Second Generation of Hydroxyethylamine BACE-1 Inhibitors: Optimizing Potency and Oral Bioavailability
Journal of Medicinal Chemistry2008Vol. 51(11), pp. 3313–3317
Citations Over TimeTop 10% of 2008 papers
Nicolas Charrier, Brian Clarke, Leanne Cutler, Emmanuel H. Demont, Colin Dingwall, R. Dunsdon, P East, Julie A. Hawkins, Colin Howes, Ishrut Hussain, Phil Jeffrey, G. Maile, Rosalie Matico, J. Mosley, Alan Naylor, Alistair O’Brien, Sally Redshaw, Paul Rowland, V. Soleil, Kathrine J. Smith, Sharon Sweitzer, Pam Theobald, D. Vesey, Daryl S. Walter, Gareth Wayne
Abstract
BACE-1 inhibition has the potential to provide a disease-modifying therapy for the treatment of Alzheimer's disease. Optimization of a first generation of BACE-1 inhibitors led to the discovery of novel hydroxyethylamines (HEAs) bearing a tricyclic nonprime side. These derivatives have nanomolar cell potency and are orally bioavailable.
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