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Automated solid-phase synthesis of linear nitrogen-linked compounds.

P W Davis¹, E E Swayze

¹Ibis Therapeutics, a Division of Isis Pharmaceuticals, 2292 Faraday Avenue, Carlsbad, California 92008, USA. pwdavis@home.com

Biotechnology and Bioengineering

|January 12, 2000

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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:

Related Experiment Videos

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.