Structure-activity relationship studies in the field of calcium antagonists. Xanthone 1,4-dihydropyridines bearing a 2,3-lactone ring

Arzneimittelforschung. 1995 Sep;45(9):957-62.

Abstract

A series of xanthone 1,4-dihydropyridine derivatives bearing a 2,3-lactone ring and a 2-acetoxymethyl group were prepared. The compounds were evaluated for inotropic, chronotropic and calcium antagonist properties. The introduction of a 2,3-lactone ring improved the negative inotropic activity and selectivity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Calcium Channel Blockers / chemical synthesis*
  • Calcium Channel Blockers / pharmacology
  • Chemical Phenomena
  • Chemistry, Physical
  • Female
  • Guinea Pigs
  • Heart Atria / drug effects
  • Heart Rate / drug effects
  • In Vitro Techniques
  • Lactones / chemical synthesis*
  • Lactones / pharmacology
  • Magnetic Resonance Spectroscopy
  • Male
  • Muscle Contraction / drug effects
  • Muscle, Smooth, Vascular / drug effects
  • Myocardial Contraction / drug effects
  • Pyridines / chemical synthesis*
  • Pyridines / pharmacology
  • Structure-Activity Relationship

Substances

  • Calcium Channel Blockers
  • Lactones
  • Pyridines
  • hydroxypyridines