Design, synthesis, docking studies and monoamine oxidase inhibition of a small library of 1-acetyl- and 1-thiocarbamoyl-3,5-diphenyl-4,5-dihydro-(1h)-pyrazoles

New N-acetyl/N-thiocarbamoylpyrazoline derivatives were designed and synthesized in high yields to assess their inhibitory activity and selectivity against human monoamine oxidase A and B. The most important chiral compounds were separated into their single enantiomers and tested. The impact of the substituents at N1, C3 and C5 positions as well the influence of the configuration of the C5 on the biological activity were analyzed. Bulky aromatic groups at C5 were not tolerated. p-Prenyloxyaryl moiety at C3 oriented the selectivity toward the B isoform. The results were also corroborated by molecular modelling studies providing new suggestions for the synthesis of privileged structures to serve as lead compounds for the treatment of mood disorders and neurodegenerative diseases

A contextual analysis of cycling environment assessment tools in a Cape Town mobility corridor

Building on recent research on barriers to cycling mobility in low-income South African contexts, this study explored the role of the built environment as a determinant of cycling practices along a mobility corridor in Cape Town, South Africa. The communities surveyed reflect the demographic and income disparities of the city, and their attitudes to cycling and the cycling environment both corroborate existing findings and pose new research questions. In particular, respondents of all income levels showed that they distorted their own journeys by bicycle to avoid areas perceived to have a high risk of criminal activity, even where this meant using routes perceived to present a high risk of physical injury. A second finding was that all road users engage in informal road behaviour, including motorists, and that this is an integral aspect of the study area's mobility culture. The methods used in this study were a series of interviews with three community bicycle-shop owners, supported by focus groups held in each community, and accompanied by a mapping exercise. Fieldwork took the form of accompaniment of youth cycling initiatives and observation of commuting practices by the author. The data obtained in fieldwork were then used to evaluate a selection of cycling environment assessment tools from the USA, UK and Australia, and a pedestrian environment assessment tool from South Africa, in order to evaluate their contextual appropriateness for the local determinants of cycling. The study concludes with recommendations towards a South African cycling environment assessment tool that would capacitate local government and civil society to deliver improvements to the cycling environment and capitalise on existing pro-cycling policies

Westerse teks, Alexandrynse teks en die oorspronklike teks van die Nuwe Testament: Is daar ’n oplossing vir die probleem?

Western text, Alexandrian text and the original text of the New Testament - is there a solution to the problem?This article discusses the debate concerning the problems of the so-called Western text in New Testament textual criticism. Traditional views, such as those of Westcott & Hort, Ropes, Metzger, Blass, Clark, and Boismard & Lamouille, all work with the notion of early local text-types. Because of this none of these ap proaches seems able to solve the problem. In contrast, a fresh approach to the history of the text in general and this problem in particular is developing in Munster. This approach describes the earliest history of the text in terms of ‘qualitative’ text-types and might therefore have the potential to solve the riddle of the Western text

Die betroubaarheid van die Nuwe Testament vanuit 'n tekskritiese oogpunt

The reliability of the New Testament from a text-critical point of view In this article the present and past state of the text of the Greek New Testament is subjected to evaluation, with the purpose of determining the reliability of the text for exegesis and translation. The subject is approached historically and centers around the discussion of the Textus Receptus, the text of Westcott and Hort and the latest editions of The Greek New Testament by the United Bible Societies, together with the 26th edition of the Nestle-Aland series of texts. A judgement is also made as to possible alternatives for the above-mentioned texts and the claims of other methodological groups are put to the test. A final conclusion as to the reliability of the text is followed by an attempt to discuss the consequences of the conclusions for the general use of the Greek New Testament

Developing long-term energy and carbon emission modelling for the operational activities of ports: A case study of Fremantle Ports

