合成和 SAR 研究 4-氨基环戊并吡咯烷作为口服活性 N 型钙通道抑制剂用于治疗炎症和神经性疼痛。
Synthesis and SAR of 4-aminocyclopentapyrrolidines as orally active N-type calcium channel inhibitors for inflammatory and neuropathic pain.
机构信息
Neuroscience Research, AbbVie, 1 N Waukegan Road, North Chicago, IL 60064, United States.
出版信息
Bioorg Med Chem Lett. 2013 Sep 1;23(17):4857-61. doi: 10.1016/j.bmcl.2013.06.074. Epub 2013 Jul 4.
PMID:23876987
Abstract
A novel series of N-type calcium channel inhibitors have been discovered. Optimization of potency and HT-ADME properties provides 4-aminocyclopentapyrrolidines with analgesic efficacy after oral dosing.
摘要
研究人员发现了一系列新型 N 型钙通道抑制剂。通过对其活性和 HT-ADME 性质进行优化，最终得到的 4-氨基环戊烷并吡啶类化合物具有口服给药后的镇痛效果。
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