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  • Molecular Diversity Preservation International  (3)
  • 2015-2019  (3)
  • 2019  (3)
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  • 2015-2019  (3)
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  • 1
    Publication Date: 2019-10-22
    Description: Non-invasive imaging of cyclooxygenase-2 (COX-2) by radiolabeled ligands is attractive for the diagnosis of cancer, and novel highly affine leads with optimized pharmacokinetic profile are of great interest for future developments. Recent findings have shown that methylsulfonyl-substituted (dihydro)pyrrolo[3,2,1-hi]indoles represent highly potent and selective COX-2 inhibitors but possess unsuitable pharmacokinetic properties for radiotracer applications. Based on these results, we herein present the development and evaluation of a second series of sulfonamide-substituted (dihydro)pyrrolo[3,2,1-hi]indoles and their conversion into the respective more hydrophilic N-propionamide-substituted analogs. In comparison to the methylsulfonyl-substituted leads, COX inhibition potency and selectivity was retained in the sulfonamide-substituted compounds; however, the high lipophilicity might hinder their future use. The N-propionamide-substituted analogs showed a significantly decreased lipophilicity and, as expected, lower or no COX-inhibition potency. Hence, the N-(sulfonyl)propionamides can be regarded as potential prodrugs, which represents a potential approach for more sophisticated radiotracer developments.
    Electronic ISSN: 1420-3049
    Topics: Chemistry and Pharmacology
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  • 2
    Publication Date: 2019-07-13
    Description: Mobile gait analysis systems using wearable sensors have the potential to analyze and monitor pathological gait in a finer scale than ever before. A closer look at gait in Parkinson’s disease (PD) reveals that turning has its own characteristics and requires its own analysis. The goal of this paper is to present a system with on-shoe wearable sensors in order to analyze the abnormalities of turning in a standardized gait test for PD. We investigated turning abnormalities in a large cohort of 108 PD patients and 42 age-matched controls. We quantified turning through several spatio-temporal parameters. Analysis of turn-derived parameters revealed differences of turn-related gait impairment in relation to different disease stages and motor impairment. Our findings confirm and extend the results from previous studies and show the applicability of our system in turning analysis. Our system can provide insight into the turning in PD and be used as a complement for physicians’ gait assessment and to monitor patients in their daily environment.
    Electronic ISSN: 1424-8220
    Topics: Chemistry and Pharmacology , Electrical Engineering, Measurement and Control Technology
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  • 3
    Publication Date: 2019-12-30
    Description: Population growth in cities leads to high raw material consumption and greenhouse gas emissions. In temperate climates were heating of buildings is among the major contributors to greenhouse gases, thermal insulation of buildings became a standard in recent years. Both population growth and greenhouse gas mitigation may thus have some influence on the quantity and composition of building material stock in cities. By using the case study of Vienna, this influence is evaluated by calculating the stock of major building materials (concrete, bricks, mortar, and plaster, steel, wood, glass, mineral wool, and polystyrene) between the years 1990 and 2015. The results show a growth of the material stock from 274 kt in the year 1990 to 345 kt in the year 2015, resulting in a total increase of 26%. During the same period, the population grew by 22%. On a material level, the increase of thermal insulation materials like polystyrene and mineral wool by factors of 6.5 and 2.5 respectively were much higher than for other materials, indicating energy efficiency and greenhouse gas mitigation in the building construction sector. The displacement of brickwork by concrete as the most important construction material, however, is rather a response to population growth as concrete buildings can be raised faster. A question for the future is to which extent this change from brickwork to high carbon-intensive concrete countervails the achievements in greenhouse gas reduction by thermal insulation.
    Electronic ISSN: 2071-1050
    Topics: Energy, Environment Protection, Nuclear Power Engineering
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