1622845-90-2Relevant academic research and scientific papers
Design, synthesis, and biological activities of 1-aryl-1,4-diazepan-2-one derivatives as novel triple reuptake inhibitors
Honda, Eiji,Ishichi, Yuji,Kimura, Eiji,Yoshikawa, Masato,Kanzaki, Naoyuki,Nakagawa, Hideyuki,Terao, Yasuko,Suzuki, Atsuko,Kawai, Takayuki,Arakawa, Yuuichi,Ohta, Hiroyuki,Terauchi, Jun
, p. 3898 - 3902 (2014/09/17)
A novel series of triple reuptake inhibitors were explored by ligand-based drug design. A cyclic structure was designed from cyclopropane derivative 5 using the core structure of reported monoamine reuptake inhibitors, leading to the formation of the 1-aryl-1,4-diazepan-2-one derivative 23j-S. Compound 23j-S was shown to act as a potent TRI with an excellent ADME-Tox profile. Oral administration of 23j-S significantly enhanced norepinephrine, dopamine, and serotonin levels in the mouse prefrontal cortex and showed significant antidepressant-like activity in tail suspension tests in mouse.
