Abstract
In this work we report the discovery of new homo and hetero bis-piperazinyl-1-propanone derivatives as selective ligands for 5-HT7 over 5-HT1A receptor. These newly synthesized compounds possess a 4-arylpiperazine linked through an acyl spacer to another substituted piperazine system and were tested for their binding properties on human cloned 5-HT1A and 5-HT7 serotonin receptors. Among these, phenyl, 4- and 2-chlorophenyl, 2-methoxyphenyl, 2-pyridyl, and 2-pyrimidyl derivatives 15, 24, 25, and 27–29 displayed nanomolar affinity values for the 5-HT7 receptor (Ki 23.5–52.0 nM) and no affinity for the 5-HT1A receptor.
Original language | English |
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Pages (from-to) | 4052-4056 |
Number of pages | 5 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 26 |
Issue number | 16 |
DOIs | |
Publication status | Published - Aug 15 2016 |
Keywords
- 5-HT selective ligands
- Bivalent ligand approach
- Hetero bis-piperazine
- Homo bis-piperazine
- Serotonin receptors
ASJC Scopus subject areas
- Biochemistry
- Clinical Biochemistry
- Molecular Biology
- Molecular Medicine
- Organic Chemistry
- Drug Discovery
- Pharmaceutical Science