Abell Advances in Amino Acid Mimetics and Peptidomimetics

1. Auflage 1997
ISBN: 978-0-08-055262-0
Verlag: Elsevier Science & Techn.
Format: PDF
Kopierschutz: 1 - PDF Watermark

E-Book, Englisch, 301 Seiten, Web PDF

Peptidomimetics are compounds which mimic the biological activity of peptides while offering the advantages of increased bioavailability, biostability, bioefficiency, and bioselectivity against the natural biological target of the parent peptide. Examples of peptidomimetics have been isolated as natural products, synthesized as libraries from novel subunits, and designed on the basis of X-ray crystallographic studies and through an intricate knowledge of the biological mode of action of natural peptides. They offer challenging synthetic targets and are increasingly important medicinal agents and biological probes. As a consequence, peptidomimetics embrace much of what is modern medicinal and organic chemistry. This volume highlights some recent and exciting developments in the area.

Autoren/Hrsg.

Abell, A.

Inhaltsverzeichnis

1;Cover;1
2;ADVANCES IN AMINO ACID MIMETICS AND PEPTIDOMIMETICS;4
3;Copyright Page;5
4;Contents;6
5;LIST OF CONTRIBUTORS;8
6;PREFACE;12
7;CHAPTER 1. THE ROLE OF COMPUTER-AIDED AND STRUCTURE BASED DESIGN TECHNIQUES IN THE DISCOVERY AND OPTIMIZATION OF CYCLIC UREA INHIBITORS OF HIV PROTEASE;14
8;CHAPTER 2. MACROCYCLIC INHIBITORS OF SERINE PROTEASES;54
9;CHAPTER 3. MIMICKING EXTENDED CONFORMATIONS OF PROTEASE SUBSTRATES: DESIGNING CYCLIC PEPTIDOMIMETICS TO INHIBIT HIV-1 PROTEASE;90
10;CHAPTER 4. PEPTIDOMIMETIC SYNTHETIC COMBINATORIAL LIBRARIES;122
11;CHAPTER 5. PEPTIDOMIMETIC LIGANDS FOR SRC HOMOLOGY-2 DOMAINS;140
12;CHAPTER 6. PEPTIDOMIMETIC INHIBITORS OF FARNESYL TRANSFERASE: AN APPROACH TO NEW ANTITUMOR AGENTS;178
13;CHAPTER 7. SYNTHETIC ROUTES TO LACTAM PEPTIDOMIMETICS;206
14;CHAPTER 8. TOWARD RATIONALLY DESIGNED PEPTIDYL-PROLYL ISOMERASE INHIBITORS;246
15;CHAPTER 9. NATURAL PRODUCT PEPTIDOMIMETICS;264
16;INDEX;308