Synthesis and binding properties of new long-chain 4-substituted piperazine derivatives as 5-HT1A and 5-HT7 receptor ligands

Add time:08/25/2019    Source:sciencedirect.com

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.

We also recommend Trading Suppliers and Manufacturers of {4-(4-Chlorophenyl)Phenylmethyl}-1- (cas 132800-11-4). Pls Click Website Link as below: cas 132800-11-4 suppliers

Prev:Gallium(III) selective sensors based on 2-amino-3-(α-N-phenylmethyl-2′-amino-1′,4′-naphthoquinonyl)-1,4 naphthoquinones in poly (vinyl chloride)
Next:Identification, structure–activity relationships and molecular modeling of potent triamine and piperazine opioid ligands)