Mixture-based Libraries Research Articles

Synthesis and Characterization of a Mixture-Based Library of Oxime Ethers Based on a Common Aromatic Scaffold

A mixture-based library of oxime ethers of general structure 4 (Scheme 2) has been prepared and characterized. Synthesis of the aromatic scaffold 3 (Scheme 1) containing two aromatic aminooxy groups followed by its reaction with 55 pairwise combinations of 11 aromatic aldehydes A−K in separate wells results in the formation of a library of sublibraries each containing four major oxime ether components. Extensive characterization of the sublibraries by LC−MS and NMR shows formation of all of the expected products in comparable amounts. The library compositions show little sensitivity of the oximation reaction to the aldehyde structure. This synthetically simple procedure provides a rapid approach to covering diversity space for this class of compounds and has implications for their use in dynamic combinatorial libraries.

New opioid peptides, peptidomimetics, and heterocyclic compounds from combinatorial libraries

Abstract: Here we review the use of combinatorial libraries in opioid receptor assays. Following a brief description of the history of the combinatorial field, methods for the generation of synthetic libraries and the deconvolution of mixture-based libraries are presented. Case studies involving opioid assays used to demonstrate the viability of combinatorial libraries are described. The identification of new opioid peptides from combinatorial libraries is reviewed. The peptides found are composed of L-amino acids, D-amino acids, or L-, D-, and unnatural amino acids, and range from tetrapeptides to decapeptides. Likewise, new opioid compounds identified from peptidomimetic libraries, such as peptoids and alkylated dipeptides, and those identified from acyclic (e.g., polyamine, urea) and heterocyclic (e.g., bicyclic guanidine) libraries, are reviewed. © 2000 John Wiley & Sons, Inc. Biopoly 51: 379–390, 1999

New opioid peptides, peptidomimetics, and heterocyclic compounds from combinatorial libraries.

Here we review the use of combinatorial libraries in opioid receptor assays. Following a brief description of the history of the combinatorial field, methods for the generation of synthetic libraries and the deconvolution of mixture-based libraries are presented. Case studies involving opioid assays used to demonstrate the viability of combinatorial libraries are described. The identification of new opioid peptides from combinatorial libraries is reviewed. The peptides found are composed of L-amino acids, D-amino acids, or L-, D-, and unnatural amino acids, and range from tetrapeptides to decapeptides. Likewise, new opioid compounds identified from peptidomimetic libraries, such as peptoids and alkylated dipeptides, and those identified from acyclic (e.g., polyamine, urea) and heterocyclic (e.g., bicyclic guanidine) libraries, are reviewed.