Referenced in: none

Automatically associated channels: Kv11.1

Title: 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.

Authors: John Skidmore, Zeenat Atcha, Emmanuelle Boucherat, Laura Castelletti, Deborah W Chen, Frank T Coppo, Leanne Cutler, Rachel M Dunsdon, Bronagh M Heath, Rio Hutchings, David N Hurst, Sahar Javed, Samuel Martin, Emma S L Maskell, David Norton, Darrel J Pemberton, Sally Redshaw, Richard Rutter, Sanjeet S Sehmi, Tiziana Scoccitti, Hannah E Temple, Pam Theobald, Robert W Ward, David M Wilson

Journal, date & volume: Bioorg. Med. Chem. Lett., 2012 May 15 , 22, 3560-3

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/22503248

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.