Literature DB >> 20056541

Piperidine-derived gamma-secretase modulators.

Adrian Hall1, Richard L Elliott, Gerard M P Giblin, Ishrut Hussain, James Musgrave, Alan Naylor, Rosemary Sasse, Beverley Smith.   

Abstract

This Letter details the SAR of a novel series of piperidine-derived gamma-secretase modulators. Compound 10h was found to be a potent modulator in vitro, which on further profiling, was found to decrease Abeta42, increase Abeta38 and have no effect on Abeta40 levels. Furthermore, 10h demonstrated excellent pharmacokinetic parameters in the mouse, rat and dog in addition to good CNS penetration in the mouse. Copyright (c) 2009. Published by Elsevier Ltd.

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Year:  2009        PMID： 20056541     DOI： 10.1016/j.bmcl.2009.08.072

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


  12 in total

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