Tryptamine Derivatives of Sesquiterpene Lactones As Effective Β-Secretase 1 Inhibitors

Modification of eudesmane-type sesquiterpene lactones and their epoxy derivatives with tryptamines was carried out using the aza-Michael reaction. A series of conjugates was obtained and their inhibitory properties were assessed against the β-secretase activity, which limits the rate of β-amyloid peptide formation and is a promising target for the treatment of Alzheimer’s disease. It was found that compounds containing a 5-methoxytryptamine moiety show the greatest activity, reducing protease activity by 65–95