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Tytuł: Spirohydantion - new ligands of central serotonergic system
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This work is concerned with preparation of new spirohydantoin and 5-arylhydantoin deńvatives and their influence of central serotonergic transmission. In the introduction part, problems related to pathomechanism of depression, epidemiologie data, prognosis of disease extension and innovative approaches for the development of new antidepressant drugs were discussed. In the expeńmental part, the synthesis of arylpiperazinylalkyl denvatives of hydantoin was presented. Their modifications were performed at 5 position in tenninal amid fragment, at length of alkylene spacer between hydantoin and arylpiperazinyl moiety and also at phenyl ring substituents in the arylpiperazinyl moiety. For all the new 44 compounds experimental and theoretical lipophilicity descńptors were determined. The durability of selected compounds in acid and basie environment was examined. In the phannacological test in vitro the affinity towards CNS receptors (5-HT1A, 5-HT2A, D2 and a1) and serotonin transporter was evaluated. For selected compounds which have shown specially promising properties in in vitro tests, their anxiolytic and antidepressant activity were investigated. Furthermore, in molecular modeling study the interaction between selected structures and the 5-HT1A receptor model was analyzed. Based on nonparametric FreeWilson analysis with Fujita-Ban modification, structureactivity relat ; ionships in the group of spirohydantoin denvatives were studied. Among the obtained compounds, two of them are simultaneously 5-HT JA receptor and serotonin transporter ligands, that is very promising for design of novel compound series.
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Data ostatniej modyfikacji:
20 lip 2022
Data dodania obiektu:
21 lis 2012
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http://dl.cm-uj.krakow.pl:8080/publication/1035
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| Nazwa wydania | Data |
|---|---|
| ZB-107998 | 20 lip 2022 |
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