一系列靶向SSRI/5-HT/5-HT的芳基烷醇和芳烷基哌嗪衍生物的合成及抗抑郁活性
Synthesis and antidepressant activity of a series of arylalkanol and aralkyl piperazine derivatives targeting SSRI/5-HT/5-HT.
作者信息
Gu Zheng-Song, Xiao Ying, Zhang Qing-Wei, Li Jian-Qi
机构信息
Novel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry, 285 Gebaini Road, Shanghai 201203, PR China.
Novel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry, 285 Gebaini Road, Shanghai 201203, PR China.
出版信息
Bioorg Med Chem Lett. 2017 Dec 15;27(24):5420-5423. doi: 10.1016/j.bmcl.2017.11.007. Epub 2017 Nov 6.
A series of arylalkanol and aralkyl piperazine derivatives have been synthesized and evaluated for 5-HT reuptake inhibitory abilities and binding affinities at the 5-HT/5-HT receptors. Antidepressant activities of the compounds in vivo were screened using the forced swimming test (FST). The results indicated that the compound 8j exhibited high affinities for the 5-HT/5-HT receptors (5-HT, k = 0.84 nM; 5-HT, k = 12 nM) coupling with moderate 5-HT reuptake inhibitory activity (RUI, IC = 100 nM) and showed a marked antidepressant-like activity in the FST model.
已经合成了一系列芳基烷醇和芳烷基哌嗪衍生物，并对其5-羟色胺再摄取抑制能力以及在5-羟色胺/5-羟色胺受体上的结合亲和力进行了评估。使用强迫游泳试验（FST）筛选了这些化合物在体内的抗抑郁活性。结果表明，化合物8j对5-羟色胺/5-羟色胺受体具有高亲和力（5-羟色胺，k = 0.84 nM；5-羟色胺，k = 12 nM），同时具有中等程度的5-羟色胺再摄取抑制活性（RUI，IC = 100 nM），并且在FST模型中显示出显著的抗抑郁样活性。
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