Amino acids, peptides and proteins in organic chemistry v. 4 Protection reactions, medicinal chemistry, combinatorial synthesis

INDICE: PROTECTION REACTIONS General Considerations Alpha-Amino Protection (Nalpha-Protection) Carboxy Protection Side Chain Protection Photocleavable Protections Conclusion Experimental Section THE HUISGEN CYCLOADDITION IN PEPTIDOMIMETIC CHEMISTRY Introduction The Huisgen [2+3] Cycloaddition Between Azides and Acetylenes Mechanistic Consideration for the Cu-Huisgen and Ru-Huisgen Cycloaddition Building Blocks for the Synthesis of Triazole Modified Peptidomimetics Cyclic Triazole Peptidomimetics Acylic Triazole Peptidomimetics Useful Experimental Procedures RECENT ADVANCES IN BETA-STRAND MIMETICS Introduction Macrocyclic Peptidomimetics Acyclic Compounds Aliphatic and Aromatic Carbocycles Ligands Containing One Ring or Multiple Rings with One Heteroatom (O, S) Ligands Containing One Ring with Two Heteroatoms (N,N) Ligands Containing One Ring with Two Heteroatoms (N,S) or Three Heteroatoms (N,N,S or N,N,N) Ligands Containing Two Rings with One Heteroatom (N or O) Ligands Containing Two Rings with Two or Three Heteroatoms (N,N or N,S or N,N,N) Concluding Remarks MEDICINAL CHEMISTRY OF ALPHA-AMINO ACIDS Introduction Glutamic Acid Conformational Restriction Bioisosterism Structure-Activity-Studies Conclusion MEDICINAL CHEMISTRY OF ALICYCLIC BETA-AMINO ACIDS Introduction Five-Membered Alicyclic Beta-Amino Acids Six-Membered Alicyclic Beta-Amino Acids MEDICINAL CHEMISTRY OF ALPHA-HYDROXY-BETA-AMINO ACIDS Introduction Alpha-Hydroxy-Beta-Amino Acids AntibacterialAgents Inhibitors of Aminopeptidases Aspartyl Proteases Inhibitors Paclitaxeland its Derivatives PEPTIDE DRUGS Lights and Shades of Peptide and Protein Drugs Peptide Drugs Available on the Market Approved Peptides in Oncology Antimicrobial Peptides Perspectives ORAL BIOAVAILABILITY OF PEPTIDE AND PEPTIDOMIMETIC DRUGS Introduction Fundamental Considerations of Intestinal Absorption Barriers Limiting Oral Peptide/Peptidomimetic Drugs Bioavailability Strategies to Improve Peptide-Based Drugs Oral Bioavailability Conclusions ASYMMETRIC SYNTHESIS OF BETA-LACTAMS VIA THE STAUDINGER REACTION Introduction The Staudinger Reaction Influence of the Geometry of the Imine on Stereoselectivity in the Reaction Influence of the Polarity of the Solvent on Stereoselectivity of the Reaction Influence of the Isomerization of the Imine Prior to its Nucleophilic Attack onto the Ketene Stereoselectivity in the Reaction Influence of the Order of Addition of the Reactants to the Reaction Influence of Chiral Substituents on the Stereoselectivity of the Reaction Asymmetric Induction from the Imine Component Asymmetric Induction from the Ketene Component Double Asymmetric Cycloinduction Influence of Catalysts on the Stereoselectivity of the Reaction Concluding Remarks ADVANCES IN N- AND O-GLYCOPEPTIDE SYNTHESIS - A TOOL TO STUDY CLYCOSYLATION AND DEVELOP NEW THERAPEUTICS Introduction O-Glycopeptide Synthesis Synthesis of Mucin Type Glycopeptides Synthesis of Tumor-Associated Glycopeptides and Glycopeptide Vaccines Synthes

• ISBN: 978-3-527-32103-2
• Editorial: Wiley-VCH
• Encuadernacion: Cartoné
• Páginas: 600
• Fecha Publicación: 16/03/2011
• Nº Volúmenes: 1
• Idioma: Inglés