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  • Title: Synthesis and binding properties of new long-chain 4-substituted piperazine derivatives as 5-HT₁A and 5-HT₇ receptor ligands.
    Author: Modica MN, Intagliata S, Pittalà V, Salerno L, Siracusa MA, Cagnotto A, Salmona M, Romeo G.
    Journal: Bioorg Med Chem Lett; 2015 Apr 01; 25(7):1427-30. PubMed ID: 25759032.
    Abstract:
    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 Ki values in the nanomolar range on both receptors, acting as dual ligands.
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