Sökning: "läkemedelskemi"

Visar resultat 6 - 10 av 228 avhandlingar innehållade ordet läkemedelskemi.

1. 6. 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

   Författare :Rebecca Fransson; Anja Sandström; John S Svendsen; Uppsala universitet; []
   Nyckelord :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;

   Sammanfattning : 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. LÄS MER

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

   Författare :Anna Skogh; Anja Sandström; Christian Sköld; Rebecca Fransson; Philip Thompson; Uppsala universitet; []
   Nyckelord :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;

   Sammanfattning : 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. LÄS MER

4. 8. Regioselective Heck Coupling Reactions : Focus on Green Chemistry

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

   Sammanfattning : 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. LÄS MER

5. 9. Design and Synthesis of Aspartic and Serine Protease Inhibitors : Targeting the BACE-1 and the HCV NS3 Protease

   Författare :Fredrik Wångsell; Mats Larhed; Jari Yli-Kauhaluoma; Uppsala universitet; []
   Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Alzheimer s disease; BACE-1; transition state mimetic; tertiary hydroxyl group; hydroxyethylene; statine; hydroxyethylamine; hepatitis C; HCV NS3; bioisostere; protease inhibitor.; Pharmaceutical chemistry; Läkemedelskemi; Medicinal Chemistry; Läkemedelskemi;

   Sammanfattning : This thesis describes work done to design and synthesize protease inhibitors, with the intention of developing therapeutic agents for Alzheimer’s disease (AD) and the chronic liver condition caused by infection of the hepatitis C virus (HCV). AD is the most common form of dementia, and HCV infection is the primary reason for liver transplantation in industrialized countries. LÄS MER

7. 10. Computational Modelling of Structures and Ligands of CYP2C9

   Författare :Lovisa Afzelius; Collen Masimirembwa; Ismael Zamora; Anders Karlén; Marcel de Groot; Uppsala universitet; []
   Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Pharmaceutical chemistry; CYP2C9; 3D QSAR; GRID; CYP450; pharmacophore modelling; homology modelling; metabolism; competitive inhibitors; CPCA; molecular dynamics simulations; Farmaceutisk kemi; Pharmaceutical chemistry; Farmaceutisk kemi; Medicinal Chemistry; läkemedelskemi;

   Sammanfattning : CYP2C9 is one of our major drug metabolising enzymes and belongs to the cytochrome P450 (CYP) super family. The aim of this thesis was to gain an understanding of the quantitative structure–activity relationships (QSAR) of CYP2C9 substrates and inhibitors. LÄS MER