- Gamma-lactams--a novel scaffold for highly potent and selective alpha 7 nicotinic acetylcholine receptor agonists.
Gamma-lactams--a novel scaffold for highly potent and selective alpha 7 nicotinic acetylcholine receptor agonists.
Bioorganic & medicinal chemistry letters (2009-02-12)
Albert Enz, Dominik Feuerbach, Mathias U Frederiksen, Conrad Gentsch, Konstanze Hurth, Werner Müller, Joachim Nozulak, Bernard L Roy
PMID19208472
ABSTRACT
A novel class of alpha7 nicotinic acetylcholine receptor (nAChR) agonists has been discovered through high-throughput screening. The cis gamma-lactam scaffold has been optimized to reveal highly potent and selective alpha7 nAChR agonists with in vitro activity and selectivity and with good brain penetration in mice.