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Automated solid-phase synthesis of linear nitrogen-linked compounds
1Ibis Therapeutics, a Division of Isis Pharmaceuticals, 2292 Faraday Avenue, Carlsbad, California 92008, USA. pwdavis@home.com
Biotechnology and Bioengineering
|January 12, 2000
Summary
Researchers developed a new method to create diverse nitrogen-linked compounds for screening potential RNA-targeting drugs. This versatile approach enables high-throughput synthesis of novel molecules for drug discovery.
Area of Science:
- Medicinal Chemistry
- Organic Synthesis
- Drug Discovery
Background:
- Targeting structured RNA is a promising strategy for drug discovery.
- Developing novel scaffolds for RNA-binding molecules is crucial.
Purpose of the Study:
- To develop a versatile synthetic library motif for creating linear, nitrogen-linked compounds.
- To enable high-throughput synthesis of potential RNA-binding molecules for drug discovery.
Main Methods:
- In situ scaffold creation using protected bifunctional compounds.
- Formation of acyl and amine links for molecular extension and functionalization.
- Utilizing a 96-well parallel-array synthesizer for high-throughput synthesis.
Main Results:
- Successful synthesis of a wide variety of modified-backbone PNA (peptide nucleic acid) type monomers.
- Demonstrated versatility in creating diverse nitrogen-linked compounds.
- Established a high-throughput synthesis approach for potential drug candidates.
Conclusions:
- The developed synthetic scheme offers a versatile approach to generating libraries of potential RNA-binding molecules.
- This method facilitates the discovery of novel therapeutics targeting structured RNA.
- High-throughput synthesis capabilities accelerate the screening process for drug candidates.