2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: alpha1a subtype selective 2'-heteroaryl compounds

Bioorg Med Chem Lett. 2003 Mar 24;13(6):1183-6. doi: 10.1016/s0960-894x(03)00050-7.

Abstract

The structure-activity relationship of 2'-pyrrole, pyrazole and triazole substituted 2-(anilinomethyl)imidazolines as alpha(1) adrenergic agonists was investigated. The size and orientation of substituents, as well as the position of the heteroatoms, were found to have a profound effect on the potency and selectivity of the molecules. Potent alpha(1A) subtype selective agonists have been identified.

MeSH terms

  • Adrenergic alpha-1 Receptor Agonists*
  • Adrenergic alpha-Agonists / chemical synthesis*
  • Adrenergic alpha-Agonists / pharmacology*
  • Pyrazoles / chemical synthesis
  • Pyrazoles / pharmacology
  • Pyrroles / chemical synthesis
  • Pyrroles / pharmacology
  • Structure-Activity Relationship
  • Triazoles / chemical synthesis
  • Triazoles / pharmacology

Substances

  • Adrenergic alpha-1 Receptor Agonists
  • Adrenergic alpha-Agonists
  • Pyrazoles
  • Pyrroles
  • Triazoles