Identification of a series of 1,3,4-oxadiazol-2-amines as potent alpha-7 agonists with efficacy in the novel object recognition model of cognition

Bioorg Med Chem Lett. 2012 May 15;22(10):3560-3. doi: 10.1016/j.bmcl.2012.03.040. Epub 2012 Mar 16.

Abstract

A series of α7 nicotinic acetylcholine receptor full-agonists with a 1,3,4-oxadiazol-2-amine core has been discovered. Systematic exploration of the structure-activity relationships for both α7 potency and selectivity with respect to interaction with the hERG channel are described. Further profiling led to the identification of compound 22, a potent full agonist showing efficacy in the novel object recognition model of cognition enhancement.

MeSH terms

  • Animals
  • Cognition / drug effects*
  • Dogs
  • Nicotinic Agonists / chemistry
  • Nicotinic Agonists / pharmacology*
  • Receptors, Nicotinic / drug effects*
  • alpha7 Nicotinic Acetylcholine Receptor

Substances

  • Nicotinic Agonists
  • Receptors, Nicotinic
  • alpha7 Nicotinic Acetylcholine Receptor