Unique spirocyclopiperazinium salt I: synthesis and structure-activity relationship of spirocyclopiperazinium salts as analgesics.
Unique spirocyclopiperazinium salt I: synthesis and structure-activity relationship of spirocyclopiperazinium salts as analgesics.
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DOI：
10.1016/s0960-894x(03)00177-x
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发表时间：
2003-05
影响因子：
2.7
通讯作者：
F. Gao;Xin Wang;Hong-Mei Zhang;T. Cheng;Run-tao Li
中科院分区：
文献类型：
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作者：
F. Gao;Xin Wang;Hong-Mei Zhang;T. Cheng;Run-tao Li
根据化合物3的结构，合成了两个系列的螺环哌嗪衍生物7a-n和10a-h，并对其体内镇痛和镇静活性进行了评价。化合物7f和10c具有良好的镇痛活性。构效关系表明，季盐的阴离子对其镇痛和镇静活性有显著影响，其中烯丙基是化合物7a-n中最有效的基团，芳环上的电子释放取代基有利于提高其镇痛活性。
Based on the structure of compound 3, two series of spirocyclopiperazinium derivatives 7a–n and 10a–h were synthesized and evaluated for their in vivo analgesic and sedative activities. Compounds 7f and 10c were discovered to exhibit excellent analgesic activity. Structure–activity relationships revealed that anion of the quaternary salt affected the analgesic and sedative activity significantly; the allyl group is a most effective group among the compounds 7a–n; the electron-released substitute on the aromatic ring is favorable to increase the analgesic activity.