Hewawasam Piyasena, Chen Nathan, Ding Min, Natale Joanne T, Boissard Christopher G, Yeola Sarita, Gribkoff Valentin K, Starrett John, Dworetzky Steven I
Department of Chemistry, The Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA.
Bioorg Med Chem Lett. 2004 Apr 5;14(7):1615-8. doi: 10.1016/j.bmcl.2004.01.073.
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.
3-氨基-4-苄基喹啉-2-酮已被鉴定为一类新型的KCNQ2通道开放剂。文中描述了其合成方法、构效关系以及作为非洲爪蟾卵母细胞中表达的克隆mKCNQ2通道激活剂的电生理评估。初步的构效关系数据表明，三氟甲基磺酰胺基和喹啉酮核上的吸电子取代基对于KCNQ2通道开放特性的表达均很重要。
