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Synthesis, crystal structure and biological activity of novel analogues of tricyclic drugs.

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dc.abstract.enA series of fourteen novel, eight-membered lactam- and dilactam-based analogues of tricyclic drugs were obtained in a simple one-pot procedure. Crystal structures of two compounds were determined by single-crystal X-ray diffraction analysis and their selected structural features were discussed and compared with those of imipramine and dibenzepine. Affinity of developed molecules for histamine receptor H1, serotonin receptors 5-HT1A, 5-HT2A, 5-HT6, 5-HT7, serotonin transporter (SERT) and dopamine receptor D2 was determined. The commercial drug dibenzepine was also checked on these molecular targets, as its mechanism of action is largely unknown. Two derivatives of 11,12-dihydrodibenzo[b,f]azocin-6(5H)-one (7,8) and two of dibenzo[b,f]azocin-6(5H)-one (9,10) were found to be active toward the H1 receptor in sub-micromolar concentrations.
dc.affiliationUniwersytet Warszawski
dc.contributor.authorSiwek, Agata
dc.contributor.authorBieszczad, Bartosz
dc.contributor.authorSatała, Grzegorz
dc.contributor.authorBojarski, Andrzej
dc.contributor.authorWilczek, Marcin
dc.contributor.authorTrzybiński, Damian
dc.contributor.authorWoźniak, Krzysztof
dc.contributor.authorMieczkowski, Adam
dc.date.accessioned2024-01-26T09:26:39Z
dc.date.available2024-01-26T09:26:39Z
dc.date.issued2020
dc.description.financePublikacja bezkosztowa
dc.description.number21
dc.description.volume30
dc.identifier.doi10.1016/J.BMCL.2020.127493
dc.identifier.issn0960-894X
dc.identifier.urihttps://repozytorium.uw.edu.pl//handle/item/121296
dc.identifier.weblinkhttps://www.sciencedirect.com/science/article/pii/S0960894X20306041
dc.languageeng
dc.pbn.affiliationchemical sciences
dc.relation.ispartofBioorganic and Medicinal Chemistry Letters
dc.relation.pages127493 (1-6)
dc.rightsClosedAccess
dc.sciencecloudnosend
dc.subject.enSERT inhibitors
dc.subject.enH1 receptor
dc.subject.enD2 receptor
dc.subject.en5 HT receptors
dc.subject.enDibenzepine
dc.subject.enTricyclic drugs
dc.titleSynthesis, crystal structure and biological activity of novel analogues of tricyclic drugs.
dc.typeJournalArticle
dspace.entity.typePublication