Piperidine-derived γ-secretase modulators
作者： Adrian Hall , Richard L. Elliott , Gerard M.P. Giblin , Ishrut Hussain , James Musgrave
DOI: 10.1016/J.BMCL.2009.08.072
关键词: Chemistry 、 In vitro 、 Cns penetration 、 Pharmacokinetics 、 Biochemistry 、 Gamma secretase 、 Piperidine
摘要: This Letter details the SAR of a novel series piperidine-derived gamma-secretase modulators. Compound 10h was found to be potent modulator in vitro, which on further profiling, decrease Abeta42, increase Abeta38 and have no effect Abeta40 levels. Furthermore, demonstrated excellent pharmacokinetic parameters mouse, rat dog addition good CNS penetration mouse.
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