Discovery of novel rivastigmine-hydroxycinnamic acid hybrids as multi-targeted agents for Alzheimer's disease

Ziwei Chen; Maria Digiacomo; Yalin Tu; Qiong Gu; Shengnan Wang; Xiaohong Yang; Jiaqi Chu; Qiuhe Chen; Yifan Han; Jingkao Chen; Giulia Nesi; Simona Sestito; Marco Macchia; Simona Rapposelli; Rongbiao Pi

doi:10.1016/j.ejmech.2016.09.052

Discovery of novel rivastigmine-hydroxycinnamic acid hybrids as multi-targeted agents for Alzheimer's disease

Ziwei Chen
, Maria Digiacomo
, Yalin Tu
, Qiong Gu
, Shengnan Wang
, Xiaohong Yang
, Jiaqi Chu
, Qiuhe Chen
, Yifan Han
, Jingkao Chen
, Giulia Nesi
, Simona Sestito
, Marco Macchia
, Simona Rapposelli
, Rongbiao Pi

Research output: Journal article publication › Journal article › Academic research › peer-review

73 Citations (Scopus)

Abstract

The new compounds exerted antioxidant neuroprotective properties and good cholinesterases (ChE) inhibitory activities. Some of them also inhibited amyloid protein (Aβ) aggregation. In particular, compound 5 emerged as promising drug candidates endowed with neuroprotective potential, ChE inhibitory, Aβ self-aggregation inhibitory and copper chelation properties. These data suggest that compound 5 offers an attractive starting point for further lead optimization in the drug-discovery process against AD.

Original language	English
Pages (from-to)	784-792
Number of pages	9
Journal	European Journal of Medicinal Chemistry
Volume	125
DOIs	https://doi.org/10.1016/j.ejmech.2016.09.052
Publication status	Published - 1 Jan 2017

Keywords

Alzheimer's disease
Caffeic acid
Ferulic acid
Hybrid
Multifunctional agents
Rivastigmine

ASJC Scopus subject areas

Pharmacology
Drug Discovery
Organic Chemistry

More information

10.1016/j.ejmech.2016.09.052

Cite this

Chen, Z., Digiacomo, M., Tu, Y., Gu, Q., Wang, S., Yang, X., Chu, J., Chen, Q., Han, Y., Chen, J., Nesi, G., Sestito, S., Macchia, M., Rapposelli, S., & Pi, R. (2017). Discovery of novel rivastigmine-hydroxycinnamic acid hybrids as multi-targeted agents for Alzheimer's disease. European Journal of Medicinal Chemistry, 125, 784-792. https://doi.org/10.1016/j.ejmech.2016.09.052

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abstract = "The new compounds exerted antioxidant neuroprotective properties and good cholinesterases (ChE) inhibitory activities. Some of them also inhibited amyloid protein (Aβ) aggregation. In particular, compound 5 emerged as promising drug candidates endowed with neuroprotective potential, ChE inhibitory, Aβ self-aggregation inhibitory and copper chelation properties. These data suggest that compound 5 offers an attractive starting point for further lead optimization in the drug-discovery process against AD.",

keywords = "Alzheimer's disease, Caffeic acid, Ferulic acid, Hybrid, Multifunctional agents, Rivastigmine",

author = "Ziwei Chen and Maria Digiacomo and Yalin Tu and Qiong Gu and Shengnan Wang and Xiaohong Yang and Jiaqi Chu and Qiuhe Chen and Yifan Han and Jingkao Chen and Giulia Nesi and Simona Sestito and Marco Macchia and Simona Rapposelli and Rongbiao Pi",

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doi = "10.1016/j.ejmech.2016.09.052",

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Chen, Z, Digiacomo, M, Tu, Y, Gu, Q, Wang, S, Yang, X, Chu, J, Chen, Q, Han, Y, Chen, J, Nesi, G, Sestito, S, Macchia, M, Rapposelli, S & Pi, R 2017, 'Discovery of novel rivastigmine-hydroxycinnamic acid hybrids as multi-targeted agents for Alzheimer's disease', European Journal of Medicinal Chemistry, vol. 125, pp. 784-792. https://doi.org/10.1016/j.ejmech.2016.09.052

TY - JOUR

T1 - Discovery of novel rivastigmine-hydroxycinnamic acid hybrids as multi-targeted agents for Alzheimer's disease

AU - Chen, Ziwei

AU - Digiacomo, Maria

AU - Tu, Yalin

AU - Gu, Qiong

AU - Wang, Shengnan

AU - Yang, Xiaohong

AU - Chu, Jiaqi

AU - Chen, Qiuhe

AU - Han, Yifan

AU - Chen, Jingkao

AU - Nesi, Giulia

AU - Sestito, Simona

AU - Macchia, Marco

AU - Rapposelli, Simona

AU - Pi, Rongbiao

PY - 2017/1/1

Y1 - 2017/1/1

N2 - The new compounds exerted antioxidant neuroprotective properties and good cholinesterases (ChE) inhibitory activities. Some of them also inhibited amyloid protein (Aβ) aggregation. In particular, compound 5 emerged as promising drug candidates endowed with neuroprotective potential, ChE inhibitory, Aβ self-aggregation inhibitory and copper chelation properties. These data suggest that compound 5 offers an attractive starting point for further lead optimization in the drug-discovery process against AD.

AB - The new compounds exerted antioxidant neuroprotective properties and good cholinesterases (ChE) inhibitory activities. Some of them also inhibited amyloid protein (Aβ) aggregation. In particular, compound 5 emerged as promising drug candidates endowed with neuroprotective potential, ChE inhibitory, Aβ self-aggregation inhibitory and copper chelation properties. These data suggest that compound 5 offers an attractive starting point for further lead optimization in the drug-discovery process against AD.

KW - Alzheimer's disease

KW - Caffeic acid

KW - Ferulic acid

KW - Hybrid

KW - Multifunctional agents

KW - Rivastigmine

UR - https://www.scopus.com/pages/publications/84991434295

U2 - 10.1016/j.ejmech.2016.09.052

DO - 10.1016/j.ejmech.2016.09.052

M3 - Journal article

SN - 0223-5234

VL - 125

SP - 784

EP - 792

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

ER -

Discovery of novel rivastigmine-hydroxycinnamic acid hybrids as multi-targeted agents for Alzheimer's disease

Abstract

Keywords

ASJC Scopus subject areas

More information

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