Novel antiasthmatic agents with dual activities of thromboxane A2 synthetase inhibition and bronchodilation. IV. 2-[2-(1-Imidazolyl)ethyl]-4-(3-pyridyl)-1(2H)-phthalazinones

Chem Pharm Bull (Tokyo). 1994 Sep;42(9):1850-3. doi: 10.1248/cpb.42.1850.

Abstract

Synthesis and pharmacological evaluation of several compounds related to 2-[2-(1-imidazolyl)ethyl]-4-(3-pyridyl)-1(2H)-phthalazinones are described. The phenyl moiety of the phthalazinone skeleton was found to play an important role in both thromboxane A2 synthetase-inhibitory and bronchodilatory activities. Further, the 3-pyridyl group at the 4-position was shown to be necessary for in vivo thromboxane A2 synthetase-inhibitory activity.

MeSH terms

  • Animals
  • Asthma / drug therapy*
  • Bronchodilator Agents / chemical synthesis*
  • Bronchodilator Agents / pharmacology*
  • Guinea Pigs
  • Imidazoles / chemical synthesis*
  • Imidazoles / pharmacology*
  • In Vitro Techniques
  • Male
  • Phthalazines / chemical synthesis*
  • Phthalazines / pharmacology*
  • Rabbits
  • Rats
  • Rats, Sprague-Dawley
  • Structure-Activity Relationship
  • Thromboxane A2 / metabolism*
  • Thromboxane-A Synthase / antagonists & inhibitors*

Substances

  • Bronchodilator Agents
  • Imidazoles
  • Phthalazines
  • Thromboxane A2
  • Thromboxane-A Synthase