Arylpiperazine substituted heterocycles as selective alpha(1a) adrenergic antagonists

Bioorg Med Chem Lett. 2002 Sep 2;12(17):2443-6. doi: 10.1016/s0960-894x(02)00436-5.

Abstract

Antagonists of the alpha(1)-adrenergic receptors (alpha(1)-ARs) are useful for the treatment of benign prostatic hyperplasia. A series of potent and subtype-selective alpha(1a)-AR antagonists has been synthesized, displaying in vitro binding affinity in the low the nanomolar range.

MeSH terms

  • Adrenergic Antagonists / chemical synthesis*
  • Adrenergic Antagonists / pharmacology
  • Adrenergic alpha-1 Receptor Antagonists*
  • Heterocyclic Compounds, 4 or More Rings / chemical synthesis
  • Heterocyclic Compounds, 4 or More Rings / pharmacology
  • Humans
  • Isoxazoles
  • Piperazines / chemical synthesis
  • Piperazines / pharmacology
  • Protein Binding
  • Receptors, Adrenergic, alpha-1
  • Sensitivity and Specificity
  • Structure-Activity Relationship

Substances

  • ADRA1A protein, human
  • Adrenergic Antagonists
  • Adrenergic alpha-1 Receptor Antagonists
  • Heterocyclic Compounds, 4 or More Rings
  • Isoxazoles
  • Piperazines
  • Receptors, Adrenergic, alpha-1