An NMR Spectroscopic Method to Identify and Classify Thiol‐Trapping Agents: Revival of Michael Acceptors for Drug Discovery?

Abstract

Speed trap: Cysteamine reacts in DMSO with electrophilic double bonds to afford Michael adducts (see scheme), whereas no trapping reaction takes place in apolar solvents. A simple and quick NMR spectroscopic method to identify Michael acceptors and sort them into reversible and irreversible thiol sinks is validated biologically in a cellular assay sensitive to thiol-trapping agents. DMSO=dimethyl sulfoxide. Detailed facts of importance to specialist readers are published as ”Supporting Information”. Such documents are peer-reviewed, but not copy-edited or typeset. They are made available as submitted by the authors. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.