A Novel Series of Potent Γ-Secretase Inhibitors Based on a Benzobicyclo[4.2.1]nonane Core

SJ Lewis,AL Smith,JG Neduvelil,GI Stevenson,MJ Lindon,AB Jones,MS Shearman,D Beher,E Clarke,JD Best, JE Peachey,T Harrison,JL Castro

Bioorganic & Medicinal Chemistry Letters（2005）SCI 4区SCI 2区

Department of Medicinal Chemistry

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摘要

A new series of gamma-secretase inhibitors was developed from an in-house screening hit based on a benzobicyclo[4.2.1]nonane core. Lead optimisation studies led to the development of a series of potent inhibitors and in vivo efficacy was demonstrated.

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关键词

gamma-secretase inhibitors

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