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ID: ALA1133131

Journal: Bioorg Med Chem Lett

Title: Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist.

Authors: Feng DD, Biftu T, Candelore MR, Cascieri MA, Colwell LF, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Miller RR, Stearns RA, Strader CD, Tota L, Wyvratt MJ, Fisher MH, Weber AE.

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.

CiteXplore: 10888324

DOI: 10.1016/s0960-894x(00)00267-5