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

Abstract

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.

Anticancer activities of a β-amino alcohol ligand and nanoparticles of its copper(ii) and zinc(ii) complexes evaluated by experimental and theoretical methods

“… 5,6 The γ-secretase inhibitory activity and notch-sparing effects were reported for some γ-amino alcohols. 7 β-Amino alcohols have been used as intermediates and chiral auxiliaries in organic synthesis, 8,9 as well as organocatalysts. 10 Amino alcohols such as mono- and diethanolamine are known to fix CO 2 and are used as absorbents for the chemical absorption of CO 2 .…”

Coordination of an amino alcoholic Schiff base ligand toward the zinc(II) ion: spectral, structural, theoretical, and docking studies

“…The γ-secretase inhibitory activity and Notch-sparing effects were reported for some γamino alcohols [2]. Some of them are used as active pharmaceutical ingredients (API's) such as αand/or β-adrenergic agonists [3,4], HIV protease inhibitors [5] and antihypertensive activity by blocking the αand/or β-adrenergic receptors [6,7].…”

Highly Efficient Synthesis of 1-Thioamidoalkyl-2-naphthols and 14-Aryl-14H-dibenzo[a,j]xanthenes using a Novel Ionic Liquid: Catalyst Preparation, Characterization and Performing the Reactions

“…The 1-thioamidoalkyl-2-naphthol derivatives are of significance as they can be readily converted to biologically important compounds namely γ-amino alcohols which show hypotensive, bradycardia, antipain, antibacterial, secretase inhibitory and notch-sparing activities [14][15][16][17]. The general method for synthesis of 1-thioamidoalkyl-2-naphthols involves the condensation reaction of arylaldehydes with 2-naphthol and thioacetamide in the presence of a catalyst [18][19][20][21][22][23][24][25].…”