New pyridazino[4,5-b]indole derivatives with inodilator and antiaggregatory activities

Arzneimittelforschung. 1993 Nov;43(11):1175-80.

Abstract

Some 4-(3,5-dimethylpyrazol) 5H-pyridazino [4,5-b]indoles (7), 1,2,4-triazolo [4,3-b]pyridazino [4,5-b]indoles (9) and 1,2,4-tetrazolo [4,5-b]pyridazino [4,5-b] indoles (11) substituted in position 1 by amino groups have been synthesized and tested as inotropic agents and inhibitors of platelet aggregation. 6-Imidazolyl-11H-1,2,4-triazolo [4,3-b]pyridazino [4,5-b]indole (9) shows an activity superior to that of amrinone, with a notable selectivity towards phosphodiesterase (PDE) IV and PDEV, vasodilator activity and a good effect on blood platelet aggregation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Aorta, Thoracic / drug effects
  • Blood Platelets / drug effects
  • Blood Platelets / enzymology
  • Cardiotonic Agents / chemical synthesis*
  • Cardiotonic Agents / pharmacology
  • Dogs
  • Female
  • Guinea Pigs
  • Heart Rate / drug effects
  • Humans
  • In Vitro Techniques
  • Indoles / chemical synthesis*
  • Indoles / pharmacology
  • Male
  • Muscle Contraction / drug effects
  • Muscle, Smooth, Vascular / drug effects
  • Myocardial Contraction / drug effects
  • Phosphodiesterase Inhibitors / chemical synthesis
  • Phosphodiesterase Inhibitors / pharmacology
  • Platelet Aggregation / drug effects
  • Platelet Aggregation Inhibitors / chemical synthesis*
  • Platelet Aggregation Inhibitors / pharmacology
  • Pyridazines / chemical synthesis*
  • Pyridazines / pharmacology
  • Rats
  • Rats, Wistar
  • Thromboxane-A Synthase / antagonists & inhibitors
  • Vasodilator Agents / chemical synthesis*
  • Vasodilator Agents / pharmacology

Substances

  • Cardiotonic Agents
  • Indoles
  • Phosphodiesterase Inhibitors
  • Platelet Aggregation Inhibitors
  • Pyridazines
  • Vasodilator Agents
  • Thromboxane-A Synthase