Structural bionic design lacks mature and scientific theories, and the excellent structural characteristics of natural organisms sometimes cannot be transferred into engineering structures effectively. Aiming at overc...Structural bionic design lacks mature and scientific theories, and the excellent structural characteristics of natural organisms sometimes cannot be transferred into engineering structures effectively. Aiming at overcoming the existing problems, this paper summarizes three related theories: similarity theory, fuzzy evaluation theory and optimization theory. Based on the related theories, a method of structural bionic design is introduced, which includes four steps: selecting the most useful structural characteristic of natural organism; analyzing the structural characteristic finally chosen for engineering problem; completing the structural bionic design for engineering structure; and verifying the structural bionic design. Similarity theory and fuzzy evaluation theory are employed to achieve Step 1. In Step 2 and Step 3, optimization theory is employed to analyze the parameters of structures. Together with the thoughts of simplification and grouping, optimization theory can reveal the relationship between organism structure and engineering structure, providing a way to structural bionic design. A general evaluation criterion is proposed in Step 4, which is feasible to evaluate the performance of different structures. Finally, based on the method, a structural bionic design of thin-walled cylindrical shell is introduced.展开更多
Considering that buildings represent 40% of greenhouse gases and approximately 10% of global gross domestic product, the target the building industry has to accomplish is to get to a high quality and low carbon living...Considering that buildings represent 40% of greenhouse gases and approximately 10% of global gross domestic product, the target the building industry has to accomplish is to get to a high quality and low carbon living, by reducing carbon emission by 2050, as said by Energy Performance of Buildings Directive. Considering these needs, designers, manufacturers and construction companies should be able to make use of web and design tools for collecting and inventorying a large variety of environmentally friendly materials, through a specific database that encloses low carbon certified products and eco-labeled ones. The eco-labels are internationally identified as the best tools to encourage the spread of green products and low carbon notions, even if in Europe, there is no specific tool to be used. The project called LoCaMat (Low Carbon Material Database) will act as the first Italian and European database that encompasses multiple data on certified green materials to be used for the construction sector, making buildings climate change resilient, ensuring an efficient use of energy and resources, getting to a complete life cycle assessment for buildings materials and components, encompassing, for the first time, green data and every kind of environmental specs for sustainable design and green practice.展开更多
In this study, a detailed evaluation was performed about the advancements in the renewable energy capacity (especially wind and solar energy) depending on progressive technological developments. Total energy consump...In this study, a detailed evaluation was performed about the advancements in the renewable energy capacity (especially wind and solar energy) depending on progressive technological developments. Total energy consumption as well as renewable energy production from natural sources is statistically evaluated in the basis of leading countries for the period of 2000-2010. The variation of energy mix, future trend of wind energy installations, cumulative capacities in daily wind and solar energy per person are worldwide investigated in this period.展开更多
Reliable service life data of building products are of great importance when completing environmental LCA (life cycle assessment) reviews, for LCC (life cycle costing) and for maintenance planning tasks. A researc...Reliable service life data of building products are of great importance when completing environmental LCA (life cycle assessment) reviews, for LCC (life cycle costing) and for maintenance planning tasks. A research project was set up to answer the following research questions: (1) what are reliable service life data of current used building products; and (2) how can generic data about the service lives of building products be tailored to specific project circumstances using the "factor method" described in the ISO (International Standard Organization) 15686 Series: "Buildings and Constructed Assets-Service-Life Planning". Experts of industry organisations for building materials and products made a final judgement of the new established reference service lives. Reference service lives of building products may show a large unknown bandwidth around the average. That will make the bandwidth of estimated service lives, taking the project situation of building components into account, very big. Experts have raised objections to the use the factor method for deriving mathematically a bandwidth of estimated service lives of a building product from the reference service life of the product. A practical analytical application of the factor method has been made by describing all factors and underlying criteria and a reference situation.展开更多
