Synthesis and structure–activity relationship of novel cinnamamide derivatives as antidepressant agents |
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| Institution: | 1. Tianjin Tasly Academy, Tasly Holding Group Co., Ltd, Tianjin 300410, China;2. School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, China;1. Fakulteta za kemijo in kemijsko tehnologijo, Univerza v Ljubljani, A?ker?eva c. 5, 1000 Ljubljana, Slovenia;2. Ru?er Bo?kovi? Institute, Zagreb, Croatia;3. Institut des Matériaux Jean Rouxel, Université de Nantes, Cedex 3, France;4. Leiden Institute of Chemistry, Leiden University, Leiden, The Netherlands;5. Department of Chemistry, King Saud University, Riyadh, Saudi Arabia;1. Department of Chemistry, College of Science, King Saud University, Girls Section, P.O. Box 2457, Riyadh 11495, Saudi Arabia;2. National Organization for Drug Control and Research, Cairo, P.O. 29, Egypt;3. Department of Chemistry, Faculty of Science, University of Tabuk, Tabuk 71491, P.O. Box 741, Saudi Arabia;4. Chemistry Department, Faculty of Science, Cairo University, Giza, Egypt;1. Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt;2. Pharmaceutical Chemistry Department, Faculty of Pharmaceutical Sciences and Pharmaceutical Industries, Future University in Egypt, Cairo, Egypt;3. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, New Giza University, Newgiza, km 22 Cairo–Alexandria Desert Road, Cairo, Egypt;1. Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, Haryana, India;2. Department of Pharmaceutical Chemistry, JCDM College of Pharmacy, Sirsa, Haryana, India;1. Chemistry Department, Faculty of Science, Minia University, 61519 El-Minia, Egypt;2. Institute of Organic Chemistry, Karlsruhe Institute of Technology, Fritz-Haber-Weg 6, 76131 Karlsruhe, Germany;3. Laboratory of Inorganic Chemistry, Department of Chemistry, University of Helsinki, P.O. Box 55, 00014 Helsinki, Finland;4. Institute of Toxicology and Genetics, Karlsruhe Institute of Technology (KIT), Hermann-von-Helmholtz-Platz 1, D-76344 Eggenstein-Leopoldshafen, Germany |
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| Abstract: | Cinnamamide 3a, a leading compound with antidepressant-like activity, and its derivatives were synthesized and their antidepressant activity and structure–activity relationship were investigated. Most of the compounds with trifluoromethyl group in methylenedioxyphenyl moiety (3f, 4b–c and 6a–b) exhibited significant antidepressant activity, measured in terms of percentage decrease in immobility duration by tail suspension test. In addition, the dose-dependent antidepressant effect of the most potent compound 3f was subsequently confirmed in tail suspension test and forced swim test. The test results showed that 3f was equal to or more effective than the standard drug fluoxetine at a concentration of 10 mg/kg. Furthermore, compound 3f did not show any central nervous system stimulant properties in the open-field test and the preliminary results were promising enough to warrant further detailed antidepressant research around this scaffold. |
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| Keywords: | Cinnamamide derivatives Structure–activity relationship Antidepressant agents Tail suspension Forced swim |
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