The port and maritime industry contributes significantly to global greenhouse gas emissions. As such, there is increasing pressure for ports to decarbonise their operations. Despite the availability of multiple port carbon inventory and emission reduction guidance documents, no published methodologies currently exist for the development of port energy consumption and carbon emission forecasting. To fill this information gap, a methodology was developed through the review and experimentation with established forecasting techniques. The ‘ISCA’ Base Case Approach was adopted as a scaffolding for model development, largely to test the usability of the approach, currently in pilot. The approach consists of a baseline scenario and an ‘actual case’ scenario. A combination of qualitative, quantitative - time series and quantitative - causal modelling techniques were incorporated into the methodology. Linear and non-linear regression analysis curve-fitting techniques were selected as the most appropriate time-series modelling method for long-term energy and emissions projections, with simple linear regression analysis used for causal models. The methodology was tested through its application in a case study for Fremantle Ports. As a result of obligations from the state government to reach net-zero emissions by 2050, Fremantle Ports required the development of long-term energy consumption and carbon emission projections for its internal operations and container terminals to 2050. Using a bottom-up strategy, categorising energy consumption and greenhouse gas emissions by trade type, energy type and facility, the methodology successfully developed long-term energy and emissions projections. As per this modelling, energy consumption at Fremantle Ports is expected to increase 53% under the baseline scenario and 46.5% under the actual case scenario (Figure 1). Despite increases of energy consumption at the port, greenhouse gas emissions are expected to decrease 71% and 74% under the baseline and actual case scenarios, respectively (Figure 2). These drastic emissions reductions are predominantly the result of projected scope 2 emission factor decreases as grid renewable electricity generation capacity increases. The usability of the ISCA Base Case Approach for energy and emissions modelling was found to be adequate, although issues were experienced distinguishing constant and variable energy use. Additionally, it is recommended that a third scenario is incorporated into the approach

4-(3-Nitrophenyl)thiazol-2-ylhydrazone derivatives as antioxidants and selective hMAO-B inhibitors: synthesis, biological activity and computational analysis

A new series of 4-(3-nitrophenyl)thiazol-2-ylhydrazone derivatives were designed, synthesised, and evaluated to assess their inhibitory effect on the human monoamine oxidase (hMAO) A and B isoforms. Different (un)substituted (hetero)aromatic substituents were linked to N1 of the hydrazone in order to establish robust structure–activity relationships. The results of the biological testing demonstrated that the presence of the hydrazothiazole nucleus bearing at C4 a phenyl ring functionalised at the meta position with a nitro group represents an important pharmacophoric feature to obtain selective and reversible human MAO-B inhibition for the treatment of neurodegenerative disorders. In addition, the most potent and selective MAO-B inhibitors were evaluated in silico as potential cholinesterase (AChE/BuChE) inhibitors and in vitro for antioxidant activities. The results obtained from molecular modelling studies provided insight into the multiple interactions and structural requirements for the reported MAO inhibitory properties

Don’t shoot the messenger: The enigmatic impact of conveying bad news during redundancy situations and how to limit the impact

.“Redundancy envoys,” the managers and HR Professionals that break bad news to staff about job losses are key to the effectiveness of an organisation’s redundancy programme. If they suffer a bad experience dealing with the change – and are not properly looked after - it can hamper an organisation’s chances of benefits being realised. A paper submitted to the CIPD’s Applied Research Conference 2020 says redundancy envoys – a job that can fall to those in critical leadership roles such as directors, managers or HR professionals – can suffer considerable psychological damage. They carry the burden of “activities such as the strategy, planning, process, implementation, communication and consultations associated with redundancies, as well as dealing with the aftermath,” explains author Dr Madeleine Petzer, senior lecturer HRM at Liverpool John Moores University. As such, it can take its toll on their emotional wellbeing triggering feelings such as guilt, fear, anger or frustration. Even worse, redundancy envoys can suffer sleepless nights and high stress levels resulting in the need for therapy or medication, and even leading to long-term absences and resignations, says the paper, Don’t shoot the messenger: The enigmatic impact of conveying bad news during redundancy situations. Despite these negative experiences, redundancy envoys are still relied upon by employers to boost engagement and motivation during a time of profound change, adds the study. Petzer argues that “with the rate of redundancies on an upward spiral” (now even more heightened amid the outbreak of Covid-19) it is imperative that organisations understand the “idiosyncrasy” of this group of people. Her research involved 36 interviews with Business directors, HR professionals, Line managers and Employee representatives as well as collecting data from a private sector organisation that underwent a redundancy programme, using four different redundancy models over four years. Results highlighted that redundancy envoys suffered a “rollercoaster of emotions”. Interestingly, directors and line managers were more prone to experiencing guilt than HR professionals. Overall, the psychological effects on all redundancy envoys had repercussions for their organisations – it curbed managers’ productivity and their ability to function effectively. Even more significantly, it led to emotional detachment reducing their effectiveness in leading and driving a programme of organisational change. “Organisations need to appreciate that the very people they ask to run their business are being put under undue stress by implementing redundancies,” says the study. It urges employers to put tailored support strategies and training in place to mitigate the negative experiences of redundancy envoys during restructure programmes. Organisations must understand the particular emotions being experienced, guilt or fear, for example, and respond with appropriate interventions

COVID-19: How to reduce stress and maintain a work-life balance while working from home

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