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Showing result 1 - 5 of 16 swedish dissertations matching the above criteria.

  1. 1. Design and Synthesis of Hepatitis C Virus NS3 Protease Inhibitors Incorporating a P2 Cyclopentane-Derived Scaffold

    Author : Marcus Bäck; Anja Sandström; Linköpings universitet; []
    Keywords : NATURVETENSKAP; NATURAL SCIENCES; HCV; NS3 protease; Proline mimic; Cyclopentane-derived scaffold; Linear inhibitors; Macrocyclic inhibitors; Organic synthesis; Organisk syntes;

    Abstract : This thesis describes the design, synthesis and structure-activity relationships analysis of potential inhibitors targeting the hepatitis C virus (HCV) NS3 protease. Also discussed is the disease caused by HCV infection and the class of enzymes known as proteases. READ MORE

  2. 2. Novel Procedures for Identification and Characterization of Viral Proteases Inhibitors

    Author : Angelica Ehrenberg; Helena Danielson; Celia Schiffer; Uppsala universitet; []
    Keywords : NATURVETENSKAP; NATURAL SCIENCES; drug discovery; viral proteases; inhibitors; Hepatitis C; NS3; cytomegalovirus; Biokemi; Biochemistry;

    Abstract : Viral proteases are often considered to be attractive drug targets because of their crucial function in the viral replication machinery. In order to increase our knowledge of these important targets and to contribute to the discovery and development of new antiviral drugs, the proteases from hepatitis C virus (HCV) and human cytomegalovirus (HCMV) have been produced and their interactions with inhibitors and fragments have been characterized, using enzyme inhibition and SPR biosensor based interaction assay. READ MORE

  3. 3. Discovery of Novel Macrocyclic Ligands for Difficult Targets : Applications to Natural Product Derived Keap1 Inhibitors

    Author : Fabio Begnini; Jan Kihlberg; Anders Bach; Uppsala universitet; []
    Keywords : NATURVETENSKAP; NATURAL SCIENCES; Macrocycles; Keap1-Nrf2; Protein-protein interactions; Natural products;

    Abstract : The development of small-molecule ligands for biological targets that possess large, featureless or highly polar binding sites is a challenging task. This thesis is focused on a novel lead generation strategy to identify macrocyclic ligands for difficult-to-drug targets, as well as on the relationship between cell permeability and the conformations of macrocycles. READ MORE

  4. 4. Development of Novel Macrocyclic Inhibitors of Protein-Protein Interactions : Applied to the Keap1-Nrf2 Complex

    Author : Fabio Begnini; Uppsala universitet; []
    Keywords : NATURVETENSKAP; NATURAL SCIENCES; Chemistry with specialization in Organic Chemistry; Kemi med inriktning mot organisk kemi;

    Abstract : .... READ MORE

  5. 5. Design and Synthesis of Serine and Aspartic Protease Inhibitors

    Author : Fredrik Wångsell; Ingemar Kvarnström; Olle Karlsson; Linköpings universitet; []
    Keywords : NATURVETENSKAP; NATURAL SCIENCES; organic chemistry; organic synthesis; metathesis; HCV; NS3; protease; proline isosteres; inhibitor; aspartic protease inhibitors; hydroxyethylene; Organic synthesis; Organisk syntes;

    Abstract : This thesis describes the design and synthesis of compounds that areintended to inhibit serine and aspartic proteases. The first part of the text deals with preparation of inhibitors of the hepatitis C virus (HCV) NS3 serine protease. Hepatitis C is predominantly a chronic disease that afflicts about 170 million people worldwide. READ MORE