Design, synthesis and docking studies of new quinoline-3-carbohydrazide derivatives as antitubercular agents

Three new series of 4-hydroxy-8-trifluoromethyl-quinoline derivatives were synthesized through multi step reactions. All the newly synthesized compounds were characterized by spectral and elemental analyses. The structure of 5j was evidenced by X-ray crystallographic study. The newly synthesized title compounds were evaluated for their antimicrobial activities including antimycobacterial activity. Amongst the tested compounds, 5b, 5e, 5h, 5j, 6c and 7c displayed promising antimicrobial activity. The mode of action of these active compounds was carried out by docking of receptor enoyl-ACP reductase with newly synthesized candidate ligands, 5b, 5e, 5h, 5j and 6c. (C) 2011 Elsevier Masson SAS. All rights reserved.

Design, synthesis of some new (2-aminothiazol-4-yl)methylester derivatives as possible antimicrobial and antitubercular agents

A series of (2-aminothiazol-4-yl)methylester (5a-t) derivatives were synthesized in good yields and characterized by H-1 NMR, C-13 NMR, mass spectral and elemental analyses. The crystal structure of 5a was evidenced by X-ray diffraction study. The compounds were evaluated for their preliminary in vitro antibacterial, antifungal activity and were screened for antitubercular activity against Mycobacterium tuberculosis H37Rv strain. The synthesized compounds displayed interesting antimicrobial activity. (C) 2012 Elsevier Masson SAS. All rights reserved.

Design of an Escherichia coli expressed HIV-1 gp120 fragment Immunogen that binds to b12 and induces broad and potent neutralizing antibodies

b12, one of the few broadly neutralizing antibodies against HIV-1, binds to the CD4 binding site (CD4bs) on the gp120 subunit of HIV-1 Env. Two small fragments of HIV-1 gp120, b121a and b122a, which display about 70% of the b12 epitope and include solubility-enhancing mutations, were designed. Bacterially expressed b121a/b122a were partially folded and could bind b12 but not the CD4bs-directed non-neutralizing antibody b6. Sera from rabbits primed with b121a or b122a protein fragments and boosted with full-length gp120 showed broad neutralizing activity in a TZM-bl assay against a 16-virus panel that included nine Tier 2 and 3 viruses as well as in a five-virus panel previously designed to screen for broad neutralization. Using a mean IC50 cut-off of 50, sera from control rabbits immunized with gp120 alone neutralized only one virus of the 14 non-Tier 1 viruses tested (7%), whereas sera from b121a- and b122a-immunized rabbits neutralized seven (50%) and twelve (86%) viruses, respectively. Serum depletion studies confirmed that neutralization was gp120-directed and that sera from animals immunized with gp120 contained lower amounts of CD4bs-directed antibodies than corresponding sera from animals immunized with b121a/b122a. Competition binding assays with b12 also showed that b121a/2a sera contained significantly higher amounts of antibodies directed toward the CD4 binding site than the gp120 sera. The data demonstrate that it is possible to elicit broadly neutralizing sera against HIV-1 in small animals.

Design and synthesis of positional isomers of 5 and 6-bromo-1-(phenyl)sulfonyl]-2-(4-nitrophenoxy)methyl]-1H-benzimida zoles as possible antimicrobial and antitubercular agents

In this Letter, we report the structure activity relationship (SAR) studies on series of positional isomers of 5(6)-bromo-1-(phenyl)sulfonyl]-2-(4-nitrophenoxy)methyl]-1H-benzim idazoles derivatives 7(a-j) and 8(a j) synthesized in good yields and characterized by H-1 NMR, C-13 NMR and mass spectral analyses. The crystal structure of 7a was evidenced by X-ray diffraction study. The newly synthesized compounds were evaluated for their in vitro antibacterial activity against Staphylococcus aureus, (Gram-positive), Escherichia coil and Klebsiella pneumoniae (Gram-negative), antifungal activity against Candida albicans, Aspergillus flavus and Rhizopus sp. and antitubercular activity against Mycobacterium tuberculosis H37Rv, Mycobacterium smegmatis, Mycobacterium fortuitum and MDR-TB strains. The synthesized compounds displayed interesting antimicrobial activity. The compounds 7b, 7e and 7h displayed significant activity against Mycobacterium tuberculosis H37Rv strain.

