(S,E)-N-[1-(3-Heteroarylphenyl)ethyl]-3-(2-fluorophenyl)- acrylamides:: synthesis and KCNQ2 potassium channel opener activity

被引：8
作者：
L'Heureux, A
Martel, A
He, H
Chen, J
Sun, LQ
Starrett, JE
Natale, J
Dworetzky, SI
Knox, RJ
Harden, DG
Weaver, D
Thompson, MW
Wu, YJ
机构：
[1] Bristol Myers Squibb Pharmaceut Res Inst, Dept Neurosci Chem, Wallingford, CT 06492 USA
[2] Bristol Myers Squibb Pharmaceut Res Inst, Dept Med Chem, Candiac, PQ J5R 1J1, Canada
[3] Bristol Myers Squibb Pharmaceut Res Inst, Dept Neurosci Biol, Wallingford, CT 06492 USA
[4] Bristol Myers Squibb Pharmaceut Res Inst, Dept New Leads Biol, Wallingford, CT 06492 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 02期
关键词：
Acrylamides; KCNQ2;
D O I：
10.1016/j.bmcl.2004.10.065
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Replacement of the morpholinyl moiety in (S,E)-N-[1-(3-morpholinophenyl)ethyl]-3-phenylacrylamide (1) with heteroaryl groups led to the identification of (S,E)-N-1-[3-(6-fluoropyridin-3-yl)phenyl]ethyl-3-(2-fluorophenyl)acrylamide (5) as a potent KCNQ2 potassium channel opener. Among this series of heteroaryl substituted acrylamides, (S,E)-N-1-[3-(1H-pyrazol-1-yl)phenyl]ethyl-3-(2-fluorophenyl)acrylamide (9) exhibits balanced potency and efficacy. The syntheses and the KCNQ2 opener activity of this series of acrylamides are described. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码：363 / 366
页数：4
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