N-alkylated galanthamine derivatives:: Potent acetylcholinesterase inhibitors from Leucojum aestivum

被引：62

作者：

Berkov, Strahil ^{[1
]}

Codina, Carles ^{[1
]}

Viladomat, Francesc ^{[1
]}

Bastida, Jaume ^{[1
]}

机构：

[1] Univ Barcelona, Fac Farm, Dept Prod Nat Biol Vegetal & Edafol, E-08028 Barcelona, Spain

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 07期

关键词：

Leucojum aestivum; Amaryllidaceae; AChE inhibitors; N-allylnorgalanthamine; N-(14-methylallyl)norgalanthamine;

D O I：

10.1016/j.bmcl.2008.03.008

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

N-(14-Methylallyl) norgalanthamine, a new natural compound, together with five known alkaloids: N-allylnorgalanthamine, galanthamine, epinorgalanthamine, narwedine, and lycorine were isolated from mother liquors (waste material) obtained after industrial production of galanthamine hydrobromide from Leucojum aestivum leaves. The structures of N-allylnorgalanthamine and N-(14-methylallyl) norgalanthamine were completely determined by H-1 and C-13 NMR spectroscopy and two-dimensional experiments. N-allylnorgalanthamine (IC50 = 0.18 mu M) and N-(14-methylallyl) norgalanthamine (IC50 = 0.16 mu M) inhibit AChE considerably more than the approved drug galanthamine (IC50 = 1.82 mu M). (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：2263 / 2266

页数：4

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