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

Comb Chem High Throughput Screen. 2005 Nov;8(7):649-53. doi: 10.2174/138620705774575328.

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.

MeSH terms

  • Agrochemicals / chemical synthesis
  • Combinatorial Chemistry Techniques*
  • Inhibitory Concentration 50
  • Insecticides / chemical synthesis*
  • Insecticides / pharmacology
  • Muscarinic Antagonists / chemical synthesis*
  • Muscarinic Antagonists / pharmacology
  • Receptors, Muscarinic / chemistry
  • Structure-Activity Relationship

Substances

  • Agrochemicals
  • Insecticides
  • Muscarinic Antagonists
  • Receptors, Muscarinic