Novel 2-imidazoles as potent and selective alpha1A adrenoceptor partial agonists

Bioorg Med Chem Lett. 2008 May 1;18(9):2930-4. doi: 10.1016/j.bmcl.2008.03.070. Epub 2008 Mar 29.

Abstract

Novel 2-imidazoles have been identified as potent partial agonists of the alpha(1A) adrenergic receptor, with good selectivity over the alpha(1B), alpha(1D) and alpha(2A) receptor sub-types. Sulfonamide 23 possessed attractive drug-like properties with respect to physicochemical and ADME properties and wide ligand selectivity.

MeSH terms

  • Adrenergic alpha-1 Receptor Agonists*
  • Adrenergic alpha-2 Receptor Agonists
  • Adrenergic alpha-Agonists / chemical synthesis
  • Adrenergic alpha-Agonists / therapeutic use*
  • Humans
  • Imidazoles / chemical synthesis
  • Imidazoles / therapeutic use*
  • Models, Chemical
  • Receptors, Adrenergic, alpha-1
  • Receptors, Adrenergic, alpha-2
  • Structure-Activity Relationship
  • Sulfonamides / chemistry
  • Sulfonamides / pharmacology
  • Urinary Incontinence / drug therapy*

Substances

  • ADRA1A protein, human
  • ADRA1B protein, human
  • ADRA1D protein, human
  • ADRA2A protein, human
  • Adrenergic alpha-1 Receptor Agonists
  • Adrenergic alpha-2 Receptor Agonists
  • Adrenergic alpha-Agonists
  • Imidazoles
  • Receptors, Adrenergic, alpha-1
  • Receptors, Adrenergic, alpha-2
  • Sulfonamides