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Peptidomimetics Protocols (Methods in Molecular Medicine)
 
 
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Peptidomimetics Protocols (Methods in Molecular Medicine) [Hardcover]

Wieslaw M. Kazmierski (Editor)

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Book Description

0896035174 978-0896035171 October 19, 1998 1
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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Editorial Reviews

Review

"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

From the Back Cover

In Peptidomimetics Protocols, Wieslaw Kazmierski assembles a state-of-the-art collection of detailed synthetic procedures that lead to a variety of scaffolds, turn mimetics, peptide-bond replacements, and enzyme inhibitors. Topics range from syntheses of unusual 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 otherwise labile 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. Peptidomimetics Protocols is the first book devoted to the practical synthetic preparation of peptide mimetics. Written by both academic and industrial synthetic organic and medicinal chemists, this book provides highly practical synthetic procedures for the generation of key peptide mimetics, and so immediately becomes a must-have desk reference and guide for all medicinal and pharmaceutical chemists engaged in the discovery and development of pharmaceuticals today.

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Inside This Book (learn more)
First Sentence:
1H and 13C NMR spectra were recorded at 270 and 67.5 MHz with tetramethylsilane as the internal standard. Read the first page
Key Phrases - Statistically Improbable Phrases (SIPs): (learn more)
concentrate the appropriate fractions, cyclic prodrug, wash with brine, glyoxylic acid chloride, ketomethylene peptide isosteres, alkenyl aziridines, dry the combined organic layers, using diisopropylamine, cyclohexylmethyl bromide, acyloxyalkoxy promoiety, chiral alkylation, combine the organic extracts, stir the reaction mixture, nonpeptide templates, remove the cooling bath, trimethyl lock, combine the organic layers, purify the crude product, aqueous citric acid, linear hexapeptide, add dichloromethane, extract the aqueous layer, allow the reaction mixture, synthon method, model hexapeptide
Key Phrases - Capitalized Phrases (CAPs): (learn more)
Tetrahedron Lett, New York, Molecular Medicine, Peptidomimetics Protocols Edited, Press Inc, Protein Res, Perkin Trans, Boc Boc, John Wiley, Mallinckrodt Chemical, Marcel Dekker, Enzyme Inhih, Pierce Chemical, Tetrahedron Left, Bioorganic Med, Controlled Release, Heterocyclic Chem, Liebigs Ann, Life Sci, Matheson Gas Products, Oxford University Press, Protective Groups, Transport of Cyclic Prodrug, Varian Gemini
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