Description |
1 online resource (320 pages) |
Contents |
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 |
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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 |
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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 |
Summary |
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 in Organic and Medicinal Chemistry outlines the concepts and synthetic strategies underlying the building of bioactive compounds of a peptidomimetic nature. Topics covered include the chemistry of unnatural amino acids, peptide- and scaffold-based peptidomimetics, amino acid-side chai |
Bibliography |
Includes bibliographical references and index |
Notes |
Print version record |
Subject |
Peptide drugs.
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Proteins -- Therapeutic use
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Drugs -- Design.
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Drug Design
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Peptidomimetics -- therapeutic use
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Peptidomimetics -- metabolism
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Drugs -- Design
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Peptide drugs
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Proteins -- Therapeutic use
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Form |
Electronic book
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Author |
Trabocchi, Andrea
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ISBN |
9781118683842 |
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1118683846 |
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9781119950608 |
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1119950600 |
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