Search for dissertations about: "peptidomimetics"

Showing result 6 - 10 of 27 swedish dissertations containing the word peptidomimetics.

2. 6. 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

4. 7. Design and Synthesis of Angiotensin IV Peptidomimetics Targeting the Insulin-Regulated Aminopeptidase (IRAP)

   Author : Hanna Andersson; Anders Hallberg; Anders Karlén; Federico Corelli; Uppsala universitet; []
   Keywords : MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; angiotensin IV; AT4; insulin-regulated aminopeptidase IRAP ; inhibitor; peptidomimetics; γ-turn mimetic; macrocycle; Pharmaceutical chemistry; Läkemedelskemi; Medicinal Chemistry; Läkemedelskemi;

   Abstract : Peptidomimetics derived from the bioactive hexapeptide angiotensin IV (Ang IV, Val1-Tyr2-Ile3-His4-Pro5-Phe6) have been designed and synthesized. These peptidomimetics are aimed at inhibiting the insulin-regulated amino peptidase (IRAP), also known as the AT4 receptor. READ MORE

5. 8. 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. 9. Towards the Development of Photoswitchable β-Hairpin Mimetics

   Author : Máté Erdélyi; Adolf Gogoll; Anders Karlén; John A. Robinson; Uppsala universitet; []
   Keywords : NATURVETENSKAP; NATURAL SCIENCES; Organic chemistry; β-hairpin; peptidomimetics; Sonogashira; NMR; photochemistry; microwave; peptide; palladium; Organisk kemi; Organic chemistry; Organisk kemi;

   Abstract : Peptide secondary structure mimetics are important tools in medicinal chemistry, as they provide analogues of endogeneous peptides with new physicochemical and pharmacological properties. The β-hairpin motif has been shown to be involved in numerous physiological processes, among others in regulation of eucariotic gene transcription. READ MORE

7. 10. Peptidomimetic Enzyme Inhibitors : Targeting M. tuberculosis Ribonucleotide Reductase and Hepatitis C Virus NS3 Protease

   Author : Johanna Nurbo; Anders Hallberg; Anders Karlén; Anja Sandström; Per Arvidsson; Uppsala universitet; []
   Keywords : MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; enzyme inhibitor; peptidomimetics; structure-activity relationship; tuberculosis; ribonucleotide reductase; hepatitis C virus; NS3 protease; Pharmaceutical chemistry; Farmaceutisk kemi; Medicinal Chemistry; Läkemedelskemi;

   Abstract : This thesis focuses on the design and synthesis of inhibitors targeting Mycobacterium tuberculosis ribonucleotide reductase (RNR) and hepatitis C virus (HCV) NS3 protease; enzymes that have been identified as potential drug targets for the treatment of tuberculosis and hepatitis C, respectively. Small peptides have been recognized as inhibitors of these enzymes. READ MORE