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