Synthesis and biological evaluation of new tetramethylpyrazine‐based chalcone derivatives as potential anti‐Alzheimer agents,Chemical Biology & Drug Design

当前位置： X-MOL 学术 › Chem. Bio. Drug Des. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

Synthesis and biological evaluation of new tetramethylpyrazine‐based chalcone derivatives as potential anti‐Alzheimer agents
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2018-07-23 , DOI: 10.1111/cbdd.13355
Meng Wang ₁ , Hua-Li Qin ₁ , Jing Leng ₁ , Ameeduzzafar ₂ , Muhammad Wahab Amjad ₃ , Maria Abdul Ghafoor Raja ₃ , Muhammad Ajaz Hussain ₄ , Syed Nasir Abbas Bukhari _{1,

2}

Affiliation

In the current study, a series of new ligustrazine‐based chalcones was synthesized. For insertion of tetramethylpyrazine (TMP, also designated as ligustrazine) in chemical backbone of chalcone, a new ligustrazine‐based aldehyde was prepared. New ketones were synthesized for inclusion of quinazolin‐4‐yl amino and pyrazin‐2‐yl amino moieties. The newly synthesized compounds were screened for acetylcholinesterase, butyrylcholinesterase, and monoamine oxidases (MAO) inhibitory activities and also for in vitro cytotoxicity on PC12 cells. The effect of these compounds against amyloid β‐induced cytotoxicity and aggregation was also investigated. The synthesized compounds effectively inhibited the related enzymes and also exhibited neuroprotective effects. Most of the compounds displayed better inhibitory potencies against Aβ aggregation than reference compounds. Some compounds such as 11e and 16b showed very potent effects on multiple targets exhibiting behavior as multifunctional anti‐Alzheimer agents.

中文翻译：

新的基于四甲基吡嗪的查尔酮衍生物作为潜在的抗阿尔茨海默病药物的合成和生物学评估

在当前的研究中，合成了一系列新的基于川new嗪的查耳酮。为了在查尔酮的化学骨架中插入四甲基吡嗪（TMP，也称为川gust嗪），制备了一种新的基于川gust嗪的醛。合成了新的酮，其中包括喹唑啉-4-基氨基和吡嗪-2-基氨基部分。筛选了新合成的化合物的乙酰胆碱酯酶，丁酰胆碱酯酶和单胺氧化酶（MAO）抑制活性，以及对PC12细胞的体外细胞毒性。还研究了这些化合物对β淀粉样蛋白诱导的细胞毒性和聚集的影响。所合成的化合物有效抑制相关酶，并且还表现出神经保护作用。与参考化合物相比，大多数化合物对Aβ聚集表现出更好的抑制作用。一些化合物，例如11e和16b对多种目标表现出非常有效的作用，这些目标表现出作为多功能抗阿尔茨海默病药物的行为。

更新日期：2018-07-23

点击分享查看原文

点击收藏

阅读更多本刊最新论文本刊介绍/投稿指南11