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Peptidomimetics in Organic and Medicinal Chemistry

2014-03-14 Science
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Release : 2014-03-14
Genre : Science
Kind : eBook
Book Rating : 145/5 ( reviews)

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Book Synopsis Peptidomimetics in Organic and Medicinal Chemistry by : Antonio Guarna

Download or read book Peptidomimetics in Organic and Medicinal Chemistry written by Antonio Guarna. This book was released on 2014-03-14. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Mid-size Drugs Based on Peptides and Peptidomimetics

2018-01-16 Science
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Release : 2018-01-16
Genre : Science
Kind : eBook
Book Rating : 91X/5 ( reviews)

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Book Synopsis Mid-size Drugs Based on Peptides and Peptidomimetics by : Hirokazu Tamamura

Download or read book Mid-size Drugs Based on Peptides and Peptidomimetics written by Hirokazu Tamamura. This book was released on 2018-01-16. Available in PDF, EPUB and Kindle. Book excerpt: This brief describes studies conducted by the authors on mid-size drugs utilizing peptides and peptidomimetics, and on the development of anti-HIV agents. Peptides are important biological molecules and have various physiological actions. Peptide-based drug discovery may help bring about the development of useful medicines that are highly safe and show potent pharmacological effects in small doses. Recently, it has been shown that there is an important drug-like space in the mid-sized region between low- and high-molecular-weight compounds. Thus, mid-size drugs such as peptide compounds are being focused on. To date, several peptidomimetics that mimic primary, secondary, and tertiary structures of peptides have been developed to maintain and improve biological activities and actions of peptides. In this book, the features and advantages of mid-size drugs are described in detail. In addition, the merits of utilizing peptidomimetics in the development of mid-size drugs are referred to. Understanding such peptide-derived mid-size drugs will lead to a comprehensive expansion of medicinal chemistry.

Amino Acids, Peptides and Proteins in Organic Chemistry, Protection Reactions, Medicinal Chemistry, Combinatorial Synthesis

2011-06-03 Science
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Release : 2011-06-03
Genre : Science
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Book Rating : 572/5 ( reviews)

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Book Synopsis Amino Acids, Peptides and Proteins in Organic Chemistry, Protection Reactions, Medicinal Chemistry, Combinatorial Synthesis by :

Download or read book Amino Acids, Peptides and Proteins in Organic Chemistry, Protection Reactions, Medicinal Chemistry, Combinatorial Synthesis written by . This book was released on 2011-06-03. Available in PDF, EPUB and Kindle. Book excerpt: This is the fourth of five books in the Amino Acids, Peptides and Proteins in Organic Synthesis series. Closing a gap in the literature, this is the only series to cover this important topic in organic and biochemistry. Drawing upon the combined expertise of the international "who's who" in amino acid research, these volumes represent a real benchmark for amino acid chemistry, providing a comprehensive discussion of the occurrence, uses and applications of amino acids and, by extension, their polymeric forms, peptides and proteins. The practical value of each volume is heightened by the inclusion of experimental procedures. The 5 volumes cover the following topics: Volume 1: Origins and Synthesis of Amino Acids Volume 2: Modified Amino Acids, Organocatalysis and Enzymes Volume 3: Building Blocks, Catalysis and Coupling Chemistry Volume 4: Protection Reactions, Medicinal Chemistry, Combinatorial Synthesis Volume 5: Analysis and Function of Amino Acids and Peptides The fourth volume in this series is structured in three main sections. The first section is about protection reactions and amino acid based peptidomimetics. The second, and most extensive, part is devoted to the medicinal chemistry of amino acids. It includes, among others, the chemistry of alpha- and beta amino acids, peptide drugs, and advances in N- and O-glycopeptide synthesis. The final part deals with amino acids in combinatorial synthesis. Methods, such as phage display, library peptide synthesis, and computational design are described. Originally planned as a six volume series, Amino Acids, Peptides and Proteins in Organic Chemistry now completes with five volumes but remains comprehensive in both scope and coverage. Further information about the 5 Volume Set and purchasing details can be viewed here.

