CAS: 683274-51-3; 1-(Thiophene-2-Carbonyl)-1,4-Diazepane

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tert-butyl 4-(thiophene-2-carbonyl)-1,4-diazepane-1-carboxylate tert-butyl 1,4-diazepine-1-carboxylate 2-Thiophenecarbonyl chloride

📜1,4-二氮杂环庚烷-1-甲酸叔丁酯置于三乙胺,三氟乙酸体系中,用 二氯甲烷 作为反应溶剂,化学反应生成 1,4-二叠氮烷-1-基(2-噻吩)甲酮
参考文献:Synthesis,Cytotoxicity Evaluation,And Computational Insights Of Novel 1,4-Diazepane-Based Sigma Ligands
标题:Synthesis,Cytotoxicity Evaluation,And Computational Insights Of Novel 1,4-Diazepane-Based Sigma Ligands
摘要:Among Several Potential Applications,Sigma Receptor Ligands Can Be Used As Antipsychotics,Antiamnesics,And Against Other Neurodegenerative Disorders As Well As Neuroprotective Agents. We Present Herein A New Series Of Diazepane-Containing Derivatives As Sigma R Ligands Obtained By A Conformational Expansion Approach Of Our Previously Synthesized Piperidine-Based Compounds. The Best Results Were Reached By Benzofurane 2C,3C And Quinoline 2D,3D-Substituted Diazepane Derivatives,Which Showed The Highest Sigma R Affinity. The Cytotoxic Activities Of Synthesized Compounds Were Evaluated Against Two Cancer Cell Lines,And The Results Indicated That None Of The Compounds Induced Significant Toxicity In These Cells. We Also Evaluated The Antioxidant Activity By Radical Scavenging Capacity Of Our Best Compounds On Abts And H2O2. The Results Obtained Reveal That Our New Derivatives Possess An Excellent Antioxidant Profile And Could Be Protective For The Cells. Overall,The Benzofurane Derivative 2C Due To Its Strong Interaction With The Active Site Of The Receptor,As Confirmed By Molecular Dynamic Simulations,Emerged As The Optimum Compound With High Sigma 1R Affinity,Low Cytotoxicity,And A Potent Antioxidant Activity.
DOI:10.1021/acsmedchemlett.9B00524