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Showing result 1 - 5 of 227 swedish dissertations matching the above criteria.

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

   Author : Karin Engen; Mats Larhed; Mikael Elofsson; Uppsala universitet; []
   Keywords : 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

4. 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 : 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

5. 3. Palladium(0)-Catalyzed Spirocyclization and Carbonylation Reactions : Ligands Targeting the Angiotensin II Type 2 Receptor

   Author : Jens Lindman; Mats Larhed; Johan Gising; Christian Sköld; Alessandra Tolomelli; Uppsala universitet; []
   Keywords : NATURVETENSKAP; NATURAL SCIENCES; MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Palladium catalysis; Mizoroki-Heck reaction; spiroindolines; spirooxindoles; amino acids; carbonylation; angiotensin II type 2 receptor; AT2R ligands; Medicinal Chemistry; Läkemedelskemi;

   Abstract : Palladium(0)-catalyzed chemistry represents one of the most important methods for the construction of carbon-carbon bonds, which are ubiquitous in organic compounds. The first part of this thesis describes the palladium(0)-catalyzed diastereoselective Mizoroki-Heck reaction of Vince lactam-derived precursors for the formation of spiroindolines (paper I) and spirooxindoles, which are scaffolds present in several natural products with interesting biological activity. READ MORE

6. 4. 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

7. 5. 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