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Sökning: WFRF:(Bergström Sven G)

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  • Kulén, Martina, et al. (författare)
  • Methyl sulfonamide substituents improve the pharmacokinetic properties of bicyclic 2-pyridone based Chlamydia trachomatis inhibitors
  • 2019
  • Ingår i: MedChemComm. - : Royal Society of Chemistry. - 2040-2503 .- 2040-2511. ; 10:11, s. 1966-1987
  • Tidskriftsartikel (refereegranskat)abstract
    • Chlamydia trachomatis infections are a global health problem and new approaches to treat C. trachomatis with drugs of high specificity would be valuable. A library of substituted ring fused 2-pyridones has been synthesized and evaluated for their ability to attenuate C. trachomatis infectivity. In vivo pharmacokinetic studies were performed, with the best candidates demonstrating that a C8-methylsulfonamide substituent improved pharmacokinetic properties important for oral administration. C8-Methyl sulfonamide analogue 30 inhibited C. trachomatis infectivity in low micromolar concentrations. Further pharmacokinetic evaluation at an oral dose of 10 mg kg(-1) showed an apparent bioavailability of 41%, compared to C8-cyclopropyl and -methoxy analogues which had negligible oral uptake. In vitro ADME (absorption, distribution, metabolism and excretion) testing of solubility and Caco-2 cell permeability revealed that both solubility and permeability is greatly improved with the C8-methyl sulfonamide 30, effectively moving it from BCS (Biopharmaceutical Classification System) class IV to II.
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  • Bergström, Gunnar, Professor, et al. (författare)
  • Reliability and factor structure of the Multidimensional Pain Inventory--Swedish Language Version (MPI-S).
  • 1998
  • Ingår i: Pain. - : LWW. - 0304-3959 .- 1872-6623. ; 75:1, s. 101-10
  • Tidskriftsartikel (refereegranskat)abstract
    • The psychological assessment of chronic pain is often accomplished using questionnaires such as the (West Haven-Yale) Multidimensional Pain Inventory ((WHY)MPI) which is constructed to capture the multidimensionality of chronic pain. The (WHY)MPI theoretically originates from behavioural and cognitive behavioural theories of pain. It is divided into three parts and measures psychosocial and behavioural consequences of pain. This questionnaire has displayed satisfactory psychometric properties and translations of the original English version into German and Dutch have been demonstrated to be reliable and valid. The aim of this study was to test the reliability and factor structure of a Swedish translation of the (WHY)MPI, the MPI-S, and also to test the generalisability of the factor structure found for the (WHY)MPI. We performed analyses of internal consistency using Cronbach's alpha, and carried out a confirmatory factor analysis (CFA) employing LISREL-8 on a population of 682 patients suffering from chronic musculoskeletal pain. Test-retest analysis was accomplished on a sub-sample of 54 individuals taken from the aforementioned population. For sections 1 and 2 of the MPI-S the overall reliability and stability were good, and after the exclusion of four items, the factor structure was similar to other versions of the MPI. For section 3, despite removal of five questions, the proposed factor structure could not be replicated. This part of the inventory is designed to measure the extent of different types of activities, and our results suggest that this section may only be used for assessing general activity level. We conclude that, with a few adjustments, the analyses yielded satisfactory results for sections 1 and 2 of the MPI-S regarding its factor structure, reliability and generalisability. For section 3 the hypothesised factor structure could not be confirmed.
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