Structure-activity relationship studies of xanthone and fluorenone-1,4-dihydropyridine-5-phosphonates

Arzneimittelforschung. 1996 Apr;46(4):374-7.

Abstract

A series of xanthone and fluorenone-1,4-dihydropyridine derivatives bearing a 5-phosphonate group were prepared. The compounds were evaluated for inotropic, chronotropic and calcium antagonistic properties. The insertion of a phosphonate group is detrimental for inotropic and calcium antagonistic activity but improves the potency and selectivity for chronotropism.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Aorta, Thoracic / drug effects
  • Calcium Channel Blockers / chemical synthesis*
  • Calcium Channel Blockers / pharmacology
  • Cardiotonic Agents / chemical synthesis*
  • Cardiotonic Agents / pharmacology
  • Dihydropyridines / chemical synthesis*
  • Dihydropyridines / pharmacology
  • Female
  • Guinea Pigs
  • Heart Atria / drug effects
  • In Vitro Techniques
  • Magnetic Resonance Spectroscopy
  • Male
  • Muscle Contraction / drug effects
  • Muscle, Smooth, Vascular / drug effects
  • Myocardial Contraction / drug effects
  • Organophosphorus Compounds / chemical synthesis*
  • Organophosphorus Compounds / pharmacology
  • Structure-Activity Relationship

Substances

  • Calcium Channel Blockers
  • Cardiotonic Agents
  • Dihydropyridines
  • Organophosphorus Compounds