According to the characteristics of ecosystem and concept of the ecosystem in mining area, the index system of the ecosystem health in mining area was set up, and the evaluation standard was established. Aiming at the...According to the characteristics of ecosystem and concept of the ecosystem in mining area, the index system of the ecosystem health in mining area was set up, and the evaluation standard was established. Aiming at the complexion in which the information lost in index ration, the matter element method was put forward to evaluate the ecosystem health in mining area. Making use of the model set up, the weight was built up by the method of index number heavy, the matter element, clas- sical field, and limit field were set up. The rating hierarchy was calculated by relating function. As a case study in the mining area of Pingyangsi Town, the results show that the ecosystem is good and sustainable from 2003 to 2006, but the healthy degree is not high, and some indexes have depravation.展开更多
The index systems are not only the tools to evaluate existing practice results, but also the guides to the future development direction and development way of practical activities. "Well-off society" is a relatively...The index systems are not only the tools to evaluate existing practice results, but also the guides to the future development direction and development way of practical activities. "Well-off society" is a relatively vague concept, and the contents of it ceaselessly change with the advancement of society and the development of productivity. Now the construction of a well-off society in an all-round way enters a critical stage, so the original evaluation standards must change with gradual advancement of the construction goal of a well-off society. So it is very necessary for us to build a comprehensive evaluation index system and make it better and better to provide effective statistical consultation and statistical supervision for constructing a well-off society in an all-round way. This paper attempts to analyze the current evaluation index system, then puts forward the general thinking and flame work of the index system of building a well-off society in an all-round way.展开更多
Effective assessment is inseparable from good teaching and learning. Just as a good tutor would practice different techniques of teaching, an assessor would usually use different strategies of assessment. Moreover, th...Effective assessment is inseparable from good teaching and learning. Just as a good tutor would practice different techniques of teaching, an assessor would usually use different strategies of assessment. Moreover, the different activities of assessment, such as teaching, are additionally executed at various times during the semester, thus, we can know in which way the student is learning. An assessment strategy lays out a well thoroughly considered choice of assessment methods that are aligned with the aims and learning outcomes. Because align the assessment with a specific kind of learning outcome, the tutor needs to choose a suitable technique of assessment. This paper draws upon a case study of the first year architectural design at Pharos University as another way to deal with realizing "how to design your assessment plan". Throughout the form of criteria based assessment, assessment can help to review the students and instructors feeling and reactions. Finally, we can learn to assist towards enhancing student learning through assessment. So, we can attract the consideration regarding the advantages of reviewing current assessment practices, and of accepting different ways to deal with assessment methods, in this manner profiting together student and tutor.展开更多
Nowadays, the number of products and also of architectural projects, qualified as "sustainable", is ever more growing. Following this trend, architectural design may exploit the use of (eco) materials and componen...Nowadays, the number of products and also of architectural projects, qualified as "sustainable", is ever more growing. Following this trend, architectural design may exploit the use of (eco) materials and components to promote a project as sustainable even without considering its impact on the environment; This can be defined as architectural greenwash. This paper considers the case of green envelopes with the aim to evaluate if these can be defined as sustainable design practice. Green envelopes provide environmental advantages together with the suggestion to a green aesthetics par excellence. In fact, the integration of vegetation in urban fabric plays an important role in improving ecological and environmental conditions of (and in) cities, although systems can have a high environmental burden. This paper aims to answer the question: Is greening the building envelope a sustainable design practice? To do so, the paper provides a literature review which includes the main research developed regarding environmental burden, benefits and LCA (life cycle assessment) calculations of green envelopes.展开更多
