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Libraries of non-polymeric organic molecules
1Eric M Gordon, Affymax Research Institute, 4001 Miranda Avenue, Palo Alto, California 94304, USA.
Current Opinion in Biotechnology
|December 1, 1995
Summary
New technology enables simultaneous chemical synthesis of diverse compounds using combinatorial chemistry on solid supports. Advances in monitoring and release methods facilitate the creation of small-molecule libraries for drug discovery.
Area of Science:
- Organic Chemistry
- Medicinal Chemistry
- Chemical Synthesis
Background:
- Combinatorial chemistry relies on solid-phase synthesis for creating diverse compound libraries.
- Development of analytical and chemical methods is crucial for solid-phase reactions.
- Progress in these areas enables efficient synthesis and characterization of novel molecules.
Purpose of the Study:
- To highlight advancements in combinatorial chemistry for synthesizing small-molecule libraries.
- To showcase the application of these libraries in medicinal chemistry.
- To emphasize the role of automation in modern chemical synthesis.
Main Methods:
- Adaptation of organic synthesis techniques to solid supports.
- Development of analytical methods for monitoring solid-phase reactions.
- Implementation of chemical approaches for compound release into solution.
Main Results:
- Successful synthesis of small-molecule libraries including 1,4-benzodiazepines, mercaptopropionyl amino acids, and peptidyl phosphonates.
- Creation of encoded combinatorial libraries yielding potent carbonic anhydrase inhibitors.
- Increasing importance and application of automated instrumentation in library synthesis.
Conclusions:
- Significant progress has been made in solid-phase combinatorial chemistry.
- These advancements facilitate the discovery of novel drug candidates.
- Automation is a key driver in the future of small-molecule library synthesis.