Synthesis,crystal structure and biological activity of novel analogues of tricyclic drugs |
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| Affiliation: | 1. Institute of Biochemistry and Biophysics, Polish Academy of Sciences, Pawińskiego 5a, 02-106 Warsaw, Poland;2. Department of Pharmacobiology, Faculty of Pharmacy, Jagiellonian University Medical College, 9 Medyczna Street, 30-688 Kraków, Poland;3. Department of Chemistry, University of Warsaw, Pasteura 1, 02-093 Warsaw, Poland;4. Biological and Chemical Research Centre, University of Warsaw, Żwirki i Wigury 101, 02-089 Warsaw, Poland;5. Maj Institute of Pharmacology, Polish Academy of Sciences, 12, Smętna Street, 31-343, Kraków, Poland;1. Biochemistry and Molecular Biology Department, Faculty of Pharmacy, Helwan University, P.O. Box 11795, Cairo, Egypt;2. Helwan Structural Biology Center for Excellence, Helwan University, P.O. Box, 11795, Cairo, Egypt;3. Pharmacology and Toxicology Department, Faculty of Pharmacy, Cairo University, P.O. Box 11562, Cairo, Egypt;4. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, P.O. Box 11795, Cairo, Egypt;5. Pharmaceutical Sciences Department, College of Pharmacy, Shaqra University, P.O. Box 11961, Dawadmi 11911, Saudi Arabia;6. Pharmacy Practice Department, College of Pharmacy, Shaqra University, P.O. Box 11961, Dawadmi 11911, Saudi Arabia;1. Section of Organic Chemistry and Biochemistry, Department of Chemistry, University of Ioannina, 451 10 Ioannina, Greece;2. Laboratory of Organic Chemistry, Department of Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis, 15771, Athens, Greece;1. U.O.C. Genetica Medica, IRCCS Istituto Giannina Gaslini, Via Gerolamo Gaslini 5, 16147 Genova, Italy;2. Dipartimento di Farmacia e Biotecnologie, Università di Bologna, Via Belmeloro 6, 40126 Bologna, Italy;1. School of Applied Sciences, RMIT University, Melbourne 3001, Australia;2. IICT-RMIT Research Centre SIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India;3. Division of Natural Products Chemistry, CSIR-IICT, Hyderabad 500 007, India;4. Health Innovations Research Institute, RMIT University, Melbourne 3083, Australia;5. Ian Potter NanoBioSensing Facility, NanoBiotechnology Research Laboratory, School of Applied Sciences, RMIT University, Melbourne 3000, Australia;6. Centre for Advanced Materials and Industrial Chemistry, RMIT University, Melbourne 3000, Australia |
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| 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 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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| Keywords: | SERT inhibitors 5 HT receptors Dibenzepine Tricyclic drugs |
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