A new series of tricyclic (aryloximino)propanolamines displaying very high selective beta 2-blocking properties

J Med Chem. 1989 Feb;32(2):315-20. doi: 10.1021/jm00122a008.

Abstract

A new class of indanones 4 easily obtained by aryne type condensations, followed by transposition of the benzocyclobutanols 3 thus formed, were transformed into the corresponding oximinopropanolamines 7. These compounds were studied for their potential beta-blocking properties. It was found that 7 have generally low beta 1-blocking properties. Their beta 2-blocking action varies from low to very high. Interestingly one of them (7b) has the highest beta 2 activity/beta 1 activity (343) value known to date.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenergic beta-Antagonists / chemical synthesis*
  • Adrenergic beta-Antagonists / pharmacology
  • Animals
  • Female
  • Guinea Pigs
  • In Vitro Techniques
  • Male
  • Propanolamines / chemical synthesis*
  • Propanolamines / pharmacology
  • Structure-Activity Relationship

Substances

  • Adrenergic beta-Antagonists
  • Propanolamines