Synthesis and structure-activity relationship of acrylamides as KCNQ2 potassium channel openers

…, LQ Sun, A L'Heureux, J Chen, P Dextraze…

文献索引：Wu, Yong-Jin; He, Huan; Sun, Li-Qiang; L'Heureux, Alexandre; Chen, Jie; Dextraze, Pierre; Starrett Jr., John E.; Boissard, Christopher G.; Gribkoff, Valentin K.; Natale, Joanne; Dworetzky, Steven I. Journal of Medicinal Chemistry, 2004 , vol. 47, # 11 p. 2887 - 2896

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被引用次数: 40

摘要

A new class of acrylamides was synthesized, and the effects of these analogues on outward potassium current were evaluated by using two electrode voltage clamp recordings from Xenopus laevis oocytes expressing cloned mKCNQ2 channels. SAR studies indicated that the pharmacophore of the acrylamide series includes the (S) absolute configuration at the (1- phenyl) ethyl moiety and the α, β-unsaturated acrylamide functionality with a free NH. This ...