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Peptidomimetics in Organic and Medicinal Chemistry.
A peptidomimetic is a small protein-like chain designed to mimic a peptide with adjusted molecular properties such as enhanced stability or biological activity. It is a very powerful approach for the generation of small-molecule-based drugs as enzyme inhibitors or receptor ligands. Peptidomimetics i...
| Clasificación: | Libro Electrónico |
|---|---|
| Autor principal: | |
| Otros Autores: | |
| Formato: | Electrónico eBook |
| Idioma: | Inglés |
| Publicado: |
Hoboken :
Wiley,
2014.
©2014 |
| Temas: | |
| Acceso en línea: | Texto completo |
Tabla de Contenidos:
- Cover; Title Page; Copyright; Contents; Preface; Abbreviations; Part I The Basics of Peptidomimetics; Chapter 1 The Basics of Peptidomimetics; 1.1 Introduction; 1.2 Definition and Classification; 1.3 Strategic Approaches to Peptidomimetic Design; 1.3.1 Modification of Amino Acids; 1.3.2 Compounds with Global Restrictions; 1.3.3 Molecular Scaffolds Mimicking the Peptidic Backbone; 1.4 Successful Examples of Peptidomimetic Drugs; 1.4.1 ACE Inhibitors; 1.4.2 Thrombin Inhibitors; 1.5 Conclusion; References; Chapter 2 Synthetic Approaches towards Peptidomimetic Design; 2.1 Introduction
- 2.2 Local Modifications2.2.1 Single Amino Acid Modifications; 2.2.2 Dipeptide Isosteres; 2.2.3 Retro-inverso Peptides; 2.2.4 N-Methylation of Peptides; 2.2.5 Azapeptides; 2.2.6 Peptoids; 2.3 Global Restrictions through Cyclic Peptidomimetics; 2.4 Peptidomimetic Scaffolds; 2.5 Conclusions; References; Part II Synthetic Methods and Molecules; Chapter 3 Peptidomimetic Bioisosteres; 3.1 Introduction; 3.2 Peptide Bond Isosteres; 3.2.1 Thioamides; 3.2.2 Esters; 3.2.3 Alkenes and Fluoroalkenes; 3.2.4 Transition-State Isosteres; 3.3 Side-Chain Isosteres
- Chapter 5 Click Chemistry: The Triazole Ring as a Privileged Peptidomimetic Scaffold5.1 Introduction; 5.1.1 CuAAC Reaction; 5.1.2 Triazole Ring as a Peptidomimetic Isostere; 5.2 Triazole-Containing Peptidomimetics Elaborated through `Click Chemistry'; 5.2.1 Macrocycles; 5.2.2 Oligomers and Foldamers; 5.3 Relevant Applications in Drug Discovery; 5.3.1 AChE Inhibitors; 5.3.2 HIV Protease Inhibitors; 5.3.3 MMP Inhibitors; 5.3.4 Integrin Ligands; 5.4 Conclusions; Acknowledgements; References; Chapter 6 Peptoids; 6.1 Introduction and Basics of Peptoids; 6.2 Synthetic Methods