Channelpedia

PubMed 15603955


Referenced in Channelpedia wiki pages of: none

Automatically associated channels: KCNQ2 , Kv7.2



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

Authors: Alexandre L'Heureux, Alain Martel, Huan He, Jie Chen, Li-Qiang Sun, John E Starrett, Joanne Natale, Steven I Dworetzky, Ronald J Knox, David G Harden, David Weaver, Mark W Thompson, Yong-Jin Wu

Journal, date & volume: Bioorg. Med. Chem. Lett., 2005 Jan 17 , 15, 363-6

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/15603955


Abstract
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.