Peptide nucleic acid precursors and methods of preparing same

Abstract

Novel and efficient syntheses create novel piperazinone intermediates which facilitate the production and use of PNAs. Such syntheses and the products enhance the feasibility of a system which permits the rapid identification of PNA oligomers useful as therapeutics, diagnostics and/or gene characterization tools. A first component of the system is a universal PNA library that most preferably incorporates one or more universal nucleotide bases into carefully selected positions within each oligomer species thereby providing the library with the screening ability of a much larger library. The second component of the system is a high throughput screening system that includes a number of assays designed to provide information on the binding activities of the different PNAs to a target nucleotide sequence (generally, a DNA or RNA sequence). The third component is a software system especially designed to provide rapid analysis of the data collected from the high throughput screening system and to determine therefrom the sequence base identities and sequence lengths of PNA oligomers most likely to bind to and appropriately affect the target molecule.