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Diethoxyphosphoryloxy‐oleanolic acid is a nanomolar‐inhibitor of butyrylcholinesterase
Chemical Biology & Drug Design ( IF 3 ) Pub Date : 2024-03-14 , DOI: 10.1111/cbdd.14506
Anastasiya V. Petrova 1 , Alexandr I. Poptsov 1 , Niels V. Heise 2 , René Csuk 2 , Oxana B. Kazakova 1
Affiliation  

A series of new betulin, lupeol, erythrodiol, and oleanolic acid phosphoryloxy‐ and furoyloxy‐derivatives has been synthesized and their structure was confirmed by NMR spectroscopy. Synthesized compounds were subjected to Ellman's assays to determine their ability to inhibit the enzymes AChE and BChE. Among them, diethoxyphosphoryloxy‐oleanolic acid inhibited BChE with a value of 99%, thereby acting as a mixed‐type inhibitor holding very low Ki values of Ki = 6.59 nM and Ki’ = 1.97 nM, respectively.

中文翻译:

二乙氧基磷酰氧基齐墩果酸是丁酰胆碱酯酶的纳摩尔抑制剂

合成了一系列新的桦木醇、羽扇豆醇、高根二醇和齐墩果酸磷酰氧基和呋喃酰氧基衍生物,并通过核磁共振波谱证实了它们的结构。合成的化合物经过 Ellman 分析以确定其抑制 AChE 和 BChE 酶的能力。其中,二乙氧基磷酰氧基齐墩果酸对 BChE 的抑制率为 99%,因此可作为混合型抑制剂,K 值非常低Ki = 6.59 nM 和 K 的值' = 1.97 nM,分别。
更新日期:2024-03-14
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