Synthesis and analgesic activity of secondary amine analogues of pyridylmethylamine and positional isomeric analogues of ABT-594.
Synthesis and analgesic activity of secondary amine analogues of pyridylmethylamine and positional isomeric analogues of ABT-594.
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DOI：
10.1002/chin.200629206
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发表时间：
2006-04
影响因子：
2.7
通讯作者：
Chuan-Xin Zhang;Z. Ge;T. Cheng;Run-tao Li
中科院分区：
文献类型：
--
作者：
Chuan-Xin Zhang;Z. Ge;T. Cheng;Run-tao Li
合成了一系列吡啶基甲胺的高度空间位阻仲胺类似物（7a-f，8a-c）和ABT-594的位置异构类似物（9a-c），并评价了它们的体内镇痛活性。化合物7a和7 d显示出较强的镇痛活性和较低的毒性。一些有趣的结构-活性关系已被揭示。
A series of highly sterically hindered secondary amine analogues of pyridylmethylamine (7a-f, 8a-c) and positional isomeric analogues of ABT-594 (9a-c) were synthesized and evaluated for their in vivo analgesic activity. The compounds 7a and 7d show potent analgesic activity and lower toxicity. Some interesting structure-activity relationships have been revealed.