forces prevent mction most of the time during the entire control process. These three characteristics imply that active control systems connected to adjacent levels of a building behave like passive damping devices with adjustable parameters, namely damping characteristics in an active control, which is the mechanism used by semi-active control devices to reach similar performance as active control systems. Two indices are defined to quantify the damping characteristics of control forces in active control systems. These two indices can also be used to quantify the capacity of semi-active control to achieve the perfonrlance of active control. Based on the above observations, two principles are founded for optimization of parameters of semi-active control devices and passive dampers. The first is that the maximum output force of a semi-active or passive device to be designed is identical to an active device, called ＂design principle＂. The other is the response equivalent principle, which states that the response of a building with semi-active or passive devices is the same as with active devices when the same maximum output force is applied. The design procedure for semi-active control devices and passive dampers is described in detail. Finally, numerical simulations of two benchmark problems is conducted to demonstrate the damping characteristics of active control and investigate the capacity of semi-active control to achieve the same performance as active control.

Molecular design,synthesis and biological activities of amidines as new ketol-acid reductoisomerase inhibitors

Diamidine （A） was identified in our in vitro bio-assay as a possible inhibitor of ketol-acid reductoisomerase （KARI） from the ACD database search based on the known three-dimensional crystal structure of KARI. An investigation on interaction of A on KARI active sites, led to the design and synthesis of 15 novel monoamidines. Some of those showed better biological activity than A on rice KARI （in vitro） and in greenhouse herbicidal tests （in vivo）. The structure-biological activity relationship was investigated, which provides valuable information to further study of potential KARI inhibitors.

Acquisition and Active Navigation of Knowledge Particles throughout Product Variation Design Process

The variation design of complex products has such features as multivariate association, weak theory coupling and implicit knowledge iteration. However, present CAD soft wares are still restricted to making decisions only according to current design status in dynamic navigation which leads to the huge drain of the knowledge hidden in design process. In this paper, a method of acquisition and active navigation of knowledge particles throughout product variation design process is put forward. The multi-objective decision information model of the variation design is established via the definition of condition attribute set and decision attribute set in finite universe. The addition and retrieval of the variation semantics is achieved through bidirectional association between the transplantable structures and variation design semantics. The mapping relationships between the topology lapping geometry elements set and constraint relations set family is built by means of geometry feature analysis. The acquisition of knowledge particles is implemented by attribute reduction based on rough set theory to make multi-objective decision of variation design. The topology lapping status of transplantable substructures is known from DOF reduction. The active navigation of knowledge particles is realized through embedded event-condition-action（ECA） rules. The independent prototype system taking Alan, Charles, Ian＇s system（ACIS） as kernel has been developed to verify the proposed method by applying variation design of complex mechanical products. The test results demonstrate that the navigation decision basis can be successfully extended from static isolated design status to dynamic continuous design process so that it more flexibly adapts to the different designers and various variation design steps. It is of profound significance for enhancing system intelligence as well as improving design quality and efficiency.

Expression of Recombinant Human Lysozyme-tachyplesin I(hLYZ-TP I)in Pichia Pastoris and Analysis of Antibacterial Activity

Antimicrobial peptides （AMPs） are making headlines in science because they demonstrate superior microbicidal characteristics compared to synthetic and semi-synthetic antibiotics.

Design and Operation of the Printing and Dyeing Wastewater Treatment Project by Combination of Coagulation Sedimentation - Hydrolytic Acidification with Aeration Tank - Biological Aerated Filter - Active Sand Filter

In order to protect quality of Baiyangdian surface water and Gaoyang groundwater,the project is applied to process printing and dyeing wastewater that contains complicated compositions,high concentrations of organics and SS,and lots of pollutants difficult to degrade by microorganism. The process and operating parameters of project are optimized and debugged,and its economic and environmental benefits are analyzed.The results show that the process of coagulation sedimentation-hydrolytic acidification with aeration tank-biological aerated filter-active sand filter is applied in Gaoyang Sewage Treatment Plant. The design scale of sewage treatment plant is 120000 m^3/d. The influent is as following: COD is 669mg/L; SS is 424mg/L; NH_3-N is 8.83mg/L; TP is 6.03mg/L. After the process,the best removal rates of COD,SS,NH_3-N and TP are 93. 5%,98. 8%,97. 1% and 96. 2%,respectively. The various indexes of effluent water complied with standard A of the first order in Pollutants Emission Standard of Urban Wastewater Treatment Plant( GB 18918-2002). The processing cost is only 0. 807 yuan/m^3. As a result,the project construction and operation not only improve the environment,but also promote regional economic development. Process design and operating parameters provide an important reference value for the printing and dyeing wastewater treatment industry.

Real-time Design Constraints in Implementing Active Vibration Control Algorithms

Although computer architectures incorporate fast processing hardware resources, high performance real-time implementation of a complex control algorithm requires an efficient design and software coding of the algorithm so as to exploit special features of the hardware and avoid associated architecture shortcomings. This paper presents an investigation into the analysis and design mechanisms that will lead to reduction in the execution time in implementing real-time control algorithms. The proposed mechanisms are exemplified by means of one algorithm, which demonstrates their applicability to real-time applications. An active vibration control （AVC） algorithm for a flexible beam system simulated using the finite difference （FD） method is considered to demonstrate the effectiveness of the proposed methods. A comparative performance evaluation of the proposed design mechanisms is presented and discussed through a set of experiments.

Systematic Analysis of Carbon Dioxide Activation of Waste Tire by Factorial Design

In this study, waste tire was used as raw material for the production of activated carbons through pyrolysis. ＇Fire char was first produced by carbomzation at 550℃ under nitrogen. A two tactortal design was used to optimize the production of activated carbon from tire char. The effects of several factors controlling the activation process, such as temperature （.830-930℃）, time （2-6h） and percentage ot carbon dioxide （70%-100%） were investigated. The production was described mathematically as a function of these three factors. First order modeling equations were developed for surface area, yield and mesopore volume. It was concluded that the yield, BET surface area and mesopore volume of activated carbon were most sensitive to activation temperature and time while percentage of carbon dioxide in the activation gas was a less significant factor.

Extraction of Herba Lycopi Polysaccharide and Study of Its Antioxidant Activity by Cellulase Method

[Objectives] To optimize the extraction process of Herba Lycopi polysaccharide by cellulase,and study its antioxidant activity.[Methods]The single factor test and orthogonal test were conducted to study the effect of p H,enzyme dosage,enzymolysis temperature and extraction time on the extraction of Herba Lycopi polysaccharide. And the test was done about its scavenging effect on DPPH radicals and superoxide anions,and the antioxidant activity was evaluated. [Results] The optimum extraction process by cellulase method was as follows: p H value of 7; enzyme dosage of 4 ml; enzymolysis temperature of 40 ℃; extraction time of 2. 5 h. The average extraction rate of Herba Lycopi polysaccharide was 10. 70%,and RSD was 0. 17%. The antioxidant activity test showed that Herba Lycopi polysaccharide had a significant scavenging effect on radicals. [Conclusions] Herba Lycopi polysaccharides had strong antioxidant activity,and could provide a scientific basis for the development and utilization of Herba Lycopi medicinal resources.