| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10591521 | Bioorganic & Medicinal Chemistry Letters | 2013 | 5 Pages |
Abstract
A series of amides bearing a variety of amidine head groups was investigated as BACE1 inhibitors with respect to inhibitory activity in a BACE1 enzyme as well as a cell-based assay. Determination of their basicity as well as their properties as substrates of P-glycoprotein revealed that a 2-amino-1,3-oxazine head group would be a suitable starting point for further development of brain penetrating compounds for potential Alzheimer's disease treatment.
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Physical Sciences and Engineering
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Authors
Thomas J. Woltering, Wolfgang Wostl, Hans Hilpert, Mark Rogers-Evans, Emmanuel Pinard, Alexander Mayweg, Martin Göbel, David W. Banner, Jörg Benz, Massimiliano Travagli, Martina Pollastrini, Guido Marconi, Emanuele Gabellieri, Wolfgang Guba,