4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 12, Issue 13, Pages 1779-1783

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0960-894X(02)00240-8

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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. (C) 2002 Elsevier Science Ltd. All rights reserved.

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