As the foundation of farm household structure,livelihood asset status is the basis for farmers to gain opportunities,adopt livelihood strategies,resist livelihood risk,and engage in positive livelihood achievements.Qu...As the foundation of farm household structure,livelihood asset status is the basis for farmers to gain opportunities,adopt livelihood strategies,resist livelihood risk,and engage in positive livelihood achievements.Quantifying farm household assets identifies future development trends that are fundamentally necessary to predict farm household vulnerability and strategy,as well as understanding farmers’current living situations.Using Zunyi City in China’s western mountainous area as a case study,we conducted stratified sampling and participatory rural investigation appraisal to collect data on the attributes of farm households’livelihood assets and livelihood strategies to establish an index evaluation system and enable evaluation and analysis of farm households with different livelihood strategies.Our research indicates that due to structural differences,total livelihood assets of farm households with different livelihood strategies are similar.Rural households have an abundance of natural and material assets and deficiencies in human,financial and social assets.Non-rural households and part-time households are abundant in human,financial and social assets and deficient in natural and material assets.展开更多
Habitat quality assessments are of great significance for protecting biodiversity.This study analyzes the changing habitat quality of Lashihai watershed based on SPOT satellite images.We extracted the land use data fo...Habitat quality assessments are of great significance for protecting biodiversity.This study analyzes the changing habitat quality of Lashihai watershed based on SPOT satellite images.We extracted the land use data for Lashihai watershed in Yunnan province for the years 2000 and 2015,and then used an INVEST model to evaluate habitat degradation,habitat quality and habitat scarcity in the study area from 2000 to 2015.Spatial statistical methods were used to determine changes to spatial dynamics.Results indicate that the number of areas with habitat degradation was generally small,and that both the number of areas with habitat degradation and the degree of degradation had fallen noticeably during the fifteen-year study period.In general,the quality of habitats was main- tained or improved,while the quality of habitats decreased in only a few areas.The scarcity of habitats for cultivated land had increased,the tension between people and land use was relatively prominent.The reason habitat quality in Lashihai watershed has improved can be attributed to three factors:1)The policy of returning farmland to forests since 2000 has been well implemented and has achieved remarkable results.Loss of forests from logging and deforestation has basically been eliminated,and great progress has been made restoring the ecological environment.2)High background value of quality habitat suitability benefits from the research area's high vegetation coverage.3)The development of the local tourism economy has transformed the area's ecological advantages into an economic bonus,greatly increasing the income level and living standards of residents.At the same time,the ecological resource bonus has increased the enthusiasm of residents for ecological protection and has helped to promote the protection of local eco-systems,both reducing ecological degradation and improving habitat quality.At the same time,increasing conflicts between land and people should be addressed.Support is needed to promote development of the ecological economy while continuously reducing ecological degradation and further increasing residents'income.There must be less reliance on industry and less pressure on both land and people,all the while ensuring that the local economy and ecology can more forward together in a sustainable way.展开更多
A series of amino organophosphorus imidazoles were designed and synthesized as a novel structural type of antimicrobial agents.Bioactive evaluation in vitro showed that compound 3f exhibited equipotent or superior ant...A series of amino organophosphorus imidazoles were designed and synthesized as a novel structural type of antimicrobial agents.Bioactive evaluation in vitro showed that compound 3f exhibited equipotent or superior anti-methicillin-resistant Staphylococcus aureus(anti-MRSA) and anti-S. cerevisiae efficiencies(minimal inhibitory concentration(MIC)=2 μg/mL) to clinical drugs,and the combinations with antibacterial or antifungal drugs enhanced the antimicrobial efficiency. Highly active molecule 3f showed low propensity for bacteria to develop resistance, and the preliminary action mechanism studies demonstrated that 3f was membrane-active, but had no significant intercalation towards MRSA DNA. The computational study on 3f reasonably explained its high antimicrobial activity. Experimental data revealed that ground-state 3f-HSA complexes were formed mainly through hydrophobic interactions and hydrogen bonds with a spontaneous process, and the non-radioactive energy transfer from HSA to 3f occurred beyond F鰎ster resonance energy transfer theory. The participation of metal ions in 3f-HSA supramolucular system could increase the concentration of free compound 3f, and shorten its storage time and half-life in the blood to improve the maximum antimicrobial efficacy.展开更多
