双环 GABAbutin 的合成与体内评价。
Synthesis and in vivo evaluation of bicyclic 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 15;20(2):461-4. doi: 10.1016/j.bmcl.2009.11.118. Epub 2009 Nov 27.
PMID:20005103
Abstract
Synthesis of a number of bicyclic five-membered ring derivatives of gabapentin led to the identification of two compounds, (-)-(11A) and (20A) which both had an excellent level of potency against alpha(2)delta and were profiled in an in vivo model of neuropathic pain.
摘要
合成了一系列加巴喷丁的双环五元环衍生物，从中鉴定出两种化合物（-）-（11A）和（20A），它们对 alpha(2)delta 的活性都非常高，并在神经病理性疼痛的体内模型中进行了研究。
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