An NMR spectroscopic method to identify and classify thiol-trapping agents: revival of Michael acceptors for drug discovery?

Although Michael acceptors are traditionally shunned in modern drug discovery, trapping of thiols by covalent coupling represents an important mechanism of bioactivity, and many biologically relevant and druggable pathways are targeted by thiol-reactive compounds. Research on Michael acceptors, long confined to the realm of toxicology, was rekindled by the development of the antioxidant inflammation modulator (AIM) homo-triterpenoid bardoxolone methyl (RTA402, 1). This orally bioavailable biological

• Publication year

  2011

• Venue

  Angewandte Chemie

• Publication date

  2011-01-10

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1002/anie.201005959PMID 21132828
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

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