The design, synthesis and screening of a muscarinic acetylcholine receptor targeted compound library |
| |
Authors: | Benting Jürgen Leonhardt Merisa Lindell Stephen D Tiebes Jörg |
| |
Institution: | Bayer CropScience GmbH, Werk H?chst, G836, D-65926 Frankfurt am Main, Germany. |
| |
Abstract: | 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. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|