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Evaluation of 1-arylpiperazine derivative of hydroxybenzamides as 5-HT1A and 5-HT7 serotonin receptor ligands: An experimental and molecular modeling approach

✍ Scribed by Piotr Kowalski; Jolanta Jaśkowska; Andrzej J. Bojarski; Beata Duszyńska; Adam Bucki; Marcin Kołaczkowski

Publisher
Journal of Heterocyclic Chemistry
Year
2010
Tongue
English
Weight
257 KB
Volume
48
Category
Article
ISSN
0022-152X

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✦ Synopsis

The synthesis and evaluation as 5-HT 1A and 5-HT 7 serotonin receptor ligands of the two sets of O-substituted hydroxybenzamides, structurally related to 2-{3-[4-(2-methoxyphenyl)piperazin-1-yl]pro-poxy}benzamide (1), (K i 5-HT 1A ¼ 21 nM, 5-HT 7 ¼ 234 nM) are reported. To affect the affinity for 5-HT 1A and 5-HT 7 receptors, an amide moiety (2-6) and a hydrocarbon chain length (7-10) were modified. The serotonergic activity of compounds 2-10 was generally higher in the case of 5-HT 1A receptors compared with 5-HT 7 ones; the most active 5-HT 1A ligands being meta-isomer 2 (K i ¼ 7 nM) and both analogs of 1 with the longest spacer, i.e., penta-and hexa-methylene derivatives 9 and 10 (K i ¼ 4 and 3 nM, respectively). The observed biological properties of compounds 1-10 were elucidated using molecular modeling procedures.

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