Peptidomimetics Protocols

"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

• Synthesis and Use of Pseudopeptides Derived from 1,2,4-Oxadiazole-, 1,3,4-Oxadiazole-, and 1,2,4-Triazole-based Dipeptidomimetics.- Synthesis of Aminobenzoic Acid-Based Nonpeptide Templates: Applications in Peptidomimetic Drug Discovery.- Synthesis of an Esterase-Sensitive Cyclic Prodrug of a Model Hexapeptide Having Enhanced Membrane Permeability and Enzymatic Stability Using an Acyloxyalkoxy Promoiety.- Synthesis of an Esterase-Sensitive Cyclic Prodrug of a Model Hexapeptide Having Enhanced Membrane Permeability and Enzymatic Stability Using a 3-(2?-Hydroxy-4?,6?-Dimethylphenyl)-3,3-Dimethyl Propionic Acid Promoiety.- Synthesis of Coumarin-Based, Esterase-Sensitive Cyclic Prodrugs of Opioid Peptides with Enhanced Membrane Permeability and Enzymatic Stability.- Azatides as Peptidomimetics: Solution and Liquid Phase Syntheses.- Synthesis of Cbz-Protected Ketomethylene Dipeptide Isosteres.- (E)-Alkene Peptide Bond Isosteres by Cuprate Opening of Vinyl Aziridines.- Syntheses of Norstatine, Its Analogs, and Dipeptide Isosteres by Means of ?-Lactam Synthon Method.- Synthesis of a Versatile Peptidomimetic Scaffold.- An Asymmetric Synthesis Protocol to Prepare Topographically Constrained ?-Substituted Aromatic Amino Acids.- Synthesis of Oligopeptides Containing an Oxirane Ring in the Place of a Peptidic Bond.- Synthesis of Protected Lactam-Bridged Dipeptides.- Synthesis of Peptidomimics Through Sugar-Based Scaffolds.- The Synthesis of Bicyclic Piperazinone and Related Derivatives.- Synthesis of Dipeptides with ?[CH20] Amide Bond Mimetics.- SNAr-Based Cycloetherification Methodology: Application in the Synthesis of Heterodectic Macrocyclic Peptides with Endo Aryl-Aryl and Aryl-Alkyl Ether Bonds.- Cyclic Aromatic Amino Acids with Constrained ?1 and ?2 DihedralAngles.- Asymmetric Syntheses of Unnatural Amino Acids and Hydroxyethylene Peptide Isosteres.- Fluoroolefin Isosteres.- Synthesis of 3-Amino-l-CarboxymethyI-Benzodiazepine (BZA) Peptidomimetics.- A Conformationally Restricted ?-Strand HIV Protease Inhibitor.- Synthesis of Cyclopropane-Containing Leu-Enkephalin Analogs.- The 1,5-Disubstituted Tetrazole Ring as a cis-Amide Bond Surrogate.- Synthesis of (2R, 3R, 4R, 5S)-5-tert-Butyloxycarbonylamino-3,4-Dihydroxy-2-1sopropyl-3,4-O,O-Isopropylidene-6-CyctohexyI-Hexanoic Acid.- Synthesis of (2S, 4S, 5S)-5-(t-Butoxycarbonylamino)-4-(t-Butyldimethylsilyloxy)-2-Isopropyl-7-Methyl Octanoic Acid.- Synthesis of ?-Vinyl Amino Acids.- A Novel Synthetic Protocol for the Preparation of Enantiopure 3-, 4-, and 5-Substituted Prolines.- Synthesis of Aminobenzoic Acid-Based Nonpeptide Templates.- Aminimides as Peptidomimetics.