Quinolizidinone carboxylic acid selective M1 allosteric modulators: SAR in the piperidine series

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1710-5. doi: 10.1016/j.bmcl.2011.01.094. Epub 2011 Jan 28.

Abstract

SAR study of the piperidine moiety in a series of quinolizidinone carboxylic acid M(1) positive allosteric modulators was examined. While the SAR was generally flat, compounds were identified with high CNS exposure to warrant additional in vivo evaluation.

MeSH terms

  • Allosteric Regulation
  • Animals
  • CHO Cells
  • Cricetinae
  • Cricetulus
  • Dose-Response Relationship, Drug
  • Piperidines / metabolism
  • Piperidines / pharmacology*
  • Structure-Activity Relationship

Substances

  • Piperidines