Annual Reports in Combinatorial Chemistry and Molecular DiversityM.R. Pavia, W.H. Moos Combinatorial chemistry and molecular diversity approaches to scientific and novel product R & D have exploded in the 1990s. For example, in the preparation of drug candidates, the automated, permutational, and combinatorial use of chemical building blocks now allows the generation and screening of unprecedented numbers of compounds. Drug discovery - better, faster, cheaper? Indeed more compounds have been made and screened in the 1990s than in the last hundred years of pharmaceutical research. The second volume in this series includes contributions on methods, solid phases, purification, analysis, carbohydrates, patent strategies and tactics, diversity profiling and combinatorial series design, and finishes with a survey of chemical libraries yielding biologically active agents and a compendium of solid phase chemistry publications. Each contribution is prepared by a recognized expert resulting in a high quality account of the recent advances in the field. |
Contents
Recent advances in solid phase synthesis | 15 |
Analytical methods for quality control of combinatorial libraries | 33 |
Patent strategies in molecular diversity | 53 |
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Activity agonist Agrafiotis aldehyde Alkylation alkyne amide amines amino acids analysis Angew antagonists Application approach aryl assay atoms automated bead biological Bioorg bond brary carboxylic acid Catalysts Chem chemical libraries chloride cleavage CO₂H combinatorial chemistry combinatorial libraries Combinatorial Synthesis complex compounds Comput construction Derivatives descriptors drug discovery Ellman encoded Engl Enzyme ester exemption FDA approval Figure fluorous Frec Frechet functional glycosylation H₂N heterocyclic hexapeptide HO₂C Houghten HPLC infringement inhibitors integrin Leznoff ligands Linker Meldal methods mixture molecular diversity molecules N-Substituted glycine NeoRX novel OH OH oligosaccharide Organic Synthesis patented invention pharmacophore phosphine Polymer Polymer Supports Polymer-Bound Polymer-Supported Polymeric polystyrene prepared protease protecting groups protein purification R₁ reaction reagents receptor reported resin bound screening selection solid phase organic Solid Phase Synthesis Solid Support solution strategy structure Synthe synthons targets techniques TentaGel Tetrahedron Lett tion trisaccharide