| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1366990 | Bioorganic & Medicinal Chemistry Letters | 2007 | 6 Pages |
Abstract
Attachment of the cyclopropylcarbamate group to the piperidine core of γ-secretase inhibitors leads to a dramatic increase of their in vitro potency. Strategies for subsequent improvement of the in vivo pharmacokinetic profile of the series are discussed. Resulting compounds significantly reduce Aβ levels in TgCRND8 mice after a single PO dosing at 30 mpk.
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Organic Chemistry
Authors
Theodros Asberom, Zhiqiang Zhao, Thomas A. Bara, John W. Clader, William J. Greenlee, Lynn A. Hyde, Hubert B. Josien, Wei Li, Andrew T. McPhail, Amin A. Nomeir, Eric M. Parker, Murali Rajagopalan, Lixin Song, Gwendolyn T. Wong, Lili Zhang, Qi Zhang,