Sökning: "Thrombin-inhibitors"

Visar resultat 6 - 10 av 13 avhandlingar innehållade ordet Thrombin-inhibitors.

  1. 6. Early assessment of efficacy and safety of novel anticoagulants as exemplified by direct thrombin inhibitors. Non-clinical pharmacodynamic studies in vitro and in vivo

    Författare :Margareta Elg; Göteborgs universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; animals; antidote; bleeding; inhibition constant; inogatran; association rate constant; melagatran; thrombin inhibitor; thrombosis; fibrinolysis;

    Sammanfattning : The drawbacks of today's anticoagulants are parenteral use (heparins), a narrow interval between efficacy and bleeding, and the high variability of effect with a consequent need for frequent monitoring (coumarins). The aim of the current studies was to evaluate properties important for efficacy and safety of novel anticoagulants, as exemplified by direct thrombin inhibitors, with non-clinical methods. LÄS MER

  2. 7. Synthesis of β-turn and pyridine based peptidomimetics

    Författare :David Blomberg; Jan Kihlberg; Kay Brickmann; Torbjörn Frejd; Umeå universitet; []
    Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; Peptidomimetics; beta-turn; beta-strand; pyridine scaffold; Grignard exchange reaction; SNAr reaction; thrombin inhibitor; Leu-enkephalin.; Organic synthesis; Organisk syntes;

    Sammanfattning : Despite the unfavorable pharmacokinetic properties associated with peptides, they are still of great interest in drug development due to a multitude of interesting biological functions. The development of peptidomimetics strives to maintain or improve the biological activity of a peptide concurrently with removing the unwanted properties. LÄS MER

  3. 8. Structure-Based Design and Synthesis of Protease Inhibitors Using Cycloalkenes as Proline Bioisosteres and Combinatorial Syntheses of a Targeted Library

    Författare :Fredrik Thorstensson; Ingemar Kvarnström; Charles Hedgecock; Linköpings universitet; []
    Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; organic chemistry; organic synthesis; combinatorial synthesis; metathesis; olefin metathesis; thrombin; HCV; NS3; protease; proline isosteres; inhibitor; Organic synthesis; Organisk syntes;

    Sammanfattning : Structure-based drug design and combinatorial chemistry play important roles in the search for new drugs, and both these elements of medicinal chemistry were included in the present studies. This thesis outlines the synthesis of protease inhibitors against thrombin and the HCV NS3 protease, as well as the synthesis of a combinatorial library using solid phase chemistry. LÄS MER

  4. 9. Design, Synthesis, and Structure-Activity Relationships Analysis of Potential Inhibitors of the Serine Protease Thrombin and the Malarial Aspartic Proteases Plasmepsin I and II

    Författare :Anders Dahlgren; Thomas Olsson; Linköpings universitet; []
    Nyckelord :NATURVETENSKAP; NATURAL SCIENCES;

    Sammanfattning : The design, synthesis, and structure-activity relationships analysis of some potential protease inhibitors are outlined in this thesis. In particular, the serine protease thrombin and the malarial aspartic proteases plasmepsin I and II (Plm I and II) are described in regard to the roles they play in living organisms, and that is followed by discussions concerning the design, synthesis, and biological test results of inhibitors of these enzymes. LÄS MER

  5. 10. Thrombin/ADP-induced platelet activation and drug intervention

    Författare :Nylander Sven; Stan Heptinstall; Linköpings universitet; []
    Nyckelord :MEDICINE; MEDICIN;

    Sammanfattning : Blood platelets are key players in haemostasis, the system that maintains an intact circulation. Circulating platelets are constantly on guard for vessel wall injury and will momentarily adhere to exposed subendothelial proteins, mainly collagens, at site of the injury. LÄS MER