4-Oxospiro[benzopyran-2,4'-piperidines] as selective alpha 1a-adrenergic receptor antagonists

Bioorg Med Chem Lett. 1999 Jan 18;9(2):291-4. doi: 10.1016/s0960-894x(98)00732-x.

Abstract

The 4-oxospiro[benzopyran-2,4'-piperidine] ring system is contained within potent class III antiarrhythmic agents. We highlight how these agents can be chemically transformed into a new class of potent (< 1 nM) and selective (> 25-fold) alpha 1a-receptor subtype adrenergic antagonists.

Publication types

  • Comparative Study

MeSH terms

  • Adrenergic alpha-1 Receptor Antagonists*
  • Animals
  • Anti-Arrhythmia Agents / chemical synthesis
  • Benzopyrans / pharmacology*
  • Humans
  • Male
  • Piperidines / pharmacology*
  • Prostatic Hyperplasia / drug therapy
  • Rats
  • Spiro Compounds / pharmacology*

Substances

  • Adrenergic alpha-1 Receptor Antagonists
  • Anti-Arrhythmia Agents
  • Benzopyrans
  • Piperidines
  • Spiro Compounds