| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1362767 | Bioorganic & Medicinal Chemistry Letters | 2010 | 8 Pages |
Abstract
Resulting from a vHTS based on a pharmacophore alignment on known β3-adrenoceptor ligands, an aryloxypropanolamine scaffold comprising a thienopyrimidine moiety was further optimized as a human β3-AR agonist, yielding a lead compound with an excellent cellular activity of EC50 = 20 pM, selectivity over hβ1- and hβ2-adrenoceptors and a promising safety profile.
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Related Topics
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Authors
Stefan Tasler, Roland Baumgartner, Astrid Ammendola, Josef Schachtner, Tanja Wieber, Marcus Blisse, Sandra Rath, Mirko Zaja, Philipp Klahn, Udo Quotschalla, Peter Ney,