A novel series of diaryl urea derivatives bearing sulfonamide moiety have been designed and synthesized. Their in vitro antitumor effect against human cancer cell lines MX-1, A375, HepG2, Ketr3 and HT-29 was screened ...A novel series of diaryl urea derivatives bearing sulfonamide moiety have been designed and synthesized. Their in vitro antitumor effect against human cancer cell lines MX-1, A375, HepG2, Ketr3 and HT-29 was screened and evaluated by the standard MTT assay with sorafenib as the positive control. Some of the compounds showed significant inhibitory activity against multiple cell lines compared to sorafenib. In particular, 2,6-dimethyl-4-{6-[3-(4-chloro-3-(trifluoromethyl)phenyl)urealnaphthalen- 2-yllsulfonyl morpholine (10d) was found to be the most potent against A375, HepG2 and Ketr3 with ICs0 values of 0.65-0.97 μmol/L, which were 5-20-fold more potent than sorafenib. Compound 10d emerged as a valuable lead for further optimization.展开更多
A series of new benzimidazole derivatives was synthesized and characterized by IR,1H NMR,13C NMR,MS,and HRMS spectra.All the new compounds were screened for their antimicrobial activities in vitro by a twofold serial ...A series of new benzimidazole derivatives was synthesized and characterized by IR,1H NMR,13C NMR,MS,and HRMS spectra.All the new compounds were screened for their antimicrobial activities in vitro by a twofold serial dilution technique.The bioactive evaluation showed that 3,5-bis(trifluoromethyl)phenyl benzimidazoles were comparably or even more strongly antibacterial and antifungal than the reference drugs Chloromycin,Norfloxacin,and Fluconazole.The combination of2,4-difluorobenzyl benzimidazole derivative 5l and its hydrochloride 7 respectively with the antibacterials Chloromycin,Norfloxacin,and the antifungal Fluconazole was more sensitive to methicillin-resistant MRSA and Fluconazole-insensitive A.flavus.In addition,the interaction of compound 5l with calf thymus DNA demonstrated that this compound could effectively intercalate into DNA to form a compound 5l-DNA complex that might block DNA replication and thereby exert good antimicrobial activity.展开更多
Persuasive technology is the use of computers,devices or applications to change a person's attitudes or behavior.Persuasibility design within the system life-cycle is a nascent area of research which is different ...Persuasive technology is the use of computers,devices or applications to change a person's attitudes or behavior.Persuasibility design within the system life-cycle is a nascent area of research which is different from design in the traditional method.This paper focuses on the research of persuasibility design and its assessment in the system life-cycle.A life-cycle oriented systemic general theory is developed in this paper to evaluate persuasibility design.Persuasibility assessment is considered as a part of persuasibility design.Its procedure and method are explored and analyzed based on the system life-cycle in this paper.A possible research direction is to create more explicit and detailed persuasion design and assessment methods which can be used not only in personal computer persuasive application,but also many other electric devices that are designed for persuasion purposes.展开更多
基金Supported by National Natural Science Foundation of China (No. 50975012)Research Fund for the Doctoral Program of Higher Education of China (No. 20091102110022)
文摘Structural bionic design lacks mature and scientific theories, and the excellent structural characteristics of natural organisms sometimes cannot be transferred into engineering structures effectively. Aiming at overcoming the existing problems, this paper summarizes three related theories: similarity theory, fuzzy evaluation theory and optimization theory. Based on the related theories, a method of structural bionic design is introduced, which includes four steps: selecting the most useful structural characteristic of natural organism; analyzing the structural characteristic finally chosen for engineering problem; completing the structural bionic design for engineering structure; and verifying the structural bionic design. Similarity theory and fuzzy evaluation theory are employed to achieve Step 1. In Step 2 and Step 3, optimization theory is employed to analyze the parameters of structures. Together with the thoughts of simplification and grouping, optimization theory can reveal the relationship between organism structure and engineering structure, providing a way to structural bionic design. A general evaluation criterion is proposed in Step 4, which is feasible to evaluate the performance of different structures. Finally, based on the method, a structural bionic design of thin-walled cylindrical shell is introduced.
