615259-81-9Relevant academic research and scientific papers
Design and synthesis of arylamidine derivatives as serotonin/norepinephrine dual reuptake inhibitors
Wen, Hui,Qin, Wen,Yang, Guangzhong,Guo, Yanshen
, (2019/02/03)
To improve the in vivo antidepressant activity of previously reported serotonin (5-HT) and norepinephrine (NE) dual reuptake inhibitors, three series of arylamidine derivatives were designed and synthesized. The in vitro 5-HT and NE reuptake inhibitory activities of these compounds were evaluated, and compound II-5 was identified as the most potent 5-HT (IC50 = 620 nM) and NE (IC50 = 10 nM) dual reuptake inhibitor. Compound II-5 exhibited potent antidepressant activity in the rat tail suspension test and showed an acceptable safety profile in a preliminary acute toxicity test in mice. Our results show that these arylamidine derivatives exhibit potent 5-HT/NE dual reuptake inhibition and should be explored further as antidepressant drug candidates.
Amide derivatives
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Page/Page column 46-47, (2008/06/13)
A medicament for enhancing an effect of a cancer therapy based on a mode of action of DNA injury, which comprises as an active ingredient a compound represented by the following general formula (I) or a salt thereof: wherein one of R1 and R2 represents hydrogen atom and the other represents the formula —X-A wherein A represents hydrogen atom or an acyl group, X represents oxgen atom or NH; one of R3 and R4 represents hydrogen atom and the other represents the following formula: wherein Y represents a sulfonyl group or a carbonyl group, R5 represents a cyclic group, Z represents a single bond or a C1 to C4 alkylene group, R6 represents hydrogen atom or a C1 to C6 alkyl group.
