Discovery of an orally bioavailable alkyl oxadiazole β 3 adrenergic receptor agonist

Abstract

5- n-Pentyl oxadiazole substituted benzenesulfonamide 8 is a potent and selective β 3 adrenergic receptor agonist (β 3 EC 50=23 nM, β 1 IC 50=3000 nM, β 2 IC 50=3000 nM). The compound has high oral bioavailability in dogs (62%) and rats (36%) and is among the most orally bioavailable β 3 adrenergic receptor agonists reported to date.