文摘Considering that buildings represent 40% of greenhouse gases and approximately 10% of global gross domestic product, the target the building industry has to accomplish is to get to a high quality and low carbon living, by reducing carbon emission by 2050, as said by Energy Performance of Buildings Directive. Considering these needs, designers, manufacturers and construction companies should be able to make use of web and design tools for collecting and inventorying a large variety of environmentally friendly materials, through a specific database that encloses low carbon certified products and eco-labeled ones. The eco-labels are internationally identified as the best tools to encourage the spread of green products and low carbon notions, even if in Europe, there is no specific tool to be used. The project called LoCaMat (Low Carbon Material Database) will act as the first Italian and European database that encompasses multiple data on certified green materials to be used for the construction sector, making buildings climate change resilient, ensuring an efficient use of energy and resources, getting to a complete life cycle assessment for buildings materials and components, encompassing, for the first time, green data and every kind of environmental specs for sustainable design and green practice.
文摘In this study, a detailed evaluation was performed about the advancements in the renewable energy capacity (especially wind and solar energy) depending on progressive technological developments. Total energy consumption as well as renewable energy production from natural sources is statistically evaluated in the basis of leading countries for the period of 2000-2010. The variation of energy mix, future trend of wind energy installations, cumulative capacities in daily wind and solar energy per person are worldwide investigated in this period.
文摘Reliable service life data of building products are of great importance when completing environmental LCA (life cycle assessment) reviews, for LCC (life cycle costing) and for maintenance planning tasks. A research project was set up to answer the following research questions: (1) what are reliable service life data of current used building products; and (2) how can generic data about the service lives of building products be tailored to specific project circumstances using the "factor method" described in the ISO (International Standard Organization) 15686 Series: "Buildings and Constructed Assets-Service-Life Planning". Experts of industry organisations for building materials and products made a final judgement of the new established reference service lives. Reference service lives of building products may show a large unknown bandwidth around the average. That will make the bandwidth of estimated service lives, taking the project situation of building components into account, very big. Experts have raised objections to the use the factor method for deriving mathematically a bandwidth of estimated service lives of a building product from the reference service life of the product. A practical analytical application of the factor method has been made by describing all factors and underlying criteria and a reference situation.
文摘According to the characteristics of ecosystem and concept of the ecosystem in mining area, the index system of the ecosystem health in mining area was set up, and the evaluation standard was established. Aiming at the complexion in which the information lost in index ration, the matter element method was put forward to evaluate the ecosystem health in mining area. Making use of the model set up, the weight was built up by the method of index number heavy, the matter element, clas- sical field, and limit field were set up. The rating hierarchy was calculated by relating function. As a case study in the mining area of Pingyangsi Town, the results show that the ecosystem is good and sustainable from 2003 to 2006, but the healthy degree is not high, and some indexes have depravation.
文摘The index systems are not only the tools to evaluate existing practice results, but also the guides to the future development direction and development way of practical activities. "Well-off society" is a relatively vague concept, and the contents of it ceaselessly change with the advancement of society and the development of productivity. Now the construction of a well-off society in an all-round way enters a critical stage, so the original evaluation standards must change with gradual advancement of the construction goal of a well-off society. So it is very necessary for us to build a comprehensive evaluation index system and make it better and better to provide effective statistical consultation and statistical supervision for constructing a well-off society in an all-round way. This paper attempts to analyze the current evaluation index system, then puts forward the general thinking and flame work of the index system of building a well-off society in an all-round way.
文摘Effective assessment is inseparable from good teaching and learning. Just as a good tutor would practice different techniques of teaching, an assessor would usually use different strategies of assessment. Moreover, the different activities of assessment, such as teaching, are additionally executed at various times during the semester, thus, we can know in which way the student is learning. An assessment strategy lays out a well thoroughly considered choice of assessment methods that are aligned with the aims and learning outcomes. Because align the assessment with a specific kind of learning outcome, the tutor needs to choose a suitable technique of assessment. This paper draws upon a case study of the first year architectural design at Pharos University as another way to deal with realizing "how to design your assessment plan". Throughout the form of criteria based assessment, assessment can help to review the students and instructors feeling and reactions. Finally, we can learn to assist towards enhancing student learning through assessment. So, we can attract the consideration regarding the advantages of reviewing current assessment practices, and of accepting different ways to deal with assessment methods, in this manner profiting together student and tutor.
