Synthesis, crystal structure and biological activity of novel analogues of tricyclic drugs.
Basic Information
ID: ALA4665756
Journal: Bioorg Med Chem Lett
Title: Synthesis, crystal structure and biological activity of novel analogues of tricyclic drugs.
Authors: Bieszczad B,Siwek A,Wilczek M,Trzybiński D,Woźniak K,Satała G,Bojarski AJ,Mieczkowski A
Abstract: 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 H, serotonin receptors 5-HT, 5-HT, 5-HT, 5-HT, serotonin transporter (SERT) and dopamine receptor D 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 H receptor in sub-micromolar concentrations.
CiteXplore: 32798652
DOI: 10.1016/j.bmcl.2020.127493
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