Synthesis and vasorelaxant activity of new 1,4-benzoxazine derivatives potassium channel openers

Bioorg Med Chem. 2002 Aug;10(8):2663-9. doi: 10.1016/s0968-0896(02)00091-3.

Abstract

As part of a search for new potassium channel openers, the synthesis and vasorelaxant activity of new 1,4-benzoxazine derivatives derived from transformation of the benzopyran skeleton of cromakalim were described. Several new 1,4-benzoxazine derivatives were provided with significant vasorelaxant activity with an overall pharmacological behavior similar to CRK (1f, 1i, 2d, 2e, 2f and 2i).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Aorta / drug effects
  • Cromakalim
  • Dose-Response Relationship, Drug
  • Ion Channel Gating / drug effects
  • Male
  • Oxazines / chemical synthesis*
  • Oxazines / pharmacology
  • Potassium Channels / drug effects*
  • Rats
  • Rats, Wistar
  • Structure-Activity Relationship
  • Vasodilation / drug effects*

Substances

  • Oxazines
  • Potassium Channels
  • Cromakalim