Search for dissertations about: "läkemedelskemi"

Showing result 1 - 5 of 203 swedish dissertations containing the word läkemedelskemi.

  1. 1. Inhibitors Targeting Insulin-Regulated Aminopeptidase (IRAP) : Identification, Synthesis and Evaluation

    Author : Karin Engen; Mats Larhed; Mikael Elofsson; Uppsala universitet; []
    Keywords : MEDICAL AND HEALTH SCIENCES; MEDICIN OCH HÄLSOVETENSKAP; MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; compound screening; insulin-regulated aminopeptidase; IRAP; inhibitors; cognitive disorders; spiro-oxindole; quinazolinone; imidazopyridine; medicinal chemistry; structure-activity relationship; microwave heating; Medicinal Chemistry; Läkemedelskemi;

    Abstract : Insulin-regulated aminopeptidase (IRAP) has emerged as a potential new therapeutic target for treatment of cognitive disorders. Inhibition of the enzymatic activity facilitates cognition in rodents. READ MORE

  2. 2. Ligands of the Angiotensin II Type 2 Receptor : Exploring structure and function of the AT2R ligand C38

    Author : Rebecka Isaksson; Mats Larhed; Annette Bayer; Uppsala universitet; []
    Keywords : MEDICAL AND HEALTH SCIENCES; MEDICIN OCH HÄLSOVETENSKAP; MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Angiotensin II type 2 receptor; AT2R antagonists; sulfonyl carbamates; bicyclic amides; metabolic stability; functional activity assay; pharmacological profile; medicinal chemistry; structure-activity relationship; Medicinal Chemistry; Läkemedelskemi;

    Abstract : The renin-angiotensin-aldosterone-system (RAAS) control blood-pressure regulation, exerted by the main effector peptide angiotensin II (AngII) binding the angiotensin II type 1 receptor (AT1R). While hypertension is the most known disease caused by over-activity in RAAS, several proteins in the system exhibit protective functions. READ MORE

  3. 3. 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 : MEDICAL AND HEALTH SCIENCES; MEDICIN OCH HÄLSOVETENSKAP; NATURAL SCIENCES; NATURVETENSKAP; NATURVETENSKAP; MEDICIN OCH HÄLSOVETENSKAP; NATURAL SCIENCES; MEDICAL AND HEALTH 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. 4. 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 : MEDICAL AND HEALTH SCIENCES; MEDICIN OCH HÄLSOVETENSKAP; 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

  5. 5. 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 : MEDICAL AND HEALTH SCIENCES; MEDICIN OCH HÄLSOVETENSKAP; 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