Ufa Institute of Chemistry, Ufa Federal Research Centre, Russian Academy of Science, Ufa, Russia.
Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Halle (Saale), Germany.
Chem Biol Drug Des. 2024 Mar;103(3):e14506. doi: 10.1111/cbdd.14506.
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 K values of Ki = 6.59 nM and K ' = 1.97 nM, respectively.
一系列新型桦木醇、羽扇豆醇、赤藓醇和齐墩果酸的磷氧基和呋喃氧基衍生物已被合成，并通过 NMR 光谱确认了它们的结构。合成的化合物被进行了 Ellman 测定以确定它们抑制 AChE 和 BChE 酶的能力。其中，二乙氧基磷氧基齐墩果酸对 BChE 的抑制率达到 99%，因此作为一种混合型抑制剂，其 Ki 值分别低至 6.59 nM 和 K '值低至 1.97 nM。
