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Combinatorial Chemistry & High Throughput Screening

Editor-in-Chief

ISSN (Print): 1386-2073
ISSN (Online): 1875-5402

The Design, Synthesis and Screening of a Muscarinic Acetylcholine Receptor Targeted Compound Library

Author(s): Jurgen Benting, Merisa Leonhardt, Stephen D. Lindell and Jorg Tiebes

Volume 8, Issue 7, 2005

Page: [649 - 653] Pages: 5

DOI: 10.2174/138620705774575328

Price: $65

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: muscarinergic, muscarinic acetylcholine receptor agonist, oxime-ether library, insecticide


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