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2005
Pyrazole derivatives
R 0180
(S,E)-N-[1-(3-Heteroarylphenyl)ethyl]-3-(2-fluorophenyl)acrylamides: Synthesis
KCNQ2 Potassium Channel Opener Activity. — The synthesis and KCNQ2
20- 116 and
opener activity of a series of heteroaryl-substituted acrylamides [cf. (III), (VII), (XI)]
is described. Among this series, derivative (VII) appears to be the most potent, but least
efficacious opener of KCNQ2 channels, while derivative (XIa) exhibits the lowest potency, but highest efficacy. Pyrazole derivative (IIIa) exhibits balanced potency and
efficacy. — (WU*, Y.-J.; et al.; Bioorg. Med. Chem. Lett. 15 (2005) 2, 363-366; Dep.
Neurosci. Chem., Bristol-Myers Squibb Pharm. Res. Inst., Wallingford, CT 06492,
USA; Eng.) — R. Staver
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