Synthesis and SAR of 4-aminocyclopentapyrrolidines as orally active N-type calcium channel inhibitors for inflammatory and neuropathic pain

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Synthesis and SAR of 4-aminocyclopentapyrrolidines as orally active N-type calcium channel inhibitors for inflammatory and neuropathic pain

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作者：Xenia Beebe ; Clinton M. Yeung ; Daria Darczak ; Shashank Shekhar ; Timothy A. Vortherms ; Loan Miller ; Ivan Milicic ; Andrew M. Swensen ; Chang Z. Zhu ; Patricia Banfor ; Jill M. Wetter ; Kennan C. Marsh ; Michael F. Jarvis ; Victoria E. Scott ; Michael R. Schrimpf ; Chih-Hung Lee
关键词：N-type calcium channels ; SAR ; Enantiomeric synthesis ; Microsomal stability ; Analgesia
刊名：Bioorganic and Medicinal Chemistry Letters
出版年：2013
出版时间：1 September, 2013
年：2013
卷：23
期：17
页码：4857-4861
全文大小：712 K

文摘

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.