Overview

A state-of-the-art collection of detailed synthetic procedures that lead to a variety of scaffolds, turn mimetics, peptide-bound replacements, and enzyme inhibitors. Topics range from unusual syntheses of amino acids to the use of a variety of linear and heterocyclic scaffolds in place of the peptide backbone. Important chemical procedures and methods include the transient protection of charged peptides as neutral prodrugs for improved blood-brain penetration and the replacement of peptide bonds with heterocyclic rings, olefins and fluoroolefins, and ketomethylenes. Synthetic protocols towards the transition-state mimics and reactive ""warheads,"" applicable in enzyme inhibitors, are also disclosed.

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9781617370595

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The editor has assembled an interesting collection of synthetic methods for preparing peptidomimetics...This book will clearly be of value to those who are interested in synthesizing nonpeptidic analogues of small peptide ligands. -Journal of Medicinal Chemistry the editor does an excellent job of bringing together a variety of different chemical syntheses that are relevant to peptide, peptidomimetic, combinatorial and medicinal chemistry. Each chapter is written in the same general format of introduction, materials, methods, notes and references, which is always valuable for a book that will be regularly consulted. In addition, many of these are reported by acknowledged leaders in the field... includes a number of novel amino acid syntheses that will be extremely valuable to those scientists trying to understand the underlying medicinal chemistry of peptides... the contents of this book are extremely valuable and I have no doubt it will find its way into many of the world's leading industrial and academic organic chemistry laboratories. -Drug Discovery Today

The editor has assembled an interesting collection of synthetic methods for preparing peptidomimetics. . .This book will clearly be of value to those who are interested in synthesizing nonpeptidic analogues of small peptide ligands. -Journal of Medicinal Chemistry the editor does an excellent job of bringing together a variety of different chemical syntheses that are relevant to peptide, peptidomimetic, combinatorial and medicinal chemistry. Each chapter is written in the same general format of introduction, materials, methods, notes and references, which is always valuable for a book that will be regularly consulted. In addition, many of these are reported by acknowledged leaders in the field. . . includes a number of novel amino acid syntheses that will be extremely valuable to those scientists trying to understand the underlying medicinal chemistry of peptides. . . the contents of this book are extremely valuable and I have no doubt it will find its way into many of the world's leading industrial and academic organic chemistry laboratories. -Drug Discovery Today

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