Second generation of hydroxyethylamine BACE-1 inhibitors: optimizing potency and oral bioavailability

Autor:	D. Vesey, Alan Naylor, Rosalie Matico, P. Jeffrey, Daryl S. Walter, Nicolas Charrier, Julie Hawkins, Sharon Sweitzer, B. Clarke, Paul Rowland, Ishrut Hussain, R. Dunsdon, A. O'Brien, Philip East, Colin Dingwall, Virginie Soleil, J. Mosley, Emmanuel Hubert Demont, Leanne Cutler, Sally Redshaw, Kathrine J. Smith, C. Howes, P. Theobald, G. Maile, Gareth Wayne
Rok vydání:	2008
Předmět:	Models Molecular medicine.drug_class Administration Oral Biological Availability Carboxamide Pharmacology Benzothiadiazines Structure-Activity Relationship Dogs In vivo Oral administration Drug Discovery medicine Ethylamines Potency Animals Cell potency chemistry.chemical_classification biology Bioavailability Cyclic S-Oxides Rats chemistry Biochemistry Enzyme inhibitor biology.protein Molecular Medicine Amyloid Precursor Protein Secretases Tricyclic
Zdroj:	Journal of medicinal chemistry. 51(11)
ISSN:	0022-2623
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3bba0eace56f44a64342f037ce8c9dae https://pubmed.ncbi.nlm.nih.gov/18457381 Zobrazit plný text záznamu