文摘Nowadays, the number of products and also of architectural projects, qualified as "sustainable", is ever more growing. Following this trend, architectural design may exploit the use of (eco) materials and components to promote a project as sustainable even without considering its impact on the environment; This can be defined as architectural greenwash. This paper considers the case of green envelopes with the aim to evaluate if these can be defined as sustainable design practice. Green envelopes provide environmental advantages together with the suggestion to a green aesthetics par excellence. In fact, the integration of vegetation in urban fabric plays an important role in improving ecological and environmental conditions of (and in) cities, although systems can have a high environmental burden. This paper aims to answer the question: Is greening the building envelope a sustainable design practice? To do so, the paper provides a literature review which includes the main research developed regarding environmental burden, benefits and LCA (life cycle assessment) calculations of green envelopes.
基金Funding Project for Academic and Technical Leaders in Major Disciplines of Jiangxi Province(20172BCB22011)Science and Technology Landing Project for Universities in Jiangxi Province(KJLD14033)+1 种基金Major Bidding Project for Economic and Social Development in Jiangxi Province(17ZD03)Science and technology Project of Jiangxi Education Department(GJJ160431)
文摘As the foundation of farm household structure,livelihood asset status is the basis for farmers to gain opportunities,adopt livelihood strategies,resist livelihood risk,and engage in positive livelihood achievements.Quantifying farm household assets identifies future development trends that are fundamentally necessary to predict farm household vulnerability and strategy,as well as understanding farmers’current living situations.Using Zunyi City in China’s western mountainous area as a case study,we conducted stratified sampling and participatory rural investigation appraisal to collect data on the attributes of farm households’livelihood assets and livelihood strategies to establish an index evaluation system and enable evaluation and analysis of farm households with different livelihood strategies.Our research indicates that due to structural differences,total livelihood assets of farm households with different livelihood strategies are similar.Rural households have an abundance of natural and material assets and deficiencies in human,financial and social assets.Non-rural households and part-time households are abundant in human,financial and social assets and deficient in natural and material assets.
基金Supported by fund for building world-class universities(disciplines) of Renmin University of China(2018)
文摘Habitat quality assessments are of great significance for protecting biodiversity.This study analyzes the changing habitat quality of Lashihai watershed based on SPOT satellite images.We extracted the land use data for Lashihai watershed in Yunnan province for the years 2000 and 2015,and then used an INVEST model to evaluate habitat degradation,habitat quality and habitat scarcity in the study area from 2000 to 2015.Spatial statistical methods were used to determine changes to spatial dynamics.Results indicate that the number of areas with habitat degradation was generally small,and that both the number of areas with habitat degradation and the degree of degradation had fallen noticeably during the fifteen-year study period.In general,the quality of habitats was main- tained or improved,while the quality of habitats decreased in only a few areas.The scarcity of habitats for cultivated land had increased,the tension between people and land use was relatively prominent.The reason habitat quality in Lashihai watershed has improved can be attributed to three factors:1)The policy of returning farmland to forests since 2000 has been well implemented and has achieved remarkable results.Loss of forests from logging and deforestation has basically been eliminated,and great progress has been made restoring the ecological environment.2)High background value of quality habitat suitability benefits from the research area's high vegetation coverage.3)The development of the local tourism economy has transformed the area's ecological advantages into an economic bonus,greatly increasing the income level and living standards of residents.At the same time,the ecological resource bonus has increased the enthusiasm of residents for ecological protection and has helped to promote the protection of local eco-systems,both reducing ecological degradation and improving habitat quality.At the same time,increasing conflicts between land and people should be addressed.Support is needed to promote development of the ecological economy while continuously reducing ecological degradation and further increasing residents'income.There must be less reliance on industry and less pressure on both land and people,all the while ensuring that the local economy and ecology can more forward together in a sustainable way.
