The Synthesis and Structure-Activity Relationships of 4-Aryl-3-aminoquinolin-2-ones: A New Class of Calcium-Dependent, Large Conductance, Potassium (Maxi-K) Channel Openers Targeted for Post-Stroke Neuroprotection.

A series of 4-aryl-3-aminoquinoline-2-one derivatives was synthesized and evaluated as activators of the cloned maxi-K channel mSlo (hSlo) expressed in Xenopus laevis oocytes using electrophysiological methods. A brain penetrable activator of maxi-K channels was identified and shown to be significantly active in the MCAO model of stroke.