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Synthesis and Biological Evaluation of Novel Jatrorrhizine Derivatives with Amino Groups Linked at the 3-Position as Inhibitors of Acetylcholinesterase
Joint Authors
Jiang, Xiaofei
Zhang, Nengling
Xiong, Nanqian
Liu, Yi
Cao, Jianfeng
Qiu, Shengxiang
Source
Issue
Vol. 2017, Issue 2017 (31 Dec. 2017), pp.1-6, 6 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2017-12-13
Country of Publication
Egypt
No. of Pages
6
Main Subjects
Abstract EN
Jatrorrhizine was considered as one of the active constituents of Coptis chinensis Franch.
Herein, jatrorrhizine derivatives with substituted amino groups linked at the 3-position were designed, synthesized, and biologically evaluated as inhibitors of acetylcholinesterase.
Jatrorrhizine derivatives inhibited the activity of acetylcholinesterase (AChE) to a greater extent than the lead compound jatrorrhizine.
All these jatrorrhizine derivatives were proved to be potent inhibitors of acetylcholinesterase (AChE) with submicromolar IC50 values, but less sensitive to butyrylcholinesterase (BuChE), which suggests that these jatrorrhizine derivatives are selective for AChE/BuChE.
Compound 3g gave the most potent inhibitor activity for AChE (IC50 = 0.301 μM), which is greater than the lead compound jatrorrhizine.
All these results demonstrated that these jatrorrhizine derivatives are potential inhibitors for AChE.
American Psychological Association (APA)
Jiang, Xiaofei& Zhang, Nengling& Xiong, Nanqian& Liu, Yi& Cao, Jianfeng& Qiu, Shengxiang. 2017. Synthesis and Biological Evaluation of Novel Jatrorrhizine Derivatives with Amino Groups Linked at the 3-Position as Inhibitors of Acetylcholinesterase. Journal of Chemistry،Vol. 2017, no. 2017, pp.1-6.
https://search.emarefa.net/detail/BIM-1171659
Modern Language Association (MLA)
Jiang, Xiaofei…[et al.]. Synthesis and Biological Evaluation of Novel Jatrorrhizine Derivatives with Amino Groups Linked at the 3-Position as Inhibitors of Acetylcholinesterase. Journal of Chemistry No. 2017 (2017), pp.1-6.
https://search.emarefa.net/detail/BIM-1171659
American Medical Association (AMA)
Jiang, Xiaofei& Zhang, Nengling& Xiong, Nanqian& Liu, Yi& Cao, Jianfeng& Qiu, Shengxiang. Synthesis and Biological Evaluation of Novel Jatrorrhizine Derivatives with Amino Groups Linked at the 3-Position as Inhibitors of Acetylcholinesterase. Journal of Chemistry. 2017. Vol. 2017, no. 2017, pp.1-6.
https://search.emarefa.net/detail/BIM-1171659
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1171659