Synthesis and screening for antiacetylcholinesterase activity of (1-benzyl-4-oxopiperidin-3-ylidene)methylindoles and -pyrroles related to donepezil

被引：60

作者：

Andreani, A ^{[1
]}

Cavalli, A ^{[1
]}

Granaiola, M ^{[1
]}

Guardigli, M ^{[1
]}

Leoni, A ^{[1
]}

Locatelli, A ^{[1
]}

Morigi, R ^{[1
]}

Rambaldi, M ^{[1
]}

Recanatini, M ^{[1
]}

Roda, A ^{[1
]}

机构：

[1] Univ Bologna, Dipartimento Sci Farmaceut, I-40126 Bologna, Italy

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2001年 / 44卷 / 23期

关键词：

D O I：

10.1021/jm0109356

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The design, synthesis, and rapid evaluation of a new class of acetylcholinesterase (AChE) inhibitors related to donepezil are reported. A molecular dynamics simulation of the complex between AChE and one representative compound of the series showed a possible inhibitor binding mode in which favorable interactions are formed between the benzylpiperidinone moiety and some active-site residues. The biochemical evaluation of this newly synthesized series was performed using a chemiluminescent method suitable for high-throughput screening.

引用

页码：4011 / 4014

页数：4

共 8 条

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