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ID: ALA1133227
Journal: Bioorg Med Chem Lett
Title: Substituted oxazole benzenesulfonamides as potent human beta3 adrenergic receptor agonists.
Authors: Ok HO, Reigle LB, Candelore MR, Cascieri MA, Colwell LF, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Strader CD, Tota L, Wang P, Wyvratt MJ, Fisher MH, Weber AE.
Abstract: As a part of our investigation into the development of orally bioavailable beta3 adrenergic receptor agonists, we have identified a series of substituted oxazole derivatives that are potent beta3 agonists with excellent selectivity against other beta receptors. Several of these compounds showed excellent oral bioavailability in dogs. One example, cyclopentylethyloxazole 5f is a potent beta3 agonist (EC50 = 14 nM, 84% activation) with 340-fold and 160-fold selectivity over beta1 and beta2 receptors, respectively, and has 38% oral bioavailability in dogs.
CiteXplore: 10915043