Peptidomimetics in Organic and Medicinal Chemistry : The Art of Transforming Peptides in Drugs

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 chain isosteres, backbone isosteres, dipeptide isosteres, beta-turn peptidomimetics, proline-mimetics as turn inducers, cyclic scaffolds, amino acid surrogates, and scaffolds for combinatorial chemistry of peptidomimetics. Case studies in the hit-to-lead process, such as the development of integrin ligands and thrombin inhibitors, illustrate the successful application of peptidomimetics in drug discovery. 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 Chain Isosteres, Backbone Isosteres, Dipeptide Isosteres, Beta-turn Peptidomimetics, Proline-mimetics As Turn Inducers, Cyclic Scaffolds, Amino Acid Surrogates, And Scaffolds For Combinatorial Chemistry Of Peptidomimetics. Case Studies In The Hit-to-lead Process, Such As The Development Of Integrin Ligands And Thrombin Inhibitors, Illustrate The Successful Application Of Peptidomimetics In Drug Discovery-- Peptidomimetics In Organic And Medicinal Chemistry Outlines The Concepts And Synthetic Strategies Underlying The Building Of Bioactive Compounds Of A Peptidomimetic Nature-- Title Page; Copyright; Dedication; 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; 1.4 Successful Examples Of Peptidomimetic Drugs; 1.5 Conclusion; References; Chapter 2: Synthetic Approaches Towards Peptidomimetic Design; 2.1 Introduction; 2.2 Local Modifications; 2.3 Global Restrictions Through Cyclic Peptidomimetics; 2.4 Peptidomimetic Scaffolds; 2.5 Conclusions; References; Part Ii: Synthetic Methods And Molecules. Chapter 3: Peptidomimetic Bioisosteres3.1 Introduction; 3.2 Peptide Bond Isosteres; 3.3 Side-chain Isosteres; 3.4 Dipeptide Isosteres; 3.5 Tripeptide Isosteres; 3.6 Conclusion; References; Chapter 4: Solid-phase Synthesis And Combinatorial Approaches To Peptidomimetics; 4.1 Introduction; 4.2 Solid-phase Synthesis Of Peptidomimetics; 4.3 Conclusion; References; Chapter 5: Click Chemistry: The Triazole Ring As A Privileged Peptidomimetic Scaffold; 5.1 Introduction; 5.2 Triazole-containing Peptidomimetics Elaborated Through 'click Chemistry'; 5.3 Relevant Applications In Drug Discovery. Dr. Andrea Trabocchi And Professor Antonio Guarna. Includes Bibliographical References And Index. Mode Of Access: World Wide Web. 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 chain isosteres, backbone isosteres, dipeptide isosteres, beta-turn peptidomimetics, proline-mimetics as turn inducers, cyclic scaffolds, amino acid surrogates, and scaffolds for combinatorial chemistry of peptidomimetics. Case studies in the hit-to-lead process, such as the development of integrin ligands and thrombin inhibitors, illustrate the successful application of peptidomimetics in drug discovery. The EPUB format of this title may not be compatible for use on all handheld devices. L'écran d"accueil indique : "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 chain isosteres, backbone isosteres, dipeptide isosteres, beta-turn peptidomimetics, proline-mimetics as turn inducers, cyclic scaffolds, amino acid surrogates, and scaffolds for combinatorial chemistry of peptidomimetics. Case studies in the hit-to-lead process, such as the development of integrin ligands and thrombin inhibitors, illustrate the successful application of peptidomimetics in drug discovery."

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 chain isosteres, backbone isosteres, dipeptide isosteres, beta-turn peptidomimetics, proline-mimetics as turn inducers, cyclic scaffolds, amino acid surrogates, and scaffolds for combinatorial chemistry of peptidomimetics. Case studies in the hit-to-lead process, such as the development of integrin ligands and thrombin inhibitors, illustrate the successful application of peptidomimetics in drug discovery.