Phosphonamidate Compounds for Butyrylcholinesterase Selective Inhibitors,Bulletin of the Korean Chemical Society

当前位置： X-MOL 学术 › Bull. Korean Chem. Soc. › 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.)

Phosphonamidate Compounds for Butyrylcholinesterase Selective Inhibitors
Bulletin of the Korean Chemical Society ( IF 2.3 ) Pub Date : 2020-11-10 , DOI: 10.1002/bkcs.12126
Jintaek Oh ₁ , Jung‐Youl Park ₂ , Kyoung Chan Park ₁ , Ji Hyun Hwang ₁ , Jeong Ho Park ₁

Affiliation

To find a new type of cholinergic drug, phosphonamidate compounds 18–32 were synthesized using a click reaction between propargylated‐9,10‐Dihydro‐9‐oxa‐10‐phosphaphenanthrene‐10‐oxide (DOPO, 2) and substituted benzyl azide. Their inhibitory activity against butyrylcholinesterase (BuChE) and acetylcholinesterase (AChE) was evaluated. Compound 31 was the most active of the 15 compounds (IC₅₀ = 3.14 ± 0.02 μM for equine BuChE), whose IC₅₀ value was slightly lower than the IC₅₀ value of galantamine (IC₅₀ = 9.4 ± 2.50 for equine BuChE).

中文翻译：

丁酰胆碱酯酶选择性抑制剂的膦酰胺化合物

为了找到一种新型的胆碱能药物，使用炔丙基化的9,10-二氢-9-氧杂-10-磷杂菲-10-氧化物（DOPO，2）和取代的叠氮化苄之间的点击反应合成了膦酰胺化合物18–32。评价了它们对丁酰胆碱酯酶（BuChE）和乙酰胆碱酯酶（AChE）的抑制活性。化合物31是15种化合物中活性最高的（马类BuChE的IC ₅₀ = 3.14±0.02μM），其IC ₅₀值略低于加兰他敏的IC ₅₀值（马类BuChE的IC ₅₀ = 9.4±2.50）。

更新日期：2020-12-18

点击分享查看原文

点击收藏

阅读更多本刊新发论文本刊介绍/投稿指南