Structure guided P1′ modifications of HEA derived β-secretase inhibitors for the treatment of Alzheimer’s disease

Autor:	Vinod F. Patel, Thomas T. Nguyen, Lewis D. Pennington, Daniel B. Horne, Michael D. Bartberger, Holger Monenschein, Stephen Hitchcock, Wenge Zhong
Rok vydání:	2012
Předmět:	Clinical Biochemistry Pharmaceutical Science Cathepsin D Biochemistry Structure-Activity Relationship stomatognathic system Aspartate protease Alzheimer Disease Catalytic Domain Drug Discovery Ethylamines Humans Moiety Computer Simulation Protease Inhibitors Molecular Biology Binding Sites Chemistry Organic Chemistry Toxicity Microsomes Liver Microsome β secretase Molecular Medicine Amine gas treating Amyloid Precursor Protein Secretases Selectivity
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 22:3607-3611
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2012.04.060
Popis:	The synthesis and SAR of a series of BACE-1 hydroxyethyl amine inhibitors containing substitutions on a spirocyclobutyl moiety is described. Selectivity against cathepsin D, a related aspartyl protease with potential off target toxicity, and improved microsomal stability is exemplified.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0ee9cf462951bcfa5784ecb95fc1ba18 https://doi.org/10.1016/j.bmcl.2012.04.060 Zobrazit plný text záznamu Full Text from ScienceDirect