Optimization of Pyrazole-Based Activators of Kv3.1

High Resolution Image Download MS PowerPoint Slide Potentiators of the Kv3.1 voltage-gated potassium channel may have utility as therapies for certain CNS disorders. A SAR survey around a previously reported Kv3.1 activator scaffold led to the identification of compounds with superior potency and higher activation levels than reported molecules. We further demonstrated that these compounds show relevant activity in a patch-clamp electrophysiology assay. Together, the defined tractability in the chemotype and the promising biological activity indicate that these compounds may be leads for continued optimization toward therapies for neurological disorders.