Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist

Bioorg Med Chem Lett. 2000 Jul 3;10(13):1427-9. doi: 10.1016/s0960-894x(00)00267-5.

Abstract

5-n-Pentyl oxadiazole substituted benzenesulfonamide 8 is a potent and selective beta3 adrenergic receptor agonist (beta3 EC50 = 23 nM, beta1 IC50 = 3000 nM, beta2 IC50 = 3000 nM). The compound has high oral bioavailability in dogs (62%) and rats (36%) and is among the most orally bioavailable beta3 adrenergic receptor agonists reported to date.

MeSH terms

  • Administration, Oral
  • Adrenergic beta-3 Receptor Agonists*
  • Adrenergic beta-Agonists / administration & dosage
  • Adrenergic beta-Agonists / chemistry
  • Adrenergic beta-Agonists / pharmacokinetics*
  • Adrenergic beta-Agonists / pharmacology*
  • Animals
  • Biological Availability
  • CHO Cells
  • Cricetinae
  • Dogs
  • Drug Design
  • Humans
  • Molecular Structure
  • Oxadiazoles / administration & dosage
  • Oxadiazoles / chemistry
  • Oxadiazoles / pharmacokinetics*
  • Oxadiazoles / pharmacology*
  • Rats
  • Structure-Activity Relationship

Substances

  • Adrenergic beta-3 Receptor Agonists
  • Adrenergic beta-Agonists
  • Oxadiazoles