Sökning: "bioisosteres"
Visar resultat 1 - 5 av 6 avhandlingar innehållade ordet bioisosteres.
1. Design and Synthesis of Potential Aminoacyl-tRNA Synthetase Inhibitors
Sammanfattning : Aminoacyl-tRNA synthetases (aaRSs) are essential enzymes present in all living organisms, their catalytic activity is involved in the translation of the genetic code into functional proteins and they are potential targets for anti-infective agents. The first step in the biosynthetic pathway catalysed by aaRSs consists of activation of the corresponding amino acid by the reaction with ATP to form an aminoacyl-adenylate (aa-AMP), the key intermediate in the biosynthesis of proteins. LÄS MER
2. The Synthesis and Use of Certain Pyridine Derivatives as Modulators of the G-protein Coupled Receptors mGlu5 and P2Y12
Sammanfattning : The glutamatergic mGlu5 receptor and the purinergic P2Y12 receptor are two important targets in the development of novel treatments of gastroesophageal reflux disease (GERD) and thrombosis, respectively. Synthesis was developed to investigate the structure-activity relationships (SAR) of a novel series of 2-alkynylpyridine derivatives as mGluR5 antagonists. LÄS MER
3. Structure-Based Design and Synthesis of Protease Inhibitors Using Cycloalkenes as Proline Bioisosteres and Combinatorial Syntheses of a Targeted Library
Sammanfattning : 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. LÄS MER
4. Design and Synthesis of Inhibitors Targeting the Hepatitis C Virus NS3 Protease : Focus on C-Terminal Acyl Sulfonamides
Sammanfattning : Hepatitis C is a global health problem that affects approximately 120–180 million people. This viral infection causes serious liver diseases and the therapy available suffers from low efficiency and severe side effects. Consequently, there is a huge unmet medical need for new therapeutic agents to combat the hepatitis C virus (HCV). LÄS MER
5. Design and Synthesis of Hepatitis C Virus NS3 Protease Inhibitors
Sammanfattning : Hepatitis C Virus (HCV) is the leading cause of chronic liver disease worldwide as well as the primary indication for liver transplantation. More than 3% of the world’s population is chronically infected with HCV and there is an urgent need for effective therapy. LÄS MER
