PubMed 20971003
Referenced in: none
Automatically associated channels: Kv11.1
Title: N-substituted pyrrolidines and tetrahydrofurans as novel AMPAR positive modulators.
Authors: Kevin M Thewlis, Laura Aldegheri, Mark H Harries, Claudette Mookherjee, Beatrice Oliosi, Simon E Ward
Journal, date & volume: Bioorg. Med. Chem. Lett., 2010 Dec 1 , 20, 7116-9
PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/20971003
Abstract
A series of novel AMPA receptor positive modulators displaying CNS penetration have been discovered with sub-micromolar activity and good selectivity over the cardiac channel receptor, hERG. We describe here the synthesis of these compounds which are biaryl pyrrolidine and tetrahydrofuran sulfonamides and disclose their activities against the human GluA2 flip isoform homotetrameric receptor.