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首页> 外文期刊>Medicinal chemistry >Substituted urea derivatives: a potent class of antidepressant agents.
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Substituted urea derivatives: a potent class of antidepressant agents.

机译:取代的尿素衍生物:一类有效的抗抑郁药。

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A series of fourteen (14) N-nitrophenyl-N'-(alkyl/aryl)urea and symmetrical 1,3-disubstituted urea derivatives were synthesized and evaluated for their antidepressant activity in mice. Among them, N-(4-nitrophenyl)-N'-(1'-phenylethyl)urea (1), demonstrated profound antidepressant property as reflected by significant reduction in the immobility time (89.83%), whereas compounds 2-6 showed activity values between 36 to 59% which were also larger than the standard phenelzine. Compounds 7-9 were less effective in reducing the immobility period of mice 26.20 to 31.01%). This variable magnitude of antidepressant activity appears to be related to the position of the nitro group to the parent molecules 1, 2, and 8. Compound 1 with the nitro group at para position showed to be the most effective antidepressant. However, the activity declined, if the nitro is attached to ortho and meta positions.
机译:合成了一系列十四(14)种N-硝基苯基-N'-(烷基/芳基)脲和对称的1,3-二取代脲衍生物,并评估了它们在小鼠中的抗抑郁活性。其中,N-(4-硝基苯基)-N'-(1'-苯乙基)脲(1)具有很强的抗抑郁作用,其固定时间显着减少(89.83%),而化合物2-6具有活性值在36%至59%之间,也比标准苯乙嗪大。化合物7-9在将小鼠的不动周期减少26.20至31.01%方面不太有效。抗抑郁活性的这种变化幅度似乎与硝基相对于母体分子1、2和8的位置有关。硝基处在对位的化合物1被证明是最有效的抗抑郁剂。但是,如果硝基连接到邻位和间位,则活性下降。

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