International Journal of Biological Macromolecules p. 2725 - 2729 (2018)
Update date:2022-08-11
Topics:
Chen, Ke-Lin
Gan, Ling
Wu, Zhen-Hua
Qin, Jin-Fang
Liao, Wen-Xia
Tang, Huang
A series of 4- substituted sampangine derivatives (4-aminoalkylaminosampangine Ar–NH(CH2)nNR1R2) has been designed, synthesized, and tested for their ability to inhibit acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and β-myloid (Aβ) aggregation. The synthetic compounds exhibited high AChE inhibitory activity and a significant in vitro inhibitory potency toward the self-induced Aβ aggregation. While, treatment of SH-SY5Y cells overexpressing the Swedish mutant form of human β-amyloid precursor protein (APPsw) with derivatives was associated with significant reduction of Aβ42 secretion levels. Moreover, most of the synthetic compounds were predicted to be able to cross the blood-brain barrier (BBB) to reach their targets in the central nervous system (CNS) according to a parallel artificial membrane permeation assay for BBB. The result encourages us to study this class of compounds thoroughly and systematically.
View MoreOnlychem (Jinan)Biotech Co.,Ltd
Contact:86-531-83175885
Address:No. 44, Honglou South Road, Jinan,China
MedicalChem(Yancheng)Manuf.Co.,Ltd.
Contact:+86-515-84383366
Address:Touzeng BinHai, YanCheng City, JiangSu Province, China
Laohekou huacheng Trade Co., Ltd.
Contact:+86-710-8360685
Address:No. 85, Beijing Road, Laohekou City, Hubei Province, China
MedicalChem(Yancheng)Manuf.Co.,Ltd.
Contact:+86-515-84383366
Address:Touzeng BinHai, YanCheng City, JiangSu Province, China
Daqing New Century Fine Chemical Co., Ltd.
Contact:010-57126694
Address:No.39, jinxing cun, honggang district
Doi:10.1016/j.molcata.2014.09.001
(2014)Doi:10.1016/S0040-4039(98)00585-1
(1998)Doi:10.1016/j.bmcl.2016.05.003
(2016)Doi:10.1039/J29710000574
(1971)Doi:10.1007/BF00807570
(1996)Doi:10.1016/j.poly.2020.114382
(2020)