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- Title
New Piperazine Derivatives of 6-Acetyl-7-hydroxy-4-methylcoumarin as 5-HT 1A Receptor Agents.
- Authors
Ostrowska, Kinga; Leśniak, Anna; Gryczka, Weronika; Dobrzycki, Łukasz; Bujalska-Zadrożny, Magdalena; Trzaskowski, Bartosz
- Abstract
A series of 15 new derivatives of 6-acetyl-7-hydroxy-4-methylcoumarin containing a piperazine group were designed with the help of computational methods and were synthesized to study their affinity for the serotonin 5-HT1A and 5-HT2A receptors. Among them, 6-acetyl-7-{4-[4-(3-bromophenyl)piperazin-1-yl]butoxy}-4-methylchromen-2-one (4) and 6-acetyl-7-{4-[4-(2-chlorophenyl)piperazin-1-yl]butoxy}-4-methylchromen-2-one (7) exhibited excellent activity for 5-HT1A receptors with Ki values 0.78 (0.4–1.4) nM and 0.57 (0.2–1.3) nM, respectively, comparable to the Ki values of 8-OH-DPAT (0.25 (0.097–0.66) nM). The equilibrium dissociation constant values of the tested compounds showed differential intrinsic activities of the agonist and antagonist modes.
- Subjects
PIPERAZINE; SEROTONIN receptors; SEROTONIN
- Publication
International Journal of Molecular Sciences, 2023, Vol 24, Issue 3, p2779
- ISSN
1661-6596
- Publication type
Article
- DOI
10.3390/ijms24032779