Synthesis and biological evaluation of 8-hydroxy- 2,7-naphthyridin-2-ium salts as novel inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE)

M. Schiedel; A. Fallarero; C. Luise; W. Sippl; P. Vuorela; M. Jung

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Synthesis and biological evaluation of 8-hydroxy- 2,7-naphthyridin-2-ium salts as novel inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE)

机译：8-羟基-2,7-萘啶-2-Ium盐作为乙酰胆碱酯酶（ACHE）和丁酰胆碱酯酶（BCHE）的新型抑制剂的合成及生物学评价

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By analogy with the natural product chelerythrine, which has been identified as an inhibitor of both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), we prepared a small series of 8-hydroxy-2,7- naphthyridin-2-ium salts. Spectroscopic analyses allowed us to elucidate the zwitterionic nature of 2,7- naphthyridin-1(7H)-ones, the neutral state of 8-hydroxy-2,7-naphthyridin-2-ium salts. Among the tested compounds, we identified dual inhibitors of AChE and BChE as well as an inhibitor showing a preferential inhibition of AChE over BChE. By in vitro characterization in combination with docking studies, we were able to identify structural features that influence the biological activity of 8-hydroxy-2,7-naphthyridin-2- ium salts.

机译：通过类似于天然产品的螯合剂，已被鉴定为乙酰胆碱酯酶（ACHE）和丁酰胆碱酯酶（BCHE）的抑制剂，我们制备了一系列的8-羟基-2,7-萘啶-2-Ium盐。光谱分析使我们允许阐明2,7-萘蓟蛋白-1（7h） - 酮的两性离子性质，其中性状态为8-羟基-2,7-萘啶-2- Ium盐。在测试的化合物中，我们鉴定了疼痛和BCHE的双重抑制剂以及显示在BCHE上疼痛的优先抑制的抑制剂。通过与对接研究组合的体外表征，我们能够识别影响8-羟基-2,7-萘啶-2- Ium盐的生物活性的结构特征。

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来源
《MedChemComm》 |2017年第2期|共6页
作者
M. Schiedel; A. Fallarero; C. Luise; W. Sippl; P. Vuorela; M. Jung;
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作者单位

Institute of Pharmaceutical Sciences University of Freiburg Albertstra?e 25 79104 Freiburg im Breisgau Germany;

Pharmaceutical Design and Discovery Research Group Division of Pharmaceutical Biosciences Faculty of Pharmacy University of Helsinki (UHEL) Helsinki Finland;

Institute of Pharmacy Martin-Luther-University Halle-Wittenberg Wolfgang- Langenbeck-Stra?e 4 06120 Halle (Saale) Germany;

Institute of Pharmacy Martin-Luther-University Halle-Wittenberg Wolfgang- Langenbeck-Stra?e 4 06120 Halle (Saale) Germany;

Pharmaceutical Design and Discovery Research Group Division of Pharmaceutical Biosciences Faculty of Pharmacy University of Helsinki (UHEL) Helsinki Finland;

Institute of Pharmaceutical Sciences University of Freiburg Albertstra?e 25 79104 Freiburg im Breisgau Germany;

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正文语种 eng
中图分类化学;
关键词
Synthesis; evaluation; (BChE);

机译：合成;评估;（左）;

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1. Synthesis and biological evaluation of 8-hydroxy- 2,7-naphthyridin-2-ium salts as novel inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) [J] . M. Schiedel, A. Fallarero, C. Luise, MedChemComm . 2017,第2期

机译：8-羟基-2,7-萘啶-2-Ium盐作为乙酰胆碱酯酶（ACHE）和丁酰胆碱酯酶（BCHE）的新型抑制剂的合成及生物学评价
2. Synthesis, docking study, and biological evaluation of novel umbellipherone/hymecromone derivatives as acetylcholinesterase/butyrylcholinesterase inhibitors [J] . Moradi Alireza, Faraji Laleh, Nadri Hamid, Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents . 2018,第7期

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3. Design, Synthesis, and Biological Evaluation of a New Series of Biphenyl/Bibenzyl Derivatives Functioning as Dual Inhibitors of Acetylcholinesterase and Butyrylcholinesterase [J] . Dong-mei Wang, Bo Feng, Hui Fu, Molecules . 2017,第1期

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4. Design, one-pot synthesis, and evaluation of 7H-thiazolo3,2-b-1,2,4-triazin-7-one derivatives as dual binding site acetylcholinesterase inhibitors [C] . Si-jie Liu, Lan-xiang Shi, Jing-yu He International Conference on Biotechnology, Chemical and Materials Engineering . 2014

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5. NG-nitro-L-arginine-containing peptidomimetics as selective neuronal nitric oxide synthase inhibitors. Structure-based design, synthesis, and biological evaluation and approaches toward enhanced CNS activity. [D] . Seo, Jiwon. 2006

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6. Synthesis and biological evaluation of 8-hydroxy-27-naphthyridin-2-ium salts as novel inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) [O] . M. Schiedel, A. Fallarero, C. Luise, 2017

机译：作为乙酰胆碱酯酶（AChE）和丁酰胆碱酯酶（BChE）的新型抑制剂的8-羟基-27-萘啶-2-盐的合成及生物学评价
7. Design, Synthesis, and Biological Evaluation of a New Series of Biphenyl/Bibenzyl Derivatives Functioning as Dual Inhibitors of Acetylcholinesterase and Butyrylcholinesterase [O] . Dong-mei Wang, Bo Feng, Hui Fu, 2017

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Synthesis and biological evaluation of 8-hydroxy- 2,7-naphthyridin-2-ium salts as novel inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE)

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