title: The design, synthesis and screening of a muscarinic acetylcholine receptor targeted compound library.
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.
authors.affiliation: Bayer CropScience GmbH, Werk Höchst, G836, D-65926 Frankfurt am Main, Germany.
authors.forename: Jürgen
authors.initials: J
authors.lastname: Benting
authors.forename: Merisa
authors.initials: M
authors.lastname: Leonhardt
authors.forename: Stephen D
authors.initials: SD
authors.lastname: Lindell
authors.forename: Jörg
authors.initials: J
authors.lastname: Tiebes
mesh_terms: 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
chemical_list: D016573:Agrochemicals; D007306:Insecticides; D018727:Muscarinic Antagonists; D011976:Receptors, Muscarinic