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The synthesis and structure-activity relationships of 3-amino-4-benzylquinolin-2-ones; discovery of novel KCNQ2 channel openers.

Piyasena Hewawasam, Nathan Chen, Min Ding, Joanne T Natale, Christopher G Boissard, Sarita Yeola, Valentin K Gribkoff, John Starrett, Steven I Dworetzky

Bioorg. Med. Chem. Lett., 2004 Apr 5 , 14, 1615-8

3-amino-4-benzylquinolin-2-ones have been identified as a novel class of KCNQ2 channel openers. Synthesis and SAR is described along with their electrophysiological evaluation as activators of the cloned mKCNQ2 channel expressed in Xenopus laevis oocytes. The preliminary SAR data suggest the importance of both the trifluoromethylsulfonamido group and electron-withdrawing substituents on the quinolone nucleus for expression of KCNQ2 channel opening properties.