The design, synthesis and screening of a muscarinic acetylcholine receptor targeted compound library.
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.
Benting
Jürgen
J
Bayer CropScience GmbH, Werk Höchst, G836, D-65926 Frankfurt am Main, Germany.
Leonhardt
Merisa
M
Lindell
Stephen D
SD
Tiebes
Jörg
J
D016573:Agrochemicals / Q000138:chemical synthesis; D020650:Combinatorial Chemistry Techniques; D020128:Inhibitory Concentration 50; D007306:Insecticides / Q000138:chemical synthesis* / Q000494:pharmacology; D018727:Muscarinic Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D011976:Receptors, Muscarinic / Q000737:chemistry; D013329:Structure-Activity Relationship
D016573:Agrochemicals; D007306:Insecticides; D018727:Muscarinic Antagonists; D011976:Receptors, Muscarinic