A Synthetic Approach towards Novel Series of 3-(3-(1-piperazinyl)propyl -1h-indole Derivatives as Monoaminergic Multi-target Agents. Docking Studies and Pharmacological Evaluation at Sert, D2, and Mao-a Receptors
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چکیده
-------------------------------------------------------------------------------------------------------------------------------------------------------------------------------------------------------------------Major depression is a common, heterogeneous and often incapacitating disorder triggered by a complex pattern of genetic, epigenetic, developmental and environmental factors. Antidepressant drug discovery has been a complex task, due to incomplete understanding of neurobiological basis of depression, thus no single molecular target can be rationalized as an ultimate therapeutic strategy. Several reports have recognized the pivotal status of the serotonergic system and the antidepressant drugs, as a central dogma of depression. Although commonly used antidepressants, such as the selective serotonin reuptake inhibitors (SSRIs) are often effective, full efficacy is only apparent after several weeks, and many patients only respond partially. For these reasons, efforts in developing newer, faster and safer antidepressant agents are still ongoing.
منابع مشابه
Synthesis, docking and pharmacological evaluation of novel homo- and hetero-bis 3-piperazinylpropylindole derivatives at SERT and 5-HT1A receptor.
A series of 3-(3-(4-(3-(1H-indol-3-yl)propyl)piperazin-1-yl)propyl)-1H-indole derivatives (3a-d and 5a-f) as homo- and hetero-bis-ligands, were synthesized and evaluated for in vitro affinity at the serotonin transporter (SERT) and the 5-HT1A receptor. Compounds 5b and 5f showed nanomolar affinities for both targets. The experimental data were rationalized according to results obtained from doc...
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تاریخ انتشار 2017