Design, synthesis and anti-Alzheimer′s disease activity of 5-akylaminomethyl substituted carbazole derivatives
10.11665/j.issn.1000-5048.20150602
- VernacularTitle:5-氨甲基咔唑衍生物的设计、合成及抗阿尔茨海默病活性
- Author:
Mengfei CHEN
1
;
Lei FANG
;
Li CHEN
Author Information
1. 中国药科大学天然药物化学教研室
- Publication Type:Journal Article
- Keywords:
carbazole derivatives;
Alzheimer′s disease;
ChE inhibitors;
neuroprotective effect;
multifunction
- From:
Journal of China Pharmaceutical University
2015;46(6):647-652
- CountryChina
- Language:Chinese
-
Abstract:
A series of carbazole derivatives were designed and synthesized via the introduction of various substituents on the carbazole template and the nitrogen atom using 5-aminomethyl substituted carbazole as the lead compound. The inhibitory activity towards AChE/BChE and the neuroprotective effect against Aβ-induced toxicity were evaluated by Ellman and MTT assay, respectively. Furthermore, the SAR of the target compounds was discussed. Among all the target compounds, compound 8a showed dual inhibitory activity toward both AChE and BChE, and could effectively protect PC12 cells from Aβ-induced toxicity, indicating compound 8a could be considered as a promising candidate against Alzheimer′s disease.
