Literature DB >> 10888324

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

D D Feng1, T Biftu, M R Candelore, M A Cascieri, L F Colwell, L Deng, W P Feeney, M J Forrest, G J Hom, D E MacIntyre, R R Miller, R A Stearns, C D Strader, L Tota, M J Wyvratt, M H Fisher, A E Weber.   

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.

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Year:  2000        PMID: 10888324     DOI: 10.1016/s0960-894x(00)00267-5

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Comparative 3D QSAR study on β(1)-, β(2)-, and β(3)-adrenoceptor agonists.

Authors:  P Senthil Kumar; Prasad V Bharatam
Journal:  Med Chem Res       Date:  2009-10-31       Impact factor: 1.965

2.  Characterization of beta3-adrenergic receptor: determination of pharmacophore and 3D QSAR model for beta3 adrenergic receptor agonism.

Authors:  Philip Prathipati; Anil K Saxena
Journal:  J Comput Aided Mol Des       Date:  2005-02       Impact factor: 3.686

Review 3.  The discovery of drugs for obesity, the metabolic effects of leptin and variable receptor pharmacology: perspectives from beta3-adrenoceptor agonists.

Authors:  Jonathan R S Arch
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2008-07-09       Impact factor: 3.000

  3 in total

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