Synthesis and binding properties of new long-chain 4-substituted piperazine derivatives as 5-HT1A and 5-HT7 receptor ligands
作者： Maria N Modica , Sebastiano Intagliata , Valeria Pittalà , Loredana Salerno , Maria A Siracusa
DOI: 10.1016/J.BMCL.2015.02.042
关键词: Chemistry 、 Piperazine 、 Aryl 、 5-HT receptor 、 Methylene 、 Stereochemistry 、 Quinazolinone 、 5-HT7 receptor 、 Quinazoline 、 Receptor
摘要: New long-chain 4-substituted piperazines linked to a thienopyrimidine or quinazoline system were synthesized and tested for their binding properties on human cloned 5-HT1A 5-HT7 serotonin receptors. Some structural modifications, concerning tree main portions, that is, terminal fragment, chain length, aryl substituents, examined. The 2- 3-substituted thienopyrimidinone quinazolinone systems selected as fragment length of four five methylene units was set. Explored substituents phenyl, phenylmethyl, 3- 4-chlorophenyl, 2-ethoxyphenyl. Title compounds showed affinity In particular, 2-ethoxyphenyl derivatives 40 45 displayed Ki values in the nanomolar range both receptors, acting dual ligands.
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