Part 2. Notch-sparing γ-secretase inhibitors: The study of novel γ-amino naphthyl alcohols

Autor:	Jing Zhang, Dennis J. Selkoe, Michael S. Wolfe, Wenjuan Ye, Han-Xun Wei, Dai Lu, Yongli Gu, Pamela Osenkowski, Corinne E. Augelli-Szafran, Vivien Sun
Rok vydání:	2016
Předmět:	0301 basic medicine Stereochemistry Clinical Biochemistry Pharmaceutical Science Naphthalenes Cleavage (embryo) Biochemistry Article Propanolamines Structure-Activity Relationship 03 medical and health sciences Drug Discovery Amyloid precursor protein Animals Humans Protease Inhibitors γ secretase Receptor Notch1 Molecular Biology Amyloid beta-Peptides 030102 biochemistry & molecular biology biology Chemistry Organic Chemistry Amino Alcohols Peptide Fragments Rats 030104 developmental biology Microsomes Liver biology.protein Molecular Medicine Amyloid Precursor Protein Secretases
Zdroj:	Bioorg Med Chem Lett
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2016.03.042
Popis:	One therapeutic approach for Alzheimer's disease is to inhibit the cleavage of the amyloid precursor protein (APP) by γ-secretase. At the beginning of a series of studies from our laboratories, a series of novel γ-amino alcohols (1) were found to possess γ-secretase inhibitory activity and Notch-sparing effects. A new one-pot synthesis of γ-amino alcohols and the structure-activity relationship (SAR) of these analogs will be discussed.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a7871e2efb9ec024eb8ebe67104c6219 https://doi.org/10.1016/j.bmcl.2016.03.042 Zobrazit plný text záznamu Full Text from ScienceDirect