Notice bibliographique
- Notice
Type(s) de contenu et mode(s) de consultation : Texte noté : électronique
Auteur(s) : Trabocchi, Andrea
Guarna, Antonio
Titre(s) : Peptidomimetics in organic and medicinal chemistry [Texte électronique] / Dr. Andrea Trabocchi and Professor Antonio Guarna
Publication : Chichester, West Sussex, UK ; Hoboken, NJ : John Wiley & Sons Inc., 2014
Description matérielle : 1 online resource
Note(s) : Includes bibliographical references and index. - Print version record and CIP data provided by publisher.
"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"
Sujet(s) : Protéines -- Emploi en thérapeutique
Indice(s) Dewey :
615.19 (23e éd.) = Chimie pharmaceutique
Identifiants, prix et caractéristiques : ISBN 9781118683033
Identifiant de la notice : ark:/12148/cb44654684k
Notice n° :
FRBNF44654684
(notice reprise d'un réservoir extérieur)
Table des matières : 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.
8.3 Bicyclic α-Amino Acids18.4 Conclusions; References; Chapter 9: β-Turn Peptidomimetics;
9.1 Introduction; 9.2 Definition and Classification of β-Turns; 9.3 Conformational
Analysis; 9.4 β-Turn Peptidomimetics; 9.5 Conclusions; References; Chapter 10: Peptidomimetic
Foldamers; 10.1 Introduction; 10.2 Classification; 10.3 Peptoids; 10.4 β-Peptides:
First Systematic Conformational Studies; 10.5 Hybrid Foldamers; 10.6 From Structural
to Functional Foldamers; 10.7 Conclusions; References; Part III: Applications in Medicinal
Chemistry.
5.4 ConclusionsAcknowledgements; References; Chapter 6: Peptoids; 6.1 Introduction
and Basics of Peptoids; 6.2 Synthetic Methods; 6.3 Macrocyclic Peptoids; 6.4 Conformational
Analysis of Folded Peptoids; 6.5 Application of Peptoids as Antimicrobial Peptidomimetics;
6.6 Conclusions; References; Chapter 7: Sugar Amino Acids; 7.1 Introduction; 7.2 α-SAAs;
7.3 β-SAAs; 7.4 γ-SAAs1; 7.5 δ-SAAs2; 7.6 Representative Applications in Medicinal
Chemistry; 7.7 Conclusions; References; Chapter 8: Cyclic α-Amino Acids as Proline
Mimetics; 8.1 Introduction; 8.2 Cyclic α-Amino Acids.
Chapter 11: Case Study 1: Peptidomimetic HIV Protease Inhibitors11.1 Introduction;
11.2 The HIV-1 Virus; 11.3 Antiretroviral Therapy; 11.4 Drug Resistance; 11.5 HIV-1
Protease Inhibitors; 11.6 Conclusions; Acknowledgements; References; Chapter 12: Case
Study 2: Peptidomimetic Ligands for αvβ3 Integrin; 12.1 Introduction; 12.2 Peptide-Based
Peptidomimetic Integrin Ligands; 12.3 Scaffold-Based Peptidomimetic Integrin Ligands;
12.4 Conclusions; References; Index.
