期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 1, 页码 346-349出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.11.001
关键词
5-HT6 receptor ligands; Antagonists; Cognition; PK profile
N-1-Arylsulfonyl-3-piperazinyl indole derivatives were designed and identified as a novel class of 5-HT6 receptors ligands. All the compounds have high affinity and antagonist activity towards 5-HT6 receptor. The compound 7a (K-i = 3.4 nM, functional assay IC50 = 310 nM) shows enhanced cognitive effect when tested in NORT and Morris water maze models. Synthesis, SAR and PK profile of these novel compounds constitute the subject matter of this Letter. (C) 2010 Published by Elsevier Ltd.
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