Search for dissertations about: "Institutionen för läkemedelskemi."

Showing result 1 - 5 of 120 swedish dissertations containing the words Institutionen för läkemedelskemi..

  2. 1. Development of HIV-1 Protease Inhibitors and Palladium-Catalyzed Synthesis of Aryl Ketones and N-Allylbenzamides

    Author : Linda Axelsson; Mats Larhed; Anders Karlén; Luke Odell; Morten Grötli; Uppsala universitet; []
    Keywords : MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; NATURVETENSKAP; NATURAL SCIENCES; palladium; aminocarbonylation; aryl ketones; decarboxylation; HIV; protease inhibitor; tertiary alcohol; macrocycles; Medicinal Chemistry; Läkemedelskemi;

    Abstract : The use of palladium-catalyzed reactions to introduce new carbon-carbon bonds is a fundamental synthetic strategy that has been widely embraced due to its high chemo- and regioselectivity and functional group tolerance. In this context, Pd(0)-catalyzed aminocarbonylations using Mo(CO)6 instead of toxic and gaseous CO and with allylamine as the nucleophile were investigated. READ MORE

  4. 2. PET imaging of beta-cell mass

    Author : Pierre Cheung; Olof Eriksson; Weibo Cai; Uppsala universitet; []
    Keywords : MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; PET imaging; diabetes; beta-cell mass; affibody; SC-islets; Medicinal Chemistry; Läkemedelskemi;

    Abstract : A hallmark of diabetes is the progressive loss of the beta-cell mass (BCM) and function. Most of the diagnostic methods for diabetes are mostly reflective of the beta-cell function, whereas current methodologies for studying the beta-cell mass are limited to post-mortem biopsies or highly invasive methods. READ MORE

  5. 3. Discovery of Small Peptides and Peptidomimetics Targeting the Substance P 1-7 Binding Site : Focus on Design, Synthesis, Structure-Activity Relationships and Drug-Like Properties

    Author : Rebecca Fransson; Anja Sandström; John S Svendsen; Uppsala universitet; []
    Keywords : MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; substance P 1-7; peptidomimetics; structure-activity relationship; drug-like properties; phenylalanine; imidazole; MAP aryl amides; carbonylation; Pharmaceutical chemistry; Farmaceutisk kemi; Medicinal Chemistry; Läkemedelskemi;

    Abstract : Biologically active peptides are important for many physiological functions in the human body and therefore serve as interesting starting points in drug discovery processes. In this work the neuropeptide substance P 1–7 (SP1–7, H-Arg-Pro-Lys-Pro-Gln-Gln-Phe-OH), which has been demonstrated to reduce neuropathic pain and attenuate opioid withdrawal symptoms in animal models, has been addressed in a medicinal chemistry program with the overall aim of transforming this bioactive peptide into more drug-like compounds. READ MORE

  6. 4. Development of Substance P 1–7 Related Peptides and Peptidomimetics : Targeting Neuropathic Pain

    Author : Anna Skogh; Anja Sandström; Christian Sköld; Rebecca Fransson; Philip Thompson; Uppsala universitet; []
    Keywords : MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Substance P 1–7; Peptidomimetics; Solid-phase Peptide Synthesis SPPS ; Palladium catalysis; Carbonylation; Imidazole; Bioisostere; Neuropathic pain; Allodynia; Structure-activity relationships; Medicinal Chemistry; Läkemedelskemi;

    Abstract : The neuropeptide substance P 1–7 (SP1–7, H-Arg1-Pro2-Lys3-Pro4-Gln5-Gln6-Phe7-OH) and its amidated analogue SP1–7 amide, have displayed intriguing effects in experimental models for neuropathic pain acting on a specific, yet unknown SP1–7 target. The aim of this thesis was to design and synthesise SP1–7 related peptides and peptidomimetics, to be used as research tools to study the SP1–7 system, and to serve as drug leads in the neuropathic pain area. READ MORE

  7. 5. Regioselective Heck Coupling Reactions : Focus on Green Chemistry

    Author : Karl S. A. Vallin; Anders Hallberg; Mats Larhed; Walter Cabri; Uppsala universitet; []
    Keywords : MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Pharmaceutical chemistry; Farmaceutisk kemi; Pharmaceutical chemistry; Farmaceutisk kemi; Medicinal Chemistry; läkemedelskemi;

    Abstract : Carbon-carbon bond formation reactions are among the most important processes in chemistry, as they represent key steps in the synthesis of more complex molecules from simple precursors. This thesis describes mainly the development of novel regioselective applications of the mild and versatile palladium-catalyzed carbon-carbon coupling method, commonly known as the Heck reaction. READ MORE