The design, synthesis and screening of a muscarinic acetylcholine receptor targeted compound library

被引：5

作者：

Benting, J ^{[1
]}

Leonhardt, M ^{[1
]}

Lindell, SD ^{[1
]}

Tiebes, J ^{[1
]}

机构：

[1] Bayer CropSci GmbH, Werk Hochst, D-65926 Frankfurt, Germany

来源：

COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING | 2005年 / 8卷 / 07期

关键词：

muscarinergic; muscarinic acetylcholine receptor agonist; oxime-ether library; insecticide;

D O I：

10.2174/138620705774575328

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Potent new agonists of the insect muscarinic acetylcholine receptor (mAChR) have been discovered by synthesizing and screening a library of 225 oxime ether amines. Library evaluation was facilitated by the development of a high throughput test enabling the rapid determination of muscarinic agonist activity. The most interesting compounds were the thiadiazole 17 and the isoxazole 24 which were potent muscarinic agonists (EC50 13 and 21 nM, respectively) and showed lead levels of insecticidal activity.

引用

页码：649 / 653

页数：5

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