Search for dissertations about: "ISOSTERES"
Showing result 1 - 5 of 12 swedish dissertations containing the word ISOSTERES.
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1. Structure-Based Design and Synthesis of Protease Inhibitors Using Cycloalkenes as Proline Bioisosteres and Combinatorial Syntheses of a Targeted Library
Abstract : Structure-based drug design and combinatorial chemistry play important roles in the search for new drugs, and both these elements of medicinal chemistry were included in the present studies. This thesis outlines the synthesis of protease inhibitors against thrombin and the HCV NS3 protease, as well as the synthesis of a combinatorial library using solid phase chemistry. READ MORE
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2. Design and Synthesis of Serine and Aspartic Protease Inhibitors
Abstract : This thesis describes the design and synthesis of compounds that areintended to inhibit serine and aspartic proteases. The first part of the text deals with preparation of inhibitors of the hepatitis C virus (HCV) NS3 serine protease. Hepatitis C is predominantly a chronic disease that afflicts about 170 million people worldwide. READ MORE
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3. The MHC-glycopeptide-T cell interaction in collagen induced arthritis : a study using glycopeptides, isosteres and statistical molecular design in a mouse model for rheumatoid arthritis
Abstract : Rheumatoid arthritis (RA) is an autoimmune disease affecting approximately 1% of the population in the western world. It is characterised by a tissue specific attack of cartilage in peripheral joints. Collagen induced arthritis (CIA) is one of the most commonly used animal models for (RA), with similar symptoms and histopathology. READ MORE
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4. Syntheses of functionalized Phe-Gly dipeptidomimetics
Abstract : The complete series of Boc-protected C-4 mono- and difluoroallyl Phe-Gly dipeptidomimetics and their corresponding saturated derivatives has been synthesized. A mechanism that rationalizes the formation of the two isomeric allylic mono-fluorides from an allylic alcohol with diethylaminosulfur trifluoride (DAST) has been investigated. READ MORE
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5. Design and Synthesis of Aspartic and Serine Protease Inhibitors : Targeting the BACE-1 and the HCV NS3 Protease
Abstract : 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. READ MORE