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CC-BY - Uznanie autorstwaNew Piperazine Derivatives of 6-Acetyl-7-hydroxy-4-methylcoumarin as 5-HT1A Receptor Agents
| dc.abstract.en | 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 mode |
| dc.affiliation | Uniwersytet Warszawski |
| dc.contributor.author | Trzaskowski, Bartosz |
| dc.contributor.author | Bujalska-Zadrożny, Magdalena |
| dc.contributor.author | Dobrzycki, Łukasz |
| dc.contributor.author | Gryczka, Weronika |
| dc.contributor.author | Leśniak, Anna |
| dc.contributor.author | Ostrowska, Kinga |
| dc.date.accessioned | 2024-01-25T13:48:31Z |
| dc.date.available | 2024-01-25T13:48:31Z |
| dc.date.copyright | 2023-02-01 |
| dc.date.issued | 2023 |
| dc.description.accesstime | AT_PUBLICATION |
| dc.description.finance | Publikacja bezkosztowa |
| dc.description.number | 3 |
| dc.description.version | FINAL_PUBLISHED |
| dc.description.volume | 24 |
| dc.identifier.doi | 10.3390/IJMS24032779 |
| dc.identifier.issn | 1422-0067 |
| dc.identifier.uri | https://repozytorium.uw.edu.pl//handle/item/113610 |
| dc.identifier.weblink | https://www.mdpi.com/1422-0067/24/3/2779/pdf |
| dc.language | eng |
| dc.pbn.affiliation | chemical sciences |
| dc.relation.ispartof | International Journal of Molecular Sciences |
| dc.relation.pages | 2779 |
| dc.rights | CC-BY |
| dc.sciencecloud | nosend |
| dc.subject.en | 6-acetyl-7-hydroxy-4-methylcoumarin |
| dc.subject.en | CNS activity |
| dc.subject.en | crystal structure |
| dc.subject.en | piperazine |
| dc.subject.en | serotonin receptors |
| dc.title | New Piperazine Derivatives of 6-Acetyl-7-hydroxy-4-methylcoumarin as 5-HT1A Receptor Agents |
| dc.type | JournalArticle |
| dspace.entity.type | Publication |