N-pyridyl and pyrimidine benzamides as KCNQ2/Q3 potassium channel openers for the treatment of epilepsy

…, G McNaughton-Smith, AD Wickenden…

文献索引：Amato, George; Roeloffs, Rosemarie; Rigdon, Greg C.; Antonio, Brett; Mersch, Theresa; McNaughton-Smith, Grant; Wickenden, Alan D.; Fritch, Paul; Suto, Mark J. ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 6 p. 481 - 484

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被引用次数: 17

摘要

A series of N-pyridyl benzamide KCNQ2/Q3 potassium channel openers were identified and found to be active in animal models of epilepsy and pain. The best compound 12 [ICA- 027243, N-(6-chloro-pyridin-3-yl)-3, 4-difluoro-benzamide] has an EC50 of 0.38 μM and is selective for KCNQ2/Q3 channels. This compound was active in several rodent models of epilepsy and pain but upon repeated dosing had a number of unacceptable toxicities that ...