Title of article
The synthesis and structure–activity relationships of 3-amino-4-benzylquinolin-2-ones: discovery of novel KCNQ2 channel openers
Author/Authors
Piyasena Hewawasam*[1]، نويسنده , , Nathan Chen، نويسنده , , Hao-Min Ding، نويسنده , , Joanne T. Natale، نويسنده , , Christopher G. Boissard، نويسنده , , Sarita Yeola، نويسنده , , Valentin K. Gribkoff، نويسنده , , John Starrett، نويسنده , , Steven I. Dworetzky، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
4
From page
1615
To page
1618
Abstract
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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794245
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