A new series of potent benzodiazepine gamma-secretase inhibitors.

Churcher, Ian; Ashton, Kate; Butcher, John W; Clarke, Earl E; Harrison, Timothy; Lewis, Huw D; Owens, Andrew P; Teall, Martin R; Williams, Susie; Wrigley, Jonathan D J

Churcher, Ian; Ashton, Kate; Butcher, John W; Clarke, Earl E; Harrison, Timothy; Lewis, Huw D; Owens, Andrew P; Teall, Martin R; Williams, Susie; Wrigley, Jonathan D J.

Affiliation

Churcher I; Department of Medicinal Chemistry, The Neuroscience Research Centre, Merck, Sharp and Dohme Research Laboratories, Terlings Park, Eastwick Road, Essex Harlow, CM20 2QR, UK. ian_churcher@merck.com

Bioorg Med Chem Lett ; 13(2): 179-83, 2003 Jan 20.

Article de En | MEDLINE | ID: mdl-12482419

ABSTRACT

ABSTRACT

A new series of benzodiazepine-containing gamma-secretase inhibitors with potential use in the treatment of Alzheimer's disease is disclosed. Structure-activity relationships of the pendant hydrocinnamate side-chain which led to the preparation of highly potent inhibitors are described.

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Collection: 01-internacional Base de données: MEDLINE Sujet principal: Endopeptidases / Inhibiteurs de protéases / Benzodiazépines Limites: Humans Langue: En Journal: Bioorg Med Chem Lett Sujet du journal: BIOQUIMICA / QUIMICA Année: 2003 Type de document: Article Pays d'affiliation: Royaume-Uni

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