Amino Acids, Peptides and Proteins in Organic Chemistry, Protection Reactions, Medicinal Chemistry, Combinatorial Synthesis

2011-04-18 Science
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Release : 2011-04-18
Genre : Science
Kind : eBook
Book Rating : 032/5 ( reviews)

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Book Synopsis Amino Acids, Peptides and Proteins in Organic Chemistry, Protection Reactions, Medicinal Chemistry, Combinatorial Synthesis by :

Download or read book Amino Acids, Peptides and Proteins in Organic Chemistry, Protection Reactions, Medicinal Chemistry, Combinatorial Synthesis written by . This book was released on 2011-04-18. Available in PDF, EPUB and Kindle. Book excerpt: This is the fourth of five books in the Amino Acids, Peptides and Proteins in Organic Synthesis series. Closing a gap in the literature, this is the only series to cover this important topic in organic and biochemistry. Drawing upon the combined expertise of the international "who's who" in amino acid research, these volumes represent a real benchmark for amino acid chemistry, providing a comprehensive discussion of the occurrence, uses and applications of amino acids and, by extension, their polymeric forms, peptides and proteins. The practical value of each volume is heightened by the inclusion of experimental procedures. The 5 volumes cover the following topics: Volume 1: Origins and Synthesis of Amino Acids Volume 2: Modified Amino Acids, Organocatalysis and Enzymes Volume 3: Building Blocks, Catalysis and Coupling Chemistry Volume 4: Protection Reactions, Medicinal Chemistry, Combinatorial Synthesis Volume 5: Analysis and Function of Amino Acids and Peptides The fourth volume in this series is structured in three main sections. The first section is about protection reactions and amino acid based peptidomimetics. The second, and most extensive, part is devoted to the medicinal chemistry of amino acids. It includes, among others, the chemistry of alpha- and beta amino acids, peptide drugs, and advances in N- and O-glycopeptide synthesis. The final part deals with amino acids in combinatorial synthesis. Methods, such as phage display, library peptide synthesis, and computational design are described. Originally planned as a six volume series, Amino Acids, Peptides and Proteins in Organic Chemistry now completes with five volumes but remains comprehensive in both scope and coverage. Further information about the 5 Volume Set and purchasing details can be viewed here.

Peptidomimetics Protocols

2010-10-28 Science
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Release : 2010-10-28
Genre : Science
Kind : eBook
Book Rating : 595/5 ( reviews)

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Book Synopsis Peptidomimetics Protocols by : Wieslaw M. Kazmierski

Download or read book Peptidomimetics Protocols written by Wieslaw M. Kazmierski. This book was released on 2010-10-28. Available in PDF, EPUB and Kindle. Book excerpt: Many physiologically important receptors and enzymes are regulated by their endogenous ligands and inhibitors. Nature chose to utilize these p- tides as chemical switches since they can be efficiently synthesized and - graded in cells, thus providing an immediate response to a fast changing environment. Such properties, so critical in cell survival, make peptides less than ideal drug candidates. Other frequently desired properties in drug m- ecules include oral bioavailability, the ability to cross membranes, including the blood-brain barrier, and sufficient stability for administration 1-2 times a day. In spite of these obstacles, some natural peptides and proteins are ind- putably successful medicines and have become drugs of choice. Further - vances in peptide-based pharmaceuticals are critically dependent on both new delivery methods and new chemical approaches to the conversion of these molecules to druglike entities. In addition, peptides are also the natural sta- ing points for optimization of their pharamacological and chemical prop- ties, which may lead to superior drugs. Peptidomimetics Protocols deals with both aspects of peptide pharmaceuticals, through the tools of modern s- thetic and medicinal chemistry. The last decade has witnessed a steady stream of new synthetic approaches to peptide mimetics, compounds that replace phy- ologically vulnerable peptide functionalities with chemical modules of - creased stability and cellular penetration. The chapters have been written by both academic and industrial chemists, and focus on the practical synthetic preparation of peptide mimetics.

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