PYRIDAZINE DERIVATIVES FOR INHIBITING BETA AMYLOID PEPTIDE PRODUCTION
The present invention relates to novel compounds that inhibit the production of β- amyloid peptide (1-42), processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated β-amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.
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Page/Page column 59-60
(2009/05/28)
Synthesis and structure-activity relationship of acrylamides as KCNQ2 potassium channel openers
A new class of acrylamides was synthesized, and the effects of these analogues on outward potassium current were evaluated by using two electrode voltage clamp recordings from Xenopus laevis oocytes expressing cloned mKCNQ2 channels. SAR studies indicated that the pharmacophore of the acrylamide series includes the (S) absolute configuration at the (1-phenyl)ethyl moiety and the α,β-unsaturated acrylamide functionality with a free NH. This study identified (S)-N-[1-(3-morpholin-4-yl-phenyl)-ethyl]-3-phenyl-acrylamide ((S)-1) and (S)-N-[1-(4-fluoro-3-morpholin-4-yl-phenyl)-ethyl]-3- (4-fluoro-phenyl)-acrylamide ((S)-2) as KCNQ2 openers for further electrophysiological evaluations. These two acrylamides demonstrated significant activity in the cortical spreading depression model of migraine as we reported previously.
Wu, Yong-Jin,He, Huan,Sun, Li-Qiang,L'Heureux, Alexandre,Chen, Jie,Dextraze, Pierre,Starrett Jr., John E.,Boissard, Christopher G.,Gribkoff, Valentin K.,Natale, Joanne,Dworetzky, Steven I.
p. 2887 - 2896
(2007/10/03)
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