| Literature DB >> 17079141 |
Theodros Asberom1, 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, Dmitri A Pissarnitski.
Abstract
Attachment of the cyclopropylcarbamate group to the piperidine core of gamma-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 Abeta levels in TgCRND8 mice after a single PO dosing at 30 mpk.Entities:
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Year: 2006 PMID： 17079141 DOI： 10.1016/j.bmcl.2006.10.011
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823