期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 25, 期 7, 页码 1427-1430出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2015.02.042
关键词
Serotonin; 5-HT1A; 5-HT7; Ligands; Binding properties
资金
- Italian MIUR
- University of Catania, Italy
New long-chain 4-substituted piperazines linked to a thienopyrimidine or a quinazoline system were synthesized and tested for their binding properties on human cloned 5-HT1A and 5-HT7 serotonin receptors. Some structural modifications, concerning tree main portions, that is, terminal fragment, chain length, and aryl substituents, were examined. The 2-and 3-substituted thienopyrimidinone and quinazolinone systems were selected as terminal fragment and a chain length of four or five methylene units was set. Explored aryl substituents were phenyl, phenylmethyl, 3-or 4-chlorophenyl, and 2-ethoxyphenyl. Title compounds showed affinity for 5-HT1A and 5-HT7 receptors. In particular, 2-ethoxyphenyl derivatives 40 and 45 displayed K-i values in the nanomolar range on both receptors, acting as dual ligands. (C) 2015 Elsevier Ltd. All rights reserved.
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