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Synthesis, crystal structure and biological activity of novel analogues of tricyclic drugs.
Bieszczad, Bartosz; Siwek, Agata; Wilczek, Marcin; Trzybinski, Damian; Wozniak, Krzysztof; Satala, Grzegorz; Bojarski, Andrzej J; Mieczkowski, Adam.
Afiliación
  • Bieszczad B; Institute of Biochemistry and Biophysics, Polish Academy of Sciences, Pawinskiego 5a, 02-106 Warsaw, Poland. Electronic address: b.bieszczad@ibb.waw.pl.
  • Siwek A; Department of Pharmacobiology, Faculty of Pharmacy, Jagiellonian University Medical College, 9 Medyczna Street, 30-688 Kraków, Poland.
  • Wilczek M; Department of Chemistry, University of Warsaw, Pasteura 1, 02-093 Warsaw, Poland.
  • Trzybinski D; Biological and Chemical Research Centre, University of Warsaw, Zwirki i Wigury 101, 02-089 Warsaw, Poland.
  • Wozniak K; Biological and Chemical Research Centre, University of Warsaw, Zwirki i Wigury 101, 02-089 Warsaw, Poland.
  • Satala G; Maj Institute of Pharmacology, Polish Academy of Sciences, 12, Smetna Street, 31-343, Kraków, Poland.
  • Bojarski AJ; Maj Institute of Pharmacology, Polish Academy of Sciences, 12, Smetna Street, 31-343, Kraków, Poland.
  • Mieczkowski A; Institute of Biochemistry and Biophysics, Polish Academy of Sciences, Pawinskiego 5a, 02-106 Warsaw, Poland. Electronic address: amiecz@ibb.waw.pl.
Bioorg Med Chem Lett ; 30(21): 127493, 2020 11 01.
Article en En | MEDLINE | ID: mdl-32798652
A 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.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Receptores Histamínicos / Receptores de Serotonina / Receptores Dopaminérgicos / Lactamas / Antidepresivos Tricíclicos Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2020 Tipo del documento: Article Pais de publicación: Reino Unido
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Receptores Histamínicos / Receptores de Serotonina / Receptores Dopaminérgicos / Lactamas / Antidepresivos Tricíclicos Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2020 Tipo del documento: Article Pais de publicación: Reino Unido