附註:Includes bibliographical references and index.
Intro; Contents; Preface; List of protocols; Abbreviations; 1 Synthesis of combinatorial libraries using the portioning-mixing procedure; 1 Introduction; 2 The portioning-mixing (split-mix) synthesis; Basic principles; Important features of the synthesis; 3 Manual and automated synthesis; Manual synthesis; Automated synthesis; 4 Preliminary considerations for library design; The weight of the libraries; The weight of the solid support; The significance of the number of resin beads; 5 Synthetic strategies for library construction; Soluble libraries; Tethered libraries; 6 Summary
AcknowledgementsReferences; 2 One-bead one-compound combinatorial library method; 1 Introduction; 2 Synthesis of the peptide library; Preparation of the amino acid solutions; Synthesis of a linear peptide library on solid phase using TentaGel resin with 19 eukaryotic amino acids (cysteine excluded); Synthesis of disulfide cyclic peptide library; Synthesis of Dpr-Dpr cyclic peptide (oxime bond) library; On-resin synthesis of a cyclic peptide library using Lys and Glu side-chains; 3 Library screening; References; 3 Synthesis and screening of positional scanning synthetic combinatorial libraries
1 Introduction2 Mixture-based synthetic combinatorial libraries; Positional scanning concept; Synthesis of a tripeptide PS-SCL; Alkylation of peptide PS-SCL; PS-SCL reduction; From peptides to small organic and heterocyclic compounds; 3 Screening mixture-based libraries; PS-SCL deconvolution; Assay optimization; 4 Library screening using ELISA; 5 Identification of T cell-specific ligands; 6 Identification of antimicrobial and antifungal compounds; 7 Library screening using a radioreceptor assay; 8 Identification of enzyme inhibitors using PS-SCLs; References
4 High-throughput combinatorial synthesis of discrete compounds In multimilligram quantities: non-chemical encoding and directed sorting1 Introduction; 2 Non-chemical encoding and directed sorting; Radiofrequency tags; Radiofrequency tagged MicroKans; Radiofrequency tagged MicroTubes; 2D bar codes and bar coded microreactors; 3 Applications in combinatorial synthesis; R[sub(f)] tagged MicroKans: synthesis of taxoid, epothilone, and muscone libraries; R[sub(f)] tagged MicroTubes: synthesis of a tyrphostin library; Bar coded microreactors: application to oligonucleotide synthesis; 4 Conclusion
摘要:Combinatorial chemistry is the synthesizing and testing of arrays of compounds. The high throughput means that combinatorial techniques are increasingly used in the biomedical sciences, especially drug discovery and related pharmaceutical research. This volume is the first practical guide to combinatorial chemistry that will enable novices to carry out successful experiments.