Design of substrate-integrated lead-carbon hybrid ultracapacitor and experimental validation

Suitability of substrate-integrated lead-carbon hybrid ultracapacitors for low-power back-up applications is studied. A practical application that provides 30 W power back-up to low-power medical gadgets for use in grid-power-deficient rural areas is presented. An ultracapacitor bank is designed for this application and the sizing calculations are provided. Experimental validation and results are also discussed.

Design and Testing of a Control System for Supply Side Electrical Load Management

India's energy demand is increasing rapidly with the intensive growth of economy. The electricity demand in India exceeded the availability, both in terms of base load energy and peak availability. The efficient use of energy source and its conversion and utilizations are the viable alternatives available to the utilities or industry. There are essentially two approaches to electrical energy management. First at the supply / utility end (Supply Side Management or SSM) and the other at the consumer end (Demand Side Management or DSM). This work is based on Supply Side Management (SSM) protocol and consists of design, fabrication and testing of a control device that will be able to automatically regulate the power flow to an individual consumer's premise. This control device can monitor the overuse of electricity (above the connected load or contracted demand) by the individual consumers. The present project work specially emphasizes on contract demand of every consumer and tries to reduce the use beyond the contract demand. This control unit design includes both software and hardware work and designed for 0.5 kW contract demand. The device is tested in laboratory and reveals its potential use in the field.

Does audit improve quality in a hospital manufacturing unit?

OBJECTIVE - To establish whether auditing improves the overall quality of a hospital manufacturing unit. DESIGN - Continuous assessment of the quality level of a hospital manufacturing unit using 14 quality indicators over a nine-month period, and two periods of audit carried out towards the beginning and end of the assessment period. SETTING - The non-sterile manufacturing, sterile manufacturing and repackaging services areas at the pharmacy manufacturing unit at Queens Hospital, Burton-on- Trent. RESULTS - Compliance ratings for the second audit were better than those for the first audit, but there was no overall improvement in quality over the study period. CONCLUSION - Auditing probably improves compliance by focusing the minds of the staff involved, rather than by initiating a sustained improvement in overall quality.

Malnutrition and chemotherapy-induced nausea and vomiting : implications for practice

PURPOSE/OBJECTIVES: To determine the prevalence of malnutrition and chemotherapy-induced nausea and vomiting (CINV) limiting dietary intake in a chemotherapy unit. DESIGN Cross sectional descriptive audit. SETTING: Chemotherapy ambulatory care unit in an Australian teaching hospital. SAMPLE 121 patients receiving chemotherapy for malignancies, ≥18yrs and able to provide verbal consent. METHODS: An Accredited Practicing Dietitian collected all data. Chi-square tests were used to determine the relationship of malnutrition with variables and demographic data. MAIN RESEARCH VARIABLES: Nutritional status, weight change, BMI, prior dietetic input, CINV and CINV that limited dietary intake. FINDINGS Thirty one (26%) participants were malnourished, 12 (10%) had intake-limiting CINV, 22 (20%) reported significant weight loss and 20 (18%) required improved nutrition symptom management. High nutrition risk diagnoses, CINV, BMI and weight loss were significantly associated with malnutrition. Thirteen (35%) participants with malnutrition, significant weight loss, intake-limiting CINV and/or critically requiring improved symptom management reported no dietetic input; the majority of whom were overweight or obese. CONCLUSIONS: This audit determined over one quarter of patients receiving chemotherapy in this ambulatory setting were malnourished and the majority of patients reporting intake-limiting CINV were malnourished. IMPLICATIONS FOR NURSING Patients with malnutrition and/or intake-limiting CINV and in need of improved nutrition symptom management may be overlooked, especially patients who are overweight or obese - an increasing proportion of the Australian population. Evidence-based practice guidelines recommend implementing validated nutrition screening tools, such as the Malnutrition Screening Tool, in patients undergoing chemotherapy to identify those at risk of malnutrition requiring dietitian referral.

