3,4-二取代 gababutin 的合成及体内评价。
Synthesis and in vivo evaluation of 3,4-disubstituted gababutins.
机构信息
Sandwich Laboratories, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK.
出版信息
Bioorg Med Chem Lett. 2010 Jan 1;20(1):248-51. doi: 10.1016/j.bmcl.2009.10.121. Epub 2009 Oct 30.
PMID:19910190
Abstract
A range of 3,4-alkylated five-membered ring derivatives of gabapentin were synthesised. One compound (21) had an excellent level of potency against alpha(2)delta and was profiled in in vivo models of pain and anxiety.
摘要
合成了一系列 3,4-烷基化的加巴喷丁五元环衍生物。其中一个化合物（21）对 α2δ 具有优异的活性，并在疼痛和焦虑的体内模型中进行了研究。
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