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Related Experiment Videos

A screening method for chiral selectors that does not require covalent attachment.

Zhi Chen1, Yanhong Yang, Stefan Werner

  • 1Department of Chemistry, University of Pittsburgh, Pittsburgh, PA 15260, USA.

Journal of the American Chemical Society
|February 16, 2006
PubMed
Summary
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A new high-throughput screening method identifies chiral selectors by measuring target distribution between liquid phases. This approach efficiently screens for compounds with chiral selectivity without covalent bonding.

Area of Science:

  • Analytical Chemistry
  • Organic Chemistry
  • Separation Science

Background:

  • Chiral selector discovery is crucial for enantioseparation.
  • Existing methods can be time-consuming and require significant material.
  • A need exists for efficient, high-throughput screening protocols for novel chiral selectors.

Purpose of the Study:

  • To develop and validate a high-throughput screening protocol for identifying chiral selectors.
  • To enable the discovery of selectors based on noncovalent intermolecular associations.
  • To facilitate the screening of small molecule libraries for chiral recognition capabilities.

Main Methods:

  • A high-throughput screening protocol modeled on biological screening.
  • Partitioning experiments measuring target distribution between aqueous and organic phases (plasticized poly(vinyl chloride)).

Related Experiment Videos

  • Utilizing 96-well plates for rapid partition ratio measurements.

    • Main Results:

    • The protocol was validated using a known chiral target/selector pair.
    • Screening of 12 cyclopropyl dipeptide isosteres against racemic econazole.
    • Eight compounds showed binding to the racemic target, with one exhibiting measurable chiral selectivity.

    Conclusions:

    • The proposed high-throughput screening method is effective for chiral selector discovery.
    • The protocol does not require covalent attachment of analytes or selectors.
    • The method requires minimal amounts (approx. 100 µg) of potential chiral selectors.