Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 30, Issue 21, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2020.127493
Keywords
SERT inhibitors; H-1 receptor; D-2 receptor; 5 HT receptors; Dibenzepine; Tricyclic drugs
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Funding
- MNiSW grant (Diamentowy Grant) [0072/DIA/2016/45]
- Centre for Preclinical Research and Technology (CePT)
- European Regional Development Fund
- Innovative Economy, The National Cohesion Strategy of Poland
- European Union from the European Regional Development Fund under the Operational Programme Innovative Economy, 2007-2013
- European Union under the European Regional Development Fund
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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-1, serotonin receptors 5-HT1A, 5-HT2A, 5-HT6, 5-HT7, serotonin transporter (SERT) and dopamine receptor D-2 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-1 receptor in sub-micromolar concentrations.
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