Synthesis and chemiluminescent high throughput screening for inhibition of acetylcholinesterase activity by imidazo[2,1-b]thiazole derivatives

被引：16

作者：

Andreani, A ^{[1
]}

Granaiola, M ^{[1
]}

Guardigli, M ^{[1
]}

Leoni, A ^{[1
]}

Locatelli, A ^{[1
]}

Morigi, R ^{[1
]}

Rambaldi, M ^{[1
]}

Roda, A ^{[1
]}

机构：

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

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2005年 / 40卷 / 12期

关键词：

imidazo[2,1-b]thiazole; bisammonium salts; chemiluminescence; antiacetylcholinesterase activity; neuromuscular transmission; Alzheimer's disease; miastenia gravis; glaucoma;

D O I：

10.1016/j.ejmech.2005.05.010

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

The synthesis of a new series of imidazo[2,1-b]thiazole derivatives is described. They were tested as acetylcholinesterase inhibitors by means of a chemiluminescent method suitable for high throughput screening. The compounds without quaternization had no appreciable inhibitory potency probably because they are poorly soluble in water. The corresponding quaternized compounds were good inhibitors with activity related to the spacer employed. (c) 2005 Elsevier SAS. All rights reserved.

引用

页码：1331 / 1334

页数：4

共 15 条

[1]

Synthesis of 6-methylimidazo[2,1-b]thiazole derivatives acting on neuromuscular transmission [J].