5-Isoquinolinesulfonamide derivatives. 1. Synthesis and vasodilatory activity of N-(2-guanidinoethyl)-5-isoquinolinesulfonamide derivatives

J Med Chem. 1989 Jan;32(1):42-6. doi: 10.1021/jm00121a009.

Abstract

Two novel series of N-(2-guanidinoalkyl)-5-isoquinolinesulfonamides, 2 and 3, were prepared. Many of the compounds possessed vasodilatory activity when injected locally into the femoral artery of dogs. The most potent compound, 1-amidino-4-(5-isoquinolylsulfonyl)-1,4-perhydrodiazepine, 33, was comparable to diltiazem, which is used clinically as a vasodilator.

MeSH terms

  • Animals
  • Calcium Channel Blockers / chemical synthesis
  • Dogs
  • Female
  • Femoral Artery / drug effects
  • Isoquinolines / chemical synthesis*
  • Isoquinolines / pharmacology
  • Male
  • Structure-Activity Relationship
  • Sulfonamides / chemical synthesis*
  • Sulfonamides / pharmacology
  • Vasodilator Agents / chemical synthesis*

Substances

  • Calcium Channel Blockers
  • Isoquinolines
  • Sulfonamides
  • Vasodilator Agents
  • N-(2-guanidinoethyl)-5-isoquinolinesulfonamide