基金supported by the National Natural Science Foundation of China(21672173,21372186)Research Fund for International Young Scientists from International(Regional)Cooperation and Exchange Program(81350110523)+1 种基金Chongqing Special Foundation for Postdoctoral Research Proposal(Xm2014127,Xm2016039)Fundamental Research Funds for the Central Universities(XDJK2016E059)
文摘A series of amino organophosphorus imidazoles were designed and synthesized as a novel structural type of antimicrobial agents.Bioactive evaluation in vitro showed that compound 3f exhibited equipotent or superior anti-methicillin-resistant Staphylococcus aureus(anti-MRSA) and anti-S. cerevisiae efficiencies(minimal inhibitory concentration(MIC)=2 μg/mL) to clinical drugs,and the combinations with antibacterial or antifungal drugs enhanced the antimicrobial efficiency. Highly active molecule 3f showed low propensity for bacteria to develop resistance, and the preliminary action mechanism studies demonstrated that 3f was membrane-active, but had no significant intercalation towards MRSA DNA. The computational study on 3f reasonably explained its high antimicrobial activity. Experimental data revealed that ground-state 3f-HSA complexes were formed mainly through hydrophobic interactions and hydrogen bonds with a spontaneous process, and the non-radioactive energy transfer from HSA to 3f occurred beyond F鰎ster resonance energy transfer theory. The participation of metal ions in 3f-HSA supramolucular system could increase the concentration of free compound 3f, and shorten its storage time and half-life in the blood to improve the maximum antimicrobial efficacy.
基金financially supported by the National Science&Technology Major Project(2009ZX09301-003-9-1)
文摘A novel series of diaryl urea derivatives bearing sulfonamide moiety have been designed and synthesized. Their in vitro antitumor effect against human cancer cell lines MX-1, A375, HepG2, Ketr3 and HT-29 was screened and evaluated by the standard MTT assay with sorafenib as the positive control. Some of the compounds showed significant inhibitory activity against multiple cell lines compared to sorafenib. In particular, 2,6-dimethyl-4-{6-[3-(4-chloro-3-(trifluoromethyl)phenyl)urealnaphthalen- 2-yllsulfonyl morpholine (10d) was found to be the most potent against A375, HepG2 and Ketr3 with ICs0 values of 0.65-0.97 μmol/L, which were 5-20-fold more potent than sorafenib. Compound 10d emerged as a valuable lead for further optimization.
基金supported by the National Natural Science Foundation of China (21172181,21372186)the Research Fellowship for International Young Scientists from the International (Regional) Cooperation and Exchange Program (81250110554,81350110338,81350110523)+1 种基金the key program from Natural Science Foundation of Chongqing (CSTC2012- jjB10026)the Specialized Research Fund for the Doctoral Program of Higher Education of China (20110182110007)
文摘A series of new benzimidazole derivatives was synthesized and characterized by IR,1H NMR,13C NMR,MS,and HRMS spectra.All the new compounds were screened for their antimicrobial activities in vitro by a twofold serial dilution technique.The bioactive evaluation showed that 3,5-bis(trifluoromethyl)phenyl benzimidazoles were comparably or even more strongly antibacterial and antifungal than the reference drugs Chloromycin,Norfloxacin,and Fluconazole.The combination of2,4-difluorobenzyl benzimidazole derivative 5l and its hydrochloride 7 respectively with the antibacterials Chloromycin,Norfloxacin,and the antifungal Fluconazole was more sensitive to methicillin-resistant MRSA and Fluconazole-insensitive A.flavus.In addition,the interaction of compound 5l with calf thymus DNA demonstrated that this compound could effectively intercalate into DNA to form a compound 5l-DNA complex that might block DNA replication and thereby exert good antimicrobial activity.
文摘Persuasive technology is the use of computers,devices or applications to change a person's attitudes or behavior.Persuasibility design within the system life-cycle is a nascent area of research which is different from design in the traditional method.This paper focuses on the research of persuasibility design and its assessment in the system life-cycle.A life-cycle oriented systemic general theory is developed in this paper to evaluate persuasibility design.Persuasibility assessment is considered as a part of persuasibility design.Its procedure and method are explored and analyzed based on the system life-cycle in this paper.A possible research direction is to create more explicit and detailed persuasion design and assessment methods which can be used not only in personal computer persuasive application,but also many other electric devices that are designed for persuasion purposes.