RT journal article
T1 Structure-activity relationship study of diterpenes for treatment of Alzheimer’s disease
A1 Franco dos Santos, Gabriel
A1 Gomes Pereira, Rondinelle
A1 Diamantino Boaventura, Maria Amélia
A1 Macías Domínguez, Francisco Antonio
A1 Silva Lima, Gesiane de
A1 Soares Coelho, Amanda Cristina
A1 González Molinillo, José María
A1 Cala Peralta, Antonio
A1 Aparecida Takahashi, Jacqueline
A2 Química Orgánica
K1 kaurane diterpenes
K1 acetylcholinesterase inhibitors
K1 Alzheimer's disease
AB Alzheimer’s disease is an irreversible, degenerative and age-related disease which is growing more and more with the increase in life expectancy. Kaurane diterpenes are a class of natural products available in large amounts in nature and isolated from plants grown worldwide. In the present work¸ twenty-seven kaurane diterpenes of natural origin and some readily available derivatives were assayed for acetylcholinesterase inhibition and the structure-activity relationship was analyzed. The kaurenoic acid derivatives screened showed to be promising inhibitors of AChE, which could provide new leads for drugs to fight Alzheimer’s disease symptoms. Among them, eleven compounds showed activities comparable or higher than the positive control galantamine. Existence of an allylic hydroxyl group showed to be an important structural feature for AChE inhibition. In addition, presence of free hydroxyl groups at C-17 and C-19, furnished a diol especially active, able to completely inhibit AChE.
PB PubliSBQ
SN 1678-7064
YR 2017
FD 2017-08-29
LK http://hdl.handle.net/10498/35660
UL http://hdl.handle.net/10498/35660
LA eng
DS Repositorio Institucional de la Universidad de Cádiz
RD 07-nov-2026