Pegasus Town : innovative marketing of a new property venture

Purpose – This paper aims to outline the challenges and tasks involved in a organising and marketing a new venture from conception to sales. It presents an interesting situation with which readers can identify and apply knowledge and skills associated with entrepreneurship and marketing and link this with the key learning objectives of a new venture marketing study unit. Design/methodology/approach – The case is constructed around key principles of marketing and entrepreneurship linked to a description of a contemporary venture written from a participant observer perspective supplemented with knowledge from interviews and archival research. Findings – The case shows how effective a diligent, creative approach to developing and selling a new venture can be. It demonstrates that effective marketing requires more than rote adoption of basic principles – it requires creative thinking and enterprising adaption of relevant principles to address the specific and well defined objectives of the venture. Research limitations/implications – The case is not intended to prescribe a particular marketing method or process; rather it is meant to stimulate creativity in the use of marketing knowledge and skills. Practical implications – The case represents an effective resource for both formal and informal teaching and learning. It demonstrates the requirement for innovative and creative adoption of marketing concepts to fit the demands of a new venture. Originality/value – The case specifically addresses an identified need for learning resources and information tailored to the area of entrepreneurial new venture marketing.

Journalling and public health education : thinking about reflecting

Purpose: The purpose of this research is to understand reflective journalling in a first year Public Health practice unit. Design/methodology/approach: This research uses pure phenomenography to interpret students descriptions of reflective journalling. Data was collected from thirty-two students enrolled in PUB215 Public Health Practice in the School of Public Health, Queensland University of Technology. Participants completed a brief open-ended questionnaire to evaluate the first assessment item in this unit, a Reflective Journal. Questionnaire responses were analysed through Dahlgren and Fallsberg’s (1991) seven phases of data analysis. Findings: The Reflective Journal required students to reflect on lecture content from five of seven guest speakers. Participants responses were categorised into four conceptions - 1) engagement in learning, 2) depth of knowledge, 3) understanding the process and 4) doing the task. Participants describe reflective journalling as a conduit to think critically about the content of the guest speakers presentations. Other participants think journalling is a vehicle to think deeply about their potential career pathways. Some define journalling as a pragmatic operation where practical issues are difficult to navigate. The Reflective Journal successfully a) engaged students learning, b) increased students depth of knowledge and c) deepened students understanding of the journalling process. Originality/value: This research gives an insight into how first year public health students understand reflective journalling, supports educators in reflective journalling assessments and confirms a Reflective Journal assessment can move student reflection towards higher order thinking about practice.

International students’ experiences of informed learning : a pedagogical case study

This case study explores the theory and practice of informed learning (Bruce, 2008) in a culturally diverse higher education context. It presents research findings about learning and teaching in a postgraduate unit of study entitled Personalised Language Development, an elective in the Master of TESOL and TEFL programs at Queensland University of Technology (QUT). This unit aims to enable international students to extend their disciplinary knowledge of English language teaching, their academic and linguistic fluency and awareness of their own information using processes. The paper outlines the case study research approach; describes the design and implementation of the unit; demonstrates how informed learning principles and characteristics underpin the unit design; presents findings about the international students’ experiences of informed learning through their reflections; and finally the paper discusses the implications of the findings for educators, including the potential transferability of informed learning across higher education disciplines.

Using real-time authentic online learning scenarios to teach criminal intelligence

Criminal intelligence is an area of expertise highly sought-after internationally and within a variety of justice-related professions; however, producing university graduates with the requisite professional knowledge, as well as analytical, organisational and technical skills presents a pedagogical and technical challenge to university educators. The situation becomes even more challenging when students are undertaking their studies by distance education. This best practice session showcases the design of an online undergraduate unit for final year justice students which uses an evolving real-time criminal scenario as the focus of authentic learning activities in order to prepare students for graduate roles within the criminal intelligence and justice professions. Within the unit, students take on the role of criminal intelligence analysts, applying relevant theories, models and strategies to solve a complex but realistic crime and complete briefings and documentation to industry standards as their major summative assessment task. The session will demonstrate how the design of the online unit corresponds to authentic learning principles, and will specifically map the elements of the unit design to Herrington & Oliver’s instructional design framework for authentic learning (2000; Herrington & Herrington 2006). The session will show how a range of technologies was used to create a rich learning experience for students that could be easily maintained over multiple unit iterations without specialist technical support. The session will also discuss the unique pedagogical affordances and challenges implicated in the location of the unit within an online learning environment, and will reflect on some of the lessons learned from the development which may be relevant to other authentic online learning contexts.

Using real-time authentic online learning scenarios to teach criminal intelligence : presentation

Criminal intelligence is an area of expertise highly sought-after internationally and within a variety of justice-related professions; however, producing university graduates with the requisite professional knowledge, as well as analytical, organisational and technical skills presents a pedagogical and technical challenge to university educators. The situation becomes even more challenging when students are undertaking their studies by distance education. This best practice session showcases the design of an online undergraduate unit for final year justice students which uses an evolving real-time criminal scenario as the focus of authentic learning activities in order to prepare students for graduate roles within the criminal intelligence and justice professions. Within the unit, students take on the role of criminal intelligence analysts, applying relevant theories, models and strategies to solve a complex but realistic crime and complete briefings and documentation to industry standards as their major summative assessment task. The session will demonstrate how the design of the online unit corresponds to authentic learning principles, and will specifically map the elements of the unit design to Herrington & Oliver’s instructional design framework for authentic learning (2000; Herrington & Herrington 2006). The session will show how a range of technologies was used to create a rich learning experience for students that could be easily maintained over multiple unit iterations without specialist technical support. The session will also discuss the unique pedagogical affordances and challenges implicated in the location of the unit within an online learning environment, and will reflect on some of the lessons learned from the development which may be relevant to other authentic online learning contexts.

Autonomous greenhouse gas sampling using multiple robotic boats

Accurately quantifying total greenhouse gas emissions (e.g. methane) from natural systems such as lakes, reservoirs and wetlands requires the spatial-temporal measurement of both diffusive and ebullitive (bubbling) emissions. Traditional, manual, measurement techniques provide only limited localised assessment of methane flux, often introducing significant errors when extrapolated to the whole-of-system. In this paper, we directly address these current sampling limitations and present a novel multiple robotic boat system configured to measure the spatiotemporal release of methane to atmosphere across inland waterways. The system, consisting of multiple networked Autonomous Surface Vehicles (ASVs) and capable of persistent operation, enables scientists to remotely evaluate the performance of sampling and modelling algorithms for real-world process quantification over extended periods of time. This paper provides an overview of the multi-robot sampling system including the vehicle and gas sampling unit design. Experimental results are shown demonstrating the system’s ability to autonomously navigate and implement an exploratory sampling algorithm to measure methane emissions on two inland reservoirs.

基于FPGA高速并行FFT处理器设计与实现

在研究快速傅里叶变换(FFT)算法的基础上,根据FPGA性能高、灵活性强、速度快的特点,提出了高效的基4-FFT处理器的实现方法。数据存储采用分块存储的方法,大大提高了存取速度。数据寻址采用新型的地址产生方法,可并行产生所需数据地址。同时,在蝶形单元的设计中很好的将并行运算技术和流水线技术相结合了起来,又进一步提高了运算速度。测试结果表明,时钟在50MHz时完成1024点FFT的时间为25.6μs,满足了应用实时性的要求。