Synthesis and Biological Evaluation of Novel Jatrorrhizine Derivatives with Amino Groups Linked at the 3-Position as Inhibitors of Acetylcholinesterase
| Autor: | Nanqian Xiong, Xiaofei Jiang, Nengling Zhang, Yi Liu, Jianfeng Cao, ShengXiang Qiu |
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| Jazyk: | angličtina |
| Rok vydání: | 2017 |
| Předmět: |
Jatrorrhizine
Article Subject biology 010405 organic chemistry Aché Stereochemistry General Chemistry Coptis chinensis biology.organism_classification 01 natural sciences Acetylcholinesterase language.human_language 0104 chemical sciences lcsh:Chemistry 010404 medicinal & biomolecular chemistry chemistry.chemical_compound chemistry lcsh:QD1-999 language IC50 Lead compound Butyrylcholinesterase Biological evaluation |
| Zdroj: | Journal of Chemistry, Vol 2017 (2017) |
| ISSN: | 2090-9071